Prediction of human pharmacokinetics and CLrenal for PF-06282999

Predicted Human Pharmacokinetics ParameteraRatDogMonkey
CLp (ml/min per kilogram)
Vdss (l/kg)
t1/2 (h)
Total CLrenal (ml/min per kg)b3.00.60.7
  • a Observed pharmacokinetics in humans was as follows: CLp = 1.8–2.1 ml/min per kilogram and Vdss = 0.65–0.78 l/kg (20–200 mg p.o. doses) obtained from the respective CL/F and Vz/F values normalized for F values corresponding to the percentage of dose eliminated in unchanged form in urine in a 24-hour period at the respective p.o. doses. Human t1/2 was estimated to be 3.9–4.2 hours (20–200 mg p.o. doses) and was calculated using the equation 0.693 × Vdss/CLp.

  • b Observed total CLrenal in humans was1.8–2.1 ml/min per kilogram (20–200 mg p.o. doses).