erlotinib (Rx)

Brand and Other Names:Tarceva
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 100mg
  • 150mg

Non-Small Cell Lung Cancer

Indicated for 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 receiving first-line, maintenance, or ≥second-line treatment after progression following at least 1 prior chemotherapy regimen

150 mg PO qDay 1 hr before or 2 hrs after meals

Continue until disease progression or unacceptable toxicity

NSCLC limitations of use

  • Not recommended for use in combination with platinum-based chemotherapy
  • Safety and efficacy has not been evaluated as first-line treatment in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution

Pancreatic Cancer

Indicated for first-line treatment in patients with locally advanced, unresectable, or metastatic pancreatic cancer

100 mg/day PO with gemcitabine

Continue until disease progression or unacceptable toxicity

Malignant Gliomas (Orphan)

Orphan sponsor: Genentech, Inc; 1 DNA Way; South San Francisco, CA 94080-4990

Dosage Modifications

Decrease dose by 50 mg decrements

  • Strong CYP3A4 inhibitors: Reduce by 50 mg decrements if severe reactions occur when coadministered with strong CYP3A4 inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole, or grapefruit or grapefruit juice)
  • CYP3A4 and CYP1A2 inhibitors: Avoid concomitant use if possible when coadministered with an inhibitor of both CYP3A4 and CYP1A2 (eg, ciprofloxacin)
  • When restarting therapy following withholding treatment for a dose-limiting toxicity that has resolved to baseline or grade ≤1

Increase dose by 50 mg increments

  • CYP3A4 inducers: Increase by 50 mg increments at 2 week intervals as tolerated to a maximum of 450 mg for concomitant use with CYP3A4 inducers (eg, rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, St. John’s Wort); if possible, avoid concomitant use
  • Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg; immediately reduce dose to recommended dose (ie, 100 mg or 150 mg daily) upon smoking cessation

Drugs affecting gastric pH

  • Proton pump inhibitors: Avoid coadministration if possible
  • H2-antagonists: Take erlotinib 10 hr after or at least 2 hr before H2-anagonist
  • Antacids: Separate erlotinib and antacid doses by several hours

Discontinue erlotinib for

  • Interstitial lung disease (ILD) Severe hepatic toxicity that is unimproved or does not resolve
  • GI perforation
  • Severe bullous, blistering, or exfoliating skin conditions
  • Corneal perforation or severe ulceration

Withhold erlotinib

  • During diagnostic evaluation for ILD
  • Severe renal toxicity (grades 3-4)
  • Total bilirubin levels >3 xULN or transaminases >5 xULN in patients without pre-existing hepatic impairment
  • In patients with pre-existing hepatic impairment for bilirubin 2 xULN or transaminases 3 xULN
  • Persistent severe diarrhea or rash unresponsive to medical management
  • Keratitis (grades 3-4, or grade 2 for >2 wk)
  • Acute/worsening ocular disorders

Safety and efficacy not established

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Interactions

Interaction Checker

and erlotinib

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            Contraindicated (6)

            • dexlansoprazole

              dexlansoprazole decreases levels of erlotinib by Other (see comment). Contraindicated. Comment: Concomitant use of proton pump inhibitors with erlotinib should be avoided if possible. Drugs that alter pH of upper GI tract may alter the solubility of erlotinib and reduce its bioavailability. .

            • esomeprazole

              esomeprazole decreases levels of erlotinib by Other (see comment). Contraindicated. Comment: Concomitant use of proton pump inhibitors with erlotinib should be avoided if possible. Drugs that alter pH of upper GI tract may alter the solubility of erlotinib and reduce its bioavailability. .

            • lansoprazole

              lansoprazole decreases levels of erlotinib by Other (see comment). Contraindicated. Comment: Concomitant use of proton pump inhibitors with erlotinib should be avoided if possible. Drugs that alter pH of upper GI tract may alter the solubility of erlotinib and reduce its bioavailability. .

            • omeprazole

              omeprazole decreases levels of erlotinib by Other (see comment). Contraindicated. Comment: Concomitant use of proton pump inhibitors with erlotinib should be avoided if possible. Drugs that alter pH of upper GI tract may alter the solubility of erlotinib and reduce its bioavailability. .

            • pantoprazole

              pantoprazole decreases levels of erlotinib by Other (see comment). Contraindicated. Comment: Concomitant use of proton pump inhibitors with erlotinib should be avoided if possible. Drugs that alter pH of upper GI tract may alter the solubility of erlotinib and reduce its bioavailability. .

            • rabeprazole

              rabeprazole decreases levels of erlotinib by Other (see comment). Contraindicated. Comment: Concomitant use of proton pump inhibitors with erlotinib should be avoided if possible. Drugs that alter pH of upper GI tract may alter the solubility of erlotinib and reduce its bioavailability. .

            Serious - Use Alternative (27)

            • abametapir

              abametapir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

            • apalutamide

              apalutamide will decrease the level or effect of erlotinib 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.

            • carbamazepine

              carbamazepine will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • chloramphenicol

              chloramphenicol will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • clarithromycin

              clarithromycin will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • enzalutamide

              enzalutamide will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin base

              erythromycin base will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • idelalisib

              idelalisib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • itraconazole

              itraconazole will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. When combination must be used, closely monitor for severe adverse reactions (eg, severe diarrhea, severe skin reactions). If severe adverse reactions do occur, reduce erlotinib dose (in 50 mg decrements).

            • ivosidenib

              ivosidenib will decrease the level or effect of erlotinib 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.

            • ketoconazole

              ketoconazole will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • lopinavir

              lopinavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • lorlatinib

              lorlatinib will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nefazodone

              nefazodone will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nizatidine

              nizatidine will decrease the level or effect of erlotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • palifermin

              palifermin increases toxicity of erlotinib 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.

            • quinidine

              quinidine will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • rifabutin

              rifabutin will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • rifampin

              rifampin will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • saquinavir

              saquinavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • St John's Wort

              St John's Wort will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • tipranavir

              tipranavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • tucatinib

              tucatinib will increase the level or effect of erlotinib 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 erlotinib 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 (104)

            • amiodarone

              amiodarone will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • amobarbital

              amobarbital will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • aprepitant

              aprepitant will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • armodafinil

              armodafinil will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • artemether/lumefantrine

              artemether/lumefantrine will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • atazanavir

              atazanavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • atorvastatin

              atorvastatin will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • bosentan

              bosentan will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • budesonide

              budesonide will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • butabarbital

              butabarbital will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • butalbital

              butalbital will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • cholera vaccine

              erlotinib 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.

            • cigarette smoking

              cigarette smoking will decrease the level or effect of erlotinib by increasing hepatic clearance. Modify Therapy/Monitor Closely. Increase dose by 50 mg increments at 2 week intervals to a maximum of 300 mg; immediately reduce dose to recommended dose upon smoking cessation

            • cimetidine

              cimetidine decreases levels of erlotinib by Other (see comment). Use Caution/Monitor. Comment: Avoid combination when possible. If concurrent use is required erlotinib should be taken 10 hours after a H2-antagonist and at least 2 hours before the next dose of H2-antagonist.

            • ciprofloxacin

              ciprofloxacin increases levels of erlotinib by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. If severe adverse effects occur consider reducing erlotinib dose.

            • clarithromycin

              clarithromycin will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • clotrimazole

              clotrimazole will decrease the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • cobicistat

              cobicistat will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If coadministration cannot be avaoided, reduce erlotinib dose by 50 mg decrements and monitor for adverse effects

            • conivaptan

              conivaptan will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cortisone

              cortisone will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • crizotinib

              crizotinib increases levels of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A.

            • crofelemer

              crofelemer increases levels of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • cyclosporine

              cyclosporine will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              cyclosporine will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dabrafenib

              dabrafenib will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • darifenacin

              darifenacin will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • darunavir

              darunavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dasatinib

              dasatinib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • deferasirox

              deferasirox will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dengue vaccine

              erlotinib 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 erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • DHEA, herbal

              DHEA, herbal will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dichlorphenamide

              dichlorphenamide and erlotinib both decrease serum potassium. Use Caution/Monitor.

            • diltiazem

              diltiazem will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dronedarone

              dronedarone will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              dronedarone will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • duvelisib

              duvelisib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.

            • efavirenz

              efavirenz will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • elagolix

              elagolix will decrease the level or effect of erlotinib 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 erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.

            • encorafenib

              encorafenib, erlotinib. 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.

            • erythromycin base

              erythromycin base will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • etravirine

              etravirine will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • famotidine

              famotidine decreases levels of erlotinib by Other (see comment). Use Caution/Monitor. Comment: Avoid combination when possible. If concurrent use is required erlotinib should be taken 10 hours after a H2-antagonist and at least 2 hours before the next dose of H2-antagonist.

            • fedratinib

              fedratinib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

            • felodipine

              felodipine will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • fluconazole

              fluconazole will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fluvoxamine

              fluvoxamine will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosamprenavir

              fosamprenavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosphenytoin

              fosphenytoin will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              fosphenytoin will decrease the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • grapefruit

              grapefruit will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • griseofulvin

              griseofulvin will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ibuprofen/famotidine

              ibuprofen/famotidine decreases levels of erlotinib by Other (see comment). Use Caution/Monitor. Comment: Avoid combination when possible. If concurrent use is required erlotinib should be taken 10 hours after a H2-antagonist and at least 2 hours before the next dose of H2-antagonist.

            • iloperidone

              iloperidone increases levels of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • indinavir

              indinavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              indinavir will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • isoniazid

              isoniazid will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of erlotinib 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.

            • ketoconazole

              ketoconazole will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lapatinib

              lapatinib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • letermovir

              letermovir increases levels of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • loratadine

              loratadine will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lumefantrine

              lumefantrine will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • marijuana

              marijuana will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • metronidazole

              metronidazole will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • miconazole vaginal

              miconazole vaginal will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • mifepristone

              mifepristone will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce dose of erlotinib by 50 mg decrements If concomitant use necessary and severe reactions occur; clinical significance of this interaction with short-term use of mifepristone for termination of pregnancy unknown

            • mitotane

              mitotane decreases levels of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • modafinil

              modafinil will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nafcillin

              nafcillin will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nefazodone

              nefazodone will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nelfinavir

              nelfinavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nevirapine

              nevirapine will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nicardipine

              nicardipine will increase the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nifedipine

              nifedipine will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nilotinib

              nilotinib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nizatidine

              nizatidine decreases levels of erlotinib by Other (see comment). Use Caution/Monitor. Comment: Avoid combination when possible. If concurrent use is required erlotinib should be taken 10 hours after a H2-antagonist and at least 2 hours before the next dose of H2-antagonist.

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • pentobarbital

              pentobarbital will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenobarbital

              phenobarbital will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenytoin

              phenytoin will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid concomitant use because there is a potential for decreased erlotinib exposure and efficacy. However, if concomitant use is clinically warranted, consider an increase in erlotinib dose as tolerated at 2 week intervals and monitor patient's safety. If the erlotinib dose is increased, reduce it immediately to the indicated starting dose upon discontinuation of phenytoin.

              phenytoin will decrease the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • posaconazole

              posaconazole will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • primidone

              primidone will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • quercetin

              quercetin will decrease the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • quinupristin/dalfopristin

              quinupristin/dalfopristin will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ribociclib

              ribociclib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifampin

              rifampin will decrease the level or effect of erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • rifapentine

              rifapentine will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ritonavir

              ritonavir will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rucaparib

              rucaparib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

            • rufinamide

              rufinamide will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • secobarbital

              secobarbital will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • siponimod

              siponimod and erlotinib 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 erlotinib 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 erlotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • stiripentol

              stiripentol, erlotinib. 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 erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tecovirimat

              tecovirimat will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • topiramate

              topiramate will decrease the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • verapamil

              verapamil will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • voriconazole

              voriconazole will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • zafirlukast

              zafirlukast will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            Minor (0)

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              Adverse Effects

              >10%

              Rash (75-76%)

              Anorexia (52-69%)

              Diarrhea (54-55%)

              Fatigue (52-79%)

              Nausea (33-40%)

              Infection (39%)

              Vomiting (23-25%)

              Dyspnea (24%)

              Stomatitis (17-19%)

              Cough (16%)

              Pruritus (13%)

              Conjunctivitis (12%)

              Dry skin (12%)

              Keratoconjunctivitis sicca (12%)

              Abdominal pain (11%)

              1-10%

              Elevated LFT's (grade 2)

              Acne

              Paronychia

              Weight loss

              Pneumonitis pulmonary infiltrate

              Pulmonary fibrosis

              <1%

              Interstitial lung disease-like events

              Postmarketing Reports

              Musculoskeletal and connective tissue disorders: Myopathy, including rhabdomyolysis, in combination with statin therapy

              Eye disorders: Ocular inflammation including uveitis

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              Warnings

              Contraindications

              None

              Cautions

              Risk of potentially fatal interstitial lung disease (ILD); withhold therapy for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever; discontinue therapy if ILD diagnosed

              Potentially fatal GI perforations

              Severe bullous, blistering, or exfoliating skin conditions

              Ocular disorders include decreased tear production, abnormal eyelash growth, corneal perforation/ulceration, keratoconjunctivitis sicca, keratitis

              Diarrhea

              Smoking reduces erlotinib plasma concentration; advise patient to quit smoking

              Monitor renal function and electrolytes, particularly in patients at risk of dehydration; withhold therapy for severe renal toxicity

              Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome; monitor periodic liver testing; withhold or discontinue therapy for severe or worsening liver tests

              Coadministration with CYP3A4 inhibitors/inducers

              CYP1A2 inducers may decrease plasma concentration

              Risk of myocardial infarction (MI)/ischemia is increased in patients with pancreatic cancer

              Risk of cerebrovascular accident is increased in patients with pancreatic cancer

              Risk of microangiopathic hemolytic anemia (MAHA) is increased in patients with pancreatic cancer

              No evidence drug has any benefit after disease progression

              Monitor if on warfarin or other coumarin-derived anticoagulants for changes in PT/INR

              Avoid pregnancy; can cause fetal harm; advise females of reproductive potential of potential risk to fetus and to use highly effective contraception during therapy and for 1 month after the last dose

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              Pregnancy & Lactation

              Pregnancy

              Based on animal data and its mechanism of action, erlotinib can cause fetal harm when administered to a pregnant woman

              Advise females of reproductive potential to use effective contraception during treatment and for 1 month after the last dose

              Lactation

              No data exist on the presence of erlotinib in human milk, or the effects of erlotinib on the breastfed infant or on milk production

              Because of the potential for serious adverse reactions in breastfed infants, including interstitial lung disease, hepatotoxicity, bullous and exfoliative skin disorders, microangiopathic hemolytic anemia, with thrombocytopenia, ocular disorders, and diarrhea

              Advise a lactating woman not to breastfeed during treatment and for 2 weeks after the final dose

              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.

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              Pharmacology

              Mechanism of Action

              EGF receptor tyrosine kinase inhibitor; TKI inhibition possibly blocks angiogenesis and cellular proliferation

              Pharmacokinetics

              Absorption: 60%

              Bioavailability: 60% (increased by food to almost 100%)

              Peak Plasma Time: 4 hr

              Half-life: 36 hr

              Clearance: 24% higher in smokers

              Protein Bound: 93%

              Metabolism: primarily by CYP3A4; to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1

              Excretion: Feces 83%; urine 8%

              Pharmacogenomics

              Erlotinib inhibits the tyrosine kinase (TK) domain of epidermal growth factors receptors (EGFRs) expressed on cell surface of lung cancers

              Patients with EGFR exon 19 deletion or exon 21 L858R mutation have significantly better response to EGFR-TKIs

              Genetic testing laboratories

              • The following companies currently offer testing for mutations in the EGFR-TK domain
              • Genzyme Genetics (http://www.genzymegenetics.com)
              • LabCorp (http://www.labcorp.com)
              • Response Genetics (http://www.responsegenetics.com)
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              Administration

              Oral Administration

              Take on empty stomach, 1 hr before or 2 hrs after meals

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              erlotinib oral
              -
              150 mg tablet
              erlotinib oral
              -
              100 mg tablet
              erlotinib oral
              -
              150 mg tablet
              erlotinib oral
              -
              100 mg tablet
              erlotinib oral
              -
              25 mg tablet
              erlotinib oral
              -
              150 mg tablet
              erlotinib oral
              -
              25 mg tablet
              erlotinib oral
              -
              100 mg tablet
              Tarceva oral
              -
              25 mg tablet
              Tarceva oral
              -
              150 mg tablet
              Tarceva oral
              -
              100 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              erlotinib oral

              ERLOTINIB - ORAL

              (er-LOE-ti-nib)

              COMMON BRAND NAME(S): Tarceva

              USES: Erlotinib is used to treat lung and pancreatic cancer. It works by slowing or stopping the growth of cancer cells.

              HOW TO USE: Take this medication by mouth on an empty stomach (at least 1 hour before or 2 hours after a meal) as directed by your doctor, usually once daily.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Medications that lower stomach acid (such as antacids, H2 blockers including ranitidine) may prevent erlotinib from working. Ask your doctor or pharmacist how to use these medications safely with erlotinib.Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

              SIDE EFFECTS: Diarrhea, dry skin, muscle/joint pain, mouth sores, unusual eyelash growth, or eye dryness/redness/irritation may occur. Diarrhea can be severe. In some cases, your doctor may prescribe medication to relieve diarrhea. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: signs of kidney problems (such as change in the amount of urine), signs of liver disease (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine), signs of dehydration (such as extreme thirst, muscle cramps, dizziness, fainting), redness/swelling around the nails, black stools, vomit that looks like coffee grounds, easy bleeding/bruising, unusual tiredness, eye pain, vision changes.Get medical help right away if you have any very serious side effects, including: new or worsening shortness of breath or cough, chest/jaw/left arm pain, weakness on one side of the body, trouble speaking, confusion, seizures.Erlotinib can commonly cause a mild rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Get medical help right away if you develop any rash.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking erlotinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, stomach/intestinal disease (such as ulcers, diverticulosis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medicine may cause stomach bleeding. Daily use of alcohol while using this medicine may increase your risk for stomach bleeding. Limit alcoholic beverages.Sunlight may worsen any skin reactions that may occur while you are taking this drug. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using erlotinib. Erlotinib may harm an unborn baby. Ask about reliable forms of birth control while using this medication and for 1 month after stopping treatment. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug and for 2 weeks after stopping treatment is not recommended. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: "blood thinners" (such as warfarin), drugs that lower stomach acid (such as proton pump inhibitors including omeprazole).Check all prescription and nonprescription medicine labels carefully since many medications contain pain relievers/fever reducers (aspirin, NSAIDs such as ibuprofen or naproxen) which may increase your risk for stomach bleeding while you are taking erlotinib. However, if your doctor has directed you to take low-dose aspirin to prevent heart attack or stroke (usually 81-162 milligrams a day), you should keep taking the aspirin unless your doctor instructs you otherwise. Ask your doctor or pharmacist for more details.Cigarette smoking decreases blood levels of this medication. Tell your doctor if you smoke or if you have recently stopped smoking.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: Do not share this medication with others.Lab and/or medical tests (such as kidney/liver function) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details

              MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              Information last revised March 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

              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.

              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.