A Phase I Study on the Pharmacokinetics and Pharmacodynamics of DJT1116PG, a Novel Selective Inhibitor of Sodium-Glucose Cotransporter Type 2, in Healthy Individuals at Steady State.

A Phase I Study on the Pharmacokinetics and Pharmacodynamics of DJT1116PG, a Novel Selective Inhibitor of Sodium-Glucose Cotransporter Type 2, in Healthy Individuals at Steady State.
Clin Ther. 2020 Apr 04;:
Authors: Zhang H, Liu J, Zhu X, Li X, Chen H, Wu M, Li C, Ding Y
Abstract
PURPOSE: DJT1116PG, which selectively inhibits renal glucose reabsorption by inhibiting sodium-glucose cotransporter type 2, was developed as an insulin-independent treatment for type 2 diabetes mellitus. This Phase I trial evaluated the pharmacokinetic and pharmacodynamic properties of DJT1116PG at steady state in healthy Chinese individuals.
METHODS: This was a multiple ascending dose study of DJT1116PG (20, 50, and 100 mg once daily for 7 days) that included 36 healthy individuals.
FINDINGS: There were no serious adverse events or deaths in these studies, and no adverse event led to study discontinuation. Oral DJT1116PG was rapidly absorbed with a Tmax of 0.75-1.5 h and a t½ of 12-16.2 h. Systemic exposure (Cmax and AUC) of DJT1116PG and its inactive metabolites (T1444, T1454, and T1830) increased in a dose-dependent manner. Urinary glucose excretion (UGE) plateaued at 50 mg of DJT1116PG in a previous single ascending dose study and on day 1 of this study. UGE plateaued at 20 mg of DJT1116PG on day 7 of this study. Serum glucose parameters were similar in individuals who received DJT1116PG or placebo.
IMPLICATIONS: DJT1116PG...

Source: Clinical Therapeutics - April 3, 2020 Category: Drugs & Pharmacology Authors: Zhang H, Liu J, Zhu X, Li X, Chen H, Wu M, Li C, Ding Y Tags: Clin Ther Source Type: research