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In the afatinib group, the most common treatment-related adverse events were diarrhea, rash/acne, and stomatitis; in the chemotherapy group, they were nausea, fatigue, and decreased appetite. Patient-reported outcomes favored afatinib, with better control of cough, dyspnea, and pain, the investigators say.
S1011. Afatinib (BIBW2992). Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt) , EGFR(L858R) , EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.EE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCÎ± and CDK1.