Drug intelligence / Profile preview

ramoplanin

Development stage
Unknown
Lead developer
Oscient Pharmaceuticals
Modality
Peptides, Small Molecules
Administration
Oral
01

Overview

Ramoplanin is a glycolipodepsipeptide antibiotic derived from Actinoplanes sp. ATCC 33076. It exhibits broad-spectrum bactericidal activity against Gram-positive aerobic and anaerobic bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), and Clostridium difficile. Ramoplanin acts by inhibiting bacterial cell wall biosynthesis, specifically blocking the transglycosylation step of peptidoglycan synthesis through binding to lipid II intermediates, thereby preventing the formation of cell wall peptidoglycan. This mechanism is distinct from glycopeptides like vancomycin, as ramoplanin does not bind to the D-Ala–D-Ala sequence but instead sequesters lipid intermediates I and II involved in peptidoglycan assembly[1][3][5][7]. Ramoplanin has been evaluated in clinical trials for oral treatment of Clostridium difficile-associated diarrhea (CDAD) and suppression of VRE colonization; it is minimally absorbed when administered orally[2][7].

Other names
ramoplanin
02

Targets

MurG (MurG glycosyltransferase)Lipid IIUndecaprenyl-diphospho-N-acetylmuramoyl-pentapeptide

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