Inhibition of mutated, activated BRAF in metastatic melanoma
Background The identification of somatic mutations in the gene encoding the serine–
threonine protein kinase B-RAF (BRAF) in the majority of melanomas offers an opportunity to
test oncogene-_targeted therapy for this disease. Methods We conducted a multicenter,
phase 1, dose-escalation trial of PLX4032 (also known as RG7204), an orally available
inhibitor of mutated BRAF, followed by an extension phase involving the maximum dose that
could be administered without adverse effects (the recommended phase 2 dose). Patients …
threonine protein kinase B-RAF (BRAF) in the majority of melanomas offers an opportunity to
test oncogene-_targeted therapy for this disease. Methods We conducted a multicenter,
phase 1, dose-escalation trial of PLX4032 (also known as RG7204), an orally available
inhibitor of mutated BRAF, followed by an extension phase involving the maximum dose that
could be administered without adverse effects (the recommended phase 2 dose). Patients …