a Department of Endocrinology , G.D Hospital & Diabetes Institute , Kolkata , India.
b Department of Gynecology , G.D Hospital and Diabetes Institute , Kolkata , India.
Expert Rev Clin Pharmacol. 2017 Jun;10(6):633-647. doi: 10.1080/17512433.2017.1318061. Epub 2017 Apr 17.
Both sodium-glucose co-transporter-2 inhibitors (SGLT-2Is) and glucagon-like peptide-1 receptor agonists (GLP-1RAs) have been consistently found to lower blood glucose, body weight and systolic blood pressure (SBP) in patients with type 2 diabetes mellitus (T2DM). While all the SGLT-2Is inhibit glucose reabsorption by blocking SGLT-2 receptor in kidney, dose-dependently, the highest licensed dose of canagliflozin 300-mg has an additional ability to inhibit SGLT-1 receptor in intestine transiently, that may lead to additional inhibition of prandial glucose absorption, unlike other approved highly selective SGLT-2Is. Areas covered: An electronic search on studies with highest licensed dose of all approved SGLT-2Is and long-acting GLP-1RAs was made up to December 2016. We systemically reviewed the studies of canagliflozin 300-mg and compared its glucose, body weight and SBP lowering with other approved SGLT-2Is and GLP-1RAs in their highest approved doses. Expert commentary: From the available evidences, it appears that canagliflozin 300-mg may have the highest potential to improve gluco-metabolic profile in T2DM, amongst the SGLT-2Is class. While the highest approved dosage of GLP-1RAs lowered HbA1c better than canagliflozin 300-mg, weight and SBP lowering could be non-inferior or slightly better with the latter drug. Nonetheless, only head-to-head trial can conclusively answer these questions.
钠-葡萄糖共转运蛋白 2 抑制剂(SGLT-2Is)和胰高血糖素样肽-1 受体激动剂(GLP-1RAs)都被发现可降低 2 型糖尿病患者的血糖、体重和收缩压(SBP)。虽然所有 SGLT-2Is 都通过阻断肾脏中的 SGLT-2 受体来抑制葡萄糖重吸收,但依剂量依赖性,卡格列净 300mg 的最高许可剂量还有另外一种能力,即短暂抑制肠道中的 SGLT-1 受体,这可能导致对餐后葡萄糖吸收的额外抑制,这与其他已批准的高选择性 SGLT-2Is 不同。
截至 2016 年 12 月,对所有已批准的 SGLT-2Is 和长效 GLP-1RAs 的最高许可剂量的研究进行了电子检索。我们系统地回顾了卡格列净 300mg 的研究,并将其与其他已批准的 SGLT-2Is 和 GLP-1RAs 的最高许可剂量相比,比较了其在降低血糖、体重和 SBP 方面的效果。
从现有证据来看,卡格列净 300mg 似乎在改善 2 型糖尿病患者的糖代谢方面具有最大的潜力,这在 SGLT-2Is 类药物中是如此。虽然 GLP-1RAs 的最高批准剂量降低 HbA1c 的效果优于卡格列净 300mg,但后者在降低体重和 SBP 方面可能非劣效或略有优势。然而,只有头对头试验才能最终回答这些问题。