礼来(LLY.US)非共价BTK抑制剂“匹妥布替尼“申报新适应症

智通财经
20 Jun

智通财经APP获悉,6月18日,CDE网站显示,礼来(LLY.US)的匹妥布替尼片剂申报新适应症。推测此次申报的适应症为接受过至少两种治疗的慢性淋巴细胞白血病或小淋巴细胞淋巴瘤(CLL/SLL)成人患者。

匹妥布替尼(pirtobrutinib)是礼来研发的first-in-class非共价BTK C481S抑制剂。共价BTK抑制剂包括伊布替尼、泽布替尼、阿可替尼和奥布替尼,都是通过与BTK的C481残基结合,阻断ATP结合口袋,抑制BTK酶的活性从而发挥抗肿瘤作用,但C481突变会引起耐药,而非共价抑制剂匹妥布替尼不依赖C481也可与BTK高选择性结合,能够克服C481突变导致的耐药。

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