Lefamulin

Lefamulin is a pleuromutilin antibiotic. It is active against methicillin-resistant S. aureus (MRSA), S. pyogenes, E. faecium, H. influenzae, M. catarrhalis, L. pneumonophilia, C. pneumoniae, and M. pneumoniae (MIC50s = 0.006-1 µg/ml). Lefamulin is also active against fluoroquinolone- and macrolide-resistant strains of N. gonorrhoeae (MIC90s = 1 mg/L for all). In vivo, lefamulin (10-40 mg/kg) reduces the number of colony-forming units (CFUs) in a mouse model of S. pneumoniae thigh infection. It also reduces LPS-induced production of TNF-alpha, IL-6, IL-1beta, and GM-CSF, bronchoalveolar lavage fluid (BALF) neutrophil infiltration, and lung matrix metalloproteinase-9 (MMP-9) levels in a mouse model of LPS-induced neutrophilia. Formulations containing lefamulin have been used in the treatment of community-acquired bacterial pneumonia (CABP).Formal Name: 2-[[(1R,2R,4R)-4-amino-2-hydroxycyclohexyl]thio]-acetic acid, (3aS,4R,5S,6S,8R,9R,9aR,10R)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester. CAS Number: 1061337-51-6. Synonyms: BC-3781. Molecular Formula: C28H45NO5S. Formula Weight: 507.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 16 mg/mL, DMSO: 12 mg/mL, Ethanol: 3 mg/mL, PBS (pH 7.2): 0.25 mg/mL. SMILES: O=C1CC[C@@]2(CC[C@H]3C)[C@@H](C)[C@H](O)[C@@](C=C)(C)C[C@@H](OC(CS[C@@H]4CC[C@@H](N)C[C@H]4O)=O)[C@@]3(C)[C@@]21[H]. InChi Code: InChI=1S/C28H45NO5S/c1-6-26(4)14-22(34-23(32)15-35-21-8-7-18(29)13-20(21)31)27(5)16(2)9-11-28(17(3)25(26)33)12-10-19(30)24(27)28/h6,16-18,20-22,24-25,31,33H,1,7-15,29H2,2-5H3/t16-,17+,18-,20-,21-,22-,24+,25+,26-,27+,28+/m1/s1. InChi Key: KPVIXBKIJXZQJX-FCEONZPQSA-N.