Pharmacokinetic parameter estimates of PF06463922 and PF06471402 in athymic mice implanted with H3122 non–small cell lung carcinomas expressing EML4-ALKL1196M
Precision of the estimates is expressed as S.E. in parentheses. PF06463922 and PF06471402 were administered to animals orally twice daily, 7 hours apart (studies 1 and 3) or continuously via subcutaneous infusion with ALZET osmotic pumps (studies 2 and 4).
| ALK Inhibitor | Study | CL/F | V/F | ka |
|---|---|---|---|---|
| l/h per kg | l/kg | h−1 | ||
| PF06463922 | 1a | 1.1 | 7.0 | 1.3 |
| (0.2) | (0.9) | (0.1) | ||
| 2 | 0.84 | 13 | 0.062 | |
| (0.04) | (1) | (0.006) | ||
| PF06471402 | 3 | 3.3 | 14 | 7.6 |
| (0.7) | (4) | (0.7) | ||
| 4 | 1.7 | 32 | 0.036 | |
| (0.4) | (7) | (0.005) |
CL/F, oral clearance; ka, absorption rate constant; V/F, oral volume of distribution.
↵a The values in study 1 are cited from the previous report (Yamazaki et al., 2014).