Chemistry:Quisinostat
From HandWiki
Short description: Chemical compound
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| Other names | JNJ-26481585 |
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| Bioavailability | oral[1] |
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| Formula | C21H26N6O2 |
| Molar mass | 394.479 g·mol−1 |
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Quisinostat (USAN;[2] development code JNJ-26481585) is an experimental drug candidate for the treatment of cancer. It is a "second generation" histone deacetylase inhibitor with antineoplastic activity.[3][4][5] It is highly potent against class I and II HDACs.[6]
History
It was developed by Janssen Pharmaceuticals and licensed to NewVac LLC.[7]
Preclinical studies show that quisinostat amplifies HDAC-repressed expression of E-cadherin, leading to a reversal of epithelial to mesenchymal transition in tumor cells.[7]
Clinical trials
Results of a phase I trials in patients with multiple myeloma in combination with bortezomib and dexamethasone were published in 2016.[8]
References
- ↑ "NCI Drug Dictionary". 2 February 2011. https://www.cancer.gov/publications/dictionaries/cancer-drug.
- ↑ "Quisinostat". American Medical Association. http://www.ama-assn.org/resources/doc/usan/quisinostat.pdf.
- ↑ "Preclinical antileukemia activity of JNJ-26481585, a potent second-generation histone deacetylase inhibitor". Leukemia Research 34 (2): 221–8. February 2010. doi:10.1016/j.leukres.2009.07.024. PMID 19682743.
- ↑ "Preclinical anti-myeloma activity of the novel HDAC-inhibitor JNJ-26481585". British Journal of Haematology 149 (4): 529–36. May 2010. doi:10.1111/j.1365-2141.2010.08126.x. PMID 20331455.
- ↑ "Quisinostat". NCI Drug Dictionary. National Cancer Institute. http://www.cancer.gov/drugdictionary?cdrid=596704.
- ↑ "Initial testing (stage 1) of the histone deacetylase inhibitor, quisinostat (JNJ-26481585), by the Pediatric Preclinical Testing Program". Pediatric Blood & Cancer 61 (2): 245–52. February 2014. doi:10.1002/pbc.24724. PMID 24038993.
- ↑ 7.0 7.1 LLC, NewVac. "NewVac Reports Primary Endpoint Met in Phase II Clinical Trial of Quisinostat in Combination with Paclitaxel and Carboplatin in Platinum-Resistant Ovarian Cancer". https://www.prnewswire.com/news-releases/newvac-reports-primary-endpoint-met-in-phase-ii-clinical-trial-of-quisinostat-in-combination-with-paclitaxel-and-carboplatin-in-platinum-resistant-ovarian-cancer-300384676.html.
- ↑ "Quisinostat, bortezomib, and dexamethasone combination therapy for relapsed multiple myeloma". Leukemia & Lymphoma 57 (7): 1546–59. July 2016. doi:10.3109/10428194.2015.1117611. PMID 26758913.
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