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NSCLC: first-line therapy for metastatic NSCLC with an epidermal growth factor receptor EGFR exon 19 deletion or exon 21 (L858R) mutation; Or after unresponsive chemotherapy for advanced NSCLC; Or as maintenance medication in the stable phase of advanced NSCLC (after 4 courses of platinum containing chemotherapy regimens).
Pancreatic cancer: in combination with gemcitabine as first-line therapy for locally advanced or unresectable or metastatic pancreatic cancer.
The recommended dose of erlotinib monotherapy for NSCLC is 150 mg / day, taken at least 1 hour before or 2 hours after eating. The medication was continued until disease progression or intolerable toxic reactions occurred. There was no evidence of patient benefit from continued treatment beyond progression.
Patients presenting with new acute onset or progressive pulmonary symptoms such as dyspnea, cough, and fever should have erlotinib treatment suspended for diagnostic evaluation. If the diagnosis of ILD is confirmed (interstitial lung disease), erlotinib should be discontinued and appropriate treatment given.
Diarrhea can usually be controlled with loperamide. Patients with severe diarrhea who fail to respond to loperamide or develop dehydration require dose reduction and temporary discontinuation of therapy. Patients with severe skin reactions also require dose reduction and temporary discontinuation of therapy.
Erlotinib should be reduced by 50 mg each time if a dose reduction is necessary.
Dose reductions should be considered when concomitantly using drugs such as strong inhibitors of CYP3A4 such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, acenocoumarol (TAO) and voriconazole, otherwise serious adverse events may occur.
Pretreatment use of the CYP3A4 inducer rifampicin reduced 2 / 3 of the erlotinib AUC. Other alternative treatments without CYP3A4 inducing activity should be considered. If there is no alternative treatment, doses of erlotinib higher than 150 mg should be considered. If the dose of erlotinib is upregulated, the dose should be reduced when rifampicin or other inducers are stopped. Other CYP3A4 inducers include, but are not limited to, rifabutin, rifapentin, phenytoin, carbamazepine, phenobarbital, and St. John's wort, which should also be avoided if possible.
Clearance of erlotinib is metabolized in the liver and secreted in the biliary tract. Erlotinib should therefore be used with caution in patients with liver dysfunction. Erlotinib tapering or suspension should be considered in case of severe adverse effects.
Smoking is known to induce CYP1A1 and CYP1A2, resulting in a 50-60% reduction in erlotinib exposure, and smokers are advised to quit smoking.
The most common adverse reactions were rash and diarrhea, with grade 3 / 4 rash and diarrhea occurring in 9% and 6%, respectively, and the median time to onset was 8 days for rash and 12 days for diarrhea. Adverse reactions occurring in greater than 10% of patients are: rash, diarrhea, decreased appetite, fatigue, dyspnea, cough, nausea, infection, vomiting, stomatitis, pruritus, dry skin, conjunctivitis, keratoconjunctivitis, abdominal pain.
Pulmonary toxicity: there are fewer reports suggesting that severe interstitial lung disease (ILD) can occur in patients with NSCLC or other solid tumors treated with Tarceva, even leading to death. The incidence of ILD was 0.8% in a randomized controlled study, and this incidence was identical in the Tarceva treatment and placebo groups. The reported ILDs include: pneumonia, interstitial pneumonia, interstitial lung disease, bronchiolitis obliterans, pulmonary fibrosis, acute respiratory stress syndrome and pulmonary effusion. Onset of symptoms ranged from 5 days to more than 9 months after treatment, with a median onset of 47 days. Most patients often had confounding factors that contributed to the development of ILD, such as: prior chemotherapy / radiotherapy, pre-existing parenchymal lung disease, lung metastasis or lung infection. When there are emerging, difficult to interpret pulmonary symptoms, such as: dyspnea, cough, fever, etc., a workup evaluation is required, and once ILD is diagnosed, Tarceva should be discontinued and appropriate therapy instituted.
Tarceva treatment can cause asymptomatic elevation of liver transaminases, therefore, liver function should be regularly reviewed during treatment, including: transaminases, bilirubin, alkaline phosphatase, etc., if liver damage is severe should be reduced or discontinued. Liver function impairment is often transient or accompanied by liver metastases. Gastrointestinal bleeding is less commonly reported and often occurs in patients receiving concomitant warfarin, so, concomitant warfarin or other anti -
Patients on coagulants should have their prothrombin time monitored.
Safety and pharmacokinetics do not differ significantly in younger and older patients, and therefore, dose adjustment is not recommended when applied to older patients.