Drug intelligence / Profile preview

PF-06835919

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

Overview

PF‑06835919 is an orally available small molecule inhibitor of ketohexokinase (KHK), also known as fructokinase, developed by Pfizer for the treatment of metabolic disorders associated with excessive fructose metabolism such as non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and type 2 diabetes mellitus. KHK catalyzes the conversion of fructose to fructose‑1-phosphate in the first step of hepatic fructose metabolism; inhibition reduces fat production in the liver and may improve glycemic control and reduce hepatic steatosis. PF‑06835919 was investigated in phase 1 and phase 2 clinical trials but development has been discontinued for NAFLD, NASH, and type 2 diabetes mellitus[1][4][7].

Other names
(1α,5α,6α)-3-[2-[(2S)-2-Methyl-1-azetidinyl]-6-(trifluoromethyl)-4-pyrimidinyl]-3-azabicyclo[3.1.0]hexane-6-acetic acid2-((1S,5R)-3-(2-((2S)-2-methylazetidin-1-yl)-6-(trifluoromethyl)pyrimidin-4-YL)-3-AZABICYCLO(3.1.0)HEXAN‑6‑YL)ACETIC ACID
02

Targets

KHK-C (Ketohexokinase C)OATP1B1 (Organic anion transporting polypeptide 1B1)

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