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adavosertib + carboplatin
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Adavosertib (AZD1775) is an orally available, highly selective small-molecule inhibitor of the WEE1 kinase. WEE1 is a key regulator of the G2 cell cycle checkpoint; its inhibition abrogates G2 arrest and sensitizes tumor cells—especially those with TP53 mutations—to DNA-damaging agents such as platinum-based chemotherapies. Carboplatin is a platinum-based chemotherapy that induces DNA crosslinking and damage. The combination of adavosertib with carboplatin has shown synergistic antitumor activity in preclinical models and clinical trials, particularly in tumors with p53 pathway deficiencies such as TP53-mutated ovarian cancer and advanced/metastatic squamous cell lung cancer. This combination aims to enhance the efficacy of chemotherapy by preventing tumor cells from repairing DNA damage before mitosis[1][2][3][4][6].
- Other names
- adavosertib + carboplatin
02
Targets
DNAWEE1 (WEE1 G2 checkpoint kinase)
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