Telavancin

Telavancin (TD-6424) is a semisynthetic lipoglycopeptide vancomycin-derivative, is a novel antimicrobial agent developed by Theravance for overcoming resistant Gram-positive bacterial infections, specifically methicillin-resistant Staphylococcus aureus (MRSA). Telavancin disrupts cell membrane integrity, can be used for research of complicated skin and skin structure infections (cSSSIs) caused by Gram-positive bacteria[1].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

Telavancin has a rapid, concentration-dependent bactericidal effect, due to disruption of cell membrane integrity[1]. Telavancin (5 μg/mL) exerts bacteriocidal effect against a MRSA strain (COL) and a VISA strain (HIP5836) at a concentration of 5 µg/mL[1].

Telavancin has been tested in various relevant animal models of infection, namely, bacteremia (40 mg/kg/d; s.c.; twice a day, with 12 h space), endocarditis (30 mg/kg/d; i.v.; twice a day, with 12 h space; 4 d), meningitis, and pneumonia with success[1] Animal Model: MRSA bacteremia model in neutropenic mice[1] Dosage: 40 mg/kg Administration: Subcutaneous injection; twice every day spaced 12 h apart  Result: Resulted a significantly higher 14-day survival compared with vancomycin-treated animals. Animal Model: Rabbit model of S. aureus endocarditis[1] Dosage: 30 mg/kg Administration: Intravenous injection; twice every day, spaced 12 h for 4 days Result: Significantly reduced MRSA densities in all target tissues and increased the percentage of these organs rendered culture negative.

[1]. Das B, et al. Telavancin: a novel semisynthetic lipoglycopeptide agent to counter the challenge of resistant Gram-positive pathogens. Ther Adv Infect Dis. 2017 Mar;4(2):49-73.