Pocenbrodib (previously FT-7051) is a small molecule inhibitor that has the potential to provide clinical benefit for patients with advanced prostate cancer, either alone or in combination with other treatments.
Pocenbrodib (previously FT-7051) works by inhibiting CREBBP/EP300 (also known as CBP/P300), which are proteins that activate genes that promote cancer cell growth and proliferation. Inhibiting these proteins impacts the expression of key cancer drivers, including the androgen receptor (AR) and its variants, making pocenbrodib relevant not only to advanced prostate cancer but to a number of other cancer indications as well either alone or in combination with other treatments.
P-500 (previously PRT811) is a selective, brain-penetrant small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) that has the potential to provide clinical benefit for patients with advanced solid tumors, including high-grade glioma and uveal melanoma.
PRMT5 is an enzyme that adds methyl groups to proteins in cells using a molecule called SAM (S-adenosylmethionine) which regulates protein function and interactions. Several processes that support cancer cell growth and spread depend on PRMT5, making P-500 relevant not only to advanced high-grade glioma and uveal melanoma (in which objective responses to P-500 were observed in the Phase 1 clinical trial) but also to a number of other cancer indications. Preclinical studies have demonstrated PRMT5 inhibition can sensitize cancer cells to other treatments, expanding the application of P-500 to combination therapy in additional indications.