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Zolinza (VORINOSTAT)

Merck & Co. · FDA-approved approved Small molecule Verified Quality 75/100

Zolinza works by blocking the action of histone deacetylase 6, an enzyme that removes acetyl groups from histones, leading to changes in gene expression.

Zolinza (Vorinostat) is a small molecule Histone Deacetylase Inhibitor (HDACi) developed by Merck and currently owned by MSD Sub Merck. It targets Histone Deacetylase 6 (HDAC6) and was FDA-approved in 2006 for the treatment of Primary Cutaneous T-cell lymphoma. Zolinza has a short half-life of 0.76 hours and moderate bioavailability of 43%. It remains a patented product with no generic manufacturers available. Key safety considerations include its potential for hepatotoxicity and thrombocytopenia.

At a glance

Generic nameVORINOSTAT
SponsorMerck & Co.
Drug classHistone Deacetylase Inhibitor [EPC]
TargetHistone deacetylase 6
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved
First approval2006

Mechanism of action

Vorinostat inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II) at nanomolar concentrations (IC50<86 nM). These enzymes catalyze the removal of acetyl groups from the lysine residues of proteins, including histones and transcription factors. In some cancer cells, there is an overexpression of HDACs, or an aberrant recruitment of HDACs to oncogenic transcription factors causing hypoacetylation of core nucleosomal histones. Hypoacetylation of histones is associated with condensed chromatin structure and repression of gene transcription. Inhibition of HDAC activity allows for the accumulation of acetyl groups on the histone lysine residues resulting in an open chromatin structure and transcriptional activation. In vitro, vorinostat causes the accumulation of acetylated histones and induces cell cycle arrest and/or apoptosis of some transformed cells. The mechanism of the antineoplastic effect of vorinostat

Approved indications

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Key clinical trials

Patents

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Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity

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