Drug intelligence / Profile preview

cefilavancin

Development stage
Phase 2
Lead developer
R-Pharm
Modality
Small Molecules
Administration
Intravenous
01

Overview

Cefilavancin is an investigational intravenous **glycopeptide-cephalosporin heterodimer antibiotic** developed by Theravance for serious Gram-positive bacterial infections, particularly complicated skin and skin-structure infections involving resistant *Staphylococcus aureus*. It covalently combines a vancomycin-derived glycopeptide pharmacophore with a cephalosporin moiety to produce multivalent inhibition of bacterial cell-wall synthesis. The glycopeptide component binds terminal D-alanyl-D-alanine residues of peptidoglycan precursors, while the cephalosporin component targets penicillin-binding proteins, including PBP2 in *Staphylococcus aureus*. A randomized Phase 2 study evaluated intravenous cefilavancin against vancomycin in complicated Gram-positive skin and skin-structure infections.

02

Targets

Lipid IIPBP2 (Penicillin-binding protein 2)D-Ala-D-Ala (D-Ala-D-Ala terminus)

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