Gefisa® (Gefitinib)

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Tablet 250 mg

Gefitinib is a tyrosine kinase inhibitor indicated 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 as detected by an FDA-approved test.

INDICATIONS

gefitinib is indicated 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 as detected by an FDA-approved test.

DOSAGE AND ADMINISTRATION

Patient Selection
Select patients for the first-line treatment of metastatic NSCLC with gefitinib based on the presence of EGFR exon 19 deletions or exon 21 L858R mutations in their tumor or plasma specimens. If these mutations are not detected in a plasma specimen, test tumor tissue if feasible.
Recommended Dose
The recommended dose of gefitinib is 250 mg orally once daily with or without food until disease progression or unacceptable toxicity. Do not take a missed dose within 12 hours of the next dose.

WARNINGS AND PRECAUTIONS

Interstitial Lung Disease (ILD) ILD or ILD-like adverse drug reactions (e.g., lung infiltration, pneumonitis, acute respiratory distress syndrome, or pulmonary fibrosis) occurred in 1.3% of the 2462 patients who received gefitib across clinical trials; of these, 0.7% were Grade 3 or higher and 3 cases were fatal. Withhold gefitinib and promptly investigate for ILD in any patient who presents with worsening of respiratory symptoms such as dyspnea, cough and fever. Permanently discontinue gefitinib if ILD is confirmed.
Hepatotoxicity
In patients who received gefitib across clinical trials, 11.4% of patients had increased alanine aminotransferase (ALT), 7.9% of patients had increased aspartate aminotransferase (AST), and 2.7% of patients had increased bilirubin. Grade 3 or higher liver test abnormalities occurred in 5.1% (ALT), 3.0% (AST), and 0.7% (bilirubin) of patients. The incidence of fatal hepatotoxicity was 0.04%. Obtain periodic liver function testing. Withhold gefitinib in patients with worsening liver function and discontinue in patients with severe hepatic impairment.
Gastrointestinal Perforation
Gastrointestinal perforation occurred in three (0.1%) of the 2462 gefitinib-treated patients across clinical trials. Permanently discontinue gefitinib in patients who develop gastrointestinal perforation.
Severe or Persistent
Diarrhea Grade 3 or 4 diarrhea occurred in 3% of 2462 IRESSA-treated patients across clinical trials. Withhold gefitinib for severe or persistent (up to 14 days) diarrhea.
Ocular Disorders including Keratitis
Ocular disorders [keratitis (0.1%), corneal erosion and aberrant eyelash growth (0.2%), conjunctivitis, blephritis and dry eye (6.7%)] occurred in the 2462 gefitinib-treated patients across clinical trials. The incidence of Grade 3 ocular disorders was 0.1%. Interrupt or discontinue gefitinib for severe, or worsening ocular disorders.
Bullous and Exfoliative Skin Disorders
Bullous conditions including toxic epidermal necrolysis, Stevens Johnson syndrome and erythema multiforme have been reported from treatment with gefitinib. Erythema multiforme and dermatitis bullous have been reported in two patients (0.08%) across NSCLC trials (Study 2, Study 3 and Study 4). gefitinib treatment should be interrupted or discontinued if the patient develops severe bullous, blistering or exfoliating conditions.
Embryo-fetal Toxicity
Based on its mechanism of action and data from animal reproduction studies gefitinib can cause fetal harm when administered to a pregnant woman. In animal reproductive studies, oral administration of gefitinib from organogenesis through weaning resulted in fetotoxicity and neonatal death at doses below the recommended human dose. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with gefitinib and for at least two weeks following completion of therapy.

DRUG INTERACTIONS

Drugs Affecting Gefitinib Exposure
-CYP3A4 Inducer Drugs that are strong inducers of CYP3A4 increase the metabolism of gefitinib and decrease gefitinib plasma concentrations. Increase IRESSA to 500 mg daily in patients receiving a strong CYP3A4 inducer (e.g., rifampicin, phenytoin, or tricyclic antidepressant) and resume gefitinib at 250 mg 7 days after discontinuation of the strong inducer.
-CYP3A4 Inhibitor Drugs that are strong inhibitors of CYP3A4 (e.g., ketoconazole and itraconazole) decrease gefitinib metabolism and increase gefitinib plasma concentrations. Monitor adverse reactions when administering strong CYP3A4 inhibitors with gefitinib.
-Drugs Affecting Gastric pH Drugs that elevate gastric pH (e.g., proton pump inhibitors, histamine H2-receptor antagonists, and antacids) may reduce plasma concentrations of gefitinib. Avoid concomitant use of gefitinib with proton pump inhibitors, if possible. If treatment with a proton-pump inhibitor is required, take gefitinib 12 hours after the last dose or 12 hours before the next dose of the proton-pump inhibitor. Take gefitinib 6 hours after or 6 hours before an H2-receptor antagonist or an antacid.
Hemorrhage in Patients taking Warfarin
International Normalized Ratio (INR) elevations and/or hemorrhage have been reported in some patients taking warfarin while on gefitinib therapy. Patients taking warfarin should be monitored regularly for changes in prothrombin time or INR.

Gefitinib <span style="font-size: 13px;">brochure</span>

Gefitinib brochure

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