Abstract: Type 2 diabetes mellitus (T2DM) is an emerging epidemic in Asian countries, especially in India. With the advent of the SGLT2 inhibitor class of drugs demonstrating benefits beyond glycemic control, viz. weight loss, blood pressure reduction, and cardiovascular and renal protection, the management of T2DM has taken a quantum leap. Remogliflozin etabonate (RE) is the latest addition to the SGLT2 inhibitor class of drugs that have been recently approved in India for the management of T2DM. RE is a potent and selective inhibitor of SGLT2 with the unique distinction of being administered as a prodrug, existence of active metabolites, and short half-life necessitating twice-daily dosing. The Phase III study of RE demonstrated it to be an efficacious and safe agent and non-inferior to the currently available SGLT2 inhibitors. This paper reviews not only the pharmacokinetics, pharmacodynamics, clinical efficacy, and safety profile of RE but also its molecular and clinical development program. This review has taken into consideration all available published as well as unpublished literature on RE and discusses the individual studies performed during its development for characterization of pharmacological profile.

Keywords: remogliflozin, etabonate, SGLT2 inhibitor, design, development, place in therapy, T2DM


中文翻译：

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雷莫格列净在2型糖尿病的治疗中的应用：设计，开发和放置。

摘要：2型糖尿病（T2DM）在亚洲国家（尤其是印度）正在流行。随着SGLT2抑制剂类药物的问世，其显示出超越血糖控制的益处，即。体重减轻，血压降低以及心血管和肾脏保护，T2DM的管理有了巨大的飞跃。依莫格列净依替膦酸盐（RE）是SGLT2抑制剂类药物的最新成员，该药物最近已在印度获得批准用于治疗T2DM。RE是SGLT2的有效和选择性抑制剂，其独特之处在于前药，活性代谢产物的存在以及半衰期短，因此需要每天两次给药。RE的III期研究表明，它是一种有效且安全的药物，并且不逊色于目前可用的SGLT2抑制剂。本文不仅回顾了RE的药代动力学，药效学，临床疗效和安全性，还回顾了其分子和临床开发计划。这篇综述考虑了关于RE的所有可用的已发表和未发表的文献，并讨论了在其发展过程中为表征药理特性而进行的个别研究。

关键字：雷莫列净，依博替尼，SGLT2抑制剂，设计，开发，治疗位置，T2DM