Drug intelligence / Profile preview

compound 23

Development stage
Preclinical
Lead developer
Presidio Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Compound 23 is an orally bioavailable ethyl ester prodrug of compound 22, an aminopyrazole–phenylalanine based GPR142 agonist. It is being developed for the treatment of type 2 diabetes. As a prodrug, it is converted in vivo to its active form, compound 22, which functions by activating GPR142, a Gq-coupled receptor predominantly expressed in pancreatic β-cells. This activation triggers an intracellular signal transduction pathway leading to β-cell insulin secretion and a subsequent lowering of plasma glucose levels. In preclinical studies, compound 23 demonstrated good efficacy in mouse oral glucose tolerance tests, showing a strong, dose-dependent glucose lowering effect comparable to sitagliptin.

Other names
ethyl ester prodrug 23
02

Targets

GPR142 (G protein-coupled receptor 142)

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