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Gefitinib
A F M Motiur Rahman1, Hesham M Korashy2, Mohammed Gabr Kassem1
1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Abstract:
Gefitinib (Iressa®) is a selective inhibitor of epidermal growth factor, a growth factor that plays a pivotal role in the control of cell growth, apoptosis, and angiogenesis. Gefitinib is clinically used for the treatment of chemoresistant non-small cell lung cancer patients. Gefitinib is freely soluble in dimethylsulphoxide but slightly soluble in methanol and ethanol. Several methods of gefitinib synthesis are included in this review. UV spectroscopy of gefitinib showed a λmax of approximately 331nm, whereas IR spectroscopy principal peaks were observed at 3400cm(-1) (NH), 2956cm(-1) (CH2, CH, alkyl), 1625cm(-1) (CC, CN), 1500cm(-1) (HCCH, aryl), 1110cm(-1) (CO), 1028cm(-1) (CF). In addition, different analytical methods for determination of gefitinib are also described in this review. Pharmacokinetically, after oral administration, gefitinib is slowly absorbed with bioavailability of approximately 60% in human. Gefitinib is metabolized extensively in the liver into five metabolites by cytochrome P450s, primarily by CYP3A4 and to a lesser extent by CYP3A5 and CYP2D6. Gefitinib is eliminated mainly hepatically with total plasma clearance of 595mL/min after intravenous administration. Most of the adverse effects associated with gefitinib therapy are mild to moderate in severity and are usually reversible and manageable with appropriate intervention, such as diarrhea, dry skin, rash, nausea, and vomiting.
Insights
Gefitinib effectively treats chemoresistant non-small cell lung cancer by inhibiting epidermal growth factor. This review details its synthesis, analytical methods, pharmacokinetics, and manageable side effects.
Area of Science:
- Pharmacology and Medicinal Chemistry
- Oncology
- Drug Metabolism
Background:
- Gefitinib (Iressa®) is a targeted therapy inhibiting epidermal growth factor receptor (EGFR).
- It is clinically utilized for non-small cell lung cancer (NSCLC) resistant to chemotherapy.
- EGFR signaling is crucial for cell proliferation, survival, and blood vessel formation.
Purpose of the Study:
- To review synthesis pathways for Gefitinib.
- To summarize analytical techniques for Gefitinib determination.
- To provide an overview of Gefitinib's pharmacokinetic and safety profile.
Main Methods:
- Literature review of Gefitinib synthesis and analysis.
- Analysis of pharmacokinetic data including absorption, metabolism, and elimination.
- Compilation of reported adverse effects from clinical use.
Main Results:
- Multiple Gefitinib synthesis routes are available.
- Spectroscopic data (UV, IR) and analytical methods for Gefitinib are described.
- Gefitinib exhibits ~60% oral bioavailability, extensive hepatic metabolism (CYP3A4, CYP3A5, CYP2D6), and a plasma clearance of 595mL/min.
- Common adverse effects include diarrhea, rash, and nausea, generally mild and manageable.
Conclusions:
- Gefitinib is a key therapeutic agent for specific NSCLC populations.
- Understanding its synthesis, analysis, and pharmacokinetics is vital for effective clinical application.
- Adverse effects are typically manageable, supporting its continued use in targeted cancer therapy.
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