Drug intelligence / Profile preview

telavancin

Development stage
Approved
Lead developer
Theravance Biopharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Peptides
Administration
Intravenous
01

Overview

Telavancin is a semi-synthetic lipoglycopeptide antibiotic derived from vancomycin, used for the treatment of serious Gram-positive bacterial infections, including complicated skin and skin structure infections (cSSSI), hospital-acquired bacterial pneumonia (HABP), and ventilator-associated bacterial pneumonia (VABP)[1][2][3][4]. It exhibits bactericidal activity primarily against Methicillin-resistant Staphylococcus aureus (MRSA) and other Gram-positive pathogens[2][5]. Telavancin acts through a dual mechanism of action: it inhibits bacterial cell wall synthesis by binding to the D-Ala-D-Ala terminus of peptidoglycan precursors, preventing polymerization and cross-linking; additionally, it disrupts the integrity of the bacterial cell membrane by depolarizing it via interaction with lipid II[5][6]. This dual action distinguishes telavancin from vancomycin. The drug is administered intravenously as a powder for solution[1]. Telavancin is reserved for cases where alternative treatments are not suitable due to its risk profile, including nephrotoxicity and potential teratogenicity. It has demonstrated higher rates of kidney failure compared to vancomycin in clinical trials[5]. The drug may cause infusion-related reactions such as "Red-man Syndrome" if administered too rapidly[1]. Developed by Theravance and manufactured/marketed in partnership with Cumberland Pharmaceuticals.

Brand names
Vibativ
Other names
TelavancinaTélavancineTelavancinum
02

Targets

D-Ala-D-Ala (D-Ala-D-Ala terminus)Lipid II

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