Drug intelligence / Profile preview

azd5099

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous
01

Overview

AZD5099 is a potent and selective antibacterial agent developed as a DNA gyrase modulator targeting bacterial type II topoisomerases (specifically GyrB/ParE subunits). It was designed to treat serious infections caused by Gram-positive and fastidious Gram-negative bacteria. The compound is derived from pyrrolamide antibacterials using fragment-based drug design to target the ATP binding site of bacterial topoisomerases. AZD5099 demonstrated notable efficacy in preclinical models against *Staphylococcus aureus*, including methicillin-resistant strains (MRSA), with low resistance frequency. However, clinical development was discontinued after phase I trials due to concerns about mitochondrial toxicity and other safety issues[6][8][3][5].

Other names
5-thiazolecarboxylic acid 2-((3S,4R)-4-(((3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl)amino)-3-methoxy-1-piperidinyl)-4-((((1S)-2-hydroxypropyl)amino)methyl)thiazolyl
02

Targets

GyrB (DNA gyrase subunit B)

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