azenosertib

Azenosertib is an orally bioavailable, small molecule inhibitor of the tyrosine kinase Wee1 (Wee1-like protein kinase). It acts as a DNA damage response (DDR) drug by selectively inhibiting WEE1, a master cell cycle regulator that controls the G1-S and G2-M checkpoints through negative regulation of CDK1 and CDK2. By blocking WEE1 activity, azenosertib prevents cell cycle arrest in response to DNA damage, forcing cancer cells—especially those with p53 deficiency or high Cyclin E1 expression—to progress through mitosis without repairing damaged DNA. This leads to replication stress, mitotic catastrophe, and ultimately apoptosis in tumor cells. Azenosertib is being developed primarily for various cancers including ovarian cancer (with Phase III trials ongoing), pancreatic cancer, uterine cancer (Phase II), triple-negative breast cancer, osteosarcoma (orphan drug status), solid tumors, acute myeloid leukemia, colorectal cancer, fallopian tube cancer, peritoneal cancer (Phase I/II), and breast cancer (Phase I). The drug has received FDA Fast Track Designation for certain indications[2][4][5][6][7].

Other names

azenosertib