Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antidiabetic agent for the treatment of type 2 diabetes mellitus. They increase endogenous levels of incretin hormones, which stimulate glucose-dependent insulin secretion, decrease glucagon secretion, and contribute to reducing postprandial hyperglycemia. Although DPP-4 inhibitors have similar benefits, they can be differentiated in terms of their chemical structure, pharmacology, efficacy and safety profiles, and clinical considerations. Gemigliptin (brand name: Zemiglo), developed by LG Life Sciences, is a potent, selective, competitive, and long acting DPP-4 inhibitor. Various studies have shown that gemigliptin is an optimized DPP-4 inhibitor in terms of efficacy, safety, and patient compliance for treatment of type 2 diabetes mellitus. In this review, we summarize the characteristics of gemigliptin and discuss its potential benefits in clinical practice.

Citations

Citations to this article as recorded by  

• A Multicenter, Randomized, Open-Label Study to Compare the Effects of Gemigliptin Add-on or Escalation of Metformin Dose on Glycemic Control and Safety in Patients with Inadequately Controlled Type 2 Diabetes Mellitus Treated with Metformin and SGLT-2 Inh
  Hae Jin Kim, Jung Hyun Noh, Min Kyong Moon, Sung Hee Choi, Seung-Hyun Ko, Eun-Jung Rhee, Kyu Yeon Hur, In-Kyung Jeong, Mark Yorek
  Journal of Diabetes Research.2024; 2024: 1.     CrossRef
• Gemigliptin, a potent selective dipeptidyl peptidase 4 inhibitor, protects endothelial progenitor cells by oxidative stress via caspase-3 dependent pathway
  Mijung Lee, Amna Rashid Tariq, Manho Kim
  Biochemistry and Biophysics Reports.2024; 38: 101673.     CrossRef
• Selective targeting of dipeptidyl‐peptidase 4 (DPP‐4) positive senescent chondrocyte ameliorates osteoarthritis progression
  Du Hyun Ro, Gun Hee Cho, Ji Yoon Kim, Seong Ki Min, Ha Ru Yang, Hee Jung Park, Sun Young Wang, You Jung Kim, Myung Chul Lee, Hyun Cheol Bae, Hyuk‐Soo Han
  Aging Cell.2024;[Epub]     CrossRef
• Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM)
  Dong-Wei Shao, Li-Jie Zhao, Jin-Feng Sun
  European Journal of Medicinal Chemistry.2024; 272: 116464.     CrossRef
• Financial Benefits of Renal Dose-Adjusted Dipeptidyl Peptidase-4 Inhibitors for Patients with Type 2 Diabetes and Chronic Kidney Disease
  Hun Jee Choe, Yeh-Hee Ko, Sun Joon Moon, Chang Ho Ahn, Kyoung Hwa Ha, Hyeongsuk Lee, Jae Hyun Bae, Hyung Joon Joo, Hyejin Lee, Jang Wook Son, Dae Jung Kim, Sin Gon Kim, Kwangsoo Kim, Young Min Cho
  Endocrinology and Metabolism.2024; 39(4): 622.     CrossRef
• Efficient integration of analytical quality-by-design and tri-hued HPLC-DAD approach for synchronized assessment of gemigliptin and rosuvastatin in their fixed-dose pills: Application to stability study
  Sara M. Mohyeldin, Hoda G. Daabees, Wael Talaat, Miranda F. Kamal
  Sustainable Chemistry and Pharmacy.2024; 42: 101777.     CrossRef
• Opportunities and challenges of incretin-based hypoglycemic agents treating type 2 diabetes mellitus from the perspective of physiological disposition
  Yaochen Xie, Qian Zhou, Qiaojun He, Xiaoyi Wang, Jincheng Wang
  Acta Pharmaceutica Sinica B.2023; 13(6): 2383.     CrossRef
• Therapeutic Effects of Switching to Anagliptin from Other DPP-4 Inhibitors in T2DM Patients with Inadequate Glycemic Control: A Non-interventional, Single-Arm, Open-Label, Multicenter Observational Study
  Sang-Yong Kim, Sungrae Kim
  Diabetes Therapy.2023; 14(1): 109.     CrossRef
• Pharmacokinetic and pharmacodynamic interaction of DWP16001, a sodium–glucose cotransporter 2 inhibitor, with gemigliptin and metformin in healthy adults
  Sae Im Jeong, Yun Kim, Jae Jin Nah, Wan Huh, In‐Jin Jang, Jun Gi Hwang, SeungHwan Lee
  British Journal of Clinical Pharmacology.2023; 89(6): 1780.     CrossRef
• 1,2,3‐Triazole analogs with bulky and conformationally rigid substructures: Synthesis and in vitro evaluation as DPP‐4 inhibitors
  Duy‐Viet Vo, Jongkook Lee, Haeil Park
  Bulletin of the Korean Chemical Society.2023; 44(5): 425.     CrossRef
• DPP-4 inhibitors for treating T2DM - hype or hope? an analysis based on the current literature
  Kunika Saini, Smriti Sharma, Yousuf Khan
  Frontiers in Molecular Biosciences.2023;[Epub]     CrossRef
• The effect of gemigliptin treatment on immune parameters including regulatory T cells in patients with type 2 diabetes and moderate to very severe chronic renal impairment
  Yanghyeon Kim, Nagyeom Lee, Sujung Heo, Ye Na Kim, Ho Sik Shin, Yeonsoon Jung, Hark Rim
  Medicine.2023; 102(49): e36455.     CrossRef
• Increasing Age Associated with Higher Dipeptidyl Peptidase-4 Inhibition Rate Is a Predictive Factor for Efficacy of Dipeptidyl Peptidase-4 Inhibitors
  Sangmo Hong, Chang Hee Jung, Song Han, Cheol-Young Park
  Diabetes & Metabolism Journal.2022; 46(1): 63.     CrossRef
• Does DPP-IV Inhibition Offer New Avenues for Therapeutic Intervention in Malignant Disease?
  Petr Busek, Jonathan S. Duke-Cohan, Aleksi Sedo
  Cancers.2022; 14(9): 2072.     CrossRef
• Divergent Reaction of Activated Pyridines with α,α-Difluorinated gem-Diols: Regioselective Synthesis of gem-Difluorinated Dihydropyridines and Dihydropyridones
  Koushik Patra, Mallu Kesava Reddy, Sumitava Mallik, Mahiuddin Baidya
  Organic Letters.2022; 24(22): 4014.     CrossRef
• Gemigliptin exerts protective effects against doxorubicin-induced hepatotoxicity by inhibiting apoptosis via the regulation of fibroblast growth factor 21 expression
  Kyeong-Min Lee, Yeo Jin Hwang, Gwon-Soo Jung
  Biochemical and Biophysical Research Communications.2022; 626: 135.     CrossRef
• FDA-Approved Trifluoromethyl Group-Containing Drugs: A Review of 20 Years
  Aathira Sujathan Nair, Ashutosh Kumar Singh, Astik Kumar, Sunil Kumar, Sunitha Sukumaran, Vishal Payyalot Koyiparambath, Leena K. Pappachen, T. M. Rangarajan, Hoon Kim, Bijo Mathew
  Processes.2022; 10(10): 2054.     CrossRef
• Glucagon-like peptide-1 (GLP-1) receptor agonists and neuroinflammation: Implications for neurodegenerative disease treatment
  Katherine O. Kopp, Elliot J. Glotfelty, Yazhou Li, Nigel H. Greig
  Pharmacological Research.2022; 186: 106550.     CrossRef
• An evaluation of drug lag for new drugs approved by the Indian regulator relative to the United States, European Union, and Japanese regulatory agencies
  Mahanjit Konwar, Mitesh R. Maurya, Tushar B. Nishandar, Urmila M. Thatte, Nithya J. Gogtay
  Perspectives in Clinical Research.2021; 12(3): 159.     CrossRef
• Pharmacokinetic and Pharmacodynamic Comparison of Two Formulations of a Fixed-Dose Combination of Gemigliptin/Rosuvastatin 50/20 mg: A Randomized, Open-Label, Single-Dose, Two-Way Crossover Study
  Eunsol Yang, Hyounggyoon Yoo, In-Jin Jang, Kyung-Sang Yu, SeungHwan Lee
  Drug Design, Development and Therapy.2021; Volume 15: 651.     CrossRef
• Efficacy and Safety of the Novel Dipeptidyl Peptidase-4 Inhibitor Gemigliptin in the Management of Type 2 Diabetes: A Meta-Analysis
  Deep Dutta, Anshita Agarwal, Indira Maisnam, Rajiv Singla, Deepak Khandelwal, Meha Sharma
  Endocrinology and Metabolism.2021; 36(2): 374.     CrossRef
• Structure–Activity Relationship Analysis of Cocrystallized Gliptin-like Pyrrolidine, Trifluorophenyl, and Pyrimidine-2,4-Dione Dipeptidyl Peptidase-4 Inhibitors
  Katarina Tomovic, Budimir S. Ilic, Andrija Smelcerovic
  Journal of Medicinal Chemistry.2021; 64(14): 9639.     CrossRef
• A review upon medicinal perspective and designing rationale of DPP-4 inhibitors
  Shubham Kumar, Anu Mittal, Amit Mittal
  Bioorganic & Medicinal Chemistry.2021; 46: 116354.     CrossRef
• Effect of Dipeptidyl Peptidase-4 (DPP-4) Inhibition on Biomarkers of Kidney Injury and Vascular Calcification in Diabetic Kidney Disease: A Randomized Controlled Trial
  Thananda Trakarnvanich, Bancha Satirapoj, Swangjit Suraamornkul, Thanit Chirananthavat, Anoma Sanpatchayapong, Torpong Claimon, Eusebio Chiefari
  Journal of Diabetes Research.2021; 2021: 1.     CrossRef
• Antidiabetic effect of gemigliptin: a systematic review and meta-analysis of randomized controlled trials with Bayesian inference through a quality management system
  Hojin Oh, Hai Duc Nguyen, In Mo Yoon, Byung-Ryong Ahn, Min-Sun Kim
  Scientific Reports.2021;[Epub]     CrossRef
• Pleiotropic Benefits of DPP-4 Inhibitors Beyond Glycemic Control
  Seon Mee Kang, Jeong Hyun Park
  Clinical Medicine Insights: Endocrinology and Diabetes.2021;[Epub]     CrossRef
• The vasodilatory effect of gemigliptin via activation of voltage-dependent K+ channels and SERCA pumps in aortic smooth muscle
  Hee Seok Jung, Mi Seon Seo, Jin Ryeol An, Minji Kang, Ryeon Heo, Hongliang Li, Won-Kyo Jung, Il-Whan Choi, Eun-Hee Cho, Hongzoo Park, Young Min Bae, Won Sun Park
  European Journal of Pharmacology.2020; 882: 173243.     CrossRef
• Development and Validation of a Rapid and Sensitive Method for the Simultaneous Estimation of Gemigliptin and Teneligliptin in Bulk and Dosage Forms by Using Liquid Chromatography-tandem Mass Spectrometry
  Amrish Chandra, Ramji Rathod, Faraat Ali, Anuj Prakash, Robin Kumar, Gyanendra Nath Singh
  Current Pharmaceutical Analysis.2020; 16(8): 1104.     CrossRef
• Incretin Mimetics as Rational Candidates for the Treatment of Traumatic Brain Injury
  Elliot J. Glotfelty, Thomas E. Delgado, Luis B. Tovar-y-Romo, Yu Luo, Barry J. Hoffer, Lars Olson, Tobias E. Karlsson, Mark P. Mattson, Brandon K. Harvey, David Tweedie, Yazhou Li, Nigel H. Greig
  ACS Pharmacology & Translational Science.2019; 2(2): 66.     CrossRef
• Mechanisms and pathways of anti‐inflammatory activity of DPP‐4 inhibitors in cardiovascular and renal protection
  Katarina Tomovic, Jelena Lazarevic, Gordana Kocic, Marina Deljanin‐Ilic, Marko Anderluh, Andrija Smelcerovic
  Medicinal Research Reviews.2019; 39(1): 404.     CrossRef
• Dipeptidyl Peptidase-4 Inhibitors versus Other Antidiabetic Drugs Added to Metformin Monotherapy in Diabetic Retinopathy Progression: A Real World-Based Cohort Study
  Yoo-Ri Chung, Kyoung Hwa Ha, Hyeon Chang Kim, Sang Jun Park, Kihwang Lee, Dae Jung Kim
  Diabetes & Metabolism Journal.2019; 43(5): 640.     CrossRef
• Effect of gemigliptin on cardiac ischemia/reperfusion and spontaneous hypertensive rat models
  Dae-Hwan Nam, Jinsook Park, Sun-Hyun Park, Ki-Suk Kim, Eun Bok Baek
  The Korean Journal of Physiology & Pharmacology.2019; 23(5): 329.     CrossRef
• Clinical Use of DPP-4 Inhibitors
  Baptist Gallwitz
  Frontiers in Endocrinology.2019;[Epub]     CrossRef
• Efficacy and Safety of Switching to Teneligliptin in Patients with Type 2 Diabetes Inadequately Controlled with Dipeptidyl Peptidase-4 Inhibitors: A 12-Week Interim Report
  Hae Jin Kim, Young Sik Kim, Chang Beom Lee, Moon-Gi Choi, Hyuk-Jae Chang, Soo Kyoung Kim, Jae Myung Yu, Tae Ho Kim, Ji Hyun Lee, Kyu Jeung Ahn, Kyoungmin Kim, Kwan Woo Lee
  Diabetes Therapy.2019; 10(4): 1271.     CrossRef
• Efficacy and Safety of Gemigliptin in Post-Transplant Patients With Type 2 Diabetes Mellitus
  Jaehyun Bae, Youjin Kim, Yongin Cho, Minyoung Lee, Ji-Yeon Lee, Yong-ho Lee, Byung-Wan Lee, Bong-Soo Cha, Dong Jin Joo, Kyu Ha Huh, Myoung Soo Kim, Yu Seun Kim, Eun Seok Kang
  Transplantation Proceedings.2019; 51(10): 3444.     CrossRef
• Protective effects of gemigliptin against type II collagen degradation in human chondrocytes
  Momin Mohetaer, Guoqing Li, Yang Wang, Li Cao
  Biomedicine & Pharmacotherapy.2018; 104: 590.     CrossRef
• Pharmacokinetic Interactions Between Gemigliptin and Metformin, and Potential Differences in the Pharmacokinetic Profile of Gemigliptin Between the Mexican and Korean Populations: A Randomized, Open-label Study in Healthy Mexican Volunteers
  Ignacio Conde-Carmona, Sandra García-Medina, Juan M. Jiménez-Vargas, Alberto Martínez-Muñoz, Sung-Hack Lee
  Clinical Therapeutics.2018; 40(10): 1729.     CrossRef
• Comparative efficacy and safety of gemigliptin versus linagliptin in type 2 diabetes patients with renal impairment: A 40‐week extension of the GUARD randomized study
  Sang Youb Han, Sun Ae Yoon, Byoung Geun Han, Sung Gyun Kim, Young‐Il Jo, Kyung Hwan Jeong, Kook‐Hwan Oh, Hyeong Cheon Park, Sun‐Hee Park, Shin‐Wook Kang, Ki‐Ryang Na, Sun Woo Kang, Nam‐Ho Kim, Younghwan Jang, Bogyeong Kim, Seonghye Shin, Dae Ryong Cha
  Diabetes, Obesity and Metabolism.2018; 20(2): 292.     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
• Gemigliptin: Newer promising gliptin for type 2 diabetes mellitus
  Manish Gutch, Abhay Joshi, Sukriti Kumar, Avinash Agarwal, RajendraKumar Pahan, SyedMohd Razi
  Indian Journal of Endocrinology and Metabolism.2017; 21(6): 898.     CrossRef
• Protective Effects of Gemigliptin, a Dipeptidyl Peptidase-4 Inhibitor, against Cisplatin-Induced Nephrotoxicity in Mice
  Seung Hee Choi, Jaechan Leem, In-Kyu Lee
  Mediators of Inflammation.2017; 2017: 1.     CrossRef
• Effects of gemigliptin, a dipeptidyl peptidase‐4 inhibitor, on lipid metabolism and endotoxemia after a high‐fat meal in patients with type 2 diabetes
  Chang Ho Ahn, Eun Ky Kim, Se Hee Min, Tae Jung Oh, Young Min Cho
  Diabetes, Obesity and Metabolism.2017; 19(3): 457.     CrossRef
• Efficacy and safety of gemigliptin, a dipeptidyl peptidase‐4 inhibitor, in patients with type 2 diabetes mellitus inadequately controlled with combination treatment of metformin and sulphonylurea: a 24‐week, multicentre, randomized, double‐blind, placebo‐
  Chang Ho Ahn, Kyung Ah Han, Jae Myung Yu, Joo Young Nam, Kyu Jeung Ahn, Tae Keun Oh, Hyoung Woo Lee, Dae Ho Lee, Jaetaek Kim, Choon Hee Chung, Tae Sun Park, Byung Joon Kim, Seok Won Park, Hyeong Kyu Park, Kwang Jae Lee, Sang‐Wook Kim, Jeong Hyun Park, Kwa
  Diabetes, Obesity and Metabolism.2017; 19(5): 635.     CrossRef