Drug intelligence / Profile preview

CCS1477 + enzalutamide

Development stage
Phase 2
Lead developer
CellCentric
Modality
Small Molecules
Administration
Oral
01

Overview

CCS1477 + enzalutamide is an investigational combination therapy under evaluation for metastatic castration-resistant prostate cancer (mCRPC) and potentially other advanced solid tumors. CCS1477 is a first-in-class, oral small molecule inhibitor targeting the bromodomain of the twin acetyltransferases p300 and CBP, transcriptional coactivators implicated in androgen receptor (AR) signaling, including AR mutations and splice variants associated with drug resistance. Enzalutamide is a well-established second-generation anti-androgen that acts as an antagonist at the androgen receptor, blocking AR signaling. The rationale behind the combination is to suppress both AR expression/function (including resistant variants) via CCS1477 and block AR signaling via enzalutamide, potentially resensitizing tumors that have progressed after prior anti-androgen therapy. Clinical trials are ongoing to determine safety, tolerability, and efficacy for patients with advanced prostate cancer, particularly those with progression after enzalutamide or abiraterone[1][3][5].

Other names
CCS1477 + enzalutamide
02

Targets

AR (Adrenergic receptors)CREBBP BD (Creb-binding protein bromodomain)EP300 BD (E1A Binding Protein p300 Bromodomain)CREBBP (CREB-binding protein)

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