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PLX2853 + olaparib
- Development stage
- Discontinued
- Lead developer
- Opna Bio
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
PLX2853 + olaparib is a combination of two investigational oral small molecules being evaluated for the treatment of metastatic castration-resistant prostate cancer (mCRPC) and other malignancies. **PLX2853** is a potent, selective inhibitor of bromodomain and extra-terminal (BET) proteins, which are chromatin adaptors involved in epigenetic regulation and are implicated in cancer cell proliferation and survival. **Olaparib** is a poly(ADP-ribose) polymerase (PARP) inhibitor that blocks PARP-mediated DNA repair, leading to increased cytotoxicity in cancer cells, especially those with deficient homologous recombination repair. The rationale for this combination is to exploit synthetic lethality—BET inhibition may sensitize tumors to PARP inhibition, particularly in tumors with mutations in genes such as ARID1A or BRCA. Trials are ongoing or planned for the combination in metastatic prostate cancer and potentially other cancer indications[2][7][9].
- Other names
- PLX2853 + olaparib
02
Targets
BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)BRDT (Bromodomain testis-specific protein)CREBBP (CREB-binding protein)EP300 (Histone acetyltransferase p300 (EP300) catalytic domain)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)BRD (Bromodomain-containing protein family)
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