Lefamulin

• CAT Number: I007398
• CAS Number: 1061337-51-6
• Molecular Formula: C28H45NO5S
• Molecular Weight: 507.73
• Purity: ≥95%
• Synonyms: BC-3781; BC 3781; BC3781; Lefamulin;(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-(((1R,2R,4R)-4-amino-2-hydroxycyclohexyl)thio)acetate
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term , or -20°C for long term.
• IUPAC Name: [(1S,2R,3S,4S,6R,7R,8R,14R)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxo-6-tricyclo[5.4.3.01,8]tetradecanyl] 2-[(1R,2R,4R)-4-amino-2-hydroxycyclohexyl]sulfanylacetate
• InChI: 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
• InChIKey: KPVIXBKIJXZQJX-FCEONZPQSA-N
• SMILES: CC1CCC23CCC(=O)C2C1(C(CC(C(C3C)O)(C)C=C)OC(=O)CSC4CCC(CC4O)N)C

Lefamulin(CAT: I007398) is a novel antibiotic used for the treatment of community-acquired bacterial pneumonia (CABP). It belongs to the pleuromutilin class of antibiotics and works by inhibiting bacterial protein synthesis. Lefamulin exhibits a broad spectrum of activity against common pathogens involved in CABP, including both typical and atypical bacteria. It is administered orally or intravenously and has shown efficacy in clinical trials, demonstrating non-inferiority to standard antibiotic therapies.

Reference

1:In Vitro Activities of Lefamulin and Other Antimicrobial Agents against Macrolide-Susceptible and Macrolide-Resistant Mycoplasma pneumoniae from the United States, Europe, and China. Waites KB, Crabb DM, Duffy LB, Jensen JS, Liu Y, Paukner S.Antimicrob Agents Chemother. 2017 Jan 24;61(2). pii: e02008-16. doi: 10.1128/AAC.02008-16. Print 2017 Feb. PMID: 27855075
2:In Vitro Activity of Lefamulin Tested against Streptococcus pneumoniae with Defined Serotypes, Including Multidrug-Resistant Isolates Causing Lower Respiratory Tract Infections in the United States. Mendes RE, Farrell DJ, Flamm RK, Talbot GH, Ivezic-Schoenfeld Z, Paukner S, Sader HS.Antimicrob Agents Chemother. 2016 Jun 20;60(7):4407-11. doi: 10.1128/AAC.00627-16. Print 2016 Jul. PMID: 27161634 Free PMC Article
3:Simultaneous assessment of the pharmacokinetics of a pleuromutilin, lefamulin, in plasma, soft tissues and pulmonary epithelial lining fluid. Zeitlinger M, Schwameis R, Burian A, Burian B, Matzneller P, Müller M, Wicha WW, Strickmann DB, Prince W.J Antimicrob Chemother. 2016 Apr;71(4):1022-6. doi: 10.1093/jac/dkv442. Epub 2016 Jan 7. PMID: 26747098