Drug intelligence / Profile preview

Debio 0123 + temozolomide

Development stage
Unknown
Lead developer
Debiopharm
Modality
Small Molecules
Administration
Oral
01

Overview

**Debio 0123 + temozolomide** is an investigational combination therapy under clinical development for the treatment of glioblastoma and other glial tumors. Debio 0123 is a brain-penetrant, highly selective small molecule inhibitor of WEE1 kinase, a key regulator of the S and G2/M cell cycle checkpoints activated in response to DNA damage. WEE1 inhibition by Debio 0123 abrogates DNA damage-induced cell cycle arrest, forcing cells with unrepaired DNA into mitosis, resulting in mitotic catastrophe and cell death. Temozolomide is an alkylating agent used as a standard-of-care chemotherapeutic in glioblastoma. By combining Debio 0123 with temozolomide, there is a synergistic effect: the DNA damage induced by temozolomide is intensified by the inhibition of repair checkpoints through WEE1 blockade, resulting in enhanced tumor cell death. The combination is currently in Phase 1/2 clinical trials for recurrent or newly diagnosed glioblastoma, including settings with radiotherapy[1][2][3][4][5][6].

Brand names
Debio 0123 + temozolomide
Other names
Debio 0123 and temozolomideDebio0123 and temozolomideDebio-0123 and temozolomide
02

Targets

WEE1 (WEE1 G2 checkpoint kinase)

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