TMC207 fumarate

TMC207 (Bedaquiline) is an diarylquionline antimycobacterial agent. TMC207 fumarate is the salt form of the antitubercular drug bedaquiline.

TMC207 fumarate may be used to study the pharmacodynamic activity of Bedaquiline loaded fucosylated/nonfucosylated liposomes (BDQ-Lipofuc/BDQ-Lipo) in a mouse model of Mycobacterium tuberculosis infection.

TMC207 (Bedaquiline) fumarate potently inhibits Mycobacterium tuberculosis (MIC50 ~0.03 µg/mL) by selectively targeting the c-subunit of its ATP synthase, thereby disrupting cellular energy and leading to cell death, while exhibiting minimal interaction with human ATP synthase (selectivity index >20,000). This specific salt formulation provides enhanced aqueous solubility and dissolution, contributing to favorable ADME properties, improved and more consistent oral bioavailability, and a very long terminal elimination half-life (approximately 5.5 months), ensuring sustained and predictable exposure at the site of infection.

Hygroscopic Store with dessicant