Dapolsertib

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An investigational drug targeting cancer


{{Drugbox | verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-(4-methylpiperazin-1-yl)phenyl]amino]-N-(3-pyridinylmethyl)-3-(trifluoromethyl)butanamide | image = Dapolsertib.svg }}

Dapolsertib is an investigational anticancer drug that functions as a selective inhibitor of protein kinases, specifically targeting the aurora kinase family. It is being studied for its potential use in the treatment of various types of cancer.

Mechanism of Action

Dapolsertib works by inhibiting the activity of aurora kinases, which are enzymes that play a crucial role in the regulation of mitosis in eukaryotic cells. Aurora kinases are involved in the processes of chromosome alignment, spindle assembly, and cytokinesis. By inhibiting these kinases, dapolsertib disrupts the normal progression of the cell cycle, leading to apoptosis or programmed cell death in rapidly dividing cancer cells.

Clinical Development

Dapolsertib is currently undergoing clinical trials to evaluate its efficacy and safety in patients with various types of cancer, including breast cancer, lung cancer, and colorectal cancer. These trials aim to determine the optimal dosing regimen and to identify any potential side effects associated with the drug.

Potential Benefits

The selective inhibition of aurora kinases by dapolsertib offers a targeted approach to cancer treatment, potentially reducing the side effects associated with traditional chemotherapy that affects both cancerous and healthy cells. This specificity may lead to improved outcomes for patients with cancers that are driven by aberrant aurora kinase activity.

Challenges and Considerations

While dapolsertib shows promise as a targeted cancer therapy, there are challenges associated with its development. These include the need to identify biomarkers that predict response to treatment, managing potential resistance mechanisms, and ensuring that the drug can be effectively delivered to tumor sites.

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Contributors: Prab R. Tumpati, MD