Oral, Brain-Penetrant Inhibitor of Oncogenic BRAF MasterKey Mutations
BDTX-4933 is designed to be a potent, brain-penetrant MasterKey BRAF inhibitor of Class I, II, & III mutations and fusions without paradoxical activation.
Oncogenic mutations affecting BRAF include the V600E (Class I) active site mutation together with families of allosteric and non-canonical mutations (Class II and Class III). While the V600E Class I mutation has been successfully targeted in melanoma, there are currently no approved therapies that target the full spectrum of Class II and Class III mutations that are expressed in melanoma together with a range of other solid tumors. Additionally, both approved drugs and product candidates that are currently in clinical development lead to paradoxical activation of wild type-RAF and select non-canonical mutations, which can lead to secondary malignancies and ineffective targeting of oncogenic mutations.
BDTX-4933 is designed to target all the MasterKey mutations comprised of Class I, Class II, and Class III mutations while avoiding paradoxical activation by inhibiting dimerized RAF kinase and to be brain penetrant to treat CNS diseases.