Generic Name and Formulations:
Gefitinib 250mg; tabs.
First-line treatment of metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
Not established in metastatic NSCLC with EGFR mutations other than exon 19 deletions or exon 21 substitution mutations.
May disperse tabs in water; drink immediately or give via NG tube. Give 250mg once daily until disease progression or unacceptable toxicity occurs. Dose modifications for adverse reactions: see full labeling. Concomitant strong CYP3A4 inducers: increase to 500mg daily; resume at 250mg seven days after discontinuation of the CYP3A4 inducer.
Permanently discontinue if confirmed interstitial lung disease (ILD), severe hepatic impairment, GI perforation, or persistent ulcerative keratitis occurs. Withhold for up to 14 days if acute onset or worsening pulmonary symptoms, NCI CTCAE Grade ≥2 ALT and/or AST elevations, Grade ≥3 diarrhea or skin reactions, or severe or worsening ocular disorders (including keratitis) occurs. Interrupt or discontinue therapy if severe bullous and exfoliative skin disorders develop. Obtain periodic LFTs. Moderate and severe hepatic impairment; monitor. Use effective contraception during treatment and for at least 2 weeks after completion. Pregnancy, nursing mothers: not recommended.
Potentiated by strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole); monitor. Antagonized by strong CYP3A4 inducers (eg, rifampicin, phenytoin, tricyclics); see Adults. May be antagonized by drugs that increase gastric pH (eg, H2-blockers, antacids); take gefitinib 6 hours after or 6 hours before an H2-blocker or antacid. Avoid concomitant PPIs; if necessary, take gefitinib 12 hours after last dose or 12 hours before next PPI dose. May potentiate warfarin; monitor INR.
Tyrosine kinase inhibitor.
Skin reactions, diarrhea, vomiting, decreased appetite, stomatitis; ILD, hepatotoxicity, GI perforation, ocular disorders.
Testing considerations: EGFR mutation analysis.
Join MIMS Learning now to manage all your CPD and notes in one place!
Already a MIMS Learning member?Sign In Now »
This red flags article explains signs and symptoms of potentially serious pathology in patients presenting...
This article by Dr Tillmann Jacobi covers the possible red flag symptoms to consider when a patient...
Dr Suneeta Kochhar provides an overview of red flag symptoms in patients presenting with headaches...
In this article, Dr David Brass and Dr Neil Rajan discuss the risk factors for BCC, making the diagnosis...
This article by Dr Rajiv Sankaranarayanan covers the diagnosis and management of cardiomyopathy. Key...
Dr Benjamin Simpson provides an in-depth overview of Parkinson’s disease, including information on risk...