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Pioglitazone as Add-on Therapy in Patients with Type 2 Diabetes Mellitus Inadequately Controlled with Dapagliflozin and Metformin: Double-Blind, Randomized, Placebo-Controlled Trial
Ji Hye Heo, Kyung Ah Han, Jun Hwa Hong, Hyun-Ae Seo, Eun-Gyoung Hong, Jae Myung Yu, Hye Seung Jung, Bong-Soo Cha
Diabetes Metab J. 2024;48(5):937-948.   Published online February 2, 2024
DOI: https://doi.org/10.4093/dmj.2023.0314
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  • 1 Crossref
AbstractAbstract PDFSupplementary MaterialPubReader   ePub   
Background
This study assessed the efficacy and safety of triple therapy with pioglitazone 15 mg add-on versus placebo in patients with type 2 diabetes mellitus (T2DM) inadequately controlled with metformin and dapagliflozin.
Methods
In this multicenter, double-blind, randomized, phase 3 study, patients with T2DM with an inadequate response to treatment with metformin (≥1,000 mg/day) plus dapagliflozin (10 mg/day) were randomized to receive additional pioglitazone 15 mg/day (n=125) or placebo (n=125) for 24 weeks. The primary endpoint was the change in glycosylated hemoglobin (HbA1c) levels from baseline to week 24 (ClinicalTrials.gov identifier: NCT05101135).
Results
At week 24, the adjusted mean change from baseline in HbA1c level compared with placebo was significantly greater with pioglitazone treatment (–0.47%; 95% confidence interval, –0.61 to –0.33; P<0.0001). A greater proportion of patients achieved HbA1c <7% or <6.5% at week 24 with pioglitazone compared to placebo as add-on to 10 mg dapagliflozin and metformin (56.8% vs. 28% for HbA1c <7%, and 23.2% vs. 9.6% for HbA1c <6.5%; P<0.0001 for all). The addition of pioglitazone also significantly improved triglyceride, highdensity lipoprotein cholesterol levels, and homeostatic model assessment of insulin resistance levels, while placebo did not. The incidence of treatment-emergent adverse events was similar between the groups, and the incidence of fluid retention-related side effects by pioglitazone was low (1.5%).
Conclusion
Triple therapy with the addition of 15 mg/day of pioglitazone to dapagliflozin plus metformin was well tolerated and produced significant improvements in HbA1c in patients with T2DM inadequately controlled with dapagliflozin plus metformin.

Citations

Citations to this article as recorded by  
  • Ideal Combination of Oral Hypoglycemic Agents for Patients with Type 2 Diabetes Mellitus
    Hye Soon Kim
    Diabetes & Metabolism Journal.2024; 48(5): 882.     CrossRef
Short Communication
Drug/Regimen
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The Efficacy of Treatment Intensification by Quadruple Oral Therapy Compared to GLP-1RA Therapy in Poorly Controlled Type 2 Diabetes Mellitus Patients: A Real-World Data Study
Minyoung Kim, Hosu Kim, Kyong Young Kim, Soo Kyoung Kim, Junghwa Jung, Jong Ryeal Hahm, Jaehoon Jung, Jong Ha Baek
Diabetes Metab J. 2023;47(1):135-139.   Published online April 29, 2022
DOI: https://doi.org/10.4093/dmj.2021.0373
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AbstractAbstract PDFSupplementary MaterialPubReader   ePub   
We compared the glycemic efficacy of treatment intensification between quadruple oral antidiabetic drug therapy and once-weekly glucagon-like peptide-1 receptor agonist (GLP-1RA)-based triple therapy in patients with poorly controlled type 2 diabetes mellitus refractory to triple oral therapy. For 24 weeks, changes in glycosylated hemoglobin (HbA1c) from baseline were compared between the two treatment groups. Of all 96 patients, 50 patients were treated with quadruple therapy, and 46 were treated with GLP-1RA therapy. Reductions in HbA1c for 24 weeks were comparable (in both, 1.1% reduction from baseline; P=0.59). Meanwhile, lower C-peptide level was associated with a lower glucose-lowering response of GLP-1RA therapy (R=0.3, P=0.04) but not with quadruple therapy (R=–0.13, P=0.40). HbA1c reduction by GLP-1RA therapy was inferior to that by quadruple therapy in the low C-peptide subgroup (mean, –0.1% vs. –1.3%; P=0.04). Treatment intensification by switching to quadruple oral therapy showed similar glucose-lowering efficacy to weekly GLP-1RA-based triple therapy. Meanwhile, the therapeutic response was affected by C-peptide levels in the GLP-1RA therapy group but not in the quadruple therapy group.
Original Articles
Drug/Regimen
A Real-World Study of Long-Term Safety and Efficacy of Lobeglitazone in Korean Patients with Type 2 Diabetes Mellitus
Bo-Yeon Kim, Hyuk-Sang Kwon, Suk Kyeong Kim, Jung-Hyun Noh, Cheol-Young Park, Hyeong-Kyu Park, Kee-Ho Song, Jong Chul Won, Jae Myung Yu, Mi Young Lee, Jae Hyuk Lee, Soo Lim, Sung Wan Chun, In-Kyung Jeong, Choon Hee Chung, Seung Jin Han, Hee-Seok Kim, Ju-Young Min, Sungrae Kim
Diabetes Metab J. 2022;46(6):855-865.   Published online March 8, 2022
DOI: https://doi.org/10.4093/dmj.2021.0264
  • 8,455 View
  • 342 Download
  • 7 Web of Science
  • 7 Crossref
AbstractAbstract PDFPubReader   ePub   
Background
Thiazolidinediones (TZDs) have been associated with various safety concerns including weight gain, bladder cancer, and congestive heart failure (CHF). This study evaluated the efficacy and safety of lobeglitazone, a novel TZD in patients with type 2 diabetes mellitus (T2DM) in real practice.
Methods
In this non-interventional, multi-center, retrospective, and observational study conducted at 15 tertiary or secondary referral hospitals in Korea, a total of 2,228 patients with T2DM who received lobeglitazone 0.5 mg for more than 1 year were enrolled.
Results
Overall adverse events (AEs) occurred in 381 patients (17.10%) including edema in 1.97% (n=44). Cerebrovascular and cardiovascular diseases were identified in 0.81% (n=18) and 0.81% (n=18), respectively. One case of CHF was reported as an AE. Edema occurred in 1.97% (n=44) of patients. Hypoglycemia occurred in 2.47% (n=55) of patients. Fracture occurred in 1.17% (n=26) of all patients. Lobeglitazone significantly decreased HbA1c level, resulting in a mean treatment difference of -1.05%± 1.35% (P<0.001), and decreased total cholesterol, triglyceride, and low-density lipoprotein cholesterol. However, it increased high-density lipoprotein cholesterol, regardless of statin administration. The patients who received lobeglitazone 0.5 mg showed an apparent reduction in glycosylated hemoglobin (HbA1c) from baseline during the first 6 months of treatment. The HbA1c levels remained stable between months 6 and 42.
Conclusion
Lobeglitazone has long-term safety profile, good glycemic-lowering effect and long-term durability of glycemic control in real-world clinical settings.

Citations

Citations to this article as recorded by  
  • Efficacy and safety of novel thiazolidinedione lobeglitazone for managing type-2 diabetes a meta-analysis
    Deep Dutta, Saptarshi Bhattacharya, Manoj Kumar, Priyankar K. Datta, Ritin Mohindra, Meha Sharma
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(1): 102697.     CrossRef
  • Efficacy and safety of lobeglitazone, a new Thiazolidinedione, as compared to the standard of care in type 2 diabetes mellitus: A systematic review and meta-analysis
    Shashank R. Joshi, Saibal Das, Suja Xaviar, Shambo Samrat Samajdar, Indranil Saha, Sougata Sarkar, Shatavisa Mukherjee, Santanu Kumar Tripathi, Jyotirmoy Pal, Nandini Chatterjee
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(1): 102703.     CrossRef
  • Will lobeglitazone rival pioglitazone? A systematic review and critical appraisal
    Kalyan Kumar Gangopadhyay, Awadhesh Kumar Singh
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(4): 102747.     CrossRef
  • Lobeglitazone

    Reactions Weekly.2023; 1948(1): 262.     CrossRef
  • Lobeglitazone, a novel thiazolidinedione, for secondary prevention in patients with ischemic stroke: a nationwide nested case-control study
    Joonsang Yoo, Jimin Jeon, Minyoul Baik, Jinkwon Kim
    Cardiovascular Diabetology.2023;[Epub]     CrossRef
  • Lobeglitazone and Its Therapeutic Benefits: A Review
    Balamurugan M, Sarumathy S, Robinson R
    Cureus.2023;[Epub]     CrossRef
  • Oldies but Goodies: Thiazolidinedione as an Insulin Sensitizer with Cardioprotection
    Eun-Hee Cho
    Diabetes & Metabolism Journal.2022; 46(6): 827.     CrossRef
Cardiovascular Risk/Epidemiology
Article image
Comparative Effects of Sodium-Glucose Cotransporter 2 Inhibitor and Thiazolidinedione Treatment on Risk of Stroke among Patients with Type 2 Diabetes Mellitus
Seung Eun Lee, Hyewon Nam, Han Seok Choi, Hoseob Kim, Dae-Sung Kyoung, Kyoung-Ah Kim
Diabetes Metab J. 2022;46(4):567-577.   Published online February 8, 2022
DOI: https://doi.org/10.4093/dmj.2021.0160
  • 6,787 View
  • 389 Download
  • 7 Web of Science
  • 8 Crossref
AbstractAbstract PDFSupplementary MaterialPubReader   ePub   
Background
Although cardiovascular outcome trials using sodium-glucose cotransporter-2 inhibitors (SGLT-2i) showed a reduction in risk of 3-point major adverse cardiovascular events (MACE), they did not demonstrate beneficial effects on stroke risk. Additionally, meta-analysis showed SGLT-2i potentially had an adverse effect on stroke risk. Contrarily, pioglitazone, a type of thiazolidinedione (TZD), has been shown to reduce recurrent stroke risk. Thus, we aimed to compare the effect of SGLT-2i and TZD on the risk of stroke in type 2 diabetes mellitus (T2DM) patients.
Methods
Using the Korean National Health Insurance Service data, we compared a 1:1 propensity score-matched cohort of patients who used SGLT-2i or TZD from January 2014 to December 2018. The primary outcome was stroke. The secondary outcomes were myocardial infarction (MI), cardiovascular death, 3-point MACE, and heart failure (HF).
Results
After propensity-matching, each group included 56,794 patients. Baseline characteristics were well balanced. During the follow-up, 862 patients were newly hospitalized for stroke. The incidence rate of stroke was 4.11 and 4.22 per 1,000 person-years for the TZD and SGLT-2i groups respectively. The hazard ratio (HR) of stroke was 1.054 (95% confidence interval [CI], 0.904 to 1.229) in the SGLT-2i group compared to the TZD group. There was no difference in the risk of MI, cardiovascular death, 3-point MACE between groups. Hospitalization for HF was significantly decreased in SGLT-2i-treated patients (HR, 0.645; 95% CI, 0.466 to 0.893). Results were consistent regardless of prior cardiovascular disease.
Conclusion
In this real-world data, the risk of stroke was comparable in T2DM patients treated with SGLT-2i or TZD.

Citations

Citations to this article as recorded by  
  • Similar incidence of stroke with SGLT2 inhibitors and GLP-1 receptor agonists in real-world cohort studies among patients with type 2 diabetes
    André J. Scheen
    Diabetes Epidemiology and Management.2024; 13: 100179.     CrossRef
  • Diabetes and Stroke: Impact of Novel Therapies for the Treatment of Type 2 Diabetes Mellitus
    Inês Henriques Vieira, Tânia Santos Carvalho, Joana Saraiva, Leonor Gomes, Isabel Paiva
    Biomedicines.2024; 12(5): 1102.     CrossRef
  • Key results from observational studies and real‐world evidence of sodium‐glucose cotransporter‐2 inhibitor effectiveness and safety in reducing cardio‐renal risk
    Thomas Nyström
    Diabetes, Obesity and Metabolism.2024; 26(S5): 35.     CrossRef
  • Comparison of Statin With Ezetimibe Combination Therapy Versus Statin Monotherapy for Primary Prevention in Middle-Aged Adults
    Jung-Joon Cha, Soon Jun Hong, Subin Lim, Ju Hyeon Kim, Hyung Joon Joo, Jae Hyoung Park, Cheol Woong Yu, Do-Sun Lim, Jang Young Kim, Jin-Ok Jeong, Jeong-Hun Shin, Chi Young Shim, Jong-Young Lee, Young-Hyo Lim, Sung Ha Park, Eun Joo Cho, Hasung Kim, Jungkuk
    Korean Circulation Journal.2024; 54(9): 534.     CrossRef
  • A Green Approach: Optimization of the UPLC Method Using DoE Software for Concurrent Quantification of Pioglitazone and Dapagliflozin in a SNEDDS Formulation for the Treatment of Diabetes
    Ehab M. Elzayat, Abdelrahman Y. Sherif, Mohamed W. Attwa, Mohammad A. Altamimi
    ACS Omega.2024; 9(45): 45011.     CrossRef
  • Cardiovascular Disease & Diabetes Statistics in Korea: Nationwide Data 2010 to 2019
    Jin Hwa Kim, Junyeop Lee, Kyungdo Han, Jae-Taek Kim, Hyuk-Sang Kwon
    Diabetes & Metabolism Journal.2024; 48(6): 1084.     CrossRef
  • Lobeglitazone, a novel thiazolidinedione, for secondary prevention in patients with ischemic stroke: a nationwide nested case-control study
    Joonsang Yoo, Jimin Jeon, Minyoul Baik, Jinkwon Kim
    Cardiovascular Diabetology.2023;[Epub]     CrossRef
  • Do SGLT2 inhibitors and GLP-1 receptor agonists modulate differently the risk of stroke ? Discordance between randomised controlled trials and observational studies
    André J. Scheen
    Diabetes & Metabolism.2023; 49(5): 101474.     CrossRef
Review
Drug/Regimen
Article image
Lobeglitazone: A Novel Thiazolidinedione for the Management of Type 2 Diabetes Mellitus
Jaehyun Bae, Taegyun Park, Hyeyoung Kim, Minyoung Lee, Bong-Soo Cha
Diabetes Metab J. 2021;45(3):326-336.   Published online April 19, 2021
DOI: https://doi.org/10.4093/dmj.2020.0272
  • 12,084 View
  • 501 Download
  • 29 Web of Science
  • 27 Crossref
Graphical AbstractGraphical Abstract AbstractAbstract PDFSupplementary MaterialPubReader   ePub   
Type 2 diabetes mellitus (T2DM) is characterized by insulin resistance and β-cell dysfunction. Among available oral antidiabetic agents, only the thiazolidinediones (TZDs) primarily target insulin resistance. TZDs improve insulin sensitivity by activating peroxisome proliferator-activated receptor γ. Rosiglitazone and pioglitazone have been used widely for T2DM treatment due to their potent glycemic efficacy and low risk of hypoglycemia. However, their use has decreased because of side effects and safety issues, such as cardiovascular concerns and bladder cancer. Lobeglitazone (Chong Kun Dang Pharmaceutical Corporation), a novel TZD, was developed to meet the demands for an effective and safe TZD. Lobeglitazone shows similar glycemic efficacy to pioglitazone, with a lower effective dose, and favorable safety results. It also showed pleiotropic effects in preclinical and clinical studies. In this article, we summarize the pharmacologic, pharmacokinetic, and clinical characteristics of lobeglitazone.

Citations

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  • Thiazolidinediones: Recent Development in Analytical Methodologies
    Tarang Patel, Vatsal Patel
    Journal of Chromatographic Science.2024; 62(8): 789.     CrossRef
  • Etiology of Drug-Induced Edema: A Review of Dihydropyridine, Thiazolidinedione, and Other Medications Causing Edema
    Evan S Sinnathamby, Bretton T Urban, Robert A Clark, Logan T Roberts, Audrey J De Witt, Danielle M Wenger, Aya Mouhaffel, Olga Willett, Shahab Ahmadzadeh, Sahar Shekoohi, Alan D Kaye, Giustino Varrassi
    Cureus.2024;[Epub]     CrossRef
  • Novel thiazolidin-4-one benzenesulfonamide hybrids as PPARγ agonists: Design, synthesis and in vivo anti-diabetic evaluation
    Islam H. Ali, Rasha M. Hassan, Ahmed M. El Kerdawy, Mahmoud T. Abo-Elfadl, Heba M.I. Abdallah, Francesca Sciandra, Iman A.Y. Ghannam
    European Journal of Medicinal Chemistry.2024; 269: 116279.     CrossRef
  • The role of the methoxy group in approved drugs
    Debora Chiodi, Yoshihiro Ishihara
    European Journal of Medicinal Chemistry.2024; 273: 116364.     CrossRef
  • Thiazolidinedione an auspicious scaffold as PPAR-γ agonist: its possible mechanism to Manoeuvre against insulin resistant diabetes mellitus
    Sourav Basak, Anjali Murmu, Balaji Wamanrao Matore, Partha Pratim Roy, Jagadish Singh
    European Journal of Medicinal Chemistry Reports.2024; 11: 100160.     CrossRef
  • Quantitative determination of lobeglitazone sulfate and glimepiride in combined tablet by robust high‐performance thin layer chromatographic method
    Ashim Kumar Sen, Tantul Sarkar, Dhanya B. Sen, Rajesh A. Maheshwari, Aarti S. Zanwar, Rajesh L. Dumpala
    SEPARATION SCIENCE PLUS.2024;[Epub]     CrossRef
  • A chemical modification of a peroxisome proliferator-activated receptor pan agonist produced a shift to a new dual alpha/gamma partial agonist endowed with mitochondrial pyruvate carrier inhibition and antidiabetic properties
    Antonio Laghezza, Carmen Cerchia, Massimo Genovese, Roberta Montanari, Davide Capelli, Judith Wackerlig, Stefan Simic, Emanuele Falbo, Lucia Pecora, Rosalba Leuci, Leonardo Brunetti, Luca Piemontese, Paolo Tortorella, Abanish Biswas, Ravi Pratap Singh, Su
    European Journal of Medicinal Chemistry.2024; 275: 116567.     CrossRef
  • Synchronized Assessment of Lobeglitazone Sulfate and Metformin Hydrochloride in Tablet by Robust, High-performance Thin-layer Chromatographic Method
    Dhanya B. Sen, Krunal Baldha, Ashim K. Sen, Rajesh A. Maheshwari, Aarti S. Zanwar, Greeshma K. P., Prasanna K. Pradhan
    Current Pharmaceutical Analysis.2024; 20(5): 345.     CrossRef
  • Efficacy and Safety of Novel Thiazolidinedione Rivoglitazone in Type-2 Diabetes a Meta-Analysis
    Deep Dutta, Jyoti Kadian, Indira Maisnam, Ashok Kumar, Saptarshi Bhattacharya, Meha Sharma
    Indian Journal of Endocrinology and Metabolism.2023; 27(4): 286.     CrossRef
  • Efficacy and safety of novel thiazolidinedione lobeglitazone for managing type-2 diabetes a meta-analysis
    Deep Dutta, Saptarshi Bhattacharya, Manoj Kumar, Priyankar K. Datta, Ritin Mohindra, Meha Sharma
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(1): 102697.     CrossRef
  • Efficacy and safety of lobeglitazone, a new Thiazolidinedione, as compared to the standard of care in type 2 diabetes mellitus: A systematic review and meta-analysis
    Shashank R. Joshi, Saibal Das, Suja Xaviar, Shambo Samrat Samajdar, Indranil Saha, Sougata Sarkar, Shatavisa Mukherjee, Santanu Kumar Tripathi, Jyotirmoy Pal, Nandini Chatterjee
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(1): 102703.     CrossRef
  • Synthesis, Characterization, and Pharmacokinetic Studies of Thiazolidine-2,4-Dione Derivatives
    Bushra Ansari, Haroon Khan, Muhammad Saeed Jan, Khalaf F. Alsharif, Khalid J. Alzahrani, Umer Rashid, Abdul Saboor Pirzada, Vinod Kumar Tiwari
    Journal of Chemistry.2023; 2023: 1.     CrossRef
  • Will lobeglitazone rival pioglitazone? A systematic review and critical appraisal
    Kalyan Kumar Gangopadhyay, Awadhesh Kumar Singh
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(4): 102747.     CrossRef
  • Evaluation of pharmacokinetic interactions between lobeglitazone, empagliflozin, and metformin in healthy subjects
    Heeyoung Kim, Choon Ok Kim, Hyeonsoo Park, Min Soo Park, Dasohm Kim, Taegon Hong, Yesong Shin, Byung Hak Jin
    Translational and Clinical Pharmacology.2023; 31(1): 59.     CrossRef
  • Lobeglitazone, a novel thiazolidinedione, for secondary prevention in patients with ischemic stroke: a nationwide nested case-control study
    Joonsang Yoo, Jimin Jeon, Minyoul Baik, Jinkwon Kim
    Cardiovascular Diabetology.2023;[Epub]     CrossRef
  • Complementary effects of dapagliflozin and lobeglitazone on metabolism in a diet-induced obese mouse model
    Yun Kyung Lee, Tae Jung Oh, Ji In Lee, Bo Yoon Choi, Hyen Chung Cho, Hak Chul Jang, Sung Hee Choi
    European Journal of Pharmacology.2023; 957: 175946.     CrossRef
  • Current Clinical Trial Status and Future Prospects of PPAR-Targeted Drugs for Treating Nonalcoholic Fatty Liver Disease
    Shotaro Kamata, Akihiro Honda, Isao Ishii
    Biomolecules.2023; 13(8): 1264.     CrossRef
  • Lobeglitazone inhibits LPS-induced NLRP3 inflammasome activation and inflammation in the liver
    Hye-Young Seo, So-Hee Lee, Ji Yeon Park, Eugene Han, Sol Han, Jae Seok Hwang, Mi Kyung Kim, Byoung Kuk Jang, Kenji Fujiwara
    PLOS ONE.2023; 18(8): e0290532.     CrossRef
  • Insulin sensitizers in 2023: lessons learned and new avenues for investigation
    Jerry R. Colca, Steven P. Tanis, Rolf F. Kletzien, Brian N. Finck
    Expert Opinion on Investigational Drugs.2023; 32(9): 803.     CrossRef
  • Treatment of type 2 diabetes mellitus with stem cells and antidiabetic drugs: a dualistic and future-focused approach
    Priyamvada Amol Arte, Kanchanlata Tungare, Mustansir Bhori, Renitta Jobby, Jyotirmoi Aich
    Human Cell.2023; 37(1): 54.     CrossRef
  • Lobeglitazone and Its Therapeutic Benefits: A Review
    Balamurugan M, Sarumathy S, Robinson R
    Cureus.2023;[Epub]     CrossRef
  • Diabetes and diabesity in the view of proteomics, drug, and plant-derived remedies
    Mohammad Reza Haeri
    Journal of Research in Medical Sciences.2023;[Epub]     CrossRef
  • A double‐blind, Randomized controlled trial on glucose‐lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase‐4 inhibitor therapy: REFIND study
    Soree Ryang, Sang Soo Kim, Ji Cheol Bae, Ji Min Han, Su Kyoung Kwon, Young Il Kim, Il Seong Nam‐Goong, Eun Sook Kim, Mi‐kyung Kim, Chang Won Lee, Soyeon Yoo, Gwanpyo Koh, Min Jeong Kwon, Jeong Hyun Park, In Joo Kim
    Diabetes, Obesity and Metabolism.2022; 24(9): 1800.     CrossRef
  • Effect of the addition of thiazolidinedione to sodium-glucose cotransporter 2 inhibitor therapy on lipid levels in type 2 diabetes mellitus: a retrospective study using Korean National Health Insurance Service data
    Taegyun Park, Kyungdo Han, Dongwook Shin, Jongho Park
    Cardiovascular Prevention and Pharmacotherapy.2022; 4(3): 114.     CrossRef
  • Design of Improved Antidiabetic Drugs: A Journey from Single to Multitarget Agents
    Vassiliki‐Panagiota Tassopoulou, Ariadni Tzara, Angeliki P. Kourounakis
    ChemMedChem.2022;[Epub]     CrossRef
  • A Real-World Study of Long-Term Safety and Efficacy of Lobeglitazone in Korean Patients with Type 2 Diabetes Mellitus
    Bo-Yeon Kim, Hyuk-Sang Kwon, Suk Kyeong Kim, Jung-Hyun Noh, Cheol-Young Park, Hyeong-Kyu Park, Kee-Ho Song, Jong Chul Won, Jae Myung Yu, Mi Young Lee, Jae Hyuk Lee, Soo Lim, Sung Wan Chun, In-Kyung Jeong, Choon Hee Chung, Seung Jin Han, Hee-Seok Kim, Ju-Y
    Diabetes & Metabolism Journal.2022; 46(6): 855.     CrossRef
  • Lobeglitazone Exerts Anti-Inflammatory Effect in Lipopolysaccharide-Induced Bone-Marrow Derived Macrophages
    Dabin Jeong, Wan-Kyu Ko, Seong-Jun Kim, Gong-Ho Han, Daye Lee, Seung-Hun Sheen, Seil Sohn
    Biomedicines.2021; 9(10): 1432.     CrossRef
Original Articles
Drug/Regimen
Efficacy and Safety of Pioglitazone versus Glimepiride after Metformin and Alogliptin Combination Therapy: A Randomized, Open-Label, Multicenter, Parallel-Controlled Study
Jeong Mi Kim, Sang Soo Kim, Jong Ho Kim, Mi Kyung Kim, Tae Nyun Kim, Soon Hee Lee, Chang Won Lee, Ja Young Park, Eun Sook Kim, Kwang Jae Lee, Young Sik Choi, Duk Kyu Kim, In Joo Kim
Diabetes Metab J. 2020;44(1):67-77.   Published online July 11, 2019
DOI: https://doi.org/10.4093/dmj.2018.0274
  • 8,853 View
  • 187 Download
  • 9 Web of Science
  • 11 Crossref
AbstractAbstract PDFPubReader   
Background

There is limited information regarding the optimal third-line therapy for managing type 2 diabetes mellitus (T2DM) that is inadequately controlled using dual combination therapy. This study assessed the efficacy and safety of pioglitazone or glimepiride when added to metformin plus alogliptin treatment for T2DM.

Methods

This multicenter, randomized, active-controlled trial (ClinicalTrials.gov: NCT02426294) recruited 135 Korean patients with T2DM that was inadequately controlled using metformin plus alogliptin. The patients were then randomized to also receive pioglitazone (15 mg/day) or glimepiride (2 mg/day) for a 26-week period, with dose titration was permitted based on the investigator's judgement.

Results

Glycosylated hemoglobin levels exhibited similar significant decreases in both groups during the treatment period (pioglitazone: −0.81%, P<0.001; glimepiride: −1.05%, P<0.001). However, the pioglitazone-treated group exhibited significantly higher high density lipoprotein cholesterol levels (P<0.001) and significantly lower homeostatic model assessment of insulin resistance values (P<0.001). Relative to pioglitazone, adding glimepiride to metformin plus alogliptin markedly increased the risk of hypoglycemia (pioglitazone: 1/69 cases [1.45%], glimepiride: 14/66 cases [21.21%]; P<0.001).

Conclusion

Among patients with T2DM inadequately controlled using metformin plus alogliptin, the addition of pioglitazone provided comparable glycemic control and various benefits (improvements in lipid profiles, insulin resistance, and hypoglycemia risk) relative to the addition of glimepiride.

Citations

Citations to this article as recorded by  
  • Efficacy and Safety of Alogliptin-Pioglitazone Combination for Type 2 Diabetes Mellitus Poorly Controlled with Metformin: A Multicenter, Double-Blind Randomized Trial
    Ji-Yeon Park, Joonyub Lee, Yoon-Hee Choi, Kyung Wan Min, Kyung Ah Han, Kyu Jeung Ahn, Soo Lim, Young-Hyun Kim, Chul Woo Ahn, Kyung Mook Choi, Kun-Ho Yoon
    Diabetes & Metabolism Journal.2024; 48(5): 915.     CrossRef
  • Efficacy and Safety of Pioglitazone Add-on in Patients with Type 2 Diabetes Mellitus Inadequately Controlled with Metformin and Dapagliflozin: A Multicenter, Randomized, Double-blind, and Placebo-controlled Study
    Yun Kyung Cho, Kyung-Soo Kim, Byung-Wan Lee, Jun Hwa Hong, Jae Myung Yu, Soo Lim, Ye An Kim, Chang Beom Lee, Sang Soo Kim, Soo Heon Kwak, Woo Je Lee
    Clinical Therapeutics.2024; 46(9): 662.     CrossRef
  • Pioglitazone as Add-on Therapy in Patients with Type 2 Diabetes Mellitus Inadequately Controlled with Dapagliflozin and Metformin: Double-Blind, Randomized, Placebo-Controlled Trial
    Ji Hye Heo, Kyung Ah Han, Jun Hwa Hong, Hyun-Ae Seo, Eun-Gyoung Hong, Jae Myung Yu, Hye Seung Jung, Bong-Soo Cha
    Diabetes & Metabolism Journal.2024; 48(5): 937.     CrossRef
  • A Green Approach: Optimization of the UPLC Method Using DoE Software for Concurrent Quantification of Pioglitazone and Dapagliflozin in a SNEDDS Formulation for the Treatment of Diabetes
    Ehab M. Elzayat, Abdelrahman Y. Sherif, Mohamed W. Attwa, Mohammad A. Altamimi
    ACS Omega.2024; 9(45): 45011.     CrossRef
  • Cost-effectiveness and budget impact analysis of fixed combination of alogliptin and pioglitazone in the treatment of type 2 diabetes mellitus
    Yu.V. Strunina, N.A. Petunina
    Medical Technologies. Assessment and Choice.2023; (3): 70.     CrossRef
  • Pioglitazone-Enhanced Brown Fat Whitening Contributes to Weight Gain in Diet-Induced Obese Mice
    Piaojian Yu, Wei Wang, Wanrong Guo, Lidan Cheng, Zhiping Wan, Yanglei Cheng, Yunfeng Shen, Fen Xu
    Experimental and Clinical Endocrinology & Diabetes.2023; 131(11): 595.     CrossRef
  • Compliance with Cardiovascular Prevention Guidelines in Type 2 Diabetes Individuals in a Middle-Income Region: A Cross-Sectional Analysis
    Joaquim Barreto, Beatriz Luchiari, Vaneza L. W. Wolf, Isabella Bonilha, Ticiane G. Bovi, Barbara S. Assato, Ikaro Breder, Sheila T. Kimura-Medorima, Daniel B. Munhoz, Thiago Quinaglia, Otavio R. Coelho-Filho, Luiz Sergio F. Carvalho, Wilson Nadruz, Andrei
    Diagnostics.2022; 12(4): 814.     CrossRef
  • Effects of Glimepiride Combined with Recombinant Human Insulin Injection on Serum IGF-1, VEGF and TRACP-5b Oxidative Stress Levels in Patients with Type 2 Diabetes Mellitus
    Xue Chen, Sheng Kang, Zeqing Bao, Ciara Hughes
    Evidence-Based Complementary and Alternative Medicine.2022; 2022: 1.     CrossRef
  • Glycaemic control with add‐on thiazolidinedione or a sodium‐glucose co‐transporter‐2 inhibitor in patients with type 2 diabetes after the failure of an oral triple antidiabetic regimen: A 24‐week, randomized controlled trial
    Jaehyun Bae, Ji Hye Huh, Minyoung Lee, Yong‐Ho Lee, Byung‐Wan Lee
    Diabetes, Obesity and Metabolism.2021; 23(2): 609.     CrossRef
  • Development and validation of a sensitive LC-MS/MS method for pioglitazone: application towards pharmacokinetic and tissue distribution study in rats
    Kusuma Kumari G., Praveen Thaggikuppe Krishnamurthy, Ravi Kiran Ammu V. V. V., Kurawattimath Vishwanath, S. T. Narenderan, B. Babu, Nagappan Krishnaveni
    RSC Advances.2021; 11(19): 11437.     CrossRef
  • Compliance with Cardiovascular Prevention Guidelines in Individuals with Type 2 Diabetes in a Middle-Income Region: Cross-Sectional Analysis
    Joaquim Barreto, Beatriz Luchiari, Vaneza Lira W. Wolf, Isabella Bonilha, Ticiane G. Bovi, Barbara S. Assato, Ikaro Breder, Sheila T. Kimura-Medorima, Daniel B. Munhoz, Thiago Quinaglia, Otavio R. Coelho-Filho, Luiz Sérgio Fernandes de Carvalho, Wilson Na
    SSRN Electronic Journal .2021;[Epub]     CrossRef
Clinical Diabetes & Therapeutics
Effects of Lobeglitazone, a Novel Thiazolidinedione, on Bone Mineral Density in Patients with Type 2 Diabetes Mellitus over 52 Weeks
Soo Lim, Kyoung Min Kim, Sin Gon Kim, Doo Man Kim, Jeong-Taek Woo, Choon Hee Chung, Kyung Soo Ko, Jeong Hyun Park, Yongsoo Park, Sang Jin Kim, Hak Chul Jang, Dong Seop Choi
Diabetes Metab J. 2017;41(5):377-385.   Published online October 24, 2017
DOI: https://doi.org/10.4093/dmj.2017.41.5.377
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AbstractAbstract PDFPubReader   
Background

The aim of this multicenter, randomized, double-blind study was to examine the effect of lobeglitazone, a novel thiazolidinedione, on the changes in bone mineral density (BMD) in patients with type 2 diabetes mellitus.

Methods

A 24-week, double-blinded phase was followed by a 28-week, open-label phase, in which the placebo group also started to receive lobeglitazone. A total of 170 patients aged 34 to 76 years were randomly assigned in a 2:1 ratio to receive lobeglitazone 0.5 mg or a matching placebo orally, once daily. BMD was assessed using dual-energy X-ray absorptiometry at week 24 and at the end of the study (week 52).

Results

During the double-blinded phase, the femur neck BMD showed decreasing patterns in both groups, without statistical significance (−0.85%±0.36% and −0.78%±0.46% in the lobeglitazone and placebo groups, respectively). The treatment difference between the groups was 0.07%, which was also not statistically significant. Further, minimal, nonsignificant decreases were observed in both groups in the total hip BMD compared to values at baseline, and these differences also did not significantly differ between the groups. During the open-label phase, the BMD was further decreased, but not significantly, by −0.32% at the femur neck and by −0.60% at the total hip in the lobeglitazone group, and these changes did not significantly differ compared with the original placebo group switched to lobeglitazone.

Conclusion

Our results indicate that treatment with lobeglitazone 0.5 mg over 52 weeks showed no detrimental effect on the BMD compared to the placebo.

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  • Medication-induced fractures: Screening and treatment strategies
    Laraib Javed, Aemen Khakwani, Uzair Khan, Mary Beth Humphrey
    The American Journal of the Medical Sciences.2024;[Epub]     CrossRef
  • Efficacy and safety of novel thiazolidinedione lobeglitazone for managing type-2 diabetes a meta-analysis
    Deep Dutta, Saptarshi Bhattacharya, Manoj Kumar, Priyankar K. Datta, Ritin Mohindra, Meha Sharma
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(1): 102697.     CrossRef
  • Efficacy and safety of lobeglitazone, a new Thiazolidinedione, as compared to the standard of care in type 2 diabetes mellitus: A systematic review and meta-analysis
    Shashank R. Joshi, Saibal Das, Suja Xaviar, Shambo Samrat Samajdar, Indranil Saha, Sougata Sarkar, Shatavisa Mukherjee, Santanu Kumar Tripathi, Jyotirmoy Pal, Nandini Chatterjee
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(1): 102703.     CrossRef
  • The benefits of adipocyte metabolism in bone health and regeneration
    Lisa-Marie Burkhardt, Christian H. Bucher, Julia Löffler, Charlotte Rinne, Georg N. Duda, Sven Geissler, Tim J. Schulz, Katharina Schmidt-Bleek
    Frontiers in Cell and Developmental Biology.2023;[Epub]     CrossRef
  • Will lobeglitazone rival pioglitazone? A systematic review and critical appraisal
    Kalyan Kumar Gangopadhyay, Awadhesh Kumar Singh
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(4): 102747.     CrossRef
  • Comparison of therapeutic efficacy and safety of sitagliptin, dapagliflozin, or lobeglitazone adjunct therapy in patients with type 2 diabetes mellitus inadequately controlled on sulfonylurea and metformin: Third agent study
    Jun Hwa Hong, Jun Sung Moon, Kayeon Seong, Soo Lim
    Diabetes Research and Clinical Practice.2023; 203: 110872.     CrossRef
  • Bone Mineral Density Evaluation Among Type 2 Diabetic Patients in Rural Haryana, India: An Analytical Cross-Sectional Study
    Nitish Khandelwal, Surbhi Rajauria, Siddhesh Pandurang Kanjalkar, Omkar Shivaji Chavanke, Sanjay Rai
    Cureus.2023;[Epub]     CrossRef
  • Lobeglitazone and Its Therapeutic Benefits: A Review
    Balamurugan M, Sarumathy S, Robinson R
    Cureus.2023;[Epub]     CrossRef
  • A double‐blind, Randomized controlled trial on glucose‐lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase‐4 inhibitor therapy: REFIND study
    Soree Ryang, Sang Soo Kim, Ji Cheol Bae, Ji Min Han, Su Kyoung Kwon, Young Il Kim, Il Seong Nam‐Goong, Eun Sook Kim, Mi‐kyung Kim, Chang Won Lee, Soyeon Yoo, Gwanpyo Koh, Min Jeong Kwon, Jeong Hyun Park, In Joo Kim
    Diabetes, Obesity and Metabolism.2022; 24(9): 1800.     CrossRef
  • A Real-World Study of Long-Term Safety and Efficacy of Lobeglitazone in Korean Patients with Type 2 Diabetes Mellitus
    Bo-Yeon Kim, Hyuk-Sang Kwon, Suk Kyeong Kim, Jung-Hyun Noh, Cheol-Young Park, Hyeong-Kyu Park, Kee-Ho Song, Jong Chul Won, Jae Myung Yu, Mi Young Lee, Jae Hyuk Lee, Soo Lim, Sung Wan Chun, In-Kyung Jeong, Choon Hee Chung, Seung Jin Han, Hee-Seok Kim, Ju-Y
    Diabetes & Metabolism Journal.2022; 46(6): 855.     CrossRef
  • Comparative Efficacy of Lobeglitazone Versus Pioglitazone on Albuminuria in Patients with Type 2 Diabetes Mellitus
    Kyung-Soo Kim, Sangmo Hong, Hong-Yup Ahn, Cheol-Young Park
    Diabetes Therapy.2021; 12(1): 171.     CrossRef
  • Lobeglitazone: A Novel Thiazolidinedione for the Management of Type 2 Diabetes Mellitus
    Jaehyun Bae, Taegyun Park, Hyeyoung Kim, Minyoung Lee, Bong-Soo Cha
    Diabetes & Metabolism Journal.2021; 45(3): 326.     CrossRef
  • Effect of lobeglitazone on motor function in rat model of Parkinson’s disease with diabetes co-morbidity
    Kambiz Hassanzadeh, Arman Rahimmi, Mohammad Raman Moloudi, Rita Maccarone, Massimo Corbo, Esmael Izadpanah, Marco Feligioni
    Brain Research Bulletin.2021; 173: 184.     CrossRef
  • Recent Perspective on Thiazolidinedione
    Won Jun Kim
    The Journal of Korean Diabetes.2021; 22(2): 97.     CrossRef
  • Use of in vitro bone models to screen for altered bone metabolism, osteopathies, and fracture healing: challenges of complex models
    Sabrina Ehnert, Helen Rinderknecht, Romina H. Aspera-Werz, Victor Häussling, Andreas K. Nussler
    Archives of Toxicology.2020; 94(12): 3937.     CrossRef
  • Update on: effects of anti-diabetic drugs on bone metabolism
    Guillaume Mabilleau, Béatrice Bouvard
    Expert Review of Endocrinology & Metabolism.2020; 15(6): 415.     CrossRef
  • The use of metformin, insulin, sulphonylureas, and thiazolidinediones and the risk of fracture: Systematic review and meta‐analysis of observational studies
    Khemayanto Hidayat, Xuan Du, Meng‐Jiao Wu, Bi‐Min Shi
    Obesity Reviews.2019; 20(10): 1494.     CrossRef
  • Diabetes pharmacotherapy and effects on the musculoskeletal system
    Evangelia Kalaitzoglou, John L. Fowlkes, Iuliana Popescu, Kathryn M. Thrailkill
    Diabetes/Metabolism Research and Reviews.2019;[Epub]     CrossRef
  • Morin Exerts Anti‐Arthritic Effects by Attenuating Synovial Angiogenesis via Activation of Peroxisome Proliferator Activated Receptor‐γ
    Mengfan Yue, Ni Zeng, Yufeng Xia, Zhifeng Wei, Yue Dai
    Molecular Nutrition & Food Research.2018;[Epub]     CrossRef
  • The effects of diabetes therapy on bone: A clinical perspective
    Karim G. Kheniser, Carmen M. Polanco Santos, Sangeeta R. Kashyap
    Journal of Diabetes and its Complications.2018; 32(7): 713.     CrossRef
  • Changes in the Bone Mineral Density of Femur Neck and Total Hip Over a 52-Week Treatment with Lobeglitazone
    Da Young Lee, Ji A Seo
    Diabetes & Metabolism Journal.2017; 41(5): 374.     CrossRef
Others
Comparison of Vildagliptin and Pioglitazone in Korean Patients with Type 2 Diabetes Inadequately Controlled with Metformin
Jong Ho Kim, Sang Soo Kim, Hong Sun Baek, In Kyu Lee, Dong Jin Chung, Ho Sang Sohn, Hak Yeon Bae, Mi Kyung Kim, Jeong Hyun Park, Young Sik Choi, Young Il Kim, Jong Ryeal Hahm, Chang Won Lee, Sung Rae Jo, Mi Kyung Park, Kwang Jae Lee, In Joo Kim
Diabetes Metab J. 2016;40(3):230-239.   Published online April 5, 2016
DOI: https://doi.org/10.4093/dmj.2016.40.3.230
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AbstractAbstract PDFSupplementary MaterialPubReader   
Background

We compared the efficacies of vildagliptin (50 mg twice daily) relative to pioglitazone (15 mg once daily) as an add-on treatment to metformin for reducing glycosylated hemoglobin (HbA1c) levels in Korean patients with type 2 diabetes.

Methods

The present study was a multicenter, randomized, active-controlled investigation comparing the effects of vildagliptin and pioglitazone in Korean patients receiving a stable dose of metformin but exhibiting inadequate glycemic control. Each patient underwent a 16-week treatment period with either vildagliptin or pioglitazone as an add-on treatment to metformin.

Results

The mean changes in HbA1c levels from baseline were –0.94% in the vildagliptin group and –0.6% in the pioglitazone group and the difference between the treatments was below the non-inferiority margin of 0.3%. The mean changes in postprandial plasma glucose (PPG) levels were –60.2 mg/dL in the vildagliptin group and –38.2 mg/dL in the pioglitazone group and these values significantly differed (P=0.040). There were significant decreases in the levels of total, low density lipoprotein, high density lipoprotein (HDL), and non-HDL cholesterol in the vildagliptin group but increases in the pioglitazone group. The mean change in body weight was –0.07 kg in the vildagliptin group and 0.69 kg in the pioglitazone group, which were also significantly different (P=0.002).

Conclusion

As an add-on to metformin, the efficacy of vildagliptin for the improvement of glycemic control is not inferior to that of pioglitazone in Korean patients with type 2 diabetes. In addition, add-on treatment with vildagliptin had beneficial effects on PPG levels, lipid profiles, and body weight compared to pioglitazone.

Citations

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  • Factors contributing to the adverse drug reactions associated with the dipeptidyl peptidase-4 (DPP-4) inhibitors: A scoping review
    Swetha R. Reghunath, Muhammed Rashid, Viji Pulikkel Chandran, Girish Thunga, K.N. Shivashankar, Leelavathi D. Acharya
    Diabetes & Metabolic Syndrome: Clinical Research & Reviews.2023; 17(7): 102790.     CrossRef
  • Efficacy and safety of evogliptin in patients with type 2 diabetes and non‐alcoholic fatty liver disease: A multicentre, double‐blind, randomized, comparative trial
    Eugene Han, Ji Hye Huh, Eun Y. Lee, Ji C. Bae, Sung W. Chun, Sung H. Yu, Soo H. Kwak, Kyong S. Park, Byung‐Wan Lee
    Diabetes, Obesity and Metabolism.2022; 24(4): 752.     CrossRef
  • A double‐blind, Randomized controlled trial on glucose‐lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase‐4 inhibitor therapy: REFIND study
    Soree Ryang, Sang Soo Kim, Ji Cheol Bae, Ji Min Han, Su Kyoung Kwon, Young Il Kim, Il Seong Nam‐Goong, Eun Sook Kim, Mi‐kyung Kim, Chang Won Lee, Soyeon Yoo, Gwanpyo Koh, Min Jeong Kwon, Jeong Hyun Park, In Joo Kim
    Diabetes, Obesity and Metabolism.2022; 24(9): 1800.     CrossRef
  • The rs12617336 and rs17574 Dipeptidyl Peptidase-4 Polymorphisms Are Associated With Hypoalphalipoproteinemia and Dipeptidyl Peptidase-4 Serum Levels: A Case-Control Study of the Genetics of Atherosclerotic Disease (GEA) Cohort
    Gilberto Vargas-Alarcón, María del Carmen González-Salazar, Christian Vázquez-Vázquez, Adrián Hernández-Díaz Couder, Fausto Sánchez-Muñoz, Juan Reyes-Barrera, Sergio A. Criales-Vera, Marco Sánchez-Guerra, Citlalli Osorio-Yáñez, Rosalinda Posadas-Sánchez
    Frontiers in Genetics.2021;[Epub]     CrossRef
  • Reduction in HbA1c with SGLT2 inhibitors vs. DPP-4 inhibitors as add-ons to metformin monotherapy according to baseline HbA1c: A systematic review of randomized controlled trials
    A.J. Scheen
    Diabetes & Metabolism.2020; 46(3): 186.     CrossRef
  • Combination Therapy of Oral Hypoglycemic Agents in Patients with Type 2 Diabetes Mellitus
    Min Kyong Moon
    The Journal of Korean Diabetes.2018; 19(1): 23.     CrossRef
  • Comparative Cardiovascular Risks of Dipeptidyl Peptidase-4 Inhibitors: Analyses of Real-world Data in Korea
    Kyoung Hwa Ha, Bongseong Kim, Hae Sol Shin, Jinhee Lee, Hansol Choi, Hyeon Chang Kim, Dae Jung Kim
    Korean Circulation Journal.2018; 48(5): 395.     CrossRef
  • Safety and efficacy of low dose pioglitazone compared with standard dose pioglitazone in type 2 diabetes with chronic kidney disease: A randomized controlled trial
    Bancha Satirapoj, Khanin Watanakijthavonkul, Ouppatham Supasyndh, Stephen L Atkin
    PLOS ONE.2018; 13(10): e0206722.     CrossRef
  • Combination therapy of oral hypoglycemic agents in patients with type 2 diabetes mellitus
    Min Kyong Moon, Kyu Yeon Hur, Seung-Hyun Ko, Seok-O Park, Byung-Wan Lee, Jin Hwa Kim, Sang Youl Rhee, Hyun Jin Kim, Kyung Mook Choi, Nan-Hee Kim
    The Korean Journal of Internal Medicine.2017; 32(6): 974.     CrossRef
  • Combination Therapy of Oral Hypoglycemic Agents in Patients with Type 2 Diabetes Mellitus
    Min Kyong Moon, Kyu-Yeon Hur, Seung-Hyun Ko, Seok-O Park, Byung-Wan Lee, Jin Hwa Kim, Sang Youl Rhee, Hyun Jin Kim, Kyung Mook Choi, Nan-Hee Kim
    Diabetes & Metabolism Journal.2017; 41(5): 357.     CrossRef
  • Efficacy and safety of adding evogliptin versus sitagliptin for metformin‐treated patients with type 2 diabetes: A 24‐week randomized, controlled trial with open label extension
    Sang‐Mo Hong, Cheol‐Young Park, Dong‐Min Hwang, Kyung Ah Han, Chang Beom Lee, Choon Hee Chung, Kun‐Ho Yoon, Ji‐Oh Mok, Kyong Soo Park, Sung‐Woo Park
    Diabetes, Obesity and Metabolism.2017; 19(5): 654.     CrossRef
  • Antihyperglycemic agent therapy for adult patients with type 2 diabetes mellitus 2017: a position statement of the Korean Diabetes Association
    Seung-Hyun Ko, Kyu-Yeon Hur, Sang Youl Rhee, Nan-Hee Kim, Min Kyong Moon, Seok-O Park, Byung-Wan Lee, Hyun Jin Kim, Kyung Mook Choi, Jin Hwa Kim
    The Korean Journal of Internal Medicine.2017; 32(6): 947.     CrossRef
  • Antihyperglycemic Agent Therapy for Adult Patients with Type 2 Diabetes Mellitus 2017: A Position Statement of the Korean Diabetes Association
    Seung-Hyun Ko, Kyu-Yeon Hur, Sang Youl Rhee, Nan-Hee Kim, Min Kyong Moon, Seok-O Park, Byung-Wan Lee, Hyun Jin Kim, Kyung Mook Choi, Jin Hwa Kim
    Diabetes & Metabolism Journal.2017; 41(5): 337.     CrossRef
Review
Targeting the Peroxisome Proliferator-Activated Receptor-γ to Counter the Inflammatory Milieu in Obesity
Cesar Corzo, Patrick R. Griffin
Diabetes Metab J. 2013;37(6):395-403.   Published online December 12, 2013
DOI: https://doi.org/10.4093/dmj.2013.37.6.395
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AbstractAbstract PDFPubReader   

Adipose tissue, which was once viewed as a simple organ for storage of triglycerides, is now considered an important endocrine organ. Abnormal adipose tissue mass is associated with defects in endocrine and metabolic functions which are the underlying causes of the metabolic syndrome. Many adipokines, hormones secreted by adipose tissue, regulate cells from the immune system. Interestingly, most of these adipokines are proinflammatory mediators, which increase dramatically in the obese state and are believed to be involved in the pathogenesis of insulin resistance. Drugs that target peroxisome proliferator-activated receptor-γ have been shown to possess anti-inflammatory effects in animal models of diabetes. These findings, and the link between inflammation and the metabolic syndrome, will be reviewed here.

Citations

Citations to this article as recorded by  
  • Lysine 222 in PPAR γ1 functions as the key site of MuRF2-mediated ubiquitination modification
    Yucheng Fan, Fangjing Xu, Rui Wang, Jun He
    Scientific Reports.2023;[Epub]     CrossRef
  • Heart failure and diabetes: Clinical significance and epidemiology of this two‐way association
    Terri Jerkins, Janet B. McGill, David S. H. Bell
    Diabetes, Obesity and Metabolism.2023; 25(S3): 3.     CrossRef
  • The pleiotropic peroxisome proliferator activated receptors: Regulation and therapeutics
    Gargi Dixit, Arati Prabhu
    Experimental and Molecular Pathology.2022; 124: 104723.     CrossRef
  • The Effect of PPARγ rs1801282 Variant on Mortality Risk Among Asians With Chronic Kidney Disease: A Cohort Study and Meta-Analysis
    Wei-Teing Chen, Chih-Chien Chiu, Dung-Jang Tsai, Pi-Shao Ko, Meng-Chang Lee, Hsiao-Ting Lin, Ying-Kai Chen, Wen Su, Yuh-Feng Lin, Sui-Lung Su
    Frontiers in Genetics.2022;[Epub]     CrossRef
  • Metabolic Spectrum of Liver Failure in Type 2 Diabetes and Obesity: From NAFLD to NASH to HCC
    Hyunmi Kim, Da Som Lee, Tae Hyeon An, Hyun-Ju Park, Won Kon Kim, Kwang-Hee Bae, Kyoung-Jin Oh
    International Journal of Molecular Sciences.2021; 22(9): 4495.     CrossRef
  • Associations between obesity-related gene expression in maternal and cord blood and newborn adiposity: findings from the Araraquara Cohort study
    P. Nakandakare, C. F. Nicoletti, N. Y. Noronha, C. B. Nonino, P. P. Argentato, N. N. Dejani, L. A. Luzia, M. M. Rogero, P. H. C. Rondó
    International Journal of Obesity.2021; 45(9): 1958.     CrossRef
  • PPARG Pro12Ala Polymorphism with CKD in Asians: A Meta-Analysis Combined with a Case-Control Study—A Key for Reaching Null Association
    Hsiang-Cheng Chen, Wei-Teing Chen, Tzu-Ling Sung, Dung-Jang Tsai, Chin Lin, Hao Su, Yuh-Feng Lin, Hung-Yi Chiu, Sui-Lung Su
    Genes.2020; 11(6): 705.     CrossRef
  • Induction of peroxisome proliferator activated receptor γ (PPARγ) mediated gene expression and inhibition of induced nitric oxide production by Maerua subcordata (Gilg) DeWolf
    Mebrahtom Gebrelibanos Hiben, Laura de Haan, Bert Spenkelink, Sebastiaan Wesseling, Jacques Vervoort, Ivonne M. C. M. Rietjens
    BMC Complementary Medicine and Therapies.2020;[Epub]     CrossRef
  • UPR modulation of host immunity by Pseudomonas aeruginosa in cystic fibrosis
    Brahmchetna Bedi, Kuo-Chuan. Lin, Nicholas M. Maurice, Zhihong Yuan, Kaiser Bijli, Michael Koval, C. Michael Hart, Joanna B. Goldberg, Arlene Stecenko, Ruxana T. Sadikot
    Clinical Science.2020; 134(14): 1911.     CrossRef
  • Sepsis Immunometabolism: From Defining Sepsis to Understanding How Energy Production Affects Immune Response
    Ioannis Koutroulis, Rachael Batabyal, Brittany McNamara, Matthew Ledda, Claire Hoptay, Robert J. Freishtat
    Critical Care Explorations.2019; 1(11): e0061.     CrossRef
  • Combining SGLT2 Inhibition With a Thiazolidinedione Additively Attenuate the Very Early Phase of Diabetic Nephropathy Progression in Type 2 Diabetes Mellitus
    Eugene Han, Eugene Shin, Gyuri Kim, Ji-Yeon Lee, Yong-ho Lee, Byung-Wan Lee, Eun Seok Kang, Bong-Soo Cha
    Frontiers in Endocrinology.2018;[Epub]     CrossRef
  • Role of oral hypoglycemic drugs on inflammatory condition associated with type 2 diabetes mellitus
    Shamim Shaikh Mohiuddin
    Journal of Diabetes, Metabolic Disorders & Control.2018; 5(2): 78.     CrossRef
  • Effects of lobeglitazone on insulin resistance and hepatic steatosis in high-fat diet-fed mice
    Bong-Hoi Choi, Zhen Jin, Chin-ok Yi, Juhong Oh, Eun Ae Jeong, Jong Youl Lee, Kyung-ah Park, Kyung Eun Kim, Jung Eun Lee, Hyun-Jin Kim, Jong Ryeal Hahm, Gu Seob Roh, Jonathan M Peterson
    PLOS ONE.2018; 13(7): e0200336.     CrossRef
  • Cucurbita ficifolia (Cucurbitaceae) modulates inflammatory cytokines and IFN-γ in obese mice
    Á. Fortis-Barrera, R. García-Macedo, J.C. Almanza-Perez, G. Blancas-Flores, A. Zamilpa-Alvarez, J.L. Flores-Sáenz, M. Cruz, R. Román-Ramos, F.J. Alarcón-Aguilar
    Canadian Journal of Physiology and Pharmacology.2017; 95(2): 170.     CrossRef
  • Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness
    Yong-ho Lee, Jae Hyeon Kim, So Ra Kim, Heung Yong Jin, Eun-Jung Rhee, Young Min Cho, Byung-Wan Lee
    Journal of Korean Medical Science.2017; 32(1): 60.     CrossRef
  • Peroxisome proliferator‐activated receptor‐γ agonists attenuate biofilm formation by Pseudomonas aeruginosa
    Brahmchetna Bedi, Nicholas M. Maurice, Vincent T. Ciavatta, K. Sabrina Lynn, Zhihong Yuan, Samuel A. Molina, Myungsoo Joo, William R. Tyor, Joanna B. Goldberg, Michael Koval, C. Michael Hart, Ruxana T. Sadikot
    The FASEB Journal.2017; 31(8): 3608.     CrossRef
  • Pioglitazone and the secondary prevention of cardiovascular disease. A meta-analysis of randomized-controlled trials
    Marit de Jong, H. Bart van der Worp, Yolanda van der Graaf, Frank L. J. Visseren, Jan Westerink
    Cardiovascular Diabetology.2017;[Epub]     CrossRef
  • Gestational diabetes mellitus was related to ambient air pollutant nitric oxide during early gestation
    Shih-Chun Pan, Ching-Chun Huang, Shio-Jean Lin, Bing-Yu Chen, Chang-Chuan Chan, Yue-Liang Leon Guo
    Environmental Research.2017; 158: 318.     CrossRef
  • The Multifaceted Haptoglobin in the Context of Adipose Tissue and Metabolism
    Margherita Maffei, Ilaria Barone, Gaia Scabia, Ferruccio Santini
    Endocrine Reviews.2016; 37(4): 403.     CrossRef
  • Enhanced Clearance of Pseudomonas aeruginosa by Peroxisome Proliferator-Activated Receptor Gamma
    Brahmchetna Bedi, Zhihong Yuan, Myungsoo Joo, Susu M. Zughaier, Joanna B. Goldberg, Jack L. Arbiser, C. Michael Hart, Ruxana T. Sadikot, B. A. McCormick
    Infection and Immunity.2016; 84(7): 1975.     CrossRef
  • F-box only protein 9 is an E3 ubiquitin ligase of PPARγ
    Kyeong Won Lee, Soo Heon Kwak, Young Do Koo, Yun-Kyung Cho, Hak Mo Lee, Hye Seung Jung, Young Min Cho, Young Joo Park, Sung Soo Chung, Kyong Soo Park
    Experimental & Molecular Medicine.2016; 48(5): e234.     CrossRef
  • The Resin fromProtium heptaphyllumPrevents High-Fat Diet-Induced Obesity in Mice: Scientific Evidence and Potential Mechanisms
    Karine Maria Martins Bezerra Carvalho, José Delano Barreto Marinho Filho, Tiago Sousa de Melo, Ana Jérsia Araújo, Josiane da Silva Quetz, Maria do Perpétuo Socorro Saldanha da Cunha, Karina Moura de Melo, Armenio Andre de Carvalho Almeida da Silva, Adrian
    Evidence-Based Complementary and Alternative Medicine.2015; 2015: 1.     CrossRef
  • Lobeglitazone and pioglitazone as add‐ons to metformin for patients with type 2 diabetes: a 24‐week, multicentre, randomized, double‐blind, parallel‐group, active‐controlled, phase III clinical trial with a 28‐week extension
    S.‐M. Jin, C.‐Y. Park, Y. M. Cho, B. J. Ku, C. W. Ahn, B.‐S. Cha, K. W. Min, Y. A. Sung, S. H. Baik, K. W. Lee, K.‐H. Yoon, M.‐K. Lee, S. W. Park
    Diabetes, Obesity and Metabolism.2015; 17(6): 599.     CrossRef
  • Deconvolution of Complex 1D NMR Spectra Using Objective Model Selection
    Travis S. Hughes, Henry D. Wilson, Ian Mitchelle S. de Vera, Douglas J. Kojetin, Paul C. Driscoll
    PLOS ONE.2015; 10(8): e0134474.     CrossRef
  • PPARγ partial agonist GQ-16 strongly represses a subset of genes in 3T3-L1 adipocytes
    Flora Aparecida Milton, Aleksandra Cvoro, Angelica A. Amato, Douglas H. Sieglaff, Carly S. Filgueira, Anithachristy Sigamani Arumanayagam, Maria do Carmo Alves de Lima, Ivan Rocha Pitta, Francisco de Assis Rocha Neves, Paul Webb
    Biochemical and Biophysical Research Communications.2015; 464(3): 718.     CrossRef
  • Voluntary exercise prevents colonic inflammation in high-fat diet-induced obese mice by up-regulating PPAR-γ activity
    Wei-Xin Liu, Ting Wang, Feng Zhou, Ying Wang, Jun-Wei Xing, Shen Zhang, Shou-Zhi Gu, Li-Xuan Sang, Cong Dai, Hai-Lan Wang
    Biochemical and Biophysical Research Communications.2015; 459(3): 475.     CrossRef
  • Effect of a new PPAR-gamma agonist, lobeglitazone, on neointimal formation after balloon injury in rats and the development of atherosclerosis
    Soo Lim, Kuy-Sook Lee, Jie Eun Lee, Ho Seon Park, Kyoung Min Kim, Jae Hoon Moon, Sung Hee Choi, Kyong Soo Park, Young Bum Kim, Hak Chul Jang
    Atherosclerosis.2015; 243(1): 107.     CrossRef
  • Antidiabetic agents: Potential anti-inflammatory activity beyond glucose control
    A.J. Scheen, N. Esser, N. Paquot
    Diabetes & Metabolism.2015; 41(3): 183.     CrossRef
  • Genomic binding and regulation of gene expression by the thyroid carcinoma-associated PAX8-PPARG fusion protein
    Yanxiao Zhang, Jingcheng Yu, Chee Lee, Bin Xu, Maureen A. Sartor, Ronald J. Koenig
    Oncotarget.2015; 6(38): 40418.     CrossRef
  • Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage
    Santiago Garcia-Vallvé, Laura Guasch, Sarah Tomas-Hernández, Josep Maria del Bas, Vincent Ollendorff, Lluís Arola, Gerard Pujadas, Miquel Mulero
    Journal of Medicinal Chemistry.2015; 58(14): 5381.     CrossRef
  • Pathway Analysis of Metabolic Syndrome Using a Genome-Wide Association Study of Korea Associated Resource (KARE) Cohorts
    Unjin Shim, Han-Na Kim, Yeon-Ah Sung, Hyung-Lae Kim
    Genomics & Informatics.2014; 12(4): 195.     CrossRef
  • Pax-8–PPAR-γ fusion protein in thyroid carcinoma
    Priyadarshini Raman, Ronald J. Koenig
    Nature Reviews Endocrinology.2014; 10(10): 616.     CrossRef
  • Insulin therapy and colorectal cancer risk among type 2 diabetes mellitus patients: a systemic review and meta-analysis
    Shinan Yin, Hua Bai, Danqing Jing
    Diagnostic Pathology.2014;[Epub]     CrossRef
  • Common biological mechanisms between bipolar disorder and type 2 diabetes: Focus on inflammation
    Ajaykumar N. Sharma, Isabelle E. Bauer, Marsal Sanches, Juan F. Galvez, Giovana B. Zunta-Soares, Joao Quevedo, Flavio Kapczinski, Jair C. Soares
    Progress in Neuro-Psychopharmacology and Biological Psychiatry.2014; 54: 289.     CrossRef
Original Article
Effects of Sulfonylureas on Peroxisome Proliferator-Activated Receptor γ Activity and on Glucose Uptake by Thiazolidinediones
Kyeong Won Lee, Yun Hyi Ku, Min Kim, Byung Yong Ahn, Sung Soo Chung, Kyong Soo Park
Diabetes Metab J. 2011;35(4):340-347.   Published online August 31, 2011
DOI: https://doi.org/10.4093/dmj.2011.35.4.340
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AbstractAbstract PDFPubReader   
Background

Sulfonylurea primarily stimulates insulin secretion by binding to its receptor on the pancreatic β-cells. Recent studies have suggested that sulfonylureas induce insulin sensitivity through peroxisome proliferator-activated receptor γ (PPARγ), one of the nuclear receptors. In this study, we investigated the effects of sulfonylurea on PPARγ transcriptional activity and on the glucose uptake via PPARγ.

Methods

Transcription reporter assays using Cos7 cells were performed to determine if specific sulfonylureas stimulate PPARγ transactivation. Glimepiride, gliquidone, and glipizide (1 to 500 µM) were used as treatment, and rosiglitazone at 1 and 10 µM was used as a control. The effects of sulfonylurea and rosiglitazone treatments on the transcriptional activity of endogenous PPARγ were observed. In addition, 3T3-L1 adipocytes were treated with rosiglitazone (10 µM), glimepiride (100 µM) or both to verify the effect of glimepiride on rosiglitazone-induced glucose uptake.

Results

Sulfonylureas, including glimepiride, gliquidone and glipizide, increased PPARγ transcriptional activity, gliquidone being the most potent PPARγ agonist. However, no additive effects were observed in the presence of rosiglitazone. When rosiglitazone was co-treated with glimepiride, PPARγ transcriptional activity and glucose uptake were reduced compared to those after treatment with rosiglitazone alone. This competitive effect of glimepiride was observed only at high concentrations that are not achieved with clinical doses.

Conclusion

Sulfonylureas like glimepiride, gliquidone and glipizide increased the transcriptional activity of PPARγ. Also, glimepiride was able to reduce the effect of rosiglitazone on PPARγ agonistic activity and glucose uptake. However, the competitive effect does not seem to occur at clinically feasible concentrations.

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  • Sulfonylureas exert antidiabetic action on adipocytes by inhibition of PPARγ serine 273 phosphorylation
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    Molecular Metabolism.2024; 85: 101956.     CrossRef
  • Chitosan-Encapsulated Nano-selenium Targeting TCF7L2, PPARγ, and CAPN10 Genes in Diabetic Rats
    Omayma A. R. Abozaid, Sawsan M. El-Sonbaty, Neama M. A. Hamam, Moustafa A. Farrag, Ahmad S. Kodous
    Biological Trace Element Research.2023; 201(1): 306.     CrossRef
  • Insights from insulin resistance pathways: Therapeutic approaches against Alzheimer associated diabetes mellitus
    Ayesha Fauzi, Ewen Se Thoe, Tang Yin Quan, Adeline Chia Yoke Yin
    Journal of Diabetes and its Complications.2023; 37(11): 108629.     CrossRef
  • Novel Sulfonanilide Inhibitors of SHIP2 Enhance Glucose Uptake into Cultured Myotubes
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    ACS Omega.2020; 5(3): 1430.     CrossRef
  • Diabetic Theory in Anti-Alzheimer’s Drug Research and Development - Part 1: Therapeutic Potential of Antidiabetic Agents
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    Current Medicinal Chemistry.2020; 27(39): 6658.     CrossRef
  • Moringa concanensis Nimmo extracts ameliorates hyperglycemia-mediated oxidative stress and upregulates PPARγ and GLUT4 gene expression in liver and pancreas of streptozotocin-nicotinamide induced diabetic rats
    Brindha Banu Balakrishnan, Kalaivani Krishnasamy, Vijayakumar Mayakrishnan, Arokiyaraj Selvaraj
    Biomedicine & Pharmacotherapy.2019; 112: 108688.     CrossRef
  • PPARγ Agonistic Activity of Sulphonylureas
    Debjani Banerjee, Harnovdeep Singh Bharaj, Moulinath Banerjee
    Endocrine, Metabolic & Immune Disorders - Drug Targets.2019; 19(4): 467.     CrossRef
  • Glimepiride treatment in a patient with type A insulin resistance syndrome due to a novel heterozygous missense mutation in the insulin receptor gene
    Zhimin Huang, Juan Liu, Kaka Ng, Xuesi Wan, Lijuan Xu, Xiaoying He, Zhihong Liao, Yanbing Li
    Journal of Diabetes Investigation.2018; 9(5): 1075.     CrossRef
  • Arsenic, Cadmium, and Lead Like Troglitazone Trigger PPARγ-Dependent Poly (ADP-Ribose) Polymerase Expression and Subsequent Apoptosis in Rat Brain Astrocytes
    Rajesh Kushwaha, Juhi Mishra, Sachin Tripathi, Puneet Khare, Sanghamitra Bandyopadhyay
    Molecular Neurobiology.2018; 55(3): 2125.     CrossRef
  • Docosahexaenoic acid up‐regulates both PI3K/AKT‐dependent FABP7–PPARγ interaction and MKP3 that enhance GFAP in developing rat brain astrocytes
    Sachin Tripathi, Rajesh Kushwaha, Juhi Mishra, Manoj Kumar Gupta, Harish Kumar, Somali Sanyal, Dhirendra Singh, Sabyasachi Sanyal, Amogh Anant Sahasrabuddhe, Mohan Kamthan, Mohana Krishna Reddy Mudiam, Sanghamitra Bandyopadhyay
    Journal of Neurochemistry.2017; 140(1): 96.     CrossRef
  • Antiglycation and cell protective actions of metformin and glipizide in erythrocytes and monocytes
    Krishna Adeshara, Rashmi Tupe
    Molecular Biology Reports.2016; 43(3): 195.     CrossRef
  • The therapeutic journey of pyridazinone
    Wasim Akhtar, M. Shaquiquzzaman, Mymoona Akhter, Garima Verma, Mohemmed Faraz Khan, M. Mumtaz Alam
    European Journal of Medicinal Chemistry.2016; 123: 256.     CrossRef
  • Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect
    Chetna Kharbanda, Mohammad Sarwar Alam, Hinna Hamid, Kalim Javed, Abhijeet Dhulap, Sameena Bano, Yakub Ali
    Bioorganic & Medicinal Chemistry Letters.2015; 25(20): 4601.     CrossRef
  • Method Development and Validation of Amlodipine, Gliquidone and Pioglitazone: Application in the Analysis of Human Serum
    Agha Zeeshan Mirza, M. Saeed Arayne, Najma Sultana
    Analytical Chemistry Letters.2014; 4(5-6): 302.     CrossRef
  • Gliquidone decreases urinary protein by promoting tubular reabsorption in diabetic Goto-Kakizaki rats
    Jian-Ting Ke, Mi Li, Shi-Qing Xu, Wen-Jian Zhang, Yong-Wei Jiang, Lan-yun Cheng, Li Chen, Jin-Ning Lou, Wei Wu
    Journal of Endocrinology.2014; 220(2): 129.     CrossRef
  • Extension of Drosophila lifespan by cinnamon through a sex-specific dependence on the insulin receptor substrate chico
    Samuel E. Schriner, Steven Kuramada, Terry E. Lopez, Stephanie Truong, Andrew Pham, Mahtab Jafari
    Experimental Gerontology.2014; 60: 220.     CrossRef
  • Crif1 Deficiency Reduces Adipose OXPHOS Capacity and Triggers Inflammation and Insulin Resistance in Mice
    Min Jeong Ryu, Soung Jung Kim, Yong Kyung Kim, Min Jeong Choi, Surendar Tadi, Min Hee Lee, Seong Eun Lee, Hyo Kyun Chung, Saet Byel Jung, Hyun-Jin Kim, Young Suk Jo, Koon Soon Kim, Sang-Hee Lee, Jin Man Kim, Gi Ryang Kweon, Ki Cheol Park, Jung Uee Lee, Yo
    PLoS Genetics.2013; 9(3): e1003356.     CrossRef
  • Glimepiride attenuates Aβ production via suppressing BACE1 activity in cortical neurons
    Feiyang Liu, Yijin Wang, Ming Yan, Luyong Zhang, Tao Pang, Hong Liao
    Neuroscience Letters.2013; 557: 90.     CrossRef
  • Pharmacologic agents for type 2 diabetes therapy and regulation of adipogenesis
    A. Cignarelli, F. Giorgino, R. Vettor
    Archives of Physiology and Biochemistry.2013; 119(4): 139.     CrossRef
  • Labisia pumilaUpregulates Peroxisome Proliferator-Activated Receptor Gamma Expression in Rat Adipose Tissues and 3T3-L1 Adipocytes
    Fazliana Mansor, Harvest F. Gu, Claes-Göran Östenson, Louise Mannerås-Holm, Elisabet Stener-Victorin, Wan Nazaimoon Wan Mohamud
    Advances in Pharmacological Sciences.2013; 2013: 1.     CrossRef
  • Protocol for effective differentiation of 3T3-L1 cells to adipocytes
    Katja Zebisch, Valerie Voigt, Martin Wabitsch, Matthias Brandsch
    Analytical Biochemistry.2012; 425(1): 88.     CrossRef
Review
Triple Combination Therapy Using Metformin, Thiazolidinedione, and a GLP-1 Analog or DPP-IV Inhibitor in Patients with Type 2 Diabetes Mellitus
Sun Woo Kim
Korean Diabetes J. 2010;34(6):331-337.   Published online December 31, 2010
DOI: https://doi.org/10.4093/kdj.2010.34.6.331
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AbstractAbstract PDFPubReader   

Although there is no HbA1c threshold for cardiovascular risk, the American Diabetic Association-recommended goal of HbA1c < 7.0% appears to be unacceptably high. To achieve an optimal HbA1c level goal of 6.0% or less, a high dosage of sulfonylureas and insulin would be required; the trade-off would be the common adverse effects of hypoglycemia and weight gain. In contrast, hypoglycemia is uncommon with insulin sensitizers and GLP-1 analogs, allowing the physician to titrate these drugs to maximum dosage to reduce HbA1c levels below 6.0% and they have been shown to preserve β-cell function. Lastly, weight gain is common with sulfonylurea and insulin therapy, whereas GLP-1 analogs induce weight loss and offset the weight gain associated with TZDs. A treatment paradigm shift is recommended in which combination therapy is initiated with diet/exercise, metformin (which has antiatherogenic effects and improves hepatic insulin sensitivity), a TZD (which improves insulin sensitivity and preserves β-cell function with proven durability), and a GLP-1 analog (which improves β, α-cell function and promotes weight loss) or a dipeptidyl peptidase IV inhibitor in patients with type 2 diabetes mellitus.

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  • Antidiabetic Agents and Bone Quality: A Focus on Glycation End Products and Incretin Pathway Modulations
    Muthanna K. Zaki, Mohammed N. Abed, Fawaz A. Alassaf
    Journal of Bone Metabolism.2024; 31(3): 169.     CrossRef
  • Design, synthesis and evaluation of l-quebrachitol derivatives against α-glycosidase
    Maoying Zhang, Xinjie Liang, Pengcheng Cai, Qixun Feng, Yongsong Chen, Xiaoxi Yu, Kuo Zhang, Xuefei Bao, Guoliang Chen
    New Journal of Chemistry.2023; 47(28): 13387.     CrossRef
  • Phase III Study on Efficacy and Safety of Triple Combination (Exenatide/Metformin/Biphasic Insulin Aspart) Therapy for Type 2 Diabetes Mellitus
    Ke Su, Chunmei Lv, Zongwen Ji, Yishu Wang, Haifeng Wang, Ying Bai, Yaping Liu
    American Journal of Therapeutics.2018; 25(6): e609.     CrossRef
  • A Case Report of Diabetes Mellitus with Herniated Intervertebral Lumbar Discs Improved by Korean Medicine Treatment
    Dong-geun Han, A-ryun Choi, You-jin Jung, Ah-hyun Kang, Hye-jin Seo, Jae-yeon Sung, Hyung-chul Lee, Gook-hyun Eom, Woo-sub Song
    The Journal of Internal Korean Medicine.2017; 38(5): 828.     CrossRef
  • A crossover study of the combination therapy of metformin and exenatide or biphasic insulin aspart 30 in overweight or obese patients newly diagnosed with type 2 diabetes mellitus
    Huibiao Quan, Huachuan Zhang, Weiping Wei, Tuanyu Fang, Daoxiong Chen, Kaining Chen
    Experimental and Therapeutic Medicine.2017; 14(4): 3279.     CrossRef
  • Gender-related different effects of a combined therapy of Exenatide and Metformin on overweight or obesity patients with type 2 diabetes mellitus
    Huibiao Quan, Huachuan Zhang, Weiping Wei, Tuanyu Fang
    Journal of Diabetes and its Complications.2016; 30(4): 686.     CrossRef
  • Bioreducible polymers for therapeutic gene delivery
    Young Sook Lee, Sung Wan Kim
    Journal of Controlled Release.2014; 190: 424.     CrossRef
  • Managing diabetes in Asia: Overcoming obstacles and the role of DPP-IV inhibitors
    Yi-Ming Mu, Anoop Misra, John M.F. Adam, Siew Pheng Chan, Francis C.C. Chow, Elaine Cheeay Cunanan, Chaicharn Deerochanawong, Hak Chul Jang, Nguyen Thy Khue, Wayne H.-H. Sheu, Kevin E.K. Tan
    Diabetes Research and Clinical Practice.2012; 95(2): 179.     CrossRef
Original Articles
Thiazolidinediones on Insulin Resistance and Insulin Secretion in Obese Diabetic OLETF Rats.
Jung hyun Noh, Seung hyun Hong, Kyoung hee Lee, Kyoung Min Min, Tae young Yang, Myung shik Lee, Kwang won Kim, Moon kyu Lee
Korean Diabetes J. 2007;31(1):33-43.   Published online January 1, 2007
DOI: https://doi.org/10.4093/jkda.2007.31.1.33
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AbstractAbstract PDF
BACKGROUND
Thiazolidinediones are synthetic peroxisome proliferator-activated receptor-gamma agonists that decrease insulin resistance but, as in vitro and in vivo studies suggest, may have direct beneficial effects on pancreatic beta cells. Here, we investigated the effects of thiazolidinediones (TZDs) on the insulin resistance, beta-cell mass and insulin secretion in obese diabetic OLETF rats. METHODS: We studied insulin resistance (by hyperinsulinemic euglycemic clamp) and insulin secretion (by hyperglycemic clamp) in TZDs administered OLETF and LETO rats. Histologic alterations of the islets were observed and beta-cell mass was also measured by point counting method. RESULTS: Chronic administration of troglitazone (TGZ, 0.15%) or pioglitazone (PGZ, 0.02%) prevented the development of glucose intolerance in OLETF rats, as assessed by oral glucose tolerance test. There was significant difference in submaximal glucose infusion rate between TGZ-treated and untreated OLETF rats during euglycemic clamp studies at 24 weeks of age. At 16 and 24 weeks of ages, beta-cell mass significantly increased in TGZ-treated OLETF rats compared to untreated animals. At 19 weeks and 30 weeks of age, first-phase insulin secretion was not different in PGZ-treated OLETF rats from untreated OLETF rats during hyperglycemic clamp study. At 30 weeks of age, late-phase insulin secretion was decreased in PGZ-treated OLETF rats compared to untreated OLETF rats. The expression of alpha-smooth muscle actin, a marker of activated pancreatic stellate cells that are involved in the fibrosis of the pancreas, in the islets was suppressed by TGZ treatment at 24 weeks of age. CONCLUSION: The treatment of TGZ prevented the development of diabetes, and increased insulin sensitivity and pancreatic beta-cell mass in OLETF rats. These results might be related with the suppression of pancreatic stellate cells. Insulin secretion was not affected by PGZ treatment.
Effects of Peroxisome Proliferator-activated Receptor-gamma(PPARgamma) on the Pancreatic beta Cell Proliferation.
Jung Hyun Noh, Tae Young Yang, In Kyung Jeong, Jae Hun Chung, Yong Ki Min, Myung Shik Lee, Kwang Won Kim, Moon Kyu Lee
Korean Diabetes J. 2003;27(3):241-252.   Published online June 1, 2003
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AbstractAbstract PDF
BACKGROUND
The effects and mechanisms of PPARgamma ligands on the cell proliferation in pancreatic beta cells were examined. METHODS: PPARgamma 1 cDNA was overexpressed in INS-1 cells using an adenoviral vector. The cell proliferations were measured by the MTT assay method, following the treatments with troglitazone (TGZ), rosiglitazone (RGZ), 15d-prostaglandin J2 (15d-PGJ2) or retinoic acid (RA), at increasing doses, in INS-1 and PPARgamma overexpressed INS-1 cells. The apoptosis, telomere length and cell cycles were determined after the PPARgamma ligand treatment. RESULTS: The long-term incubation, with PPARgamma ligands over 24 hr, inhibited the INS-1 cell proliferation rate. Apoptosis was not observed with the PPARgamma ligand treatment. G1 cell cycle arrest was observed with the troglitazone treatment. The telomere length remained unchanged following the TGZ treatment. The basal cell proliferation rate was unaffected by the overexpression of PPARgamma . After 48 h of TGZ treatment, the proliferation of the INS-1 cells was inhibited, in a dose- dependent manner, both with and without the overexpression. Moreover, the degree of inhibition was exaggerated in the PPARgamma overexpressed cells compared to beta gal overexpressed cells. CONCLUSION: PPARgamma ligands have direct inhibitory effects on the proliferation of INS-1 cells. Although the basal cell proliferation rate was not affected by PPARgamma overexpression, the PPARgamma overexpression and PPARgamma ligands have a synergistic inhibitory effect on the cell proliferation rate in pancreatic beta cells. G1 cell cycle arrest may be involved in the reduction of cell proliferation due to PPARgamma ligands.

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