Drug intelligence / Profile preview

debio 0123 + carboplatin

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

Overview

Debio 0123 + carboplatin is a combination of two agents used in cancer therapy. **Debio 0123** is an orally available, highly selective, ATP-competitive inhibitor of WEE1 kinase, which governs the G2/M cell cycle checkpoint by phosphorylating cyclin-dependent kinase 1 (CDK1), thereby allowing DNA repair and preventing mitotic catastrophe. By inhibiting WEE1, Debio 0123 abrogates the S phase and G2/M checkpoints, promoting mitosis without repair and leading to increased DNA damage, mitotic catastrophe, and cancer cell death. **Carboplatin** is a platinum-based chemotherapeutic agent that induces DNA crosslinking and damage, facilitating apoptosis. In combination, Debio 0123 enhances the cytotoxicity of carboplatin, showing synergistic antitumor activity especially in tumors previously treated with platinum agents, including platinum-resistant ovarian cancer. The combination is under clinical investigation for advanced solid tumors[1][3][5].

02

Targets

DNAWEE1 (WEE1 G2 checkpoint kinase)PLK2 (Polo-like kinase 2)

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