| 体内研究: |
TCA1 (40 mg/kg; oral gavage; 1 time/d for 5 d/week; for 4 weeks) is efficacious in acute and chronic Mtb infection mouse models. In a mouse model of Mtb infection, after i.v. administration, TCA1 exhibits a low clearance and steady-state volume of distribution, with an elimination half-life of 0.73 h. After oral administration of 20 and 50 mg/kg in solution formulation, TCA1 shows a high Cmax (2122 and 5653 nM, respectively), moderate exposure with oral bioavailability ranging from 19% to 46%, and a half-life of 1.8 h. BALB/c mice infected with Mtb H37Rv 40 mg/kg Oral gavage; 1 time/d for 5 d/week; for 4 weeks Effectively inhibits Mtb in vivo. |