Osimertinib is a potent, selective, irreversible inhibitor of mutant EFGR tyrosine kinase.1 Osimertinib inhibits phosphorylation of EGFR in T790M-mutant cell lines (IC50 <15 nM) but was less potent at inhibition of EGFR phosphorylation in wild-type cells (IC50s in the range of 480 to 1,865 nM). It produces sustained tumor regression in EGFR-mutant tumor xenograft and transgenic rodent models.2 Tumor cells develop resistance to osimertinib but combination treatment with an IL-6 antibody reverses resistance to a certain extent.3 In clinical use for treatment of non-small cell lung cancer.4
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