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Updated: Aug 3, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

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Published on: September 19, 2013

Pharmacokinetic evaluation of gefitinib when administered with chemotherapy

Lisa A Hammond1

  • 1Institute for Drug Development, Cancer Therapy Research Center, San Antonio, TX, USA. lhammond@idd.org

Clinical Lung Cancer
|December 4, 2003
PubMed

Insights

Gefitinib combined with chemotherapy shows promise for solid tumors. This epidermal growth factor receptor-tyrosine kinase inhibitor was well tolerated and did not increase chemotherapy toxicity in early trials.

Area of Science:

  • Oncology
  • Pharmacology
  • Medical Oncology

Background:

  • Gefitinib is an epidermal growth factor receptor-tyrosine kinase (EGFR-TK) inhibitor.
  • Preclinical data suggest gefitinib enhances antitumor effects with cytotoxic agents.
  • Phase I trials indicate gefitinib is well tolerated at doses below maximum tolerated levels.

Purpose of the Study:

  • To evaluate the safety and pharmacokinetic interactions of gefitinib in combination with chemotherapy for solid tumors.
  • To assess the tolerability and potential drug interactions of gefitinib with carboplatin/paclitaxel and cisplatin/gemcitabine.

Main Methods:

  • Phase I studies investigated gefitinib (250 mg or 500 mg daily) with chemotherapy in solid tumors.
  • A randomized crossover study assessed gefitinib and carboplatin/paclitaxel in advanced non-small-cell lung cancer (NSCLC).
  • An open-label trial combined gefitinib with cisplatin/gemcitabine in various solid tumors, including NSCLC.

Main Results:

  • Gefitinib combined with chemotherapy was generally well tolerated.
  • No increased exposure to tested chemotherapy agents was observed.
  • Increased gefitinib exposure occurred with the carboplatin/paclitaxel regimen.
  • No apparent increase in higher-grade toxicity was noted.

Conclusions:

  • Gefitinib can be safely combined with certain chemotherapy regimens for solid tumors.
  • Combination therapy did not significantly increase chemotherapy toxicity in initial studies.
  • Further trials are ongoing to explore gefitinib's role in combination cancer therapy.

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