Delving into the Latest Updates on BRD9185 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

PfDHODH

Action

inhibitors

Mechanism

PfDHODH inhibitors(P. falciparum dihydroorotate dehydrogenase inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication-

Inactive Indication

Malaria

Originator Organization

The Broad Institute, Inc.

Active Organization-

Inactive Organization

The Broad Institute, Inc.

Harvard University

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Dihydroorotate dehydrogenase (DHODH) is an enzyme necessary for pyrimidine biosynthesis in protozoan parasites of the genus Plasmodium, the causative agents of malaria. We recently reported the identification of novel compounds derived from diversity-oriented synthesis with activity in multiple stages of the malaria parasite life cycle. Here, we report the optimization of a potent series of antimalarial inhibitors consisting of azetidine-2-carbonitriles, which we had previously shown to target P. falciparum DHODH in a biochemical assay. Optimized compound BRD9185 (27) has in vitro activity against multidrug-resistant blood-stage parasites (EC₅₀ = 0.016 μM) and is curative after just three doses in a P. berghei mouse model. BRD9185 has a long half-life (15 h) and low clearance in mice and represents a new structural class of DHODH inhibitors with potential as antimalarial drugs.

100 Deals associated with BRD9185

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