Almonertinib (HS-10296) hydrochloride 是一种口服的、不可逆的第三代 EGFR 酪氨酸激酶抑制剂，对 EGFR 致敏和 T790M 耐药突变具有高选择性。 HS-10296 hydrochloride 对 T790M、T790M/L858R 和 T790M/Del19 具有很强的抑制活性（IC50 分别为 0.37、0.29 和 0.21 nM），而对野生型的抑制效果较差（3.39 nM）。 HS-10296 hydrochloride 用于非小细胞肺癌的研究。
HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
HS-10296 hydrochloride is an orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity, which canbe used to treat NSCLC[1]. Additionaly, HS-10296 could also inhibit other EGFR sensitive mutations, including G719X, del19, L858R and L861Q[2].
[1]. Sullivan I, et al. Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First Line. Front Med (Lausanne). 2017 Jan 18;3:76. [2]. Wu SG, et al. Management of acquired resistance to EGFR TKI-targeted therapy in advanced non-small cell lung cancer. Mol Cancer. 2018 Feb 19;17(1):38.
动态评分
0.0