What is Gefitinib?

Gefitinib is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used primarily for the treatment of non‑small cell lung cancer (NSCLC) in patients whose tumors harbor specific EGFR mutations. By blocking EGFR signaling, gefitinib helps to inhibit tumor cell proliferation and induce apoptosis, thereby improving clinical outcomes in appropriately selected patients.

Reference: U.S. Food and Drug Administration (FDA) Gefitinib Prescribing Information; ClinicalTrials.gov (e.g., NCT00121090)

What are the other popular names for Gefitinib?

Gefitinib is most commonly marketed under the brand name Iressa®. It is also known by its research designation ZD1839.

Reference: MedlinePlus; U.S. FDA

What is the drug classification of Gefitinib?

Gefitinib is classified as an EGFR tyrosine kinase inhibitor (TKI), a subset of targeted anticancer agents. It belongs to the broader category of molecular targeted therapies used in oncology.

Reference: World Health Organization (WHO) guidelines on cancer treatment; U.S. FDA

What is the mode of action of Gefitinib?

Gefitinib acts by selectively binding to the adenosine triphosphate (ATP) binding site of the EGFR tyrosine kinase domain. This inhibits the receptor’s autophosphorylation and downstream signaling through pathways such as MAPK, PI3K/AKT, and STAT, which are critical for tumor growth and survival. Consequently, gefitinib impedes cancer cell proliferation and promotes apoptosis in tumors with EGFR mutations.

Reference: PubMed (e.g., Lynch et al., 2004, “Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib”); U.S. FDA

What are the primary uses of Gefitinib?

Gefitinib is primarily used for the treatment of advanced or metastatic non‑small cell lung cancer (NSCLC) in patients whose tumors have specific activating mutations in the EGFR gene. It is typically prescribed for patients who have either progressed on or are intolerant to standard chemotherapy or other treatments.

Reference: U.S. FDA; ClinicalTrials.gov (e.g., NCT00121090, NCT00333590)

What is the recommended dosage and administration for Gefitinib?

• Dosage: The standard oral dosage for gefitinib is 250 mg once daily.
• Administration:
  • Gefitinib is taken by mouth, with or without food, at approximately the same time each day to maintain steady plasma levels.
  • Patients should follow dosing instructions as prescribed by their healthcare provider.

Reference: U.S. FDA Gefitinib Prescribing Information; ClinicalTrials.gov

What prescribing information is important for Gefitinib?

• Indications: Gefitinib is indicated for patients with advanced NSCLC with sensitizing EGFR mutations.
• Contraindications:
  • It is contraindicated in patients with known hypersensitivity to gefitinib or any of its components.
  • Caution is advised in patients with significant interstitial lung disease.
• Monitoring:
  • Regular evaluation of liver function tests, lung imaging (if respiratory symptoms occur), and monitoring for dermatologic and gastrointestinal adverse effects are essential.
• Special Considerations:
  • EGFR mutation testing is recommended before initiating therapy.
  • Use in pregnant or breastfeeding women is not recommended due to potential teratogenicity.

Reference: U.S. FDA; National Comprehensive Cancer Network (NCCN) Guidelines; WHO

What safety information, side effects, warnings, and cautions are associated with Gefitinib?

• Common Side Effects:
  • Skin rash, diarrhea, nausea, vomiting, and dry skin.
  • Mild elevations in liver enzymes may occur.
• Serious Side Effects:
  • Interstitial lung disease (ILD), which can be fatal; any new or worsening respiratory symptoms should prompt immediate evaluation.
  • Hepatotoxicity and rare cases of severe skin reactions such as Stevens-Johnson syndrome.
• Warnings & Cautions:
  • Interstitial Lung Disease: Patients should be monitored for signs of ILD; treatment should be interrupted if ILD is suspected.
  • Liver Function: Periodic liver function tests are recommended; dose adjustment or discontinuation may be necessary if significant abnormalities occur.
  • Dermatologic Reactions: Severe skin reactions require prompt medical attention.
  • Drug Interactions: Monitor for potential interactions with CYP3A4 inhibitors or inducers, which may alter gefitinib plasma levels.
• Pregnancy:
  • Gefitinib is contraindicated in pregnant or breastfeeding women due to teratogenic risks.

Reference: U.S. FDA Gefitinib Prescribing Information; PubMed; WHO

What drug interactions should be considered with Gefitinib?

• CYP3A4 Modulators:
  • Strong CYP3A4 inhibitors (e.g., ketoconazole) can increase gefitinib levels, while inducers (e.g., rifampin) may decrease its effectiveness.
• Other Medications:
  • Concomitant use of drugs that affect liver enzymes may alter gefitinib metabolism.
  • Use caution with drugs that can exacerbate gastrointestinal toxicity or dermatologic reactions.

Reference: U.S. FDA; Clinical Pharmacology Reviews on PubMed

Frequently Asked Questions (FAQs)

Q: How quickly does Gefitinib start working?
A: Some patients may begin to see improvements in symptoms within a few weeks, but maximum therapeutic effects are usually observed after several months of continuous treatment.

Q: Can Gefitinib be taken with food?
A: Yes, gefitinib can be taken with or without food. However, it is important to take it at the same time each day to maintain consistent drug levels.

Q: What should I do if I experience a severe skin rash or breathing difficulty while on Gefitinib?
A: Seek immediate medical attention, as these may be signs of serious adverse reactions such as Stevens-Johnson syndrome or interstitial lung disease.

Q: Is EGFR mutation testing required before starting Gefitinib?
A: Yes, testing for EGFR mutations is typically recommended to ensure that patients with NSCLC will benefit from gefitinib therapy.

Q: How should missed doses be managed?
A: If you miss a dose, take it as soon as you remember unless it is near the time of your next dose. Do not double the dose to catch up.

Reference: U.S. FDA; NCCN Guidelines; PubMed

Where can I find additional clinical evidence and detailed information about Gefitinib?

For more in-depth clinical data, dosing guidelines, and safety monitoring, please refer to:

• U.S. Food and Drug Administration (FDA) Website: FDA.gov
• ClinicalTrials.gov: Search for gefitinib studies (e.g., NCT00121090, NCT00333540)
• PubMed: For peer‑reviewed research articles on gefitinib and EGFR inhibitors
• World Health Organization (WHO): Guidelines on lung cancer management
• National Comprehensive Cancer Network (NCCN) Guidelines: For treatment protocols in NSCLC

Reference: U.S. FDA; ClinicalTrials.gov; PubMed; NCCN; WHO

Final Thoughts

Gefitinib (marketed as Iressa® and known by its research designation ZD1839) is a cornerstone targeted therapy for patients with advanced NSCLC harboring EGFR mutations. By inhibiting the EGFR tyrosine kinase, it effectively reduces tumor growth and improves clinical outcomes. However, careful patient selection (including EGFR mutation testing), monitoring for adverse effects (especially interstitial lung disease and hepatotoxicity), and managing potential drug interactions are essential for safe and effective therapy. Always consult with your healthcare provider to ensure that gefitinib is the appropriate treatment for your condition.

Disclaimer: This guide is intended for educational purposes only and should not replace professional medical advice. Always consult with your healthcare provider before initiating or modifying any medication regimen.