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Evaluation of the Absolute Oral Bioavailability and Bioequivalence of Erlotinib, an Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in a Randomized, Crossover Study in Healthy Subjects
Author(s) -
Frohna Paul,
Lu Jianfeng,
Eppler Steve,
Hamilton Marta,
Wolf Julie,
Rakhit Ashok,
Ling Jie,
KenkareMitra Saraswati R.,
Lum Bert L.
Publication year - 2006
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270005284193
Subject(s) - erlotinib , bioequivalence , bioavailability , pharmacology , crossover study , pharmacokinetics , medicine , erlotinib hydrochloride , oral administration , epidermal growth factor receptor , cancer , placebo , alternative medicine , pathology
A randomized, open‐label, 2‐period crossover study was conducted to evaluate the bioequivalence of 6 tablets of erlotinib 25 mg and 1 tablet of erlotinib 150 mg (arm A, n = 42) and the oral bioavailability of the 150‐mg tablet versus a 25‐mg intravenous infusion (arm B, n = 20) in healthy subjects. The washout period was 2 weeks between treatments. Plasma concentrations of erlotinib and its active metabolite, OSI‐420, were measured after each dose. The ratios of geometric means for AUC 0‐∞ and C max of erlotinib following 6 tablets of erlotinib 25 mg and 1 tablet of erlotinib 150 mg were (1 and 0.95) within the predefined bioequivalence range of 0.80 to 1.25. The mean absolute oral bioavailability, using compartmental analysis, was estimated as 59% (95% confidence interval, 55%–63%). Overall, 6 tablets of erlotinib 25 mg are bioequivalent to a single 150‐mg tablet. Both intravenous and oral erlotinib were generally well tolerated with an estimated bioavailability of 59% following oral administration.