Fotagliptin

Fotagliptin
Clinical data
Other names	SAL067
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name 2-[[3-[(3R)-3-Aminopiperidin-1-yl]-6-methyl-5-oxo-1,2,4-triazin-4-yl]methyl]-4-fluorobenzonitrile;
CAS Number	1312954-58-7;
PubChem CID	53258570;
Chemical and physical data
Formula	C17H19FN6O
Molar mass	342.378 g·mol−1

Fotagliptin (SAL067) is a DPP-4 inhibitor under development for the treatment of type 2 diabetes. Like other DPP-4 inhibitors, it works by increasing endogenously produced GLP-1 and GIP.^[1]^[2]^[3] In a phase 3 trial it showed similar results as alogliptin.^[4]

References

^ Wu, Min; Li, Qian‐Qian; Zhang, Hong; Zhu, Xiao‐Xue; Li, Xiao‐Jiao; Li, Ying; Sun, Hai‐Gang; Ding, Yan‐Hua (June 2021). "Safety, Pharmacokinetics, and Pharmacodynamics of a Dipeptidyl Peptidase‐4 Inhibitor: A Randomized, Double‐Blinded, Placebo‐Controlled Daily Administration of Fotagliptin Benzoate for 14 Days for Type 2 Diabetes Mellitus". Clinical Pharmacology in Drug Development. 10 (6): 660–668. doi:10.1002/cpdd.895. ISSN 2160-763X. PMID 33440080. S2CID 231606176.
^ Fang, Lan; Gao, Zhenguo; Wu, Songgu; Jia, Shengzhe; Wang, Jingkang; Rohani, Sohrab; Gong, Junbo (1 August 2021). "Ultrasound-assisted solution crystallization of fotagliptin benzoate: Process intensification and crystal product optimization". Ultrasonics Sonochemistry. 76: 105634. doi:10.1016/j.ultsonch.2021.105634. ISSN 1350-4177. PMC 8261672. PMID 34218067.
^ Ding, Yanhua; Zhang, Hong; Li, Cuiyun; Zheng, WenBo; Wang, Meng; Li, Ying; Sun, HaiGang; Wu, Min (3 June 2021). "Safety and pharmacokinetic interaction between fotagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin in healthy subjects". Expert Opinion on Drug Metabolism & Toxicology. 17 (6): 725–731. doi:10.1080/17425255.2021.1915283. PMID 33899649. S2CID 233400233.
^ Xu, Mingtong; Sun, Kan; Xu, Wenjie; Wang, Chuan; Yan, Dewen; Li, Shu; Cong, Li; Pi, Yinzhen; Song, Weihong; Sun, Qingyuan; Xiao, Rijun; Peng, Weixia; Wang, Jianping; Peng, Hui; Zhang, Yawei; Duan, Peng; Zhang, Meiying; Liu, Jianying; Huang, Qingmei; Li, Xuefeng; Bao, Yan; Zeng, Tianshu; Wang, Kun; Qin, Li; Wu, Chaoming; Deng, Chunying; Huang, Chenghu; Yan, Shuang; Zhang, Wei; Li, Meizi; Sun, Li; Wang, Yanjun; Li, HongMei; Wang, Guang; Pang, Shuguang; Zheng, Xianling; Wang, Haifang; Wang, Fujun; Su, Xiuhai; Ma, Yujin; Zhang, Wei; Li, Ziling; Xie, Zuoling; Xu, Ning; Ni, Lin; Zhang, Li; Deng, Xiangqun; Pan, Tianrong; Dong, Qijuan; Wu, Xiaohong; Shen, Xingping; Zhang, Xin; Zou, Qijing; Jiang, Chengxia; Xi, Jue; Ma, Jianhua; Sun, Jingchao; Yan, Li (2023). "Fotagliptin monotherapy with alogliptin as an active comparator in patients with uncontrolled type 2 diabetes mellitus: a randomized, multicenter, double-blind, placebo-controlled, phase 3 trial". BMC Medicine. 21 (1): 388. doi:10.1186/s12916-023-03089-x. ISSN 1741-7015. PMC 10563289. PMID 37814306.

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[1] Wu, Min; Li, Qian‐Qian; Zhang, Hong; Zhu, Xiao‐Xue; Li, Xiao‐Jiao; Li, Ying; Sun, Hai‐Gang; Ding, Yan‐Hua (June 2021). "Safety, Pharmacokinetics, and Pharmacodynamics of a Dipeptidyl Peptidase‐4 Inhibitor: A Randomized, Double‐Blinded, Placebo‐Controlled Daily Administration of Fotagliptin Benzoate for 14 Days for Type 2 Diabetes Mellitus". Clinical Pharmacology in Drug Development. 10 (6): 660–668. doi:10.1002/cpdd.895. ISSN 2160-763X. PMID 33440080. S2CID 231606176.

[2] Fang, Lan; Gao, Zhenguo; Wu, Songgu; Jia, Shengzhe; Wang, Jingkang; Rohani, Sohrab; Gong, Junbo (1 August 2021). "Ultrasound-assisted solution crystallization of fotagliptin benzoate: Process intensification and crystal product optimization". Ultrasonics Sonochemistry. 76: 105634. doi:10.1016/j.ultsonch.2021.105634. ISSN 1350-4177. PMC 8261672. PMID 34218067.

[3] Ding, Yanhua; Zhang, Hong; Li, Cuiyun; Zheng, WenBo; Wang, Meng; Li, Ying; Sun, HaiGang; Wu, Min (3 June 2021). "Safety and pharmacokinetic interaction between fotagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin in healthy subjects". Expert Opinion on Drug Metabolism & Toxicology. 17 (6): 725–731. doi:10.1080/17425255.2021.1915283. PMID 33899649. S2CID 233400233.

[4] Xu, Mingtong; Sun, Kan; Xu, Wenjie; Wang, Chuan; Yan, Dewen; Li, Shu; Cong, Li; Pi, Yinzhen; Song, Weihong; Sun, Qingyuan; Xiao, Rijun; Peng, Weixia; Wang, Jianping; Peng, Hui; Zhang, Yawei; Duan, Peng; Zhang, Meiying; Liu, Jianying; Huang, Qingmei; Li, Xuefeng; Bao, Yan; Zeng, Tianshu; Wang, Kun; Qin, Li; Wu, Chaoming; Deng, Chunying; Huang, Chenghu; Yan, Shuang; Zhang, Wei; Li, Meizi; Sun, Li; Wang, Yanjun; Li, HongMei; Wang, Guang; Pang, Shuguang; Zheng, Xianling; Wang, Haifang; Wang, Fujun; Su, Xiuhai; Ma, Yujin; Zhang, Wei; Li, Ziling; Xie, Zuoling; Xu, Ning; Ni, Lin; Zhang, Li; Deng, Xiangqun; Pan, Tianrong; Dong, Qijuan; Wu, Xiaohong; Shen, Xingping; Zhang, Xin; Zou, Qijing; Jiang, Chengxia; Xi, Jue; Ma, Jianhua; Sun, Jingchao; Yan, Li (2023). "Fotagliptin monotherapy with alogliptin as an active comparator in patients with uncontrolled type 2 diabetes mellitus: a randomized, multicenter, double-blind, placebo-controlled, phase 3 trial". BMC Medicine. 21 (1): 388. doi:10.1186/s12916-023-03089-x. ISSN 1741-7015. PMC 10563289. PMID 37814306.

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