Delving into the Latest Updates on Genz-669178 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

PfDHODH

Mechanism

PfDHODH inhibitors(P. falciparum dihydroorotate dehydrogenase inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication

Malaria

Inactive Indication-

Originator Organization-

Active Organization

Genzyme Corp.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

SignificanceDrug resistance is a major problem in treating malaria infections. Resistance pathways are limited by evolutionary fitness constraints, and these pathways can be anticipated and preemptively blocked. We identified compounds selective for mutant malaria parasites that are resistant to either clinically used (chloroquine) or in-development dihydroorotate dehydrogenase (DHODH) inhibitor therapies. In both cases, resistance selections of mutant parasites with the matching mutant-selective drug led to a reversion to the wild-type phenotype. Additionally, combination selection of wild-type parasites with paired wild-type and mutant-type DHODH inhibitors failed to produce resistant parasites. These findings indicate that pairing inhibitors that target the bulk wild-type population and the small, emerging resistant population can suppress the rise and spread of drug resistance.

100 Deals associated with Genz-669178

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