Delving into the Latest Updates on Viquidacin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Bacterial DNA gyrase x Bacterial top IV

Mechanism

Bacterial DNA gyrase inhibitors, Bacterial top IV inhibitors(Bacterial topoisomerase IV inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication-

Inactive Indication

Cross InfectionGram-Positive Bacterial InfectionsStaphylococcal Infections

Originator Organization

Sanofi

Active Organization-

Inactive Organization

Sanofi

Novexel SA

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

Login to view timeline

Structure

Molecular FormulaC25H29FN2O4S2

InChIKeyUSGHRRVFKSLEJT-WVBUVRCRSA-N

CAS Registry904302-98-3

ABSTRACT NXL101 is one of a new class of quinoline antibacterial DNA gyrase and topoisomerase IV inhibitors showing potent activity against gram-positive bacteria, including methicillin- and fluoroquinolone-resistant strains. NXL101 inhibited topoisomerase IV more effectively than gyrase from Escherichia coli , whereas the converse is true of enzymes from Staphylococcus aureus . This apparent target preference is opposite to that which is associated with most fluoroquinolone antibiotics. In vitro isolation of S. aureus mutants resistant to NXL101 followed by cloning and sequencing of the genes encoding gyrase and topoisomerase IV led to the identification of several different point mutations within, or close to, the quinolone resistance-determining region (QRDR) of GyrA. However, the mutations were not those that are most frequently associated with decreased sensitivity to quinolones. A fluoroquinolone-resistant mutant variant of gyrase generated in vitro was highly resistant to inhibition by the fluoroquinolones ciprofloxacin and moxifloxacin but remained fully susceptible to inhibition by NXL101. Two mutant gyrases constructed in vitro, with mutations in gyrA engineered according to those most frequently found in S. aureus strains resistant to NXL101, were insensitive to inhibition by NXL101 and had a diminished sensitivity to ciprofloxacin and moxifloxacin. Certain combinations of mutations giving rise to NXL101 resistance and those giving rise to fluoroquinolone resistance may be mutually exclusive.

100 Deals associated with Viquidacin

Login to view more data