Objective: 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 25 mg of a test formulation of lenalidomide and a 25 mg Revlimid® capsule in healthy, Chinese adult males for good quality anti-cancer medicine with lower costs.
Methods: 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.
Results: 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 ± 121 ng/mL, respectively; an AUC0-t of 1660 ± 211 and 1660 ± 235 h ng/mL, respectively; and an AUC0-∞ of 1670 ± 210 and 1670 ± 237 h ng/mL, respectively. In the fed state, the subjects had a Cmax of 389 ± 105 and 383 ± 101 ng/mL, respectively; an AUC0-t of 1770 ± 314 and 1740 ± 360 h ng/mL, respectively; and an AUC0-∞ of 1800 ± 316 and 1760 ± 362 h ng/mL, respectively. Both capsules were well tolerated, with no serious adverse events observed.
Conclusion: According to the criteria for bioequivalence, the test formulation of lenalidomide and Revlimid® was determined to be bioequivalent.
Keywords: Bioequivalence; LS-MS/MS; Lenalidomide; Pharmacokinetics; Revlimid®.