ZEN003694 + niraparib

ZEN003694 + niraparib is an experimental combination therapy being evaluated in a Phase I clinical trial (NCT04400240) led by Haider Mahdi for the treatment of metastatic or recurrent solid tumors, specifically ovarian, fallopian tube, and primary peritoneal cancers. ZEN003694 (ZEN-3694) is a small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins (including BRD2, BRD3, and BRD4), which act as epigenetic readers to regulate the transcription of oncogenes involved in cell survival and proliferation. Niraparib (Zejula) is a potent inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, primarily PARP1 and PARP2, which are essential for repairing single-strand DNA breaks. By combining these two agents, the treatment aims to exploit synthetic lethality and potentially reverse resistance to PARP inhibitors by modulating the expression of genes involved in DNA repair and tumor cell survival, such as NSD3.

Brand names

Zejula

Other names

ZEN003694 plus niraparibZEN-003694 plus niraparibZEN 003694 plus niraparibBET inhibitor ZEN003694 combined with niraparib