Drug intelligence / Profile preview

GDC-5780

Development stage
Unknown
Lead developer
Genentech
Modality
Small Molecules
Administration
Intravenous
01

Overview

GDC-5780 is an investigational small molecule antibiotic developed by Genentech (a subsidiary of Roche) for the treatment of complicated urinary tract infections (cUTI) caused by Gram-negative bacteria. It acts as a potent and selective inhibitor of **UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC)**, a zinc-dependent enzyme that catalyzes the first committed step in the biosynthesis of Lipid A. Lipid A is a fundamental component of the lipopolysaccharide (LPS) layer in the outer membrane of Gram-negative pathogens, such as *Pseudomonas aeruginosa* and *Enterobacteriaceae*. By blocking LpxC, GDC-5780 inhibits the formation of the bacterial outer membrane, leading to compromised structural integrity and bacterial cell death. The drug is administered intravenously and has been evaluated in Phase 1 clinical trials to assess its safety, tolerability, and pharmacokinetics in healthy volunteers.

02

Targets

LpxC (UDP-3-O-[3-hydroxymyristoyl] N-acetylglucosamine Deacetylase)

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