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Bedaquiline inhibits the growth of TDR M. tuberculosis strains, with MIC values ranging from 0.125 to 0.5 mg/L. Among slowly growing mycobacteria (SGM), bedaquiline exhibits the highest activity against Mycobacterium avium with MIC50 and MIC90 values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) seem more susceptible to bedaquiline than Mycobacterium fortuitum, with MIC50 and MIC90 values of 0.13 and >16 mg/L, respectively, for both species. Bedaquiline also shows moderate in vitro activity against NTM species. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis.
| Cell Experiment | |
|---|---|
| Cell lines | M. tuberculosis |
| Preparation method | M. tuberculosis was cultured in 7H9 broth and grown to an A600 nm of 0.8. Cultures were treated with 0.1, 1 or 10 mg ml 1 BDQ for 24 h. NADH and NAD þ concentrations were determined and the NADH/NAD þ ratio was calculated as described. |
| Concentrations | 0.1, 1 and 10 mg/ml |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c mice |
| Formulation | |
| Dosages | 25 mg/kg |
| Administration | i.v. |
| Molecular Weight | 671.58 |
| Formula | C36H35BrN2O6 |
| CAS Number | 845533-86-0 |
| Form | Solid |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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