luvixasertib

Luvixasertib (CFI-402257) is an orally bioavailable, potent, and highly selective small molecule inhibitor of threonine tyrosine kinase (TTK), also known as monopolar spindle 1 kinase (Mps1). TTK is a dual-specificity protein kinase that plays a critical role in the spindle assembly checkpoint during mitosis, ensuring proper chromosome alignment and segregation. Inhibition of TTK by luvixasertib disrupts this checkpoint, leading to chromosomal missegregation, aneuploidy, and ultimately cell death. This mechanism underlies its antineoplastic activity across various solid tumors. Preclinical studies have shown that luvixasertib induces apoptosis and senescence-like responses in cancer cells and can activate the DDX41-STING cytosolic DNA sensing pathway to promote anti-tumor immunity. The drug has demonstrated efficacy both as monotherapy and in combination with immune checkpoint inhibitors such as anti–PD‑1 antibodies. Luvixasertib is being developed primarily for advanced solid tumors including hepatocellular carcinoma and ER+/HER2– advanced breast cancer after progression on prior CDK4/6 inhibitors and endocrine therapy[2][3][4][5][6][8].

Other names

N-cyclopropyl-4-(7-(((cis-3-hydroxy-3-methylcyclobutyl)methyl)amino)-5-(3-pyridinyloxy)pyrazolo(1,5-a)pyrimidin-3-yl)-2-methylbenzamide