Drug intelligence / Profile preview

pofenbrodib + 177Lu-PSMA-617

Development stage: Unknown
Lead developer: Novartis
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Oral (pofenbrodib), Intravenous (177Lu-PSMA-617)

Overview

**pofenbrodib + 177Lu-PSMA-617** is an investigational drug combination being studied for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Pofenbrodib (also known as FT-7051 or P-300) is an orally bioavailable small molecule inhibitor of the CBP/p300 bromodomain, which blocks the activity of the transcriptional co-activators CREB-binding protein (CBP) and p300, disrupting androgen receptor (AR) signaling and gene transcription critical for prostate cancer proliferation. 177Lu-PSMA-617 (Pluvicto) is a radioligand therapy targeting prostate-specific membrane antigen (PSMA) expressed on prostate cancer cells, delivering a radioactive beta-emitting lutetium-177 payload directly to tumor cells to induce DNA damage and cell death. The combination is under investigation for its synergistic potential to overcome resistance mechanisms to AR-targeted therapy and to more effectively target cancer cells via distinct, complementary mechanisms.

Brand names: Pluvicto (for 177Lu-PSMA-617)
Other names: pocenbrodib hydrochloridepocenbrodib (INN/USAN)FT-7051 (pocenbrodib)lutetium Lu 177 vipivotide tetraxetan (synonym for 177Lu-PSMA-617)

Targets

DNAEP300 (Histone acetyltransferase p300 (EP300) catalytic domain)CREBBP (CREB-binding protein)

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