Drug intelligence / Profile preview

azenosertib + pegylated liposomal doxorubicin

Development stage
Phase 1
Lead developer
Zentalis Pharmaceuticals
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Oral, Intravenous
01

Overview

Azenosertib + pegylated liposomal doxorubicin is a **combination regimen** under clinical investigation for cancer treatment, primarily ovarian cancer. Azenosertib is a small molecule inhibitor targeting WEE1, a DNA damage response kinase involved in cell cycle regulation. By inhibiting WEE1, azenosertib prevents phosphorylation and inactivation of Cyclin/CDK complexes, forcing cancer cells with unrepaired DNA into mitosis, resulting in replication stress, mitotic catastrophe, and apoptosis[1]. Pegylated liposomal doxorubicin is a liposome-encapsulated formulation of the anthracycline doxorubicin, which intercalates DNA and inhibits topoisomerase II, leading to DNA damage and apoptotic cell death. The combination is being studied for potential synergy in inducing cancer cell death through complementary DNA-damaging and cell cycle checkpoint-disrupting mechanisms, particularly in ovarian cancer and other solid tumors[2].

Other names
ZN-c3 + pegylated liposomal doxorubicin
02

Targets

DNAWEE1 (WEE1 G2 checkpoint kinase)TOP2A (DNA topoisomerase II)

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