BI-4020

BI-4020 is a fourth-generation, non-covalent, and orally active inhibitor of EGFR tyrosine kinase. (In Vitro) :BI-4020 inhibits p-EGFR del19 T790M C797S (IC50: 0.6 nM) . BI-4020 inhibits not only the triple mutant EGFR (del19/T790M/C797S) variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR (del19/T790M) and primary mutant EGFR del19 (IC50: 1 nM) . BI-4020 also shows activity against EGFR wt (IC50: 190 nM) . BI-4020 shows high kinome selectivity and good DMPK properties. (In Vivo) :In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions.