依帕列净；恩格列净；BI-10773；BI 10773；BI10773-abs817359

一、产品概述

二、产品信息

Empagliflozin shows >2500-fold selectivity for hSGLT-2 over hSGLT-1 (IC50 8300 nM) and >3500-fold selectivity over hSGLT-4, it exhibits >350-fold selectivity over hSGLT-5 (IC50=1100 nM) and >600-fold selectivity over hSGLT-6. No relevant inhibition of GLUT1 is observed up to 10 μM Empagliflozin. In a kinetic binding experiments, -empagliflozin displays a high affinity for SGLT-2 with a mean Kd of 57 nM in the absence of glucose, and shows a half-life of -empagliflozin-binding to SGLT-2 of 59 min in the absence of glucose.Its binding to SGLT-2 is competitive with glucose.

High exposure of empagliflozin is achieved in dogs, with plasma concentrations >100-fold above IC50 measured 24 h after administration of 5 mg/kg empagliflozin. The total plasma clearance of empagliflozin in ZDF rat is 43 mL/min/kg, while in dogs is lower at 1.8 mL/min/kg. Cmax of empagliflozin in ZDF rat and dogs is 167 nM and 17254 nM, respectively. Terminal elimination half-life in ZDF rat and dogs is 1.5 h and 6.3 h, respectively. Bioavailability of empagliflozin in ZDF rat is 33.2%, while in dogs is higher at 89.0%. Long-term treatment with empagliflozin, improves glycaemic controland features of metabolic syndrome in diabetic rats.

三、背景

四、制备和贮存

五、产品特点

六、注意事项