pofenbrodib + olaparib

**Pofenbrodib + olaparib** is an investigational oral combination therapy under clinical development for advanced cancers, particularly metastatic castration-resistant prostate cancer (mCRPC). - **Pofenbrodib** is a small molecule inhibitor of the bromodomain of the histone acetyltransferases CREB-binding protein (CBP, also known as CREBBP) and p300 (also known as EP300). By inhibiting these proteins, which are transcriptional co-activators, poenbrodib disrupts acetylation of histones and other proteins, impeding transcriptional activation of several oncogenic pathways and reducing tumor proliferation, especially in tumors reliant on AR (androgen receptor) signaling[2][4][6]. - **Olaparib** is a small molecule inhibitor of poly-ADP ribose polymerase (PARP), involved in DNA repair processes. By blocking PARP, olaparib induces synthetic lethality in tumor cells with homologous recombination repair deficiencies, most prominently BRCA1/2 mutant cancers[5]. - The **combination** is intended to deliver synergistic antitumor activity by impairing both gene regulation and DNA repair. This regimen is currently being studied in Phase 1b/2a trials for patients with mCRPC, and pharmacodynamic rationale/risk includes targeting epigenetic modulation (CBP/p300) and DNA repair (PARP) pathways simultaneously[4]. - Olaparib is approved as Lynparza for several indications including ovarian and prostate cancer; poenbrodib is investigational.

Brand names

Lynparza

Other names

pocenbrodibFT-7051FT7051FT 7051