Sotuletinib (BLZ945, BLZ-945)是可口服的、脑渗透性CSF-1R选择性抑制剂，IC₅₀为1 nM。CSF-1R是M-CSF的受体，调节前体巨噬细胞和单核细胞谱系破骨细胞相关功能。Sotuletinib可通过改变巨噬细胞极化来发挥抗肿瘤活性。

参考文献

1.Pyonteck SM, et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 2013 Oct;19(10):1264-72.

2.Strachan DC, et al. CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8⁺ T cells. Oncoimmunology. 2013 Dec 1;2(12):e26968.

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