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2 results on '"BM635"'

1. Pharmaceutical salt of BM635 with improved bioavailability.

Author

Poce, Giovanna, Consalvi, Sara, Cocozza, Martina, Fernandez-Menendez, Raquel, Bates, Robert H., Ortega Muro, Fátima, Barros Aguirre, David, Ballell, Lluis, and Biava, Mariangela

Subjects
*DRUG bioavailability, *ANTIBACTERIAL agents, *HALOTHERAPY, *DRUG lipophilicity, *BIOPHARMACEUTICS
Abstract

BM635 is a small molecule endowed with outstanding anti-mycobacterial activity (minimum inhibitory concentration of 0.12 μM 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 (C max = 1.62 μM) and a moderate bioavailability (46%). The present study aimed to develop salt forms of BM635 with pharmaceutically accepted hydrochloric, methanesulphonic, phosphoric, tartaric, and citric acids to overcome these drawbacks. BM635 salts (BM635-HCl, BM635-Mes, BM635-PA, BM635-TA and BM635-CA) were evaluated for physicochemical as well as biopharmaceutical attributes. [ABSTRACT FROM AUTHOR]

Published
2017
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2. Pharmaceutical salt of BM635 with improved bioavailability

Author

Robert H. Bates, Martina Cocozza, David Barros Aguirre, Giovanna Poce, Fátima Ortega Muro, Raquel Fernandez-Menendez, Sara Consalvi, Lluis Ballell, and Mariangela Biava

Subjects
Stereochemistry, Cmax, Biological Availability, Pharmaceutical Science, Salt (chemistry), Drug development, 02 engineering and technology, 030226 pharmacology & pharmacy, 03 medical and health sciences, Minimum inhibitory concentration, 0302 clinical medicine, In vivo, BM635, MmpL3, Pharmaceutical salts, Tuberculosis, 3003, chemistry.chemical_classification, Chromatography, Chemistry, Water, Mycobacterium tuberculosis, Hydrogen-Ion Concentration, 021001 nanoscience & nanotechnology, Small molecule, Anti-Bacterial Agents, Bioavailability, Biopharmaceutical, Solubility, Lipophilicity, Salts, 0210 nano-technology, Half-Life
Abstract

BM635 is a small molecule endowed with outstanding anti-mycobacterial activity (minimum inhibitory concentration of 0.12μM 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 1h, allowing a reasonable maximum concentration (Cmax=1.62μM) and a moderate bioavailability (46%). The present study aimed to develop salt forms of BM635 with pharmaceutically accepted hydrochloric, methanesulphonic, phosphoric, tartaric, and citric acids to overcome these drawbacks. BM635 salts (BM635-HCl, BM635-Mes, BM635-PA, BM635-TA and BM635-CA) were evaluated for physicochemical as well as biopharmaceutical attributes.

Published
2017

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