Brief Description |
BIBW2992 (Afatinib) is an ATP-competitive, small molecule irreversible inhibitor for EGFR/HER2, displaying inhibitory potency against EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2, with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. |
References |
1. Li, D. et al., BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models, Oncogene 2008, 27 (34), 4702-4711.
2. Minkovsky, N. et al., BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors. Curr Opin Investig Drugs (December 2008), 9 (12), 1336-46. |