AZD 9291

AZD 9291 is an inhibitor of mutant EGFRs (IC₅₀s = 1, 12, and 5 nM for EGFR^L858R/T790M, EGFR^L858R, and EGFR^L861Q, respectively).¹ It is selective for these mutant EGFRs over wild-type EGFR (IC₅₀ = 184 nM), as well as over a panel of approximately 280 other kinases at 1 µM. AZD 9291 selectively inhibits the proliferation of mutant EGFR-containing non-small cell lung cancer (NSCLC) cells, including H1975 cells containing the L858R activating and T790M resistance mutations, PC-9 cells containing the activating exon 19 deletion, and vandetanib-resistant PC-9 cells, which contain the exon 19 deletion and T790M mutation (IC₅₀s = 11, 8, and 40 nM, respectively), over wild-type EGFR-containing Calu-3 and NCI H2073 NSCLC cells (IC₅₀s = 650 and 461 nM, respectively). It induces tumor regression in a vandetanib-resistant PC-9 mouse xenograft model when administered at doses ranging from 1 to 10 mg/kg. Formulations containing AZD 9291 have been used in the treatment of EGFR mutant-containing NSCLC.

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