Vorinostat (Zolinza)

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General information

Class/mechanism: Histone deacetylase (HDAC) inhibitor. Vorinostat inhibits histone deacetylases HDAC1, HDAC2, and HDAC3 (Class I), as well as HDAC6 (Class II). HDACs normally catalyze removal of acetyl groups from acetylated lysine residues in histones and non-histone proteins, which helps to regulate gene expression. Inhibition of histone deacetylases results in hyperacetylation of histones and modulates gene expression by creating an open chromatin state that leads to expression of previously silenced genes. Although the mechanism of action is not fully understood, inhibiting HDACs has been observed to result in cell cycle arrest and apoptosis of cancer cells.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Patient drug information

Diseases for which it is used

Diseases for which it was used

History of changes in FDA indication

  • 2006-10-06: Initial FDA approval: treatment of cutaneous manifestations in patients with cutaneous T-cell lymphoma who have progressive, persistent or recurrent disease on or following two systemic therapies. (Based on Duvic et al. 2006 & Merck 0683-001)

History of changes in EMA indication

  • 2010-09-20: Orphan designation for the treatment of malignant mesothelioma.
  • 2013-03-12: Orphan designation withdrawn.

History of changes in Health Canada indication

  • 2009-06-11: Initial notice of compliance

History of changes in PMDA indication

Also known as

  • Brand name: Zolinza