Cahn Avivit, Cernea Simona, Raz Itamar
a The Diabetes Research Unit, Internal Medicine Section , Hadassah Hebrew University Hospital , Jerusalem , Israel.
b Endocrinology and Metabolism Unit, Internal Medicine Section , Hadassah Hebrew University Hospital , Jerusalem , Israel.
Expert Opin Emerg Drugs. 2016 Dec;21(4):409-419. doi: 10.1080/14728214.2016.1257608. Epub 2016 Nov 18.
DPP-4 inhibitors are a class of compounds used for the treatment of type 2 diabetes. The drugs inhibit the degradation of GLP-1, thus amplifying the incretin effect. They have moderate glycemic efficacy, a low propensity of causing hypoglycaemia and are weight neutral. The drugs are often used as second line therapy after metformin. Areas covered: This review summarizes the available compounds in the market and discusses the novel compounds that are currently under development. Several large cardiovascular outcome trials with some of the compounds have been completed, and their results and implications are considered. Fixed dose combination pills are currently the main focus of research and the contribution of these to the care of patients with diabetes is further discussed. Expert opinion: The DPP-4 inhibitors have been a successful class in drug development for diabetes. Taken orally and available as fixed dose combinations with metformin or with SGLT-2 inhibitors, they have reached a large market share of over 7 billion dollars. Other than retagliptin, it does not appear that any additional compound will be launched soon. Currently, the main focus is on the development of additional fixed dose combinations with SGLT-2 inhibitors, but the success of these combinations remains to be seen.
二肽基肽酶-4(DPP-4)抑制剂是一类用于治疗2型糖尿病的化合物。这些药物可抑制胰高血糖素样肽-1(GLP-1)的降解,从而增强肠促胰岛素效应。它们具有中等程度的降糖疗效,引起低血糖的倾向较低,且对体重无影响。这些药物常作为二甲双胍之后的二线治疗药物。涵盖领域:本综述总结了市场上现有的化合物,并讨论了目前正在研发的新型化合物。已经完成了一些使用其中某些化合物的大型心血管结局试验,并对其结果及影响进行了考量。固定剂量复方制剂目前是研究的主要焦点,且进一步讨论了它们对糖尿病患者治疗的贡献。专家观点:DPP-4抑制剂在糖尿病药物研发领域是成功的一类药物。口服给药,可与二甲双胍或钠-葡萄糖协同转运蛋白2(SGLT-2)抑制剂制成固定剂量复方制剂,它们已占据了超过70亿美元的庞大市场份额。除了利格列汀之外,似乎近期不会再有其他化合物上市。目前,主要焦点在于研发与SGLT-2抑制剂的更多固定剂量复方制剂,但其能否成功仍有待观察。