Delving into the Latest Updates on PF-03671148 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

ALK5

Action

inhibitors

Mechanism

ALK5 inhibitors(Transforming growth factor beta receptor 1 inhibitors)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Cicatrix

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Author: Leroy Lu ; Elena M. Drummond ; Karen E. Sexton ; Richard B. Gilbertsen ; Richard Gowan ; Erli Zhang ; Sneha Patel ; David J. Pocalyko ; Christopher L. Chio ; N. A. Payne ; Paul R. Keller ; Stephen D. Barrett ; Catherine R. Kostlan ; Stephen Fakhoury ; Mostofa A. Hena ; Samarendra N. Maiti ; John D. Knafels ; Rone Eisma ; Victoria L. Downs ; Neil Raheja ; Mark L. Boys ; Donna M. Iula ; Patrick McConnell ; Barry C. Finzel ; Gary F. Filzen ; Zhi Wang ; Paul Angell ; James B. Kramer ; Larry D. Bratton ; Venkataraman Thanabal ; Fang Sun ; Feng Bian ; Maria N. Nguyen ; Edmund L. Ellsworth ; Xiao Dan Ren ; Diane Alessi ; Huifen Chen ; Susan M. Ciotti ; Ann McCarthy ; Deepak S. Lala

A series of 2-(1H-pyrazol-1-yl)pyridines are described as inhibitors of ALK5 (TGFβ receptor I kinase). Modeling compounds in the ALK5 kinase domain enabled some optimization of potency via substitutions on the pyrazole core. One of these compounds PF-03671148 gave a dose dependent reduction in TGFβ induced fibrotic gene expression in human fibroblasts. A similar reduction in fibrotic gene expression was observed when PF-03671148 was applied topically in a rat wound repair model. Thus these compounds have potential utility for the prevention of dermal scarring.

100 Deals associated with PF-03671148

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