Drug intelligence / Profile preview

PF-04991532

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF-04991532 is a potent and selective hepatoselective glucokinase activator developed by Pfizer for the treatment of type 2 diabetes mellitus. As a small molecule drug in the pyridinecarboxylic acids class, it targets glucokinase in the liver to enhance glucose metabolism and lower blood glucose levels without causing hepatic steatosis or significant hypoglycemia. The compound was investigated as an oral therapy aiming to improve glycemic control by increasing hepatic glucose uptake and utilization. Despite promising preclinical results showing efficacy in lowering hyperglycemia with minimal risk of hypoglycemia or fatty liver disease, clinical development was hindered due to insufficient effectiveness in improving HbA1c and fasting plasma glucose compared to placebo[1][5][7][8].

Other names
GKA PF-04991532(S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid3-pyridinecarboxylic acid, 6-[[(2S)-3-cyclopentyl-1-oxo-2-[4-(trifluoromethyl)-1H-imidazol-1-yl]propyl]amino]-CAS 1215197-37-7CAS1215197-37-7CAS-1215197-37-7
02

Targets

GCK (Glucokinase)

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