Abexinostat

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Abexinostat (INN), formerly known as PCI-24781, is an experimental drug that has been primarily investigated for the treatment of various cancer types. It was originally developed by Pharmacyclics and later licensed to Xynomic. The drug functions as a pan-histone deacetylase inhibitor and also affects the function of RAD51, a protein integral to the process of DNA double strand break repair.

Development and Licensing

Abexinostat was first synthesized and researched by Pharmacyclics, a biopharmaceutical company known for its work in oncology. Recognizing its potential, Xynomic, another pharmaceutical entity, acquired the licensing rights to further explore its therapeutic possibilities and to navigate its progression through clinical trials.

Mechanism of Action

Abexinostat's anticancer activity arises from its dual role in inhibiting key cellular processes:

• Pan-Histone Deacetylase Inhibition: Histone deacetylases (HDACs) are enzymes responsible for the removal of acetyl groups from histones, which results in the compacting of DNA and suppression of gene expression. By inhibiting HDACs, Abexinostat promotes the acetylation of histones, leading to a more relaxed chromatin structure and facilitating gene transcription. This can reactivate genes that suppress tumors and induce cancer cell death.
• RAD51 Inhibition: RAD51 is a crucial protein in the homologous recombination pathway, which repairs DNA double-strand breaks. By inhibiting RAD51, Abexinostat impairs the DNA repair mechanism, leading to the accumulation of DNA damage in cancer cells, which can result in cell death.

Clinical Trials

As an experimental drug, Abexinostat has been subjected to multiple phases of clinical trials. Its efficacy, safety, and optimal dosing regimens are still under investigation. Preliminary results have shown promise in specific cancer subtypes, but further studies are needed to establish its place in oncology therapeutics.

Potential Side Effects

As with all cancer treatments, Abexinostat may come with a range of side effects. Commonly reported side effects in clinical trials include fatigue, nausea, and hematological abnormalities. It is essential to consider the risk-to-benefit ratio before integrating it into therapeutic protocols.

Current Status

Abexinostat remains an experimental drug and has not yet received approval from global health regulatory bodies. Its potential therapeutic value is balanced against its safety profile, and further research will determine its viability as a mainstream cancer treatment.

See Also

• Histone deacetylase inhibitor
• DNA repair
• Oncology
• Pharmacology

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