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RG7204*: An oncogenic BRAF signaling inhibitor

Oncogenic BRAF signaling is implicated in multiple malignancies including melanoma, thyroid, ovarian, and colorectal cancer, with BRAFV600E accounting for ~90% of BRAF mutations.1,12

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Oncogenic BRAF

Oncogenic BRAF Signaling

References

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In preclinical studies, elimination of the BRAFV600E allele resulted in loss of cell proliferation and increased apoptosis, therefore, validating this target for further cancer research.5 RG7204 is an oral agent being developed by Roche and Genentech, in partnership with Plexxikon Inc. RG7204 is a potential first-in-class therapeutic small molecule designed to selectively inhibit mutated V600 BRAF.5

  1. RG7204 is an orally bioavailable small molecule designed to inhibit oncogenic BRAF, a key driver of cellular transformation.13

    BRAF 1

  2. In preclinical models, RG7204 was shown to bind oncogenic BRAF and inhibit its activity as reflected by the inhibition of downstream molecules MEK and ERK.5,13

    BRAF 2

  3. The inhibition of oncogenic BRAF leads to a block in tumor cell proliferation and the induction of apoptosis. In preclinical studies, RG7204 has been shown to cause significant growth delay or regression in tumors harboring this mutation.5,13

    BRAF 3

*RG7204 is also known as PLX4032

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