Drug intelligence / Profile preview

novobiocin

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Novobiocin is an aminocoumarin antibiotic produced by the actinomycete Streptomyces niveus. It acts primarily as a competitive inhibitor of the ATPase activity of the GyrB subunit of bacterial DNA gyrase, thereby inhibiting bacterial DNA synthesis and cell division. Novobiocin is mainly active against Gram-positive bacteria, particularly Staphylococcus aureus, and was historically used to treat serious infections caused by susceptible strains when other antibiotics were ineffective or contraindicated. The drug also has weak inhibitory effects on eukaryotic Hsp90 protein and can activate the Gram-negative lipopolysaccharide transporter LptBFGC. Novobiocin was originally approved in 1964 but has since been withdrawn from clinical use due to safety or efficacy concerns[1][2][3][4].

Brand names
AlbamycinPanalbaAlbamycin-T
Other names
StreptonivicinCardelmycinInamycinalbamycin
02

Targets

ParE (DNA topoisomerase 4 subunit B)LptC (Lipopolysaccharide export system protein LptC)HSP90 (Heat shock protein 90 chaperone complex)GyrB (DNA gyrase subunit B)

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