erlotinib (Rx)

Brand and Other Names:Tarceva
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 100mg
  • 150mg
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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

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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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            Formulary

            FormularyPatient Discounts

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            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.