2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-ethoxy-6-quinazolinyl]-4-(dimethylamino)-, (2E)-

Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFRwt, EGFRL858R/T790M, EGFRL858R and EGFRT790M, respectively[1].

EGFR (WT): 0.24 nM (IC₅₀); EGFR^L858R/T790M: 7.25 nM (IC₅₀); EGFR^L858R: 0.46 nM (IC₅₀); EGFR^T790M: 1.79 nM (IC₅₀)

[1] Yidong Feng, et al. "NEP010, a novel compound with minor structural modification from afatinib, exhibited significantly improved antitumor activity." European Journal of Pharmacology 946 (2023): 175620. DOI:10.1016/j.ejphar.2023.175620