TBI-166, a riminophenazine analogue, is an orally active anti-tuberculosis agent with fewer adverse reactions than the lead riminophenazine compound, Clofazimine ( HY-B1046 ) .
In Vitro
TBI-166 inhibits M. tuberculosis H37Rv replicates (MIC: 0.063 μg/mL), and is effective against 16 drug-sensitive clinical isolates (Mycobacterial species) with MICs of 0.005-0.15 μg/mL. TBI-166 (0-1 μg/mL, 3 days) inhibits intracellular M. tuberculosis in M. tuberculosis infecting J774A.1 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TBI-166 (10-80 mg/kg, p.o., 8 weeks) displays antituberculosis activity in chronic murine M. tuberculosis H37Rv infected model . TBI-166 displays a LD50 more than 3,000 mg/kg in mice . TBI-166 has a short half-life (41.25 h) and reduces the potential for skin pigmentation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Chronic murine M. tuberculosis H37Rv infected model Dosage: 10, 20, 80 mg/kg Administration: Oral administration, 8 weeks. Result: Reduced CFU counts in lung.
