zedoresertib

zedoresertib is an orally bioavailable, brain-penetrant, highly selective small-molecule inhibitor of the serine/threonine-protein kinase WEE1 that is being developed as an anticancer therapy for difficult-to-treat solid tumors, including glioblastoma, CCNE1-amplified ovarian cancer, and advanced breast cancers.[1][3][5][7] By inhibiting WEE1, a key regulator of the G2/M and S phase DNA damage checkpoints, zedoresertib prevents phosphorylation of CDC2/CDK1, forcing cells with unrepaired DNA damage to prematurely enter mitosis, leading to replication stress, mitotic catastrophe, and apoptosis, particularly in combination with DNA-damaging agents such as temozolomide, carboplatin, and etoposide.[1][5][7] The compound was initially discovered by Almac Discovery and later licensed and clinically developed by Debiopharm, and is currently in Phase 1/2 trials as monotherapy and in combination regimens for advanced solid tumors, recurrent or newly diagnosed glioblastoma, small cell lung cancer, and subtype-defined breast cancers.[1][3][7]

Other names

zedoresertib