Imran Bushra, Ahsan Farogh, Mahmood Tarique, Khan Mohd Masih Uzzaman, Bano Shahzadi, Zaidi Syed Mehdi Hasan, Ansari Jamal Akhtar, Singh Aditya
Department of Pharmacy, Integral University, Dasauli, Kursi Road, Lucknow (U.P), India.
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Kingdom of Saudi Arabia.
Drug Res (Stuttg). 2025 Jul;75(6):183-201. doi: 10.1055/a-2577-1899. Epub 2025 Apr 28.
Canagliflozin is a synthetic sodium glucose transporter inhibitor (SGLT2i). It is the latest approved class of medicine used in the treatment of type 2 diabetes mellitus. As diabetes is emerging as the most common metabolic disorder, SGLT2i has lightened up the path of treatment with additional benefits. SGLT2 is located in the proximal convoluted tubules of the nephron and is responsible for glucose reabsorption. Thus, inhibiting the SGLT2 leads to a decline in glucose concentration in the plasma. The secondary effects of canagliflozin, such as cardiac protection, renoprotective, and decreased obesity, have made it more putative in the treatment of diabetes mellitus. There are some side effects of canagliflozin, such as volume depletion, genital and urinary tract infection, and lower limb amputation, which could be a matter of concern for patients. Being an anti-diabetic drug, canagliflozin also possesses anti-inflammatory and anti-cancer properties. Several studies have been conducted to determine the efficacy of canagliflozin as an anti-cancer agent. Its pharmacokinetics indicate rapid absorption, reaching peak plasma concentrations within 1-2 hours. With a half-life of approximately 12 hours, it undergoes minimal hepatic metabolism and is primarily excreted unchanged via urine. Common adverse drug reactions (ADRs) include urinary tract infections and dehydration. Clinical trials on canagliflozin, both alone and in combination with other diabetes complications, have been conducted, with some completed and others in various phases. This review article contains information about the pharmacokinetics, drug safety, and efficacy profile of canagliflozin, along with details regarding toxicological studies of canagliflozin.
卡格列净是一种合成的钠葡萄糖协同转运蛋白抑制剂（SGLT2i）。它是最新获批用于治疗2型糖尿病的一类药物。随着糖尿病成为最常见的代谢紊乱疾病，SGLT2i为治疗带来了更多益处，照亮了治疗之路。SGLT2位于肾单位的近端小管，负责葡萄糖重吸收。因此，抑制SGLT2会导致血浆中葡萄糖浓度下降。卡格列净的次要作用，如心脏保护、肾脏保护和减轻肥胖，使其在糖尿病治疗中更具潜力。卡格列净存在一些副作用，如血容量减少、生殖器和尿路感染以及下肢截肢，这可能是患者需要关注的问题。作为一种抗糖尿病药物，卡格列净还具有抗炎和抗癌特性。已经进行了多项研究以确定卡格列净作为抗癌药物的疗效。其药代动力学表明吸收迅速，在1 - 2小时内达到血浆峰值浓度。半衰期约为12小时，肝脏代谢极少，主要通过尿液原形排泄。常见的药物不良反应包括尿路感染和脱水。已经开展了关于卡格列净单独使用以及与其他糖尿病并发症联合使用的临床试验，有些已经完成，有些处于不同阶段。这篇综述文章包含了卡格列净的药代动力学、药物安全性和疗效概况的信息，以及关于卡格列净毒理学研究的详细内容。
