molecules of the month


p300/CBP bromodomain inhibitor

PD observed in serial biopsies from Ph. I

50 mg QD, 3-d-on-4-off; origin not discussed

Cancer Discovery, Jan. 11, 2021

ICR / Royal Marsden / CellCentric, UK

Chemical structure of molecule CCS1477 Bromodomain inhibitor
1 min read

The CellCentric p300/CBP inhibitor, CCS1477, is an orally available drug in early development for advanced prostate cancer, and is structurally distinct from the p300/CBP inhibitor we covered in Apr. 2020. In agreement with its proposed MoA, it impacts AR and MYC signaling in serial tumor biopsies acquired from its first-in-human Ph. I trial. It will be interesting to see whether the agent is able to demonstrate a significant survival and quality-of-life benefit in late-stage disease given the likely on-target effects of p300/CBP inhibition on certain healthy cells.

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