Pharmaceutical salt of BM635 with improved bioavailability
BM635 is a small molecule endowed with outstanding anti-mycobacterial activity (minimum inhibitory concentration of 0.12 ?M against M. tuberculosis H37Rv) identified during a hit-to-lead campaign. Its poor aqueous solubility together with its high lipophilicity led to low exposure in vivo. Indeed, the half-life in vivo of BM635 was 1 h, allowing a reasonable maximum concentration (Cmax = 1.62 ?M) and a moderate bioavailability (46%).