Table 1

Kinetic evaluation of delavirdine metabolism by liver microsomes from several species

SpeciesConditionKM(μM)Vmax (nmol/min/mg)Vmax/KM (ml/min/mg)
HumanPooled6.8  ± 0.80.44  ± 0.0164
RatMale9.9  ± 1.00.40  ± 0.140
MonkeyCynomolgus4.4  ± 0.60.60  ± 0.02135
DogBeagle12.6  ± 1.90.07  ± 0.016
  • Initial rate of delavirdine desalkylation was determined.KM and Vmax were estimated by nonlinear curve fitting based on a single experiment using 8–11 substrate concentrations.