Overview

Generic Name(s):
vorinostat
Trade Name(s):
Zolinza
NCI Definition [1]:
A synthetic hydroxamic acid derivative with antineoplastic activity. Vorinostat, a second generation polar-planar compound, binds to the catalytic domain of the histone deacetylases (HDACs). This allows the hydroxamic moiety to chelate zinc ion located in the catalytic pockets of HDAC, thereby inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors. Hyperacetylation of histone proteins results in the upregulation of the cyclin-dependant kinase p21, followed by G1 arrest. Hyperacetylation of non-histone proteins such as tumor suppressor p53, alpha tubulin, and heat-shock protein 90 produces additional anti-proliferative effects. This agent also induces apoptosis and sensitizes tumor cells to cell death processes. Vorinostat crosses the blood-brain barrier.

Vorinostat has been investigated in 30 clinical trials, of which 23 are open and 7 are closed. Of the trials investigating vorinostat, 13 are phase 1 (13 open), 5 are phase 1/phase 2 (4 open), 10 are phase 2 (5 open), 1 is phase 2/phase 3 (1 open), and 1 is phase 3 (0 open).

KMT2A Fusion, BCR-ABL1 Fusion, and KMT2A-AFF1 Fusion are the most frequent biomarker inclusion criteria for vorinostat clinical trials.

Acute myeloid leukemia, acute lymphoblastic leukemia, and breast carcinoma are the most common diseases being investigated in vorinostat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Vorinostat
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Vorinostat
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating vorinostat and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
mk 0683, Zolinza, merck brand of vorinostat, suberoylanilide hydroxamic acid, suberoylanilide hydroxamic acid, shh, nhnpoda, l-001079038, suberoylanilide hydroxamic acid, suberanilohydroxamic acid, n-hydroxy-n'-phenyloctanediamide, vorinostat, octanedioic acid hydroxyamide phenylamide, suberanilohydroxamic acid, n-hydroxy-n'-phenyl octanediamide, vorinostat (substance), saha, n-hydroxy-n'-phenyloctanediamide, msk390, vorinostat, n1-hydroxy-n8-phenyloctanediamide, suberanilohydroxamic acid, vorinostatum, vorinostat (product), vorinostat [chemical/ingredient], msk-390
Drug Categories [2]:
Histone deactylase/HDAC inhibitors
Drug Target(s) [2]:
HDAC1, HDAC2, HDAC3, HDAC6
NCIT ID [1]:
C1796
SNOMED ID [1]:
C-781F2

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.