Delving into the Latest Updates on PF-06815189 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

PDE2A

Action

inhibitors

Mechanism

PDE2A inhibitors(Phosphodiesterase 2A inhibitors)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Author: Tran, Tuan P. ; Brodney, Michael A. ; Obach, R. Scott ; Verhoest, Patrick R. ; Fisher, Ethan L. ; Stepan, Antonia F. ; Chang, Cheng ; Sharma, Raman ; Helal, Christopher J. ; Brown, Maria S. ; Yang, Edward X. ; Walker, Gregory S. ; Wager, Travis T. ; Kormos, Bethany L. ; Doran, Shawn D. ; Karanian, David ; Jenkinson, Stephen ; Wright, Ann S. ; O’Connor, Rebecca E. ; De Vivo, Michael

Late-stage oxidation using liver microsomes was applied to phosphodiesterase 2 inhibitor 1 to reduce its clearance by cytochrome P450 enzymes, introduce renal clearance, and minimize the risk for victim drug-drug interactions. This approach yielded PF-06815189 (2) with improved physicochemical properties and a mixed metabolic profile. This example highlights the importance of C-H diversification methods to drug discovery.

100 Deals associated with PF-06815189

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