Kang Sang-Uk
Kosin University, Department of Life Sciences, 149-1, Dongsam-dong, Yeongdogu, Busan, South Korea.
Drug Discov Today. 2013 Dec;18(23-24):1309-15. doi: 10.1016/j.drudis.2013.09.011. Epub 2013 Sep 20.
Ever since its advent as a promising therapeutic target for type 2 diabetes mellitus (T2DM), G-protein-coupled receptor 119 (GPR119) has received much interest from the pharmaceutical industry. This interest peaked in June 2010, when Sanofi-Aventis agreed to pay Metabolex (Cymabay Therapeutics) US$375 million for MBX-2982, which was a representative orally active GPR119 agonist. However, Sanofi-Aventis opted to terminate the deal in May 2011 and another leading GPR119 agonist, GSK1292263, had a loss of efficacy during its clinical trial. In this review, I discuss the pros and cons of GPR119 through a strengths, weaknesses, opportunities, and threats (SWOT) analysis and propose development strategies for the eventual success of a GPR119 agonist development program.
自从作为2型糖尿病(T2DM)的一个有前景的治疗靶点出现以来,G蛋白偶联受体119(GPR119)就引起了制药行业的广泛关注。这种关注在2010年6月达到顶峰,当时赛诺菲-安万特公司同意向美达步勒克斯公司(西马贝治疗公司)支付3.75亿美元购买MBX-2982,它是一种具有代表性的口服活性GPR119激动剂。然而,赛诺菲-安万特公司在2011年5月选择终止该交易,并且另一种主要的GPR119激动剂GSK1292263在其临床试验期间出现了疗效丧失。在这篇综述中,我通过优势、劣势、机会和威胁(SWOT)分析来讨论GPR119的利弊,并为GPR119激动剂开发项目最终取得成功提出发展策略。