AZD5153 + olaparib

AZD5153 + olaparib is an investigational oral combination therapy comprising AZD5153, a reversible, bivalent small-molecule inhibitor of the bromodomain and extraterminal (BET) family protein BRD4, and olaparib, a poly(ADP-ribose) polymerase (PARP) inhibitor approved as Lynparza. The combination is designed to harness the anti-tumorigenic effects of BRD4 inhibition and the DNA repair inhibition from PARP blockade. AZD5153 binds to both bromodomains of BRD4 and modulates oncogenic pathways such as MYC, contributing to tumor growth arrest, while olaparib inhibits DNA damage repair, promoting cancer cell death. Developed by AstraZeneca, this combination is primarily being explored in phase I trials for relapsed and refractory solid tumors and lymphoma, with additional investigation in pancreatic cancer and other tumor types. The therapy is administered orally in fixed dosing regimens, with dose-limiting toxicities such as thrombocytopenia and gastrointestinal side effects observed. Early clinical results show tolerability and biomarker modulation, with evidence of anti-tumor activity in some patients[1][3][4].

Other names

AZD5153 plus olaparibAZD-5153 plus olaparibAZD 5153 plus olaparibAZD5153 and olaparibAZD-5153 and olaparibAZD 5153 and olaparibAZD5153/olaparib