Ricolinostat (ACY-1215)
General information
Class/mechanism from the NCI Drug Dictionary: An orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. Ricolinostat selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. This leads to an accumulation of unfolded and misfolded ubiquitinated proteins and may eventually induce cancer cell apoptosis, and inhibition of cancer cell growth.[1][2][3]
Route: PO
Extravasation: n/a
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Preliminary data
Multiple myeloma
- Vogl DT, Raje N, Jagannath S, Richardson P, Hari P, Orlowski R, Supko JG, Tamang D, Yang M, Jones SS, Wheeler C, Markelewicz RJ, Lonial S. Ricolinostat, the First Selective Histone Deacetylase 6 Inhibitor, in Combination with Bortezomib and Dexamethasone for Relapsed or Refractory Multiple Myeloma. Clin Cancer Res. 2017 Jul 1;23(13):3307-3315. Epub 2017 Jan 4. link to original article link to PMC article PubMed
Also known as
- Code name: ACY-1215
- Generic name: rocilinostat
References
- ↑ Ricolinostat in Multiple Myeloma, Acetylon Pharmaceuticals
- ↑ Andrew J Yee, MD, Peter M. Voorhees, MD, William Bensinger, Jesus G. Berdeja, MD, Jeffrey G Supko, PhD, Paul G. Richardson, David Tamang, PhD, Simon S Jones, PhD, Gretchen Patrick, Catherine Wheeler, MD and Noopur Raje, MD. Ricolinostat (ACY-1215), a Selective HDAC6 Inhibitor, in Combination with Lenalidomide and Dexamethasone: Results of a Phase 1b Trial in Relapsed and Relapsed Refractory Multiple Myeloma. 2014 ASH Annual Meeting abstract 4772. link to abstract
- ↑ Noopur Raje, MD, Parameswaran N Hari, MD, MRCP, MS, Dan T. Vogl, MD, MSCE, Sundar Jagannath, MD, Robert Z. Orlowski, M.D., Ph.D., Jeffrey G Supko, PhD, Patricia Stephenson, ScD, Simon S Jones8, Catherine Wheeler, MD and Sagar Lonial, MD. Rocilinostat (ACY-1215), a Selective HDAC6 Inhibitor, Alone and in Combination with Bortezomib in Multiple Myeloma: Preliminary Results From the First-in-Humans Phase I/II Study. 2012 ASH Annual Meeting abstract 4061. link to abstract