HSK42360

HSK42360 is a next-generation, brain-permeable small molecule inhibitor that selectively targets BRAF V600 mutations. It is classified as a "BRAF paradox breaker," meaning it inhibits mutant BRAF-driven signaling with significantly less paradoxical activation of the MAPK pathway compared to approved BRAF inhibitors and spares wild-type BRAF-containing RAF dimers. Preclinical studies have demonstrated excellent anti-tumor efficacy in multiple solid tumor models harboring BRAFV600 mutations, including strong activity against brain metastases and tumors resistant to first-generation BRAF inhibitors due to RAF dimerization. The drug shows good tolerability and a large safety window in preclinical models. Clinically, it is being developed for the treatment of advanced or metastatic solid tumors with BRAFV600 mutations, including primary brain cancers and brain metastases[1][3][4][6][9].