Table 1.
VX-765 and VRT-043198 are detected in plasma after a single IP dose of VX-765.
| Time (h) | Mouse 1 VX-765 (μM) | Mouse 2 VX-765 (μM) | Mouse 1 VRT-043198 (μM) | Mouse 2 VRT-043198 (μM) | Mean VX-765 (μM)(a) | Mean VRT-043198 (μM)(b) |
|---|---|---|---|---|---|---|
| 0.25 | 0.31 | 0.27 | 201.8 | 180.4 | 0.29 | 191.1 |
| 0.50 | 1.54 | 0.49 | 338.1 | 104.1 | 1.01 | 221.1 |
| 1 | 0.87 | 1.63 | 24.4 | 51.0 | 1.25 | 37.7 |
| 3 | 0.45 | 0.35 | 1.16 | 0.78 | 0.40 | 0.97 |
| 6 | 0.43 | 0.22 | 0.46 | 0.30 | 0.33 | 0.38 |
| 8 | 0.2 | 0.45 | 0.35 | 0.24 | 0.32 | 0.30 |
| 24 | 0.008 | 0.014 | NQ | NQ | 0.01 | – |
| Cmax (μM)(c) | 1.54 | 1.63 | 338.1 | 180.4 | 1.59 | 259.3 |
| Tmax (h)(d) | 0.50 | 1.00 | 0.50 | 0.25 | 0.75 | 0.40 |
| Half-life (t1/2) (h)(e) | 3.22 | 3.17 | NR | NR | 3.2 | – |
| MRTinf (h)(f) | 4.80 | 5.64 | 0.67 | 0.78 | 5.22 | 0.70 |
NQ: not quantifiable. No peak of below lower limit of quantification: 0.05 μM for VX-765 and 0.098 μM for VRT-043198.
NR: not reported. Only two points used for terminal slope calculation or the span of the terminal phase is too short to allow for accurate estimation of half-life.
Individual data points showing VX-765 and VRT-043198 concentrations up to 24 h post-injection (n = 2 per time point). (a) VX-765 and (b) VRT-043198 mean concentrations at each time point. (c) Maximum concentration achieved (Cmax), (d) time to reach Cmax (Tmax), (e) half-life (t1/2) and (f) mean residence time (MRT) in plasma for VX-765 and VRT-043198.