Table 3

CLint values and in vitro half-lives for selected progestins, derived from human liver microsomal incubations with either 2 or 15 μM drug concentrations and an incubation time of 60 min

Compound2 μM15 μM
In Vitro CLintScaled In Vivo CLintt1/2In Vitro CLintScaled In Vivo CLintt1/2
ml/min/mg liters/hr min ml/min/mg liters/hr min
3-Keto-desogestrel0.02486104.454.60.0160067.276.4
Desogestrel0.0130955.068.80.0131655.375.6
Norgestimate0.06600277.220.80.02700113.438.4
Levonorgestrel0.0172972.678.80.0102443.0127
Gestodene0.02471103.847.50.0094339.6131
Norethisterone0.0192981.073.70.0174373.270
Dienogest0.0191480.464.90.0090037.8127