abivertinib

Avitinib (AC0010) 是一种不可逆的、突变体选择性的EGFR 抑制剂，可有效抑制非小细胞肺癌中EGFR T790M 耐药突变。阿比替尼也是一种新型BTK 抑制剂。

Avitinib maleate 是基于吡咯并嘧啶的不可逆的表皮生长因子受体抑制剂，IC50值为7.68 nM。

Abivertinib, also known as AC0010 and Avitinib, is a third-generation EGFR tyrosine kinase inhibitor and BTK Inhibitor that demonstrated clinical efficacy and manageable adverse events (AEs). Abivertinib inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. Abivertinib was also found to be more sensitive than ibrutinib in treating AML. Abivertinib may be a promising novel agent for AML, with potential for combination treatment with HHT.

Avitinib (Abivertinib) maleate dihydrate 是一种第三代的不可逆EGFR抑制剂，具有口服活性，对EGFRL858R、EGFRT790M和野生型EGFR的IC50分别为0.18 nM、0.18 nM和7.68 nM。该化合物也是BTK抑制剂，能够诱导套细胞淋巴瘤细胞发生凋亡 (apoptosis) 并阻断BTK的磷酸化，具有抗癌特性。