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INCB057643 + rucaparib
- Development stage
- Discontinued
- Lead developer
- Incyte
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
INCB057643 + rucaparib is an investigational combination therapy consisting of the selective bromodomain and extraterminal (BET) inhibitor INCB057643 and the PARP inhibitor rucaparib. INCB057643 acts by inhibiting BET family proteins, regulators of gene transcription involved in cancer cell proliferation and survival. Rucaparib targets poly(ADP-ribose) polymerase 1/2 (PARP1/2) enzymes, impeding single-strand DNA break repair and synthetic lethality in tumors with deficient homologous recombination repair, such as BRCA-mutated cancers. This combination has been studied in early-phase clinical trials for advanced/metastatic solid tumors, including BRCA-wild type platinum-resistant high-grade serous ovarian cancer and other solid tumors, but with very limited patient data and limited efficacy. The development was undertaken by Incyte (for INCB057643) and Clovis Oncology (for rucaparib; now marketed by pharma companies after Clovis’ bankruptcy).
- Other names
- INCB57643INCB-57643INCB 57643Rubraca
02
Targets
BRD4 (Bromodomain-containing protein 4)PARP3 (Poly(adp-ribose) polymerase 3)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)BRDT (Bromodomain testis-specific protein)PARP2 (Poly (adp-ribose) polymerase 2)
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