Steps in discovery of alogliptin

S. Chaudhry, Abhijit Tailokya, Gopal Wawde, Yogesh Bhide, Kavita Inamdar
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Abstract

Alogliptin was initially approved to treat T2DM in Japan in 2010 and then approved by FDA and by EMA in 2013. Alogliptin, a highly potent and selective, noncovalent inhibitor of DPP-4. Inhibition of DPP-4 activity, alogliptin slows the inactivation of incretin hormones, glucagon-like peptide-1 (GLP-1). In terms of drug safety alogliptin is generally well-tolerated, with a low risk of hypoglycemia, weight gain, acute pancreatitis, and hepatotoxicity. Alogliptin has been effectively combined with Metformin or Pioglitazone to provide better glycaemic control. The drug can be used in mild hepatic or renal impairment with appropriate dosage adjustment. Treatment with alogliptin has shown less weight gain compared with sulfonylureas. Alogliptin and FDC of Alogliptin + Metformin approved and available in India with brand name Aloja & Aloja M/Forte, with well documented safety and efficacy through phase IV study conducted in India.
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发现阿格列汀的步骤
阿格列汀最初于 2010 年在日本获批用于治疗 T2DM,随后于 2013 年获得美国食品药品管理局和欧洲药品管理局的批准。阿格列汀是一种强效、高选择性的 DPP-4 非共价抑制剂。通过抑制 DPP-4 的活性,阿格列汀可减缓增量素激素、胰高血糖素样肽-1(GLP-1)的灭活。就药物安全性而言,阿格列汀一般耐受性良好,发生低血糖、体重增加、急性胰腺炎和肝毒性的风险较低。阿格列汀与二甲双胍或吡格列酮联用可有效控制血糖。在适当调整剂量的情况下,该药物可用于轻度肝功能或肾功能受损的患者。与磺脲类药物相比,阿格列汀治疗后体重增加较少。阿格列汀和阿格列汀+二甲双胍的 FDC 已获批准并在印度上市,品牌名称为 Aloja & Aloja M/Forte,在印度进行的 IV 期研究充分证明了其安全性和有效性。
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