VORINOSTAT

Details

Stereochemistry	ACHIRAL
Molecular Formula	C14H20N2O3
Molecular Weight	264.3202
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1

InChI

InChIKey=WAEXFXRVDQXREF-UHFFFAOYSA-N

InChI=1S/C14H20N2O3/c17-13(15-12-8-4-3-5-9-12)10-6-1-2-7-11-14(18)16-19/h3-5,8-9,19H,1-2,6-7,10-11H2,(H,15,17)(H,16,18)

HIDE SMILES / InChI

Molecular Formula	C14H20N2O3
Molecular Weight	264.3202
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.drugbank.ca/drugs/DB02546
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021991s002lbl.pdf

Vorinostat (rINN) or suberoylanilide hydroxamic acid (SAHA), is a drug currently under investigation for the treatment of cutaneous T cell lymphoma (CTCL). 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 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. Vorinostat is used 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. Vorinostat is marketed under the name Zolinza by Merck for the treatment of cutaneous manifestations in patients with cutaneous T cell lymphoma (CTCL) when the disease persists, gets worse, or comes back during or after two systemic therapies.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Plasmodium falciparum 3D7 7 Target ID: CHEMBL2366922 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26199860	Inhibitor 8504	0.12 µM [IC50]
NCI-H661 1 Target ID: CHEMBL1075544 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8504	0.13 µM [IC50]
Histone deacetylase 1 51 Target ID: CHEMBL325 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8504	0.15 µM [IC50]
Histone deacetylase 2 37 Target ID: CHEMBL1937 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8504	0.28 µM [IC50]
Histone deacetylase 8 16 Target ID: CHEMBL3192 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8504	1.68 µM [IC50]
Histone deacetylase 3 35 Target ID: CHEMBL1829 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19410459	Inhibitor 8504	57.0 nM [IC50]
Histone deacetylase 6 28 Target ID: CHEMBL1865 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25734520	Inhibitor 8504	1.0 µM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cutaneous T-cell lymphoma 10 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021991s002lbl.pdf	Primary		Approved 8583	Zolinza Approved Use Treatment of cutaneous manifestations in patients with cutaneous T cell lymphoma (CTCL) who have progressive, persistent or recurrent disease on or following two systemic therapies. Launch Date 2006

C_max

Value	Dose	Analyte	Population
0.83 uM Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00771472	400 mg single, oral dose: 400 mg route of administration: oral experiment type: single co-administered:	VORINOSTAT plasma	Homo sapiens population: unhealthy age: sex: food status:
1.17 uM Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00771472	400 mg 1 times / day steady, oral dose: 400 mg route of administration: oral experiment type: steady co-administered:	VORINOSTAT plasma	Homo sapiens population: unhealthy age: sex: food status:
1.2 μM DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021991s002lbl.pdf	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VORINOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

AUC

Value	Dose	Analyte	Population
4.59 uM*h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00771472	400 mg single, oral dose: 400 mg route of administration: oral experiment type: single co-administered:	VORINOSTAT plasma	Homo sapiens population: unhealthy age: sex: food status:
5.59 uM*h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00771472	400 mg 1 times / day steady, oral dose: 400 mg route of administration: oral experiment type: steady co-administered:	VORINOSTAT plasma	Homo sapiens population: unhealthy age: sex: food status:
5.5 μM × h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021991s002lbl.pdf	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VORINOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

T_1/2

Value	Dose	Analyte	Population
1.94 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00771472	400 mg single, oral dose: 400 mg route of administration: oral experiment type: single co-administered:	VORINOSTAT plasma	Homo sapiens population: unhealthy age: sex: food status:
2.3 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00771472	400 mg 1 times / day steady, oral dose: 400 mg route of administration: oral experiment type: steady co-administered:	VORINOSTAT plasma	Homo sapiens population: unhealthy age: sex: food status:
2 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021991s002lbl.pdf	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	VORINOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

F_unbound

Value	Dose	Co-administered	Analyte	Population
29% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021991s002lbl.pdf	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:		VORINOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

Doses

Dose	Population	Adverse events
250 mg 2 times / day multiple, oral Dose: 250 mg, 2 times / day Route: oral Route: multiple Dose: 250 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18297527	unhealthy, 63 years (range: 38 - 74 years) Health Status: unhealthy Age Group: 63 years (range: 38 - 74 years) Sources: https://pubmed.ncbi.nlm.nih.gov/18297527	DLT: Fatigue... Dose limiting toxicities: Fatigue (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/18297527
300 mg 2 times / day multiple, oral Highest studied dose Dose: 300 mg, 2 times / day Route: oral Route: multiple Dose: 300 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021991lbl.pdf https://pubmed.ncbi.nlm.nih.gov/16960145	unhealthy, 69 years (range: 26.0 - 80.0 years) Health Status: unhealthy Age Group: 69 years (range: 26.0 - 80.0 years) Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021991lbl.pdf https://pubmed.ncbi.nlm.nih.gov/16960145	Disc. AE: Thrombocytopenia, Anemia... Other AEs: Hypotension, Sepsis... AEs leading to discontinuation/dose reduction: Thrombocytopenia (grade 3-4, 8%) Anemia (grade 3-4, 17%) Deep vein thrombosis (grade 3-4, 25%) Pyrexia (grade 3-4, 25%) Pulmonary embolism (grade 3-4, 17%) Other AEs: Hypotension (grade 3-4, 17%) Sepsis (grade 3-4, 8%) Fatigue (all grades, 27%) Diarrhea (11%) Nausea (8%) Dysgeusia (11%) Weight loss (3%) Vomiting (11%) Anorexia (3%) Blood creatinine increased (8%) Dehydration (5%) Anemia (5%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021991lbl.pdf https://pubmed.ncbi.nlm.nih.gov/16960145

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087 supressor 22	inhibitor 2438 inducer 440	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP 110 P-gp 1741 CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057	CYP 303 P-gp 2052 UGT1A1 479 UGT1A3 470 UGT1A7 249 UGT1A8 323 UGT1A9 423 UGT2B7 456 UGT2B17 237	CYP1A2 832 CYP2B6 669 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4, 6, 27	inconclusive	no (co-administration study) Comment: vorinostat has no inhibitory effect on the tranport of vinblastine Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4, 6, 27
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 79.8 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP 150	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf Page: 9.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 25.0	yes
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP3A4 2633	supressor 160 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_PharmR.pdf Page: 37.0	yes

Drug as victim

Target	Modality	Activity
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4, 6, 27	inconclusive
CYP 303	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6.0	no
UGT1A1 479	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A3 470	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A7 249	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A8 323	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A9 423	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4.0	yes
UGT2B17 237	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4.0	yes
UGT2B7 456	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_PharmR.pdf Page: 31.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:45716	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:45716
ChemicalBook	CB3506806	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB3506806
eMolecules	1989084	https://www.emolecules.com/cgi-bin/more?vid=1989084
MolPort	MolPort-003-850-293	https://www.molport.com/shop/molecule-link/MolPort-003-850-293
Selleck Chemicals	Vorinostat-(SAHA)	http://www.selleckchem.com/products/Vorinostat-(SAHA).html
ZINC	ZINC000001543873	http://zinc15.docking.org/substances/ZINC000001543873

PubMed

Title	Date	PubMed
SAHA-sensitized prostate cancer cells to TNFalpha-related apoptosis-inducing ligand (TRAIL): mechanisms leading to synergistic apoptosis.	2006-07-01	16450389
Carbonyl- and sulfur-containing analogs of suberoylanilide hydroxamic acid: Potent inhibition of histone deacetylases.	2006-05-15	16434199
Loss of interleukin-2-dependency in HTLV-I-infected T cells on gene silencing of thioredoxin-binding protein-2.	2006-04-06	16314839
Suberoylanilide hydroxamic acid potentiates apoptosis, inhibits invasion, and abolishes osteoclastogenesis by suppressing nuclear factor-kappaB activation.	2006-03-03	16377638
Histone deacetylase inhibitors induce cell death and enhance the susceptibility to ionizing radiation, etoposide, and TRAIL in medulloblastoma cells.	2006-03	16465382
Clinical experience with intravenous and oral formulations of the novel histone deacetylase inhibitor suberoylanilide hydroxamic acid in patients with advanced hematologic malignancies.	2006-01-01	16330674
Histone deacetylase inhibitors reduce VEGF production and induce growth suppression and apoptosis in human mantle cell lymphoma.	2006-01	16343270
SAHA, a HDAC inhibitor, has profound anti-growth activity against non-small cell lung cancer cells.	2006-01	16328054
5-Aza-2'-deoxycytidine (decitabine) can relieve p21WAF1 repression in human acute myeloid leukemia by a mechanism involving release of histone deacetylase 1 (HDAC1) without requiring p21WAF1 promoter demethylation.	2006-01	16043219
Histone deacetylase inhibitors induce differentiation of human endometrial adenocarcinoma cells through up-regulation of glycodelin.	2005-12	16123169
Crystal structure of a bacterial class 2 histone deacetylase homologue.	2005-11-18	16242151
Suberoylanilide hydroxamic acid enhances gap junctional intercellular communication via acetylation of histone containing connexin 43 gene locus.	2005-11-01	16266998
Selective induction of apoptosis by histone deacetylase inhibitor SAHA in cutaneous T-cell lymphoma cells: relevance to mechanism of therapeutic action.	2005-11	16297208
Histone deacetylases in acute myeloid leukaemia show a distinctive pattern of expression that changes selectively in response to deacetylase inhibitors.	2005-10	16121216
Histone deacetylase inhibitors suppress the induction of c-Jun and its target genes including COX-2.	2005-09-23	15994313
Activity of suberoylanilide hydroxamic Acid against human breast cancer cells with amplification of her-2.	2005-09-01	16144943
Induction of polyploidy by histone deacetylase inhibitor: a pathway for antitumor effects.	2005-09-01	16140952
Early clinical data and potential clinical utility of novel histone deacetylase inhibitors in prostate cancer.	2005-09	16197607
Synergistic interactions between MEK1/2 and histone deacetylase inhibitors in BCR/ABL+ human leukemia cells.	2005-09	16015388
It's about time: scheduling alters effect of histone deacetylase inhibitors on camptothecin-treated cells.	2005-08-01	16061681
Suberoylanilide hydroxamic acid combined with gemcitabine enhances apoptosis in non-small cell lung cancer.	2005-08	16153448
Synergistic apoptosis induction by proteasome and histone deacetylase inhibitors is dependent on protein synthesis.	2005-08	16133866
Histone deacetylase inhibitors induced caspase-independent apoptosis in human pancreatic adenocarcinoma cell lines.	2005-08	16093438
A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells.	2005-07-28	16033284
Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent.	2005-07-01	15927839
Interactive effects of HDAC inhibitors and TRAIL on apoptosis are associated with changes in mitochondrial functions and expressions of cell cycle regulatory genes in multiple myeloma.	2005-07	16026644
Blockade of histone deacetylase inhibitor-induced RelA/p65 acetylation and NF-kappaB activation potentiates apoptosis in leukemia cells through a process mediated by oxidative damage, XIAP downregulation, and c-Jun N-terminal kinase 1 activation.	2005-07	15964800
Effect of inhibitors of histone deacetylase on the induction of cell differentiation in murine and human erythroleukemia cell lines.	2005-07	15930892
Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer.	2005-06-10	15897550
The histone-deacetylase inhibitor SAHA potentiates proapoptotic effects of 5-fluorouracil and irinotecan in hepatoma cells.	2005-06	15754201
Novel histone deacetylase inhibitors in the treatment of thyroid cancer.	2005-05-15	15897598
Modulation of radiation response by histone deacetylase inhibition.	2005-05-01	15850925
The role of histone acetylation in SMN gene expression.	2005-05-01	15772088
Suberoylanilide hydroxamic acid (SAHA) has potent anti-glioma properties in vitro, ex vivo and in vivo.	2005-05	15857402
Histone deacetylase inhibitors in programmed cell death and cancer therapy.	2005-04	15738652
Cotreatment with suberanoylanilide hydroxamic acid and 17-allylamino 17-demethoxygeldanamycin synergistically induces apoptosis in Bcr-Abl+ Cells sensitive and resistant to STI571 (imatinib mesylate) in association with down-regulation of Bcr-Abl, abrogation of signal transducer and activator of transcription 5 activity, and Bax conformational change.	2005-04	15625278
Coadministration of histone deacetylase inhibitors and perifosine synergistically induces apoptosis in human leukemia cells through Akt and ERK1/2 inactivation and the generation of ceramide and reactive oxygen species.	2005-03-15	15781658
[Histone deacetylase inhibitors as a new generation of anti-cancer agents].	2005-03-11	15928589
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells.	2005-03-01	15713371
Drug insight: Histone deacetylase inhibitors--development of the new targeted anticancer agent suberoylanilide hydroxamic acid.	2005-03	16264908
4-Hydroxybenzoyl derivative from the aqueous extract of the hydroid Campanularia sp.	2005-03	15787459
Histone deacetylase inhibitors interact synergistically with tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) to induce apoptosis in carcinoma cell lines.	2005-03	15744585
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.	2005-02-24	15715470
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.	2005-01-17	15603949
Histone deacetylase inhibitors profoundly decrease proliferation of human lymphoid cancer cell lines.	2005-01	15661398
The histone deacetylase inhibitor suberoylanilide hydroxamic acid down-regulates expression levels of Bcr-abl, c-Myc and HDAC3 in chronic myeloid leukemia cell lines.	2005-01	15583844
High turbulence liquid chromatography online extraction and tandem mass spectrometry for the simultaneous determination of suberoylanilide hydroxamic acid and its two metabolites in human serum.	2005	15945019
The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces apoptosis via induction of 15-lipoxygenase-1 in colorectal cancer cells.	2004-12-01	15574791
Histone deacetylase inhibitors up-regulate the expression of tight junction proteins.	2004-12	15634758
Proteasome inhibition sensitizes non-small cell lung cancer to histone deacetylase inhibitor-induced apoptosis through the generation of reactive oxygen species.	2004-11	15514602

Patents

Sample Use Guides

In Vivo Use Guide

400 mg orally once daily with food. If patient is intolerant to therapy, the dose may be reduced to 300 mg orally once daily with food. If necessary, the dose may be further reduced to 300 mg once daily with food for 5 consecutive days each week.

Route of Administration: Oral

In Vitro Use Guide

Concentrations of vorinostat higher than 0.5 uM significantly inhibited the upregulated gene expression of MMP-1 and MMP-13 induced by IL-1β, whereas 0.1 uM vorinostat showed no obvious effect. Conversely, 0.5 uM vorinostat or higher concentration increased the TIMP-1 expression.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 06:51:50 GMT 2025` Edited by `admin` on `Wed Apr 02 06:51:50 GMT 2025`
Record UNII	58IFB293JI
Record Status	`Validated (UNII)`
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Name

Type

Language

N-HYDROXY-N'-PHENYLOCTANEDIAMIDE

Preferred Name

English

VORINOSTAT

Official Name

English

VORINOSTAT [MI]

Common Name

English

NSC-759852

Code

English

VORINOSTAT [ORANGE BOOK]

Common Name

English

NSC-701852

Code

English

NSC-748799

Code

English

ZOLINZA

Brand Name

English

MK0683

Code

English

VORINOSTAT [MART.]

Common Name

English

MK-0683

Code

English

VORINOSTAT [USAN]

Common Name

English

OCTANEDIAMIDE, N-HYDROXY-N'-PHENYL-

Systematic Name

English

vorinostat [INN]

Common Name

English

Vorinostat [WHO-DD]

Common Name

English

SUBEROYLANILIDE HYDROXAMIC ACID

Common Name

English

VORINOSTAT [JAN]

Common Name

English

VORINOSTAT [VANDF]

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

177203