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Drugs. 2013 Jun;73(9):979-88. doi: 10.1007/s40265-013-0064-9.
Canagliflozin (Invokana™), an oral selective sodium-glucose co-transporter 2 (SGLT2) inhibitor, is under global development with Mitsubishi Tanabe Pharma and Janssen Pharmaceuticals, a subsidiary of Johnson and Johnson, for the treatment of type 2 diabetes mellitus. SGLT2 are mainly located in the proximal tubule of the kidney and are involved in the reabsorption of filtered glucose from the glomeruli into the body. Inhibition of SGLT2 lowers blood glucose in an insulin independent manner as a consequence of blocking reabsorption of filtered glucose in the glomeruli, thereby increasing urinary excretion of glucose and, in turn, potentially reducing bodyweight. Canagliflozin is the first SGLT2 inhibitor to be approved in the USA and is under regulatory review in the EU. This article summarizes the milestones in the development of canagliflozin, leading to its first approval for use in adults with type 2 diabetes.
卡格列净（Invokana™），一种口服选择性钠-葡萄糖共转运蛋白 2（SGLT2）抑制剂，由武田制药和强生旗下杨森制药公司共同开发，用于治疗 2 型糖尿病。SGLT2 主要位于肾脏的近端小管，参与从肾小球滤过的葡萄糖重吸收到体内。SGLT2 的抑制作用可降低血糖，其机制为阻止肾小球滤过的葡萄糖重吸收，从而增加尿葡萄糖排泄，进而可能降低体重。卡格列净是首个在美国获批的 SGLT2 抑制剂，在欧盟也正在接受监管审查。本文总结了卡格列净的研发里程碑，最终使其获得批准，用于治疗成人 2 型糖尿病。
