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Association details:
| Biomarker: | MAP2K1 mutation |
|---|---|
| Cancer: | Melanoma |
| Drug: | DS03090629 (MEK inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Discovery of a Novel ATP-Competitive MEK Inhibitor DS03090629 that Overcomes Resistance Conferred by BRAF Overexpression in BRAF-Mutated Melanoma
Published date:
03/02/2023
Excerpt:
In both in vitro and in vivo settings, potent inhibition of MEK by DS03090629 or its combination with the BRAF inhibitor dabrafenib was demonstrated in a mutant BRAF-overexpressing melanoma cell line model…DS03090629 also exhibited superior efficacy against a melanoma cell line–expressing mutant MEK1 protein compared with dabrafenib and trametinib....These results suggest that DS03090629 may be a novel therapeutic option for patients who acquire resistance to the current BRAF- and MEK-targeting therapies.
DOI:
10.1158/1535-7163.MCT-22-0306
