Dosing & Uses
Dosage Forms & Strengths
tablet
- 250mg
Non-small Cell Lung Cancer
Indicated for the 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
250 mg PO qDay until disease progression or unacceptable toxicity
Dosage Modifications
Withhold for up to 14 days following adverse effects
- Acute onset or worsening pulmonary symptoms (dyspnea, cough, fever)
- ≥Grade 2 ALT and/or AST elevations
- ≥Grade 3 diarrhea
- Signs and symptoms of severe or worsening ocular disorders including keratitis
- ≥Grade 3 skin reactions
- May resume gefitinib when adverse effect fully resolves or improves to Grade 1
Permanently discontinue for
- Confirmed interstitial lung disease
- Severe hepatic impairment
- Gastrointestinal perforation
- Persistent ulcerative keratitis
Coadministration with strong CYP3A4 inducers
- Increase dose to 500 mg PO qDay in the absence of severe adverse drug reactions
- Resume 250 mg qDay after discontinuation of the strong CYP3A4 inducer
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (10)
- alpelisib
gefitinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.
- apalutamide
apalutamide will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- fexinidazole
fexinidazole will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- ivosidenib
ivosidenib will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- ozanimod
gefitinib increases toxicity of ozanimod by Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of ozanimod (a BCRP substrate) with BCRP inhibitors increases the exposure of the minor (RP101988, RP101075) and major active metabolites (CC112273, CC1084037) of ozanimod, which may increase the risk of ozanimod adverse reactions. .
- palifermin
palifermin increases toxicity of gefitinib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- rimegepant
gefitinib will increase the level or effect of rimegepant by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of rimegepant (a BCRP substrate) with inhibitors of BCRP.
- talazoparib
gefitinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- tucatinib
tucatinib will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- voxelotor
voxelotor will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (87)
- aluminum hydroxide
aluminum hydroxide decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and antacid doses by at least 6 hr.
- aspirin/citric acid/sodium bicarbonate
aspirin/citric acid/sodium bicarbonate decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and antacid doses by at least 6 hr.
- atazanavir
atazanavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- belzutifan
belzutifan will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- berotralstat
gefitinib increases levels of berotralstat by Other (see comment). Modify Therapy/Monitor Closely. Comment: Reduced dose of berotralstat (a BCRP substrate) to 110 mg/day when coadministered with BCRP inhibitors.
- bosentan
bosentan will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- calcium carbonate
calcium carbonate decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and antacid doses by at least 6 hr.
- carbamazepine
carbamazepine will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- cenobamate
cenobamate will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- ceritinib
ceritinib will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- chloramphenicol
chloramphenicol will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- cholera vaccine
gefitinib decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.
- cimetidine
cimetidine decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and H2-antagonist doses by at least 6 hr.
- clarithromycin
clarithromycin increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- cobicistat
cobicistat increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- conivaptan
conivaptan increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- dabrafenib
dabrafenib will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- darunavir
darunavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- dengue vaccine
gefitinib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.
- dexamethasone
dexamethasone will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- dexlansoprazole
dexlansoprazole decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Avoid coadministration of gefitinib with PPIs if possible. If treatment with a PPI is required, separate gefitinib and PPI doses by 12 hr.
- duvelisib
gefitinib will increase the level or effect of duvelisib by Other (see comment). Use Caution/Monitor. Coadministration of duvelisib (a BCRP substrate) with a BCRP transport inhibitor may increase levels or effects of duvelisib.
- efavirenz
efavirenz will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- elagolix
elagolix decreases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- encorafenib
encorafenib, gefitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- enzalutamide
enzalutamide will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- esomeprazole
esomeprazole decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Avoid coadministration of gefitinib with PPIs if possible. If treatment with a PPI is required, separate gefitinib and PPI doses by 12 hr.
- etravirine
etravirine will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- famotidine
famotidine decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and H2-antagonist doses by at least 6 hr.
- fedratinib
fedratinib will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fosamprenavir
fosamprenavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- fosphenytoin
fosphenytoin will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- glecaprevir/pibrentasvir
gefitinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.
- grapefruit
grapefruit increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- ibuprofen/famotidine
ibuprofen/famotidine decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and H2-antagonist doses by at least 6 hr.
- idelalisib
idelalisib increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- imatinib
imatinib increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- indinavir
indinavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- isoniazid
isoniazid increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- istradefylline
istradefylline will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- itraconazole
itraconazole increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- ketoconazole
ketoconazole increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- lansoprazole
lansoprazole decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Avoid coadministration of gefitinib with PPIs if possible. If treatment with a PPI is required, separate gefitinib and PPI doses by 12 hr.
- lenacapavir
lenacapavir will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- levoketoconazole
levoketoconazole increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- lopinavir
lopinavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- lorlatinib
lorlatinib will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- magnesium oxide
magnesium oxide decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and antacid doses by at least 6 hr.
- mavacamten
gefitinib will increase the level or effect of mavacamten by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Inititiation of weak CYP2C19 inhibitors may require decreased mavacamten dose.
- mifepristone
mifepristone will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mitotane
mitotane will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- nafcillin
nafcillin will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- nefazodone
nefazodone increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- nelfinavir
nelfinavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- nevirapine
nevirapine will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- nicardipine
nicardipine increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- nizatidine
nizatidine decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Separate gefitinib and H2-antagonist doses by at least 6 hr.
- omeprazole
omeprazole decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Avoid coadministration of gefitinib with PPIs if possible. If treatment with a PPI is required, separate gefitinib and PPI doses by 12 hr.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- pantoprazole
pantoprazole decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Avoid coadministration of gefitinib with PPIs if possible. If treatment with a PPI is required, separate gefitinib and PPI doses by 12 hr.
- pentobarbital
pentobarbital will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- phenobarbital
phenobarbital will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- phenytoin
phenytoin will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- posaconazole
posaconazole increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- primidone
primidone will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- quinidine
quinidine increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- rabeprazole
rabeprazole decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Avoid coadministration of gefitinib with PPIs if possible. If treatment with a PPI is required, separate gefitinib and PPI doses by 12 hr.
- ribociclib
ribociclib will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifabutin
rifabutin will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- rifampin
rifampin will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- rifapentine
rifapentine will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- ritonavir
ritonavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- rucaparib
rucaparib will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- saquinavir
saquinavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- selexipag
gefitinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- siponimod
siponimod and gefitinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- sodium zirconium cyclosilicate
sodium zirconium cyclosilicate will decrease the level or effect of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Check specific recommendations for drugs that exhibit pH-dependent solubility that may affect their systemic exposure and efficacy. In general, administer drugs at least 2 hr before or after sodium zirconium cyclosilicate.
- St John's Wort
St John's Wort will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase gefitinib to 500 mg daily if coadministered with a strong CYP3A4 inducer. Resume gefitinib dose at 250 mg/day 7 days after discontinuing the strong inducer.
- stiripentol
stiripentol, gefitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
- tazemetostat
tazemetostat will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- tipranavir
tipranavir increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- voriconazole
voriconazole increases levels of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration of strong CYP3A4 inhibitors may increase risk for gefitinib adverse effects.
- warfarin
gefitinib increases effects of warfarin by unspecified interaction mechanism. Use Caution/Monitor.
Minor (4)
- acetazolamide
acetazolamide will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
Skin reactions, all grades (47%)
Diarrhea, all grades (29%)
Decreased appetite, all grades (17%)
Vomiting, all grades (14%)
Increased ALT, all grades (11.4%)
1-10%
Increased AST, all grades (7.9%)
Stomatitis, all grades (7%)
Conjunctivitis, blepharitis, and dry eye (6.7%)
Conjunctivitis/blepharitis/dry eye (6%)
Increased ALT, grades 3-4 (5.1%)
Nail disorders, all grades (5%)
Diarrhea, grades 3-4 (3%)
Increased AST, grades 3-4 (3%)
Increased bilirubin, all grades (2.7%)
Decreased appetite, grades 2-3 (2.3%)
Skin reactions, grades 3-4 (2%)
Interstitial lung disease, all grades (1.3%)
Vomiting, grades 3-4 (1.2%)
<1%
Interstitial lung disease, grades 3-4 (0.7%)
Increased bilirubin, grades 3-4 (0.7%)
Stomatitis, all grades (0.3%)
Corneal erosion and aberrant eyelash growth (0.2%)
Nail disorders, grades 3-4 (0.1%)
Gastrointestinal perforation (0.1%)
Ocular keratitis (0.1%)
Erythema multiforme and dermatitis bullous (0.08%)
Fatal hepatoxicity (0.04%)
Postmarketing Reports
Renal and urinary disorders: Cystitis, hemorrhagic cystitis
Skin and subcutaneous tissue disorders: Cutaneous vasculitis
Warnings
Contraindications
None
Cautions
Interstitial lung disease (ILD) or ILD-like adverse drug reactions reported (eg, lung infiltration, pneumonitis, acute respiratory distress syndrome, or pulmonary fibrosis); permanently discontinue if confirmed
Increased ALT, AST, and bilirubin reported; obtain periodic liver function testing and withhold drug for worsening liver function or discontinue with severe hepatic impairment
Gastrointestinal perforation reported; permanently discontinue
Severe or persistent diarrhea may occur; withhold drug for up to 14 days
Ocular disorders reported (eg, keratitis, corneal erosion, aberrant eyelash growth, conjunctivitis, blepharitis, dry eye); interrupt or discontinue for severe, or worsening ocular disorders
Bullous conditions including toxic epidermal necrolysis, Stevens Johnson syndrome and erythema multiforme reported rarely; discontinue drug
Based on its mechanism of action and data from animal reproduction studies, gefitinib can cause fetal harm when administered to a pregnant woman (see Pregnancy)
Pregnancy
Pregnancy
Based on its mechanism of action and animal data, gefitinib can cause fetal harm when administered to a pregnant woman
Advise females of reproductive potential to use effective contraception during treatment with gefitinib and for at least 2 weeks following completion of therapy
Advise pregnant women of the potential hazard to a fetus or potential risk for loss of the pregnancy
Animal studies
- 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
Lactation
Unknown if distributed in human breast milk; not recommended
Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition
Animal studies
- 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, advise women to discontinue breastfeeding during treatment
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Reversibly inhibits the kinase activity of wild-type and certain activating mutations of epidermal growth factor receptor (EGFR), preventing autophosphorylation of tyrosine residues associated with the receptor, thereby inhibiting further downstream signalling and blocking EGFR-dependent proliferation
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
Binding affinity for EGFR exon 19 deletion or exon 21 point mutation L858R mutations is higher than its affinity for the wild-type EGFR
Absorption
Oral bioavailability, mean: 60%
Peak plasma concentration: 3-7 hr
Steady-state achieved: 10 days
Distribution
Protein bound: 90%
Vd: 1400 L
Metabolism
Extensive hepatic metabolism, predominantly by CYP3A4
Major active metabolite component was O-desmethyl gefitinib produced by CYP2D6 metabolism and accounted for 14% of the dose
Elimination
Half-life: 48 hr
Excretion: 86% feces; <4% urine
Pharmacogenomics
CYP2D6 poor metabolizers
- CYP2D6 metabolizes gefitinib to O-desmethyl gefitinib in vitro
- In healthy CYP2D6 poor metabolizers, O-desmethyl gefitinib concentration was not measurable and the mean exposure to gefitinib was 2-fold higher as compared to the extensive metabolizers
- This increase in exposure may be clinically important because some adverse drug reactions are related to higher exposure of gefitinib
- No dose adjustment is recommended in patients with a known CYP2D6 poor metabolizer genotype, but these patients should be closely monitored for adverse reactions
Administration
Instructions
May take with or without food
Missed dose: Do not take a missed dose within 12 hr of the next scheduled dose
Difficulty swallowing
- Immerse tablet in 4-8 ounces of water and stir for approximately 15 minutes
- Immediately drink the liquid or administer through a NG tube
- Rinse the container with an additional 4-8 ounces of water and immediately drink or administer through the NG tube to assure complete dose
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Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
