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2013 (v.21 no.2)

The Journal of Korean Society for Clinical Pharmacology and Therapeutics

Korean Society for Clinical Pharmacology and Therapeutics
Semiannual
ISSN: 1225-5467

  • Bioequivalence of Two Erlotinib Formulations in Healthy Volunteers

    JaeWoo Kim, Eun-Heui Jin, Youn-Woong Choi, Byung-Gu Min, Byung-Hoon Lee, Jin-Seong Chung, Kyu-Yeol Nam, Won-Tae Jung, Soo-Hwan Kim, Hye J. Lee, Jang-Hee Hong

    J Korean Soc Clin Pharmacol Ther | v.21, no.2, pp.159-165, Dec, 2013

    Abstract

    Background: Erlotinib is a tyrosine kinase inhibitor prescribed for the treatment of non-small cell lung
    cancer and pancreatic cancer. The aim of this study was to compare the safety and pharmacokinetics
    (PK) of a generic (test) formulation of erlotinib with those of a reference formulation in healthy
    volunteers.
    Methods: A randomized, open-label, single-dose two-treatment, two-period, two-sequence, crossover
    study was conducted in Clinical Trials Center, Chungnam National University Hospital with 40 healthy
    men. Subjects orally received either one 150 mg tablet of the test or the corresponding dose of the
    reference, and crossover phases were separated by 14-day washout. Plasma samples were collected up
    to 72 hr post-dose. Plasma erlotinib concentrations were determined by liquid chromatography-tandem
    mass spectrometry. PK parameters were calculated by non-compartmental analysis. The safety was
    monitored throughout the study.
    Results: A total of 21 cases of adverse events were reported. They are mild and relieved without an
    intervention. There was no serious adverse event. Median times to peak concentration of two
    formulations were 3.0. Means [SD] for peak concentration (Cmax) and area under the plasma
    concentration-time curve (AUC) of the test were 1,298 [346] μg/L and 25,318 [7,668] hr×μg/L. Those of
    the reference were 1,193 [378] μg/L and 24,853 [8,419] hr×μg/L. Geometric mean ratios (90 % confidence
    intervals) for the test to the reference were 1.10 (1.02?1.18) for Cmax and 1.02 (0.97?1.09) for AUC.
    Conclusion: Two formulations were safe and well-tolerated. PK findings suggest that the test
    formulation is equivalent to the reference in terms of pharmacokinetics.

    Keyword

    Erlotinib, Pharmacokinetics, Bioequivalence, Healthy, Volunteer