SB-216

SB-216 is a potent, brain-penetrable small molecule tubulin inhibitor that specifically targets the colchicine binding site (CBSI). Developed to address the clinical challenge of breast cancer brain metastasis (BCBM), particularly in patients with aggressive molecular subtypes like triple-negative breast cancer (TNBC), SB-216 is designed to effectively cross the blood-brain barrier (BBB). Its mechanism of action involves the disruption of microtubule dynamics, which inhibits tumor cell growth and migration and induces apoptosis with low nanomolar potency. Preclinical studies have demonstrated that SB-216 can reduce both brain and concurrent extracranial metastases in preventive dosing paradigms and suppress the expansion of pre-established brain lesions, leading to extended overall survival in animal models.