Chemistry:LPC-233
LPC-233 is an experimental antibiotic drug. It acts as a potent and selective inhibitor of the bacterial enzyme UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC), which is important for the production of Lipid A, a key component of the cell membrane of Gram-negative bacteria. Various inhibitors of LpxC have been developed but none have yet progressed into clinical trials in humans, mostly because of off-target cardiovascular toxicity.[1][2][3] LPC-233 is one of the most advanced drugs of this type in preclinical testing, showing activity against several pathogens of concern such as multidrug-resistant Pseudomonas aeruginosa and carbapenem resistant Enterobacter strains, and with no cardiovascular toxicity evident in testing on mice and dogs.[4][5]
See also
- TP0586532
References
- ↑ "Insights into the Zinc-Dependent Deacetylase LpxC: Biochemical Properties and Inhibitor Design". Current Topics in Medicinal Chemistry 16 (21): 2379–2430. 2016. doi:10.2174/1568026616666160413135835. PMID 27072691.
- ↑ "LpxC inhibitors: a patent review (2010-2016)". Expert Opinion on Therapeutic Patents 27 (11): 1227–1250. November 2017. doi:10.1080/13543776.2017.1360282. PMID 28742403.
- ↑ "Small molecule LpxC inhibitors against gram-negative bacteria: Advances and future perspectives". European Journal of Medicinal Chemistry 253. May 2023. doi:10.1016/j.ejmech.2023.115326. PMID 37023679.
- ↑ "Preclinical safety and efficacy characterization of an LpxC inhibitor against Gram-negative pathogens". Science Translational Medicine 15 (708). August 2023. doi:10.1126/scitranslmed.adf5668. PMID 37556556.
- ↑ "LpxC inhibitor eliminates bacterial infections". Nature Reviews. Drug Discovery 22 (10): 787. October 2023. doi:10.1038/d41573-023-00144-3. PMID 37666971.
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