Gefitinib
Generic Name: gefitinib
Brand Names:
Gefitinib
11 DESCRIPTION Gefitinib is a kinase inhibitor. The chemical name of gefitinib is N-(3ʹ-Chloro-4ʹ-fluorophenyl)-7-methoxy-6-{3-(4- morpholinyl)proproxy}-4-quinazolinamine and the following structural formula: Gefitinib has the molecular formula C 22 H 24 ClFN 4 O 3 , a relative molecular mass of 446.9 daltons and is a White to off-white crystalline powder. Gefitinib is a free base. The molecule has pKa1 is 6.5 & pKa2 is 6.9.
Overview
11 DESCRIPTION Gefitinib is a kinase inhibitor. The chemical name of gefitinib is N-(3ʹ-Chloro-4ʹ-fluorophenyl)-7-methoxy-6-{3-(4- morpholinyl)proproxy}-4-quinazolinamine and the following structural formula: Gefitinib has the molecular formula C 22 H 24 ClFN 4 O 3 , a relative molecular mass of 446.9 daltons and is a White to off-white crystalline powder. Gefitinib is a free base. The molecule has pKa1 is 6.5 & pKa2 is 6.9.
Uses
1 INDICATIONS AND USAGE Gefitinib tablets are 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 [see Clinical Studies (14) ]. Limitation of Use: Safety and efficacy of gefitinib tablets have not been established in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution mutations [see Clinical Studies (14) ].
Dosage
2 DOSAGE AND ADMINISTRATION Recommended dose is 250 mg orally, once daily with or without food. ( 2.2 ) 2.1 Patient Selection Select patients for the first-line treatment of metastatic NSCLC with gefitinib tablets are based on the presence of EGFR exon 19 deletions or exon 21 (L858R) mutations in their tumor or plasma specimens [see Indications and Usage (1) , Clinical Studies (14) ]. If these mutations are not detected in a plasma specimen, test tumor tissue if feasible. Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: http://www.fda.gov/Companion Diagnostics. 2.2 Recommended Dose The recommended dose of gefitinib tablets is 250 mg orally once daily with or without food until disease progression or unacceptable toxicity.
Side Effects
6 ADVERSE REACTIONS The following adverse drug reactions are discussed in more detail in other sections of the labeling: Interstitial Lung Disease [see Warnings and Precautions (5.1) ] Hepatotoxicity [see Warnings and Precautions (5.2) ] Gastrointestinal Perforation [see Warnings and Precautions (5.3) ] Severe or Persistent Diarrhea [see Warnings and Precautions (5.4) ] Ocular Disorders including Keratitis [see Warnings and Precautions (5.5) ] Bullous and Exfoliative Skin Disorders [see Warning and Precautions (5.6) ] The most commonly reported adverse drug reactions (ADRs), reported in more than 20% of the patients and greater than placebo were skin reactions and diarrhea.
Interactions
7 DRUG INTERACTIONS CYP3A4 Inducer: Increase gefitinib tablets to 500 mg daily in patients receiving a strong CYP3A4 inducer. ( 2.4 , 7.1 ) CYP3A4 Inhibitor: Monitor adverse reactions if concomitant use with gefitinib tablets. ( 7.1 ) Drugs Affecting Gastric pH: Avoid concomitant use of gefitinib tablets with proton pump inhibitors, if possible. ( 7.1 ) Hemorrhage in patients taking warfarin: Monitor changes in prothrombin time or INR. ( 7.2 ) 7.1 Drugs Affecting Gefitinib Exposure CYP3A4 Inducer Drugs that are strong inducers of CYP3A4 increase the metabolism of gefitinib and decrease gefitinib plasma concentrations.
Warnings
5 WARNINGS AND PRECAUTIONS Interstitial lung disease (ILD): ILD occurred in patients taking gefitinib tablets Withhold gefitinib tablets for worsening of respiratory symptoms. Discontinue gefitinib tablets if ILD is confirmed. ( 2.4 , 5.1 ) Hepatotoxicity: Obtain periodic liver function testing. Withhold gefitinib tablets for Grade 2 or higher for ALT and/or AST elevations. Discontinue for severe hepatic impairment. ( 2.4 , 5.2 ) Gastrointestinal perforation: Discontinue gefitinib tablets for gastrointestinal perforation. ( 2.4 , 5.3 ) Diarrhea: Withhold gefitinib tablets for Grade 3 or higher diarrhea. ( 2.4 , 5.4 ) Ocular Disorders including Keratitis: Withhold gefitinib tablets for signs and symptoms of severe or worsening ocular disorders including keratitis. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on its mechanism of action and animal data, gefitinib tablets 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 (see Animal Data). Advise pregnant women of the potential hazard to a fetus or potential risk for loss of the pregnancy.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Gefitinib tablets are available as 250 mg. 250 mg tablets: brown colored, round shaped, film coated tablets debossed with ‘N’ on one side and ‘250’ on other side. Gefitinib tablets are supplied as: Bottle of 30 Tablets (NDC 69339-168-03) Store at controlled room temperature 20°C-25°C (68°F-77°F) [see USP Controlled Room Temperature].
Frequently Asked Questions
What is Gefitinib used for?▼
1 INDICATIONS AND USAGE Gefitinib tablets are 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 [see Clinical Studies (14) ]. Limitation of Use: Safety and efficacy of gefitinib tablets have not been established in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution mutations [see Clinical Studies (14) ].
What are the side effects of Gefitinib?▼
6 ADVERSE REACTIONS The following adverse drug reactions are discussed in more detail in other sections of the labeling: Interstitial Lung Disease [see Warnings and Precautions (5.1) ] Hepatotoxicity [see Warnings and Precautions (5.2) ] Gastrointestinal Perforation [see Warnings and Precautions (5.3) ] Severe or Persistent Diarrhea [see Warnings and Precautions (5.4) ] Ocular Disorders including Keratitis [see Warnings and Precautions (5.5) ] Bullous and Exfoliative Skin Disorders [see Warning and Precautions (5.6) ] The most commonly reported adverse drug reactions (ADRs), reported in more than 20% of the patients and greater than placebo were skin reactions and diarrhea.
Can I take Gefitinib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on its mechanism of action and animal data, gefitinib tablets 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 (see Animal Data). Advise pregnant women of the potential hazard to a fetus or potential risk for loss of the pregnancy.
What are the important warnings for Gefitinib?▼
5 WARNINGS AND PRECAUTIONS Interstitial lung disease (ILD): ILD occurred in patients taking gefitinib tablets Withhold gefitinib tablets for worsening of respiratory symptoms. Discontinue gefitinib tablets if ILD is confirmed. ( 2.4 , 5.1 ) Hepatotoxicity: Obtain periodic liver function testing. Withhold gefitinib tablets for Grade 2 or higher for ALT and/or AST elevations. Discontinue for severe hepatic impairment. ( 2.4 , 5.2 ) Gastrointestinal perforation: Discontinue gefitinib tablets for gastrointestinal perforation. ( 2.4 , 5.3 ) Diarrhea: Withhold gefitinib tablets for Grade 3 or higher diarrhea. ( 2.4 , 5.4 ) Ocular Disorders including Keratitis: Withhold gefitinib tablets for signs and symptoms of severe or worsening ocular disorders including keratitis. 4 CONTRAINDICATIONS None. None. ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.