Bioequivalence study of single-dose lenalidomide capsule vs. Revlimid® capsule in healthy Chinese males.

Abstract

Lenalidomide is a 4-amino-glutaryl derivative of thalidomide and belongs to a new generation of immunomodulatory agents for the treatment of patients with myelodysplastic syndrome and multiple myeloma. The aim of this study is to evaluate the bioequivalence and safety of a capsule containing 25mg of a test formulation of lenalidomide and a 25mg Revlimid® capsule in healthy, Chinese adult males for good quality anti-cancer medicine with lower costs. This was a single-center, randomized, open-label, single-dose, two-period, crossover pharmacokinetic study. Forty-eight healthy, adult Chinese males were administered a test lenalidomide or Revlimid® capsule, 24 in a fasted and 24 in a fed state, followed by crossover to the other capsule. Twenty-four subjects in the fasting group and 23 in the postprandial group completed the clinical trial. Subjects administered test lenalidomide and Revlimid® capsules in the fasting state had a Cmax of 564 ± 153 and 609 ± 121ng/mL, respectively; an AUC0-t of 1660 ± 211 and 1660 ± 235hng/mL, respectively; and an AUC0-∞ of 1670 ± 210 and 1670 ± 237hng/mL, respectively. In the fed state, the subjects had a Cmax of 389 ± 105 and 383 ± 101ng/mL, respectively; an AUC0-t of 1770 ± 314 and 1740 ± 360hng/mL, respectively; and an AUC0-∞ of 1800 ± 316 and 1760 ± 362hng/mL, respectively. Both capsules were well tolerated, with no serious adverse events observed. According to the criteria for bioequivalence, the test formulation of lenalidomide and Revlimid® was determined to be bioequivalent.