Gefitinib

GEFITINIB

Manufacturer: Natco Pharma USA LLC

Score: 142.0

Quick Summary

Gefitinib is a kinase inhibitor used for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations. The recommended dose is 250 mg orally once daily with or without food. Gefitinib can cause fetal harm when administered to a pregnant woman and has several important safety warnings, including interstitial lung disease, hepatotoxicity, and gastrointestinal perforation.

Key Clinical Findings and Indications

First-line treatment of metastatic NSCLC with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations
Kinase inhibitor that reversibly inhibits the kinase activity of wild-type and certain activating mutations of EGFR

Important Safety Information

Warning

Gefitinib can cause fetal harm when administered to a pregnant woman and has several important safety warnings, including interstitial lung disease, hepatotoxicity, and gastrointestinal perforation.

Contraindications

None

Adverse Reactions

Skin reactions
Diarrhea
Nausea
Vomiting
Stomatitis
Conjunctivitis/blepharitis/dry eye

Dosing Recommendations

General Guidance

Increase to 500 mg daily in patients receiving a strong CYP3A4 inducer, and resume at 250 mg 7 days after discontinuation of the strong inducer.

Metastatic NSCLC with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations

Adult Dose

250 mg orally once daily with or without food

Pediatric Dose

Not established

Special Population Considerations

Pregnancy

Can cause fetal harm when administered to a pregnant woman
Advise pregnant women of the potential hazard to a fetus or potential risk for loss of the pregnancy

Nursing Mothers

May result in reduced fertility in females of reproductive potential
Advise females of reproductive potential to use effective contraception during treatment with gefitinib and for at least two weeks following completion of therapy

Pediatric Use

The safety and effectiveness of gefitinib in pediatric patients have not been established

Geriatric Use

No overall differences in safety were observed between patients 65 years and older and those younger than 65 years
There is insufficient information to assess for differences in efficacy between older and younger patients