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
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  μg/L and 25,318 [7,668] hr×μg/L. Those of
the reference were 1,193  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.