Generic Name and Formulations:
Erlotinib (as HCl) 25mg, 100mg, 150mg; tabs.
Company:
Genentech, Inc.
In combination with gemcitabine: first-line treatment of locally advanced, unresectable or metastatic pancreatic cancer.
Take on empty stomach. 100mg once daily + gemcitabine (see literature). 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).
Not recommended.
Human epidermal growth factor receptor type 1/epidermal growth factor receptor tyrosine kinase inhibitor.
Discontinue if interstitial lung disease, hepatic failure, or GI perforation occurs; interrupt or discontinue therapy in patients with dehydration at risk for renal failure, or with severe bullous, blistering or exfoliative skin conditions, or with acute/worsening ocular disorders. 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. History of peptic ulcers or diverticular disease. Pregnancy (Cat.D); use adequate contraception (see literature). Nursing mothers: not recommended.
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. Increased risk of GI perforation with concomitant anti-angiogenic agents, steroids, NSAIDs, taxane-based chemotherapy. Monitor for bleeding with oral anticoagulants, NSAIDs.
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 perforation (may be fatal), ocular disorders (eg, conjunctivitis, keratitis, corneal ulceration/perforation), MI/ischemia, hemolytic anemia, cerebrovascular accidents, interstitial lung disease; hepatic or renal failure and hepatorenal syndrome (may be fatal); bullous, blistering and exfoliative skin conditions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis).
Testing considerations: K-RAS mutation analysis, EGFR amplification analysis
Tabs—30
Maintenance treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) whose disease has not progressed after four cycles of platinum-based first-line chemotherapy. Treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) after failure of at least one prior chemotherapy regimen.
Take on empty stomach. 150mg once daily. 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).
Not recommended.
Human epidermal growth factor receptor type 1/epidermal growth factor receptor tyrosine kinase inhibitor.
Discontinue if interstitial lung disease, hepatic failure, or GI perforation occurs; interrupt or discontinue therapy in patients with dehydration at risk for renal failure, or with severe bullous, blistering or exfoliative skin conditions, or with acute/worsening ocular disorders. 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. History of peptic ulcers or diverticular disease. Pregnancy (Cat.D); use adequate contraception (see literature). Nursing mothers: not recommended.
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. Increased risk of GI perforation with concomitant anti-angiogenic agents, steroids, NSAIDs, taxane-based chemotherapy. Monitor for bleeding with oral anticoagulants, NSAIDs.
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 perforation (may be fatal), ocular disorders (eg, conjunctivitis, keratitis, corneal ulceration/perforation), MI/ischemia, hemolytic anemia, cerebrovascular accidents, interstitial lung disease; hepatic or renal failure and hepatorenal syndrome (may be fatal); bullous, blistering and exfoliative skin conditions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis).
Testing considerations: K-RAS mutation analysis, EGFR amplification analysis
Tabs—30