Metabolite Characterization of Anti-cancer Agent Gefitinib in Human Hepatocytes

ISSN: 1874-0758 (Online)
ISSN: 1872-3128 (Print)

Volume 11, 4 Issues, 2017

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Drug Metabolism Letters

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Zhiyang Zhao
Alliance Pharma
Malvern, PA

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Metabolite Characterization of Anti-cancer Agent Gefitinib in Human Hepatocytes

Drug Metabolism Letters, 7(2): 126-136.

Author(s): Prashant Surve, Selvan Ravindran, Arghya Acharjee, Himanshu Rastogi, Sudipta Basu and Pradnya Honrao.

Affiliation: Departments of Bio- Analytical and Biotransformation, Drug Metabolism and Pharmacokinetics Unit, Sai Life Sciences Limited, Building 1, Plot No 2, Chrysalis Enclave, International Biotech Park, Pune 411057, Maharashtra, India.


Intensive Biotransformation studies on Gefitinib could play a significant role in designing and synthesizing new drugs around the core structure of Gefitinib. These studies may be useful in developing an entirely new drug by blocking the metabolic spots in Gefitinib. Gefitinib (Iressa) was the first oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. Gefitinib shows toxicity to cancer cells and has the capability to inhibit the growth of cancer cells. Gefitinib is considered as one of the selective EGFR inhibitors to be available in clinical practice. In 2003, FDA had approved Gefitinib for metastatic non-small-cell lung cancer therapy (NSCLC). However, it was observed that NSCLC Patients who responded to treatment developed resistance to Gefitinib. Hence, in the present study Gefitinib was incubated with hepatocytes to identify both phase-I and Phase-II metabolites. Identified Phase –I metabolites were due to oxidative defluorination, N-dealkylation and loss of morpholine ring. One of the phase-II metabolites identified i.e. the glutathione adduct suggests the need to modify the structure of the drug for higher potency and safety.


Drug metabolism, gefitinib, liquid chromatography, mass spectrometry, metabolites.

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Article Details

Volume: 7
Issue Number: 2
First Page: 126
Last Page: 136
Page Count: 11
DOI: 10.2174/1872312808666140317154110
Price: $58

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