502487-67-4

Oral administration of SQ109 (0.1-25 mg/kg per day) to the mice for 28 days results in dose-dependent reductions of mycobacterial load in both spleen and lung comparable to that of EMB administered at 100 mg/kg per day, but is less potent than isoniazid (INH) at 25 mg/kg per day. Pharmacokinetic profiles of SQ109 in mice following a single administration showed its C_max as 1038 (intravenous (i.v.)) and 135 ng/mL (p.o.), with an oral T_max of 0.31 h. The elimination t_1/2 of SQ109 is 3.5 (i.v.) and 5.2 h (p.o.). The oral bioavailability is 4%^[2]. The terminal half-life (t_1/2) of SQ109 in dogs (12-29 h, mean 29.3 h) is longer than in rats (7-8 h, mean 7.4 h), as reflected by the significantly larger volume of distribution of SQ109 in dogs. The oral bioavailability of SQ109 in rats and dogs is determined to be 12% and 5%, respectively^[3].