Delving into the Latest Updates on UDM-001651 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

PAR-4

Mechanism

PAR-4 antagonists(Protease-activated receptor-4 antagonists)

Therapeutic Areas

Hemic and Lymphatic Diseases

Active Indication

Blood Platelet Disorders

Inactive Indication

Cardiovascular Diseases

Originator Organization

Bristol Myers Squibb Co.

Active Organization

University of Montréal

Inactive Organization

Bristol Myers Squibb Co.

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure

Molecular FormulaC28H23N3O5S

InChIKeyLFOIDLOIBZFWDO-UHFFFAOYSA-N

CAS Registry1477497-01-0

Author: Ruediger, Edward ; Hartl, Karen ; Malmstrom, Sarah ; Miller, Michael M. ; Wong, Pancras ; Rémillard, Roger ; Lavallée, Jean-François ; Yang, Yanou ; Allegretto, Nick J. ; Hangeland, Jon J. ; Priestley, E. Scott ; Yang, Jing ; Bouvier, Michel ; Martel, Alain ; Watson, Carol ; Harden, David G. ; Marinier, Anne ; Wexler, Ruth R. ; Harper, Timothy W. ; Posy, Shana L. ; Zhang, Ge ; O’Grady, Harold ; Friends, Todd J. ; Gagnon, Mark ; Seiffert, Dietmar A. ; Lawrence, R. Michael ; Tremblay, François ; Josephs, Jonathan ; Banville, Jacques ; Guarino, Victor R.

In an effort to identify novel antithrombotics, we have investigated protease-activated receptor 4 (PAR4) antagonism by developing and evaluating a tool compound, UDM-001651, in a monkey thrombosis model. Beginning with a high-throughput screening hit, we identified an imidazothiadiazole-based PAR4 antagonist chemotype. Detailed structure-activity relationship studies enabled optimization to a potent, selective, and orally bioavailable PAR4 antagonist, UDM-001651. UDM-001651 was evaluated in a monkey thrombosis model and shown to have robust antithrombotic efficacy and no prolongation of kidney bleeding time. This combination of excellent efficacy and safety margin strongly validates PAR4 antagonism as a promising antithrombotic mechanism.

100 Deals associated with UDM-001651

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