Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible, orally active selective EGFR inhibitor with IC50 values of 0.18 nM for EGFRL858R and EGFRT790M, and 7.68 nM for wild-type EGFR. Additionally, Avitinib maleate dihydrate functions as a BTK inhibitor, promoting apoptosis in mantle cell lymphoma cells and inhibiting BTK phosphorylation, demonstrating anticancer properties.

Avitinib maleate dihydrate (AC0010; 0.13 nM-2 μM; 2 h) selectively inhibits the phosphorylation of mutant EGFR in NCI-H1975 and NIH/3T3_TC32T8 cells, with IC 50 values of 7.3 nM and 2.8 nM, showing approximately 115-fold and 298-fold greater sensitivity compared to wild-type EGFR in A431 cells. This compound effectively suppresses EGFR-Tyr1068 phosphorylation in NCI-H1975 cells, exhibiting a selectivity ratio for NCI-H1975 over A431 cells of 65-fold. Additionally, Avitinib maleate dihydrate inhibits the phosphorylation of downstream targets Akt and ERK1/2 in both NCI-H1975 and HCC827 cells [1].

Avitinib maleate dihydrate (AC0010; 12.5-500 mg/kg; oral; once daily; for 14 days) effectively inhibits the growth of EGFR mutant tumors in xenograft models over an extended period, without affecting the growth of wild-type EGFR tumors [1].