Chemistry:Entinostat
From HandWiki
Entinostat, also known as SNDX-275 and MS-275, is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers.[1][2][3][4]
Entinostat inhibits class I HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively.[5]
Syndax pharmaceuticals currently holds the rights to entinostat and recently received $26.6 million in funds to advance treatments of resistant cancers using epigenetic tools.[6]
It has also been investigated as a potential male contraceptive drug.[7]
References
- ↑ "Phase I trial of 5-azacitidine (5AC) and SNDX-275 in advanced lung cancer (NSCLC).". Journal of Clinical Oncology 26 (15_suppl): 19036-. May 2008. doi:10.1200/jco.2008.26.15_suppl.19036.
- ↑ "The Histone Deacetylase Inhibitor Entinostat/Syndax 275 in Osteosarcoma". Current Advances in Osteosarcoma. Advances in Experimental Medicine and Biology. 1257. 2020. pp. 75–83. doi:10.1007/978-3-030-43032-0_7. ISBN 978-3-030-43031-3.
- ↑ "Targeting cancer epigenetic pathways with small-molecule compounds: Therapeutic efficacy and combination therapies". Pharmacological Research 173. November 2021. doi:10.1016/j.phrs.2021.105702. PMID 34102228.
- ↑ "Inhibition of histone deacetylases attenuates tumor progression and improves immunotherapy in breast cancer". Frontiers in Immunology 14. 2023. doi:10.3389/fimmu.2023.1164514. PMID 36969235.
- ↑ Maier T, Beckers T, Hummel RP, Feth M, Muller M, Bar T, Volz J, "Novel Sulphonylpyrroles as Inhibitors of Hdac S Novel Sulphonylpyrroles", US patent 2009/0263353, issued 31 July 2012
- ↑ "Company Prepares for Pivotal Phase 3 Study of Entinostat, Most Advanced HDAC Inhibitor in Development for ER+ Metastatic Breast Cancer". Syndax Pharmaceuticals. 27 August 2013. http://www.syndax.com/assets/130827%20Syndax%20Series%20B%20news%20release.pdf.
- ↑ "Targeting nuclear receptor corepressors for reversible male contraception". Proceedings of the National Academy of Sciences of the United States of America 121 (9). February 2024. doi:10.1073/pnas.2320129121. PMID 38377195. Bibcode: 2024PNAS..12120129H.
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