elimusertib + niraparib

Elimuseritb + niraparib is a combination of two small molecule inhibitors under investigation for cancer therapy, specifically targeting tumors with DNA damage response (DDR) alterations. Elimusertib (BAY1895344) is a potent and highly selective inhibitor of Ataxia Telangiectasia and Rad3-related protein (ATR), which regulates DNA damage repair checkpoint activation and replication stress response[2][5]. Niraparib (ZeJula) is an inhibitor of poly(ADP-ribose) polymerase (PARP), a family of enzymes critical for DNA single-strand break repair[5][6]. The combination is being explored to enhance antitumor activity in PARP inhibitor (PARPi)-resistant cancers and to overcome resistance by synergistically blocking two essential DDR pathways. Preclinical studies show this combination improves efficacy compared to monotherapy in patient-derived xenograft (PDX) models with DDR defects[1][3]. Clinical trials are underway to investigate its utility in advanced solid tumors and ovarian cancer, focusing on optimal dosing and toxicity management[5].

Other names

BAY1895344 + niraparibelimusertib + niraparib