GSK-2849466

Overview of the experimental drug GSK-2849466

GSK-2849466

Chemical structure of GSK-2849466

GSK-2849466 is an experimental drug developed by GlaxoSmithKline (GSK) that acts as a potent and selective inhibitor of the enzyme poly (ADP-ribose) polymerase (PARP). This compound is part of a class of drugs known as PARP inhibitors, which are being investigated for their potential use in the treatment of various types of cancer.

Mechanism of Action

GSK-2849466 functions by inhibiting the activity of PARP enzymes, which play a crucial role in the repair of DNA single-strand breaks through the base excision repair pathway. By blocking PARP activity, GSK-2849466 prevents the repair of DNA damage in cancer cells, leading to the accumulation of DNA breaks and ultimately causing cell death. This mechanism is particularly effective in cancer cells that are already deficient in other DNA repair pathways, such as those with BRCA1 or BRCA2 mutations.

Clinical Development

GSK-2849466 is currently undergoing clinical trials to evaluate its safety and efficacy in patients with various types of cancer, including breast cancer, ovarian cancer, and prostate cancer. The drug is being tested both as a monotherapy and in combination with other anticancer agents to determine its potential benefits in different therapeutic contexts.

Potential Benefits

The use of GSK-2849466 as a PARP inhibitor offers several potential benefits in cancer treatment. By specifically targeting cancer cells with defective DNA repair mechanisms, it may provide a more targeted approach to therapy, reducing damage to normal cells and minimizing side effects. Additionally, the combination of GSK-2849466 with other treatments may enhance the overall effectiveness of cancer therapy.

Challenges and Considerations

While GSK-2849466 shows promise, there are challenges associated with its development and use. These include the need to identify patients who are most likely to benefit from PARP inhibition, managing potential resistance mechanisms that cancer cells may develop, and addressing any adverse effects that may arise during treatment.

Related Pages

• PARP inhibitor
• GlaxoSmithKline
• Cancer treatment
• BRCA mutation