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BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv.

BM635 has potent MIC (0.12 μM), Tox50:MIC ratio of >100, and good microsomal stability in mice (1.4 mL/min/g). When tested in an acute murine infection model at multiple doses, BM635 exhibits potent anti-tubercular activity, with an ED99 of 49 mg/Kg (IC95%: 43-54 mg/Kg)[1]. The half-life in vivo of BM635 is 1h, allowing a reasonable maximum concentration (Cmax=1.62 μM) and a moderate bioavailability (46%). Its poor aqueous solubility together with its high lipophilicity leads to low exposure in vivo[2].

[1]. Poce G, et al. Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection. PLoS One. 2013;8(2):e56980. [2]. Poce G, et al. Pharmaceutical salt of BM635 with improved bioavailability. Eur J Pharm Sci. 2017 Mar 1;99:17-23.

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