Gefitinib
Tablet, Film Coated · Oral
Uses
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) ]. Gefitinib tablets are 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. ( 1 ) Limitation of Use: Safety and efficacy of gefitinib tablets have not been established in patients whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution mutations. ( 1 )
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. Do not take a missed dose within 12 hours of the next dose. 2.3 Administration to Patients Who Have Difficulty Swallowing Solids Immerse gefitinib tablet in 4 to 8 ounces of water by dropping the tablet in water, and stir for approximately 15 minutes. Immediately drink the liquid or administer through a naso-gastric tube. Rinse the container with 4 to 8 ounces of water and immediately drink or administer through the naso-gastric tube. 2.4 Dose Modification Dose Modifications for Adverse Drug Reactions Withhold gefitinib tablets (for up to 14 days) for any of the following: Acute onset or worsening of pulmonary symptoms (dyspnea, cough, fever) [see Warnings and Precautions (5.1) ] NCI CTCAE Grade 2 or higher in ALT and/or AST elevations [see Warnings and Precautions (5.2) ] NCI CTCAE Grade 3 or higher diarrhea [see Warnings and Precautions (5.4) ] Signs and symptoms of severe or worsening ocular disorders including keratitis [see Warnings and Precautions (5.5) ] NCI CTCAE Grade 3 or higher skin reactions [see Warnings and Precautions (5.6) ] Resume treatment with gefitinib tablets when the adverse reaction fully resolves or improves to NCI CTCAE Grade 1. Permanently discontinue gefitinib tablets for: Confirmed interstitial lung disease (ILD) [see Warnings and Precautions (5.1) ] Severe hepatic impairment [see Warnings and Precautions (5.2) ] Gastrointestinal perforation [see Warnings and Precautions (5.3) ] Persistent ulcerative keratitis [see Warnings and Precautions (5.5) ] Dose Modifications for Drug Interactions Strong CYP3A4 Inducers Increase gefitinib tablets to 500 mg daily in the absence of severe adverse drug reaction, and resume gefitinib tablets at 250 mg seven days after discontinuation of the strong CYP3A4 inducer [see Drug Interactions (7) , Clinical Pharmacology (12.3) ].
Dosage forms and strengths
250 mg tablets: brown colored, round shaped, film-coated, tablets debossed with ‘N’ on one side and ‘250’ on other side. Tablets: 250 mg. ( 3 )
Contraindications
None. None. ( 4 )
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. Discontinue for persistent ulcerative keratitis. ( 2.4 , 5.5 ) Bullous and Exfoliative Skin Disorders: Withhold gefitinib tablets for Grade 3 or higher skin reactions or exfoliative conditions. ( 2.4 , 5.6 ) Embryo-fetal Toxicity: Can cause fetal harm. Advise of potential risk to a fetus and use of effective contraception. ( 5.7 , 8.1 , 8.3 ) 5.1 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 gefitinib tablets across clinical trials; of these, 0.7% were Grade 3 or higher and 3 cases were fatal. Withhold gefitinib tablets and promptly investigate for ILD in any patient who presents with worsening of respiratory symptoms such as dyspnea, cough and fever. Permanently discontinue gefitinib tablets if ILD is confirmed [see Dosage and Administration (2.4) , Adverse Reactions (6.1) ]. 5.2 Hepatotoxicity In patients who received gefitinib tablets 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 tablets in patients with worsening liver function and discontinue in patients with severe hepatic impairment [see Dosage and Administration (2.4) , Adverse Reactions (6.1) , Use in Specific Populations (8.7) ]. 5.3 Gastrointestinal Perforation Gastrointestinal perforation occurred in three (0.1%) of the 2462 gefitinib tablets-treated patients across clinical trials [see Adverse Reactions (6.1)]. Permanently discontinue gefitinib tablets in patients who develop gastrointestinal perforation [see Dosage and Administration (2.4) ]. 5.4 Severe or Persistent Diarrhea Grade 3 or 4 diarrhea occurred in 3% of 2462 gefitinib tablets-treated patients across clinical trials. Withhold gefitinib tablets for severe or persistent (up to 14 days) diarrhea [see Dosage and Administration (2.4) , Adverse Reactions (6.1) ]. 5.5 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 tablets -treated patients across clinical trials. The incidence of Grade 3 ocular disorders was 0.1% [see Adverse Reactions (6.1) ]. Interrupt or discontinue gefitinib tablets for severe, or worsening ocular disorders [see Dosage and Administration (2.4) ]. 5.6 Bullous and Exfoliative Skin Disorders Bullous conditions including toxic epidermal necrolysis, Stevens Johnson syndrome and erythema multiforme have been reported from treatment with gefitinib tablets. Erythema multiforme and dermatitis bullous have been reported in two patients (0.08%) across NSCLC trials (Study 2, Study 3 and Study 4). Gefitinib tablets treatment should be interrupted or discontinued if the patient develops severe bullous, blistering or exfoliating conditions. 5.7 Embryo-fetal Toxicity Based on its mechanism of action and data from animal reproduction studies 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. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with gefitinib tablets and for at least two weeks following completion of therapy [see Use in Specific Populations (8.1 , 8.3 )].
Side effects
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. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Natco Pharma USA LLC at 201-786-6500 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety gefitinib tablets of is based on the data from 2462 patients with NSCLC who received gefitinib tablets 250 mg daily monotherapy in three randomized clinical studies (Study 2, Study 3 and Study 4). Patients with a history of interstitial lung disease, drug-induced interstitial disease, radiation pneumonitis that required steroid treatment or any evidence of clinically active interstitial lung disease were excluded from these studies. Controlled Studies: Study 2 was a randomized, multicenter, open-label trial in which 1217 patients were randomized to receive first-line treatment for metastatic NSCLC; 607 patients received gefitinib tablets 250 mg daily and 589 patients received carboplatin/paclitaxel. The median duration of treatment with gefitinib tablets was 5.9 months. The study population characteristics were: median age 57 years, age less than 65 years (73%), female (79%), Asian (100%), NSCLC adenocarcinoma histology (100%), never smoker (94%), light ex-smoker (6%), ECOG PS 0 or 1 (90%). Study 3 was a randomized, multicenter, double-blind, placebo-controlled trial in which 1692 patients were randomized to receive second-or third-line treatment for metastatic NSCLC; of which 1126 patients received gefitinib tablets 250 mg daily and 562 patients received placebo. The median duration of treatment with gefitinib tablets was 2.9 months. The study population characteristics were: median age 62 years, age less than 65 years (60%), female (33%), Caucasian (75%), Asian (21%), NSCLC adenocarcinoma histology (48%), never smoker (22%), ECOG PS 0 or 1 (65%), PS 2 (29%), PS 3 (5%) and two or more prior therapies (51%). Study 4 was a randomized, multicenter, open-label trial in which 1466 patients were randomized to receive second-line treatment for metastatic NSCLC; 729 patients received gefitinib tablets 250 mg daily and 715 patients received docetaxel. The median duration of treatment with gefitinib tablets was 2.4 months. The study population characteristics were: median age 61 years, age less than 65 years (61%), female (36%), Caucasian (79%), Asian (21%), NSCLC adenocarcinoma histology (54%), never smoker (20%), ECOG PS 0 or 1 (88%) and two or more prior therapies (16%). The pooled safety database from the three randomized trials was used to evaluate for serious and uncommon adverse drug reactions. Common adverse reactions were evaluated in Study 3. The most frequent adverse reactions in Study 3 (incidence of >20% and greater than placebo) reported in gefitinib tablets-treated patients were skin reactions (47%) and diarrhea (29%). The most frequent fatal adverse reactions in gefitinib tablets-treated patients were respiratory failure (0.9%), pneumonia (0.8%), and pulmonary embolism (0.5%). Approximately 5% of gefitinib tablets -treated patients and 2.3% of placebo-treated patients discontinued treatment due to and adverse event. The most frequent adverse reactions that led to discontinuation in patients treated with gefitinib tablets were nausea (0.5%), vomiting (0.5%) and diarrhea (0.4%).
Drug 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. Increase gefitinib tablets to 500 mg daily in patients receiving a strong CYP3A4 inducer (e.g., rifampicin, phenytoin, or tricyclic antidepressant) and resume gefitinib tablets at 250 mg 7 days after discontinuation of the strong inducer [see Dosage and Administration (2.4) , Clinical Pharmacology (12.3) ]. 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 tablets. 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 tablets with proton pump inhibitors, if possible. If treatment with a proton-pump inhibitor is required, take gefitinib tablets 12 hours after the last dose or 12 hours before the next dose of the proton-pump inhibitor. Take gefitinib tablets 6 hours after or 6 hours before an H2-receptor antagonist or an antacid [see Clinical Pharmacology (12.3) ]. 7.2 Hemorrhage in Patients taking Warfarin International Normalized Ratio (INR) elevations and/or hemorrhage have been reported in some patients taking warfarin while on gefitinib tablets therapy. Patients taking warfarin should be monitored regularly for changes in prothrombin time or INR.
Use in specific populations
Lactation: Discontinue breast-feeding. ( 8.2 ) 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. The background risk of major birth defects and miscarriage for the indicated population is unknown; however, the background risk in the U.S. general population of major birth defects is 2 - 4% and miscarriage is 15 - 20% of clinically recognized pregnancies. Data Animal Data A single dose study in rats showed that gefitinib crosses the placenta after an oral dose of 5 mg/kg (30 mg/m 2 , about 0.2 times the recommended human dose on a mg/m 2 basis). When pregnant rats were treated with 5 mg/kg from the beginning of organogenesis to the end of weaning there was a reduction in the number of offspring born alive. This effect was more severe at 20 mg/kg (approximate the human clinical dose on a mg/m 2 basis) and was accompanied by high neonatal mortality soon after parturition. In rabbits, a dose of 20 mg/kg/day (240 mg/m 2 , about twice the recommended dose in humans on a mg/m 2 basis) caused reduced fetal weight. 8.2 Lactation Risk Summary It is not known whether gefitinib tablets is excreted in human milk. Animal studies indicate the gefitinib and its metabolites are present in rat milk at a concentration higher than those in maternal plasma. Because of the potential for serious adverse reactions in nursing infants from gefitinib tablets, advise women to discontinue breast-feeding during treatment with gefitinib tablets. Data Animal Data Levels of gefitinib and its metabolites were 11-to-19-fold higher in milk than in blood, after oral exposure of lactating rats to a dose of 5 mg/kg. 8.3 Females and Males of Reproductive Potential Contraception Based on its mechanism of action and animal data, gefitinib tablets can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1) ]. Advise females of reproductive potential to use effective contraception during treatment with gefitinib tablets and for at least two weeks following completion of therapy. Infertility Gefitinib tablets may result in reduced fertility in females of reproductive potential [see Nonclinical Toxicology (13.1) ]. 8.4 Pediatric Use The safety and effectiveness of gefitinib tablets in pediatric patients have not been established. 8.5 Geriatric Use Of the 823 patients enrolled in two randomized, active-controlled clinical trials 374 patients (45%) were 65 years and older, and 93 patients (11%) were 75 years and older. 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. 8.6 Renal Impairment Less than four percent (<4%) of gefitinib and its metabolites are excreted via the kidney. No clinical studies were conducted with gefitinib tablets in patients with severe renal impairment. 8.7 Hepatic Impairment The systemic exposure of gefitinib was compared in patients with mild, moderate, or severe hepatic impairment due to cirrhosis (according to Child-Pugh classification) and healthy subjects with normal hepatic function (N=10/group). The mean systemic exposure (AUC 0-∞ ) was increased by 40% in patients with mild impairment, 263% in patients with moderate impairment, and 166% in patients with severe hepatic impairment. Monitor adverse reactions when gefitinib tablets are administered to patients with moderate and severe hepatic impairment. In a study comparing 13 patients with liver metastases and moderate hepatic impairment (addition of CTC grade of baseline AST/SGOT, ALP, and bilirubin equals 3 to 5) to 14 patients with liver metastases and normal hepatic function, the systemic exposure of gefitinib was similar [see Warnings and Precautions (5.2) ].
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. The background risk of major birth defects and miscarriage for the indicated population is unknown; however, the background risk in the U.S. general population of major birth defects is 2 - 4% and miscarriage is 15 - 20% of clinically recognized pregnancies. Data Animal Data A single dose study in rats showed that gefitinib crosses the placenta after an oral dose of 5 mg/kg (30 mg/m 2 , about 0.2 times the recommended human dose on a mg/m 2 basis). When pregnant rats were treated with 5 mg/kg from the beginning of organogenesis to the end of weaning there was a reduction in the number of offspring born alive. This effect was more severe at 20 mg/kg (approximate the human clinical dose on a mg/m 2 basis) and was accompanied by high neonatal mortality soon after parturition. In rabbits, a dose of 20 mg/kg/day (240 mg/m 2 , about twice the recommended dose in humans on a mg/m 2 basis) caused reduced fetal weight.
Pediatric use
8.4 Pediatric Use The safety and effectiveness of gefitinib tablets in pediatric patients have not been established.
Geriatric use
8.5 Geriatric Use Of the 823 patients enrolled in two randomized, active-controlled clinical trials 374 patients (45%) were 65 years and older, and 93 patients (11%) were 75 years and older. 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.
Overdosage
Twenty three patients were treated weekly with doses from 1500 mg to 3500 mg, and gefitinib tablets exposure did not increase with increasing dose. Adverse events were mostly mild to moderate in severity, and were consistent with the known safety profile of gefitinib tablets. In the event of suspected overdose, interrupt gefitinib tablets, institute supportive care, and observe until clinical stabilization. There are no specific measures/treatments that should be taken following gefitinib tablets overdosing.
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. Gefitinib can be defined as soluble at pH 1, but insoluble above pH 7, freely soluble in dimethylformamide and acetic acid, slightly soluble in methanol. Gefitinib tablets are available as brown film-coated tablets, containing 250 mg of gefitinib, for oral administration. The inactive ingredients of the tablet core of gefitinib tablets are lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, and sodium lauryl sulfate and magnesium stearate. Tablet coating contains: polyvinyl alcohol, polyethylene glycol/PEG, talc, titanium dioxide, yellow iron oxide and red iron oxide. structure
Mechanism of action
12.1 Mechanism of Action The epidermal growth factor receptor (EGFR) is expressed on the cell surface of both normal and cancer cells and plays a role in the processes of cell growth and proliferation. Some EGFR activating mutations (exon 19 deletion or exon 21 point mutation L858R) within NSCLC cells have been identified as contributing to the promotion of tumor cell growth, blocking of apoptosis, increasing the production of angiogenic factors and facilitating the processes of metastasis. Gefitinib reversibly inhibits the kinase activity of wild-type and certain activating mutations of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor, thereby inhibiting further downstream signaling and blocking EGFR-dependent proliferation. Gefitinib binding affinity for EGFR exon 19 deletion or exon 21 point mutation L858R mutations is higher than its affinity for the wild-type EGFR. Gefitinib also inhibits IGF and PDGF-mediated signaling at clinically relevant concentrations; inhibition of other tyrosine kinase receptors has not been fully characterized.
How supplied
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].
Patient information
Advise the patient to read the FDA-approved patient labelling (Patient Information). Interstitial Lung Disease : Advise patients to immediately contact their healthcare provider for new onset or worsening of pulmonary symptoms such as dyspnea, cough and fever [see Warnings and Precautions (5.1) ]. Hepatotoxicity : Inform patients that they will need to undergo lab tests to monitor for liver function. Advise patients to contact their healthcare provider to report any new symptoms indicating hepatic toxicity [see Warnings and Precautions (5.2) ]. Gastrointestinal Perforation : Advise patients that gefitinib tablets can increase the risk of gastrointestinal perforation and to seek immediate medical attention for severe abdominal pain [see Warnings and Precautions (5.3) ]. Severe or Persistent Diarrhea : Advise patients to contact their healthcare provider for severe or persistent diarrhea [see Warnings and Precautions (5.4) ]. Ocular Disorders including Keratitis : Advise patients promptly to contact their healthcare provider if they develop eye symptoms, lacrimation, light sensitivity, blurred vision, eye pain, red eye or changes in vision [see Warnings and Precautions (5.5) ] Bullous and Exfoliative Skin Disorders : Advise patients that gefitinib tablets can increase the risk of bullous and exfoliative skin disorders and to seek immediately medical attention for severe skin reactions [see Warnings and Precautions (5.6) ]. Embryo-fetal Toxicity : Advise pregnant women of the potential risk to a fetus or potential risk for loss of the pregnancy [see Warnings and Precautions (5.7) , Use in Specific Populations (8.1)]. Advise females of reproductive potential to use effective contraception during treatment with gefitinib tablets and for at least two weeks following completion of therapy [see Use in Specific Populations (8.3) ]. Lactation : Advise women to discontinue breast-feeding during treatment with gefitinib tablets [see Use in Specific Populations (8.2) ]. Manufactured by : Natco Pharma Limited Kothur – 509228, India Manufactured for: Natco Pharma USA LLC. Parsippany, NJ 07054, USA Patient Information Gefitinib (ge-FI-tye-nib) tablets What are gefitinib tablets? Gefitinib tablets are prescription medicine used to treat people with non-small cell lung cancer (NSCLC) that has spread to other parts of the body and: that have certain types of abnormal epidermal growth factor receptor (EGFR) genes, and who have not had previous treatment for cancer Your healthcare provider will perform a test to make sure that gefitinib tablets are right for you. It is not known if gefitinib tablets are safe and effective in people with NSCLC that have other types of EGFR genes. It is not known if gefitinib tablets are safe and effective in children. Before taking gefitinib tablets, tell your healthcare provider about all of your medical conditions, including if you: have lung or breathing problems ever had liver problems have vision or eye problems are pregnant or plan to become pregnant. Gefitinib tablets can harm your unborn baby Females who are able to become pregnant should use an effective method of birth control during treatment with gefitinib tablets and for at least 2 weeks after the last dose of gefitinib tablets. You should avoid becoming pregnant during treatment with gefitinib tablets. Tell your healthcare provider right away if you become pregnant during treatment with gefitinib tablets. are breastfeeding or plan to breastfeed. It is not known if gefitinib passes into your breast milk. Do not breastfeed during treatment with gefitinib tablets. Talk to your healthcare provider about the best way to feed your baby during this time. Tell your healthcare provider about all the medicines you take, including prescription and over -the-counter medicines vitamins, or herbal supplements. If you take a proton pump inhibitor (PPI), H2 blocker, or an antacid medicine, talk to your healthcare provider about the best time to take it during treatment with gefitinib tablets. If you take a blood thinner called warfarin, your healthcare provider should do blood tests regularly to check how fast your blood clots, during treatment with gefitinib tablets. How should I take gefitinib tablets? Take gefitinib tablets exactly as your healthcare provider tells you to take it. Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with gefitinib tablets if you have side effects. Take gefitinib tablet 1 time each day. You can take gefitinib tablets with or without food. If you miss a dose of gefitinib tablets, take it as soon as you remember. If it is less than 12 hours until your next dose, skip the missed dose. Take your next dose at your regular time. If you take too much gefitinib tablets, call your healthcare provider or go to the nearest emergency room right away. If you cannot swallow gefitinib tablets whole: place your dose of gefitinib tablet in a container with 4 to 8 ounces of water and stir for about 15 minutes drink the mixture right away place another 4 to 8 ounces of water in the same container, and drink it right away What are the possible side effects of gefitinib tablets? Gefitinib tablets may cause serious side effects, including: lung or breathing problems . Gefitinib tablets may cause inflammation of the lung that may lead to death. Symptoms may be similar to those symptoms from lung cancer. Tell your healthcare provider right away if you have any new or worsening lung problems, or any combination of the following symptoms: trouble breathing or shortness of breath, cough, or fever. Iiver problems . Gefitinib tablets may cause inflammation of the liver that may lead to death.
Label text from the FDA structured product label by Natco Pharma USA LLC (revised Mar 10, 2026). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Gefitinib in 4 products
Gefitinib NDC products (4)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 50742-366 | Gefitinib 250 mg/1 Tablet, Coated | Ingenus Pharmaceuticals, LLC | ANDA |
| 69339-168 | Gefitinib 250 mg/1 Tablet, Film Coated | Natco Pharma USA LLC | ANDA |
| 67184-0531 | Gefitinib 250 mg/1 Tablet, Coated | Qilu Pharmaceutical Co., Ltd. | ANDA |
| 0480-4053 | Gefitinib 250 mg/1 Tablet, Film Coated | Teva Pharmaceuticals, Inc. | ANDA |
Frequently asked questions
What is Gefitinib used for?
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…
What are the side effects of Gefitinib?
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… See the full label for the complete list.
Who makes Gefitinib?
Gefitinib is listed by 4 labelers in the FDA NDC directory, including Ingenus Pharmaceuticals, LLC, Natco Pharma USA LLC, Qilu Pharmaceutical Co., Ltd., Teva Pharmaceuticals, Inc..