Institut d'Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), Rosselló, 149-153, 08036, Barcelona, Spain.
Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) MultiMedica, Milan, Italy.
Drugs. 2019 May;79(7):733-750. doi: 10.1007/s40265-019-01086-0.
Teneligliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that was approved for the treatment of type 2 diabetes mellitus (T2DM) in Japan and Korea and is being researched in several countries. Teneligliptin is a potent, selective, and long-lasting DPP-4 inhibitor with a t of approximately 24 h and unique pharmacokinetic properties: it is metabolized by cytochrome P450 (CYP) 3A4 and flavin-containing monooxygenase 3 (FMO3), or excreted from the kidney in an unchanged form. Because of its multiple elimination pathways, dose adjustment is not needed in patients with hepatic or renal impairment, and it is considered to have a low potential for drug-drug interactions. Clinical studies and postmarketing surveillance show that teneligliptin, administered as monotherapy and/or in combination with antihyperglycemic agents, is effective and well tolerated in T2DM patients, including in elderly patients and those with renal impairment. Furthermore, teneligliptin has antioxidative properties, which induce the antioxidant cascade, as well as ·OH scavenging properties. In addition, it has shown endothelial protective effects in several non-clinical and clinical studies. From its unique profile and clinical data, teneligliptin represents a potential therapeutic option in a wide variety of patients, including elderly diabetic patients and those with renal impairment. The fixed-dose combination (FDC) tablet of teneligliptin and canagliflozin has been approved in Japan; this is the first FDC tablet of a DPP-4 inhibitor and sodium glucose co-transporter 2 inhibitor in Japan, and the third globally. The FDC tablet may also provide additional prescribing and adherence benefits.
替格列汀是一种二肽基肽酶-4（DPP-4）抑制剂，已在日本和韩国获批用于治疗 2 型糖尿病（T2DM），并正在多个国家进行研究。替格列汀是一种强效、选择性和长效的 DPP-4 抑制剂，t1/2 约为 24 小时，具有独特的药代动力学特性：它主要通过细胞色素 P450（CYP）3A4 和黄素单加氧酶 3（FMO3）代谢，或以原形从肾脏排泄。由于其具有多种消除途径，因此肝或肾功能损害的患者无需调整剂量，并且认为其与药物相互作用的潜力较低。临床研究和上市后监测表明，替格列汀作为单药治疗和/或与抗高血糖药物联合使用，在 T2DM 患者中有效且耐受性良好，包括老年患者和肾功能损害患者。此外，替格列汀具有抗氧化特性，可诱导抗氧化级联反应和·OH 清除特性。此外，它在几项非临床和临床研究中表现出内皮保护作用。从其独特的特征和临床数据来看，替格列汀代表了广泛的患者，包括老年糖尿病患者和肾功能损害患者的潜在治疗选择。替格列汀和卡格列净的固定剂量复方片剂已在日本获得批准；这是日本首个 DPP-4 抑制剂和钠-葡萄糖共转运蛋白 2 抑制剂的固定剂量复方片剂，也是全球第三个。固定剂量复方片剂还可能提供额外的处方和依从性益处。
