Drug intelligence / Profile preview

platensimycin

Development stage
Preclinical
Lead developer
Merck
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Experimental/parenteral (animal Studies), Oral (investigational/animal Studies)
01

Overview

Platensimycin is a natural antibiotic compound produced by the bacterium *Streptomyces platensis*. It is a small molecule belonging to the class of hydroxybenzoic acid derivatives, with the chemical formula C24H27NO7 and a molecular weight of 441.47. Platensimycin acts as a potent and selective inhibitor of bacterial fatty acid synthesis by targeting β-ketoacyl-(acyl-carrier-protein) synthase I/II (FabF/B), key enzymes in the fatty acid biosynthesis pathway. This unique mechanism disrupts lipid biosynthesis in Gram-positive bacteria, leading to strong antibacterial activity, including efficacy against drug-resistant strains such as methicillin-resistant *Staphylococcus aureus* (MRSA) and vancomycin-resistant enterococci. Platensimycin does not show cross-resistance with other major antibiotics and has demonstrated in vivo efficacy in animal models when administered continuously[2][3][5][6]. The compound was first discovered by Merck through screening natural product extracts from soil-derived actinomycetes[2].

Other names
(−)-platensimycin
02

Targets

FabF (Beta-ketoacyl-ACP synthase 2 (KAS II))KAS I (3-oxoacyl-[acyl-carrier-protein] synthase, mitochondrial)FabH (3-oxoacyl-[acyl-carrier-protein] synthase 3)

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