Quabodepistat (OPC-167832) (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokineticcharacteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 hQuabodepistat distribution in the lungs is approximately 2 times higher than that in plasma, and theCmaxand AUCt of Quabodepistat in plasma and the lungs shows dose dependency[1].Quabodepistat (oral administration; 0.625-10 mg/kg; 4weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625mg/kg to 2.5mg/kg. In aM. tuberculosisKurono-infected ICR female mice model. Quabodepistat combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].Quabodepistat (oral gavage; 2.5mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1].
| Animal Model: | ICR mice[1] |
| Dosage: | 0.625-10 mg/kg |
| Administration: | Oral administration; 0.625-10 mg/kg; 4weeks |
| Result: | Exhibited in vivoefficacy against a mouse chronic TB model. |