Janagliflozin

Janagliflozin
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name (2S,3R,4R,5S,6R)-2-[3-[[4-[[(1R,5S)-3-bicyclo[3.1.0]hexanyl]oxy]phenyl]methyl]-4-chlorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol;
CAS Number	1800115-22-3;
PubChem CID	91820686;
DrugBank	DB16209;
UNII	WK4RT85HCA;
Chemical and physical data
Formula	C25H29ClO6
Molar mass	460.95 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1[C@H]2[C@@H]1CC(C2)OC3=CC=C(C=C3)CC4=C(C=CC(=C4)[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O)Cl;
	InChI InChI=1S/C25H29ClO6/c26-20-6-3-14(25-24(30)23(29)22(28)21(12-27)32-25)8-17(20)7-13-1-4-18(5-2-13)31-19-10-15-9-16(15)11-19/h1-6,8,15-16,19,21-25,27-30H,7,9-12H2/t15-,16+,19?,21-,22-,23+,24-,25+/m1/s1; Key:WDBIPGHUEJEKTC-VWQPKTIXSA-N;

Janagliflozin is an experimental SGLT2 inhibitor developed by Sihuan Pharmaceutical.^[1]^[2]^[3]^[4]^[5]^[6]

References

^ Song, Ling; Yao, Xueting; Liu, Yang; Zhong, Wen; Jiang, Ji; Liu, Hongzhong; Zhou, Huimin; Shi, Chongtie; Zong, Kaiqi; Wang, Chong; Ma, Chuanxiang; Liu, Dongyang; Hu, Pei (April 2020). "Translational prediction of first-in-human pharmacokinetics and pharmacodynamics of janagliflozin, a selective SGLT2 inhibitor, using allometric scaling, dedrick and PK/PD modeling methods". European Journal of Pharmaceutical Sciences. 147: 105281. doi:10.1016/j.ejps.2020.105281. S2CID 212405270.
^ Liu, Dongyang; Song, Ling; Wang, Xiaoxu; Liu, Xu; Cao, Fangrui; Liu, Hongzhong; Ding, Yanhua; Xiao, Xinhua; Jiang, Ji; Hu, Pei (1 June 2019). "154-LB: Accelerating Clinical Development of Janagliflozin, a Novel Antidiabetic Drug, Using Model-Informed Drug Development Strategy". Diabetes. 68 (Supplement_1). doi:10.2337/db19-154-LB. S2CID 195440798.
^ Zhao, Hengli; Wei, Yilin; He, Kun; Zhao, Xiaoyu; Mu, Hongli; Wen, Qing (December 2022). "Prediction of janagliflozin pharmacokinetics in type 2 diabetes mellitus patients with liver cirrhosis or renal impairment using a physiologically based pharmacokinetic model". European Journal of Pharmaceutical Sciences. 179: 106298. doi:10.1016/j.ejps.2022.106298. PMID 36162752. S2CID 252505056.
^ Zhao, Hengli; Zhao, Zhirui; He, Kun; Mi, Nianrong; Lou, Kai; Dong, Xiaolin; Zhang, Wenyu; Sun, Jingfang; Hu, Xinyu; Pang, Shuguang; Cheng, Hong; Wen, Qing (August 2023). "Pharmacokinetics, Pharmacodynamics and Safety of Janagliflozin in Chinese Type 2 Diabetes Mellitus Patients with Renal Impairment". Clinical Pharmacokinetics. 62 (8): 1093–1103. doi:10.1007/s40262-023-01256-0. PMID 37284974. S2CID 259097798.
^ Gao, Leili; Cheng, Zhifeng; Su, Benli; Su, Xiuhai; Song, Weihong; Guo, Yushan; Liao, Lin; Chen, Xiaowen; Li, Jiarui; Tan, Xingrong; Xu, Fangjiang; Pang, Shuguang; Wang, Kun; Ye, Jun; Wang, Yuan; Chen, Lili; Sun, Jingfang; Ji, Linong (March 2023). "Efficacy and safety of janagliflozin as add‐on therapy to metformin in Chinese patients with type 2 diabetes inadequately controlled with metformin alone: A multicentre, randomized, double‐blind, placebo‐controlled, phase 3 trial". Diabetes, Obesity and Metabolism. 25 (3): 785–795. doi:10.1111/dom.14926. PMID 36433709. S2CID 253967474.
^ Ji, Linong; Jiang, Xiaozhen; Hao, Qingshun; Cheng, Zhifeng; Wang, Kun; Pang, Shuguang; Liu, Meiying; Guo, Yushan; Chen, Xiaowen; Su, Xiuhai; Ning, Tao; Liu, Jie; Bian, Fang; Li, Yulan; Zhang, Zhinong; Song, Weihong; Sun, Jingfang (May 2023). "Efficacy and safety of janagliflozin monotherapy in Chinese patients with type 2 diabetes mellitus inadequately controlled on diet and exercise: A multicentre, randomized, double‐blind, placebo‐controlled, Phase 3 trial". Diabetes, Obesity and Metabolism. 25 (5): 1229–1240. doi:10.1111/dom.14971. PMID 36594724. S2CID 255474211.

[1] Song, Ling; Yao, Xueting; Liu, Yang; Zhong, Wen; Jiang, Ji; Liu, Hongzhong; Zhou, Huimin; Shi, Chongtie; Zong, Kaiqi; Wang, Chong; Ma, Chuanxiang; Liu, Dongyang; Hu, Pei (April 2020). "Translational prediction of first-in-human pharmacokinetics and pharmacodynamics of janagliflozin, a selective SGLT2 inhibitor, using allometric scaling, dedrick and PK/PD modeling methods". European Journal of Pharmaceutical Sciences. 147: 105281. doi:10.1016/j.ejps.2020.105281. S2CID 212405270.

[2] Liu, Dongyang; Song, Ling; Wang, Xiaoxu; Liu, Xu; Cao, Fangrui; Liu, Hongzhong; Ding, Yanhua; Xiao, Xinhua; Jiang, Ji; Hu, Pei (1 June 2019). "154-LB: Accelerating Clinical Development of Janagliflozin, a Novel Antidiabetic Drug, Using Model-Informed Drug Development Strategy". Diabetes. 68 (Supplement_1). doi:10.2337/db19-154-LB. S2CID 195440798.

[3] Zhao, Hengli; Wei, Yilin; He, Kun; Zhao, Xiaoyu; Mu, Hongli; Wen, Qing (December 2022). "Prediction of janagliflozin pharmacokinetics in type 2 diabetes mellitus patients with liver cirrhosis or renal impairment using a physiologically based pharmacokinetic model". European Journal of Pharmaceutical Sciences. 179: 106298. doi:10.1016/j.ejps.2022.106298. PMID 36162752. S2CID 252505056.

[4] Zhao, Hengli; Zhao, Zhirui; He, Kun; Mi, Nianrong; Lou, Kai; Dong, Xiaolin; Zhang, Wenyu; Sun, Jingfang; Hu, Xinyu; Pang, Shuguang; Cheng, Hong; Wen, Qing (August 2023). "Pharmacokinetics, Pharmacodynamics and Safety of Janagliflozin in Chinese Type 2 Diabetes Mellitus Patients with Renal Impairment". Clinical Pharmacokinetics. 62 (8): 1093–1103. doi:10.1007/s40262-023-01256-0. PMID 37284974. S2CID 259097798.

[5] Gao, Leili; Cheng, Zhifeng; Su, Benli; Su, Xiuhai; Song, Weihong; Guo, Yushan; Liao, Lin; Chen, Xiaowen; Li, Jiarui; Tan, Xingrong; Xu, Fangjiang; Pang, Shuguang; Wang, Kun; Ye, Jun; Wang, Yuan; Chen, Lili; Sun, Jingfang; Ji, Linong (March 2023). "Efficacy and safety of janagliflozin as add‐on therapy to metformin in Chinese patients with type 2 diabetes inadequately controlled with metformin alone: A multicentre, randomized, double‐blind, placebo‐controlled, phase 3 trial". Diabetes, Obesity and Metabolism. 25 (3): 785–795. doi:10.1111/dom.14926. PMID 36433709. S2CID 253967474.

[6] Ji, Linong; Jiang, Xiaozhen; Hao, Qingshun; Cheng, Zhifeng; Wang, Kun; Pang, Shuguang; Liu, Meiying; Guo, Yushan; Chen, Xiaowen; Su, Xiuhai; Ning, Tao; Liu, Jie; Bian, Fang; Li, Yulan; Zhang, Zhinong; Song, Weihong; Sun, Jingfang (May 2023). "Efficacy and safety of janagliflozin monotherapy in Chinese patients with type 2 diabetes mellitus inadequately controlled on diet and exercise: A multicentre, randomized, double‐blind, placebo‐controlled, Phase 3 trial". Diabetes, Obesity and Metabolism. 25 (5): 1229–1240. doi:10.1111/dom.14971. PMID 36594724. S2CID 255474211.

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