Quisinostat

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Quisinostat
Quisinostat.svg
Clinical data
Synonyms JNJ-26481585
ATC code
  • None
Pharmacokinetic data
Bioavailability oral[1]
Identifiers
PubChem CID
ChemSpider
KEGG
Chemical and physical data
Formula C21H26N6O2
Molar mass 394.470 g/mol
3D model (JSmol)

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]

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.[8] Results of a phase I trials in patients with multiple myeloma in combination with bortezomib and dexamethasone were published in 2016.[9]

References[edit]

  1. ^ https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=596704[full citation needed]
  2. ^ "Quisinostat" (PDF). American Medical Association. 
  3. ^ Tong, Wei-Gang; Wei, Yue; Stevenson, William; Kuang, Shao-Qing; Fang, Zhihong; Zhang, Ming; Arts, Janine; Garcia-Manero, Guillermo (2010). "Preclinical antileukemia activity of JNJ-26481585, a potent second-generation histone deacetylase inhibitor". Leukemia Research. 34 (2): 221–8. doi:10.1016/j.leukres.2009.07.024. PMID 19682743. 
  4. ^ Stühmer, Thorsten; Arts, Janine; Chatterjee, Manik; Borawski, Johanna; Wolff, André; King, Peter; Einsele, Hermann; Leo, Eugen; Bargou, Ralf C. (2010). "Preclinical anti-myeloma activity of the novel HDAC-inhibitor JNJ-26481585". British Journal of Haematology. 149 (4): 529–36. doi:10.1111/j.1365-2141.2010.08126.x. PMID 20331455. 
  5. ^ "Quisinostat". NCI Drug Dictionary. National Cancer Institute. 
  6. ^ Carol, Hernan; Gorlick, Richard; Kolb, E. Anders; Morton, Christopher L.; Manesh, Donya Moradi; Keir, Stephen T.; Reynolds, C. Patrick; Kang, Min H.; Maris, John M.; Wozniak, Amy; Hickson, Ian; Lyalin, Dmitry; Kurmasheva, Raushan T.; Houghton, Peter J.; Smith, Malcolm A.; Lock, Richard (2014). "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. doi:10.1002/pbc.24724. PMC 4225045Freely accessible. PMID 24038993. 
  7. ^ http://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[full citation needed]
  8. ^ http://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[full citation needed]
  9. ^ Moreau, Philippe; Facon, Thierry; Touzeau, Cyrille; Benboubker, Lotfi; Delain, Martine; Badamo-Dotzis, Julie; Phelps, Charles; Doty, Christopher; Smit, Hans; Fourneau, Nele; Forslund, Ann; Hellemans, Peter; Leleu, Xavier (2016). "Quisinostat, bortezomib, and dexamethasone combination therapy for relapsed multiple myeloma". Leukemia & Lymphoma. 57 (7): 1546–59. doi:10.3109/10428194.2015.1117611. PMID 26758913.