Repositioning Candidate Details

Candidate ID: R0566
Source ID: DB02546
Source Type: approved; investigational
Compound Type: small molecule
Compound Name: Vorinostat
Synonyms: Octanedioic acid hydroxyamide phenylamide; SAHA; SHH; Suberanilohydroxamic acid; Suberoylanilide hydroxamic acid
Molecular Formula: C14H20N2O3
SMILES: ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1
Structure:
DrugBank Description: Vorinostat (rINN) or suberoylanilide hydroxamic acid (SAHA), is a drug currently under investigation for the treatment of cutaneous T cell lymphoma (CTCL), a type of skin cancer, to be used when the disease persists, gets worse, or comes back during or after treatment with other medicines. It is the first in a new class of agents known as histone deacetylase inhibitors. A recent study suggested that vorinostat also possesses some activity against recurrent glioblastoma multiforme, resulting in a median overall survival of 5.7 months (compared to 4 - 4.4 months in earlier studies). Further brain tumor trials are planned using combinations of vorinostat with other drugs.
CAS Number: 149647-78-9
Molecular Weight: 264.3202
DrugBank Indication: For the treatment of cutaneous manifestations in patients with cutaneous T-cell lymphoma who have progressive, persistent or recurrent disease on or following two systemic therapies.
DrugBank Pharmacology: --
DrugBank MoA: Vorinostat inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II) at nanomolar concentrations (IC<sub>50</sub>&lt; 86 nM). These enzymes catalyze the removal of acetyl groups from the lysine residues of histones proteins. 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. By inhibiting histone deacetylase, 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 has not been fully characterized.
Targets: Histone deacetylase 1 inhibitor; Histone deacetylase 2 inhibitor; Histone deacetylase 3 inhibitor; Histone deacetylase 6 inhibitor; Histone deacetylase 8; Acetoin utilization protein
Inclusion Criteria: Therapeutic strategy associated