Drug intelligence / Profile preview

ART6043 + niraparib

Development stage
Unknown
Lead developer
Artios Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

ART6043 + niraparib is a **combination therapy** under investigation for the treatment of advanced or metastatic solid tumors, including breast cancer with certain genetic mutations. ART6043 is a small molecule oral inhibitor of DNA polymerase theta, an enzyme involved in the repair of damaged DNA in cancer cells. Niraparib is an approved small molecule PARP (poly ADP-ribose polymerase) inhibitor that interferes with DNA repair in cancer cells, leading to cell death; it is approved for several cancers including ovarian, fallopian tube, and peritoneal cancer. The combination aims to exploit dual synthetic lethality in tumors with deficient DNA repair, particularly those with BRCA mutations or other homologous recombination deficiencies, by blocking complementary DNA repair pathways[1][3][7]. ART6043 is being developed and tested both alone and with niraparib in early-phase clinical trials.

02

Targets

POLQ (DNA polymerase theta)PARP2 (Poly (adp-ribose) polymerase 2)PARP1 (Poly (adp-ribose) polymerase 1)

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