Drug intelligence / Profile preview

alobresib + enzalutamide

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

**Alobresib + enzalutamide** is an investigational combination therapy composed of alobresib (a BET bromodomain inhibitor) and enzalutamide (a second-generation androgen receptor inhibitor). This combination is under clinical investigation mainly for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Alobresib inhibits the bromodomain and extra-terminal motif (BET) proteins, thereby reducing the expression and signaling of the androgen receptor (AR) including splice variant AR-V7 that drives resistance to standard AR-directed therapies. Enzalutamide inhibits androgen receptor signaling by binding to the receptor, blocking androgen-induced receptor translocation and DNA binding. The rationale for combination is that BET inhibition may overcome resistance to AR antagonists by reducing AR signaling and associated resistance pathways.

Brand names
enzalutamide
Other names
BET inhibitor + enzalutamide
02

Targets

AR (Adrenergic receptors)BRD4 (Bromodomain-containing protein 4)

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