Carotegrast methyl
The mean ± standard deviation (SD) of Cmax and AUC0-t for carotegrast with/without rifampicin was 11724.5 ± 6097.6 vs 2620.1 ± 1843.0 ng mL-1, and 55046.0 ± 23427.8 vs 9849.9 ± 4580.6 ng h mL-1, respectively. The geometric mean (95% CI) ± standard deviation (SD) of Cmax of carotegrast methyl after a single oral administration of carotegrast methyl alone and in combination with rifampicin was 803.4 (572.7, 1126.9) ng mL-1 and 1670.4 (1252.7, 2227.3) and ng h mL-1, respectively. The AUC0-t was 2199.1 (1674.1, 2888.7) and 4450.1 (3432.7, 5769.1) ng h mL-1, respectively.
The Cmax and AUC of carotegrast methyl were approximately doubled by coadministration with rifampicin with a statistically significant difference between the treatments (p = 0.0005 and 0.0004, respectively). The median (min – max) Tmax of carotegrast methyl in the absence and presence of rifampicin was 1.0 (0.5 – 4.0) and 2.0 (0.5 – 4.0) h, respectively, and tended to be delayed by coadministration with rifampicin. The geometric mean (95% CI) t1/2 of carotegrast methyl after administration of carotegrast methyl alone and in combination with rifampicin was 2.8 (2.2, 3.5) h and 3.7 (3.1, 4.4) h, respectively. The geometric mean (95% CI) MRT0-t of carotegrast methyl after administration of carotegrast methyl alone and in combination with rifampicin was 2.2 (1.9, 2.5) h and 2.3 (2.1, 2.6) h, respectively, with no significant difference between the treatments.