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

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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