Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study

Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study Publisher

Summary: Can two gefitinib tablets work alike? A validated LC-MS/MS assay found test and reference 250-mg formulations bioequivalent in a pharmacokinetic study. #LungCancer #Pharmacology

Hamishehkar H ; Hosseinpour R ; Sadri F ; Emami J

Source: Mass Spectrometry Letters Published:2026

Abstract

Gefitinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, is approved for first-line treatment of metastatic non-small cell lung cancer. Accurate quantification of gefitinib in plasma is essential for pharmacokinetic and bioequiva-lence studies. This study aimed to develop and validate a rapid, sensitive, and cost-effective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for determining gefitinib in human plasma and to apply it to a bioequivalence study. Gefitinib was extracted from human plasma by protein precipitation using erlotinib as the internal standard. Chromatographic separation was performed on a Hypurity C18 column (30 × 2.1 mm, 3 μm) under isocratic conditions with 0.1% formic acid in acetonitrile and 0.1% formic acid in water (40:60, v/v). Quantification was achieved using a triple quadrupole mass spectrometer in positive ionization mode. The method was validated according to regulatory guidelines and applied to a bioequivalence study of 250 mg gefitinib tablets in 24 healthy volunteers. The assay was linear over 2.5–750 ng/mL (Formula present) with a lower limit of quantification of 2.5 ng/mL using 0.4 mL plasma. Precision was acceptable, with relative standard deviations ranging from 0.30% to 17.57%. Mean CPD[ was 326.99 ± 127.67 ng/mL at 4.17 ± 1.34 h. The 90% confidence intervals for log-transformed CPD[, AUC0±00, and AUC0±’ were within regulatory bioequivalence limits. The validated LC-MS/MS method was accurate, sensitive, and suitable for pharmacokinetic studies. Application to a bioequivalence study demonstrated bioequivalence between the test and reference 250 mg gefitinib formulations. © 2026, Korean Society for Mass Spectrometry. All rights reserved.

Style	Citing Format
MLA	Hamishehkar H, et al.. "Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study." Mass Spectrometry Letters, vol. 17, no. 3, 2026, pp. 153-167.
APA	Hamishehkar H, Hosseinpour R, Sadri F, Emami J (2026). Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study. Mass Spectrometry Letters, 17(3), 153-167.
Chicago	Hamishehkar H, Hosseinpour R, Sadri F, Emami J. "Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study." Mass Spectrometry Letters 17, no. 3 (2026): 153-167.
Harvard	Hamishehkar H et al. (2026) 'Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study', Mass Spectrometry Letters, 17(3), pp. 153-167.
Vancouver	Hamishehkar H, Hosseinpour R, Sadri F, Emami J. Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study. Mass Spectrometry Letters. 2026;17(3):153-167.
BibTex	@article{ author = {Hamishehkar H and Hosseinpour R and Sadri F and Emami J}, title = {Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study}, journal = {Mass Spectrometry Letters}, volume = {17}, number = {3}, pages = {153-167}, year = {2026} }
RIS	TY - JOUR AU - Hamishehkar H AU - Hosseinpour R AU - Sadri F AU - Emami J TI - Development of an Lc-Ms/Ms Method for Gefitinib Quantification and Its Application to a Bioequivalence Study JO - Mass Spectrometry Letters VL - 17 IS - 3 SP - 153 EP - 167 PY - 2026 ER -

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