Erlotinib
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.CYP3A4 inhibitors: Tarceva is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Tarceva AUC by 67%. When Tarceva was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Tarceva exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Tarceva decreased Tarceva AUC by 58% to 80%. Dose modifications are recommended.Drugs affecting gastric pH: Co-administration of Tarceva with omeprazole decreased Tarceva AUC by 46% and co-administration of Tarceva with Ranitidine 300 mg decreased Tarceva AUC by 33%.
The most common adverse reactions (20%) with Tarceva from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.Interstitial Lung Disease (ILD)Renal FailureHepatotoxicity with or without Hepatic ImpairmentGastrointestinal PerforationBullous and Exfoliative Skin DisordersMyocardial Infarction/IschemiaCerebrovascular AccidentMicroangiopathic Hemolytic Anemia with ThrombocytopeniaOcular DisordersHemorrhage in Patients Taking Warfarin
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Tarceva for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Tarceva if ILD is diagnosed.Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Tarceva for severe renal toxicity.Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Tarceva for severe or worsening liver tests.Gastrointestinal perforations-discontinue Tarceva.Bullous and exfoliative skin disorders-discontinue Tarceva.Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
Single oral doses of Tarceva up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Tarceva in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Tarceva should be withheld and symptomatic treatment instituted.
Targeted Cancer Therapy
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Pediatric use: The safety and effectiveness of Tarceva in pediatric patients have not been established.Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
{'Description': 'Tarceva, a kinase inhibitor, is a quinazolinamine with the chemical name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)4-quinazolinamine. Tarceva reversibly inhibits the kinase activity of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor and thereby inhibiting further downstream signaling. Tarceva binding affinity for EGFR exon 19 deletion or exon 21 (L858R) mutations is higher than its affinity for the wild-type receptor. Tarceva inhibition of other tyrosine kinase receptors has not been fully characterized.'}