art6043

ART6043 is a selective, orally bioavailable small-molecule inhibitor of DNA polymerase theta (Polθ), a DNA repair enzyme that is overexpressed in many cancer cells but largely absent from normal tissues. By inhibiting Polθ, ART6043 disrupts the microhomology-mediated end joining (MMEJ) pathway of DNA double-strand break repair. This leads to the accumulation of unrepaired DNA damage in cancer cells—especially those with deficiencies in other DNA damage response (DDR) pathways such as BRCA1/2 mutations—ultimately causing cell death. Healthy cells are less affected due to their limited reliance on Polθ for DNA repair. ART6043 is being developed primarily for advanced or metastatic solid tumors and is under investigation both as monotherapy and in combination with PARP inhibitors like olaparib and niraparib[1][2][3][6][7].

Other names

ART6043ART-6043ART 6043