Bioequivalence study of single-dose lenalidomide capsule vs. Revlimid® capsule in healthy Chinese males
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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.
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 ± 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.
According to the criteria for bioequivalence, the test formulation of lenalidomide and Revlimid® was determined to be bioequivalent.
KeywordsLenalidomide Revlimid® Pharmacokinetics Bioequivalence LS-MS/MS
JW and XHW made substantial contributions to the conception and design of this study, to the acquisition of data, and to the analysis and interpretation of the data. LQ, ZJW, GC, CL, XNL, YW, YL, and CPL made substantial contributions to the implementation of the study. All authors read and approved the final manuscript.
Compliance with ethical standards
Conflict of interest
The authors indicate that they have no conflicts of interest regarding the content of this article.
- 21.FDA Contains Nonbinding Recommendations, Draft Guidance on Lenalidomide (2013) https://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM326798.pdf