High Quality Entinostat CAS 209783-80-2

Entinostat More Info

Entinostat (CAS No. 209783-80-2) is a synthetic benzamide derivative classified as a selective histone deacetylase (HDAC) inhibitor, specifically targeting HDAC1, HDAC2, and HDAC3 isoforms. It was developed as part of ongoing research into epigenetic modulation, a field focused on regulating gene expression without altering DNA sequences. By inhibiting HDAC enzymes, entinostat promotes histone acetylation, leading to chromatin relaxation and reactivation of silenced tumor suppressor genes. This mechanism has positioned it as a promising candidate in oncology, particularly for cancers resistant to conventional therapies. Its development reflects the growing interest in epigenetic drugs as a next-generation approach to cancer treatment.

Applications and Fields of Use

Entinostat has been primarily investigated for its potential in cancer therapy, particularly in hematologic malignancies and solid tumors such as breast cancer, non-small cell lung cancer (NSCLC), and lymphoma. Clinical studies have explored its use as a monotherapy and in combination with immunotherapies, hormone therapies, or chemotherapy to enhance treatment efficacy. Beyond oncology, research suggests possible applications in inflammatory and autoimmune diseases due to its immunomodulatory effects. Additionally, its ability to reverse epigenetic silencing has prompted exploratory studies in neurodegenerative disorders, though this remains a secondary focus compared to its anticancer applications.

Market and Industry Relevance

The market for HDAC inhibitors is expanding, driven by increasing recognition of epigenetics' role in disease and the demand for targeted cancer therapies. Entinostat is positioned as a differentiated candidate due to its selective HDAC inhibition, potentially offering a better safety profile than pan-HDAC inhibitors. While still under clinical investigation, its development has attracted interest from pharmaceutical companies specializing in oncology and precision medicine. Success in late-stage trials could establish entinostat as a valuable addition to combination therapies, particularly in hormone receptor-positive breast cancer and other hard-to-treat malignancies. However, competition with approved HDAC inhibitors like vorinostat and panobinostat necessitates robust clinical data to demonstrate superior efficacy or tolerability.

Considerations and Precautions

Entinostat’s use requires careful monitoring due to potential side effects, including fatigue, gastrointestinal disturbances, hematologic abnormalities, and electrolyte imbalances. As with many epigenetic drugs, optimal dosing and long-term safety profiles are still being refined in clinical trials. Patient selection is critical, as biomarkers for responsiveness (e.g., HDAC expression levels) may influence therapeutic outcomes. Regulatory approval pathways will depend on demonstrating clinically meaningful benefits in specific indications, with rigorous post-marketing surveillance needed to identify rare adverse effects. Researchers and clinicians should adhere to ethical guidelines in clinical trials, ensuring transparent reporting of efficacy and safety data to support informed decision-making in therapeutic applications.

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