Erlotinib

Abstract

Erlotinib (Tarceva), an oral epidermal growth factor receptor tyrosine kinase inhibitor, is associated with modest improvements in survival in patients with advanced non-small cell lung cancer (NSCLC) who have previously received one or more prior chemotherapy regimens. In a well designed clinical trial in this patient population, median overall survival and progression-free survival were significantly longer in patients receiving erlotinib 150 mg/day than in those receiving placebo. Erlotinib is generally well tolerated, with most adverse events being of mild to moderate severity. A large body of modelled pharmacoeconomic data suggests that second- or third-line erlotinib 150 mg/day is a cost-saving option relative to treatment with the approved second-line intravenous chemotherapies of docetaxel and pemetrexed in patients with advanced NSCLC. In patients who had received at least one prior chemotherapy regimen, erlotinib was predicted to be dominant (i.e. more effective and less costly) or cost saving (i.e. equally effective and less costly) relative to docetaxel or pemetrexed with regard to the cost per QALY or life-year gained in cost-effectiveness analyses. Although the effect of erlotinib on overall survival was generally assumed to be equivalent to that of the chemotherapies, the estimated amount of QALYs gained was slightly greater with erlotinib than with docetaxel. In cost-minimization and national budgetary impact analyses, estimated total direct costs with erlotinib were lower than those with docetaxel and pemetrexed, because of the generally lower drug acquisition, administration and adverse event management costs associated with erlotinib. Cost advantages with erlotinib were predicted across analyses, regardless of the type of model developed, specific costs that were included, country that the study was conducted in and year of costing. Sensitivity analyses consistently showed that these results were robust to plausible changes in the key model assumptions. In conclusion, in patients with advanced NSCLC, second- or third-line treatment with erlotinib is clinically effective in improving survival. Available pharmacoeconomic data from several countries, despite some inherent limitations, support the use of erlotinib as a cost-saving treatment relative to chemotherapy with docetaxel or pemetrexed in this patient population.

Alendronate-Modified Polymeric Micelles for the Treatment of Breast Cancer Bone Metastasis

“…DTX, a microtubule-stabilizing taxane, is used in clinic for the treatment of metastatic breast cancer 27,28 . Along with its potent anticancer activity, DTX also exhibits serious doselimiting toxicities partly due to the formulation excipients.…”

<p>Design, synthesis, and biological study of 4-[(2-nitroimidazole-1<em>H</em>-alkyloxyl)aniline]-quinazolines as EGFR inhibitors exerting cytotoxicities both under normoxia and hypoxia</p>

“…In other words, if a drug can inhibit EGFR, and also be activated under carcinoma hypoxia, it may exert a stronger effect. Recently, many small molecule EGFR inhibitors have been successfully developed and introduced onto the market, these drugs include gefitinib ( 1 ),9 erlotinib ( 2 ),10 lapatinib ( 3 ),11 osimertinib ( 4 ),12 etc (Figure 1). In addition, reagents targeting carcinoma-hypoxia have been massively explored, including the 2-nitroimidazole derivative pimonidazole ( 5 ),13 nimorazole ( 6 ),14 and so on (Figure 1).…”

Cost comparison of second-line treatment options for late stage non-small-cell lung cancer: cost analysis for Italy

“…Previous cost comparisons (including a review) published prior to loss of patent for docetaxel, showed that erlotinib was less costly than docetaxel, which in turn was less costly than pemetrexed, across different health care settings and different years of publication 26–32…”