摘要
托格列净(Tofogliflozin)是一种口服活性小分子SGLT2抑制剂,由日本中外(Chugai)制药开发并用于2型糖尿病(T2DM)的治疗。托格列净对SGLT2的选择性抑制作用是SGLT1的2900多倍,与达格列净、坎格列净、伊格列净、伊帕列净和鲁格列净相比具有更强的选择性。本文对托格列净的发现、药效学、药代动力学、副作用及合成路线进行综述。
Tofogliflozin, an orally active small molecule sodium-glucose co-transporter type 2（SGLT2） inhibitor, has been developed by Chugai Pharmaceutical for the treatment of type 2 diabetes mellitus（T2DM）. The IC50 for SGLT1 over SGLT2 was 2900, indicating that tofogliflozin had greater selectivity than dapagliflozin, canagliflozin, ipragliflozin, empagliflozin and luseogliflozin. The discovery, pharmacodynamics, pharmacokinetics, adverse events and synthesis route are summarized in the article.
出处
《国外医药（抗生素分册）》
CAS
2016年第4期154-160,共7页
World Notes on Antibiotics
基金
药食同源植物资源开发四川省高校重点实验室开放基金资助项目(10Y201607)
