Monograph Details
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Neoplasms
> Kinase inhibitors
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TARCEVA |
| Manufacturer |
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Genentech, Inc. |
| Legal Classification |
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Rx
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| Pharmacological Class |
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Human epidermal growth factor receptor type 1/epidermal growth factor receptor tyrosine kinase inhibitor. |
| Generic Name |
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Erlotinib (as HCl) 25mg, 100mg, 150mg; tabs. |
| Indications |
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Treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) after failure of at least one prior chemotherapy regimen. In combination with gemcitabine: first-line treatment of locally advanced, unresectable or metastatic pancreatic cancer. |
| Children |
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Not recommended. |
| Adults |
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Take on empty stomach. NSCLC: 150mg once daily. Pancreatic cancer: 100mg once daily + gemcitabine (see literature). Both: use until disease progression or unacceptable toxicity occurs. Diarrhea unresponsive to loperamide, severe skin reactions, strong CYP3A4 inhibitors (see Interactions), hepatic impairment: reduce in 50mg decrements. CYP3A4 inducers (see Interactions): consider increased dose (see literature). |
| Precautions |
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Hepatic impairment. Monitor liver function tests periodically; if tests worsen, consider withholding or reducing dose; interrupt or discontinue therapy if severe changes (eg, total bilirubin >3xULN, and/or transaminases >5xULN) occur. Monitor renal function, serum electrolytes, pulmonary function, INR, prothrombin time. Pregnancy (Cat.D); use adequate contraception (see literature). Nursing mothers: not recommended. |
| Interactions |
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Potentiated by CYP3A4 inhibitors (eg, clarithromycin, ritonavir, ketoconazole). Plasma levels decreased by CYP3A4 inducers (eg, rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort), proton pump inhibitors or H2 blockers, and smoking. Antagonizes midazolam. Monitor for bleeding with oral anticoagulants, NSAIDs. |
| Adverse Reactions |
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Rash, diarrhea, GI upset, anorexia, fatigue, elevated LFTs, unexplained pulmonary symptoms (eg, dyspnea, cough, fever; discontinue and follow-up if occurs), stomatitis, infection; rare: GI bleeding, conjunctivitis, keratitis, corneal ulceration, MI/ischemia, hemolytic anemia, cerebrovascular accidents; interstitial lung disease (discontinue if occurs); hepatic or renal failure and hepatorenal syndrome (may be fatal). |
| How Supplied |
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Tabs—30 |
| Additional Resources |
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• Related Prescribing Note |
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