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 6 Target ID: CHEMBL2366922 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26199860	Inhibitor 8228	0.12 µM [IC50]
NCI-H661 1 Target ID: CHEMBL1075544 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8228	0.13 µM [IC50]
Histone deacetylase 1 51 Target ID: CHEMBL325 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8228	0.15 µM [IC50]
Histone deacetylase 2 37 Target ID: CHEMBL1937 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8228	0.28 µM [IC50]
Histone deacetylase 8 17 Target ID: CHEMBL3192 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25953722	Inhibitor 8228	1.68 µM [IC50]
Histone deacetylase 3 35 Target ID: CHEMBL1829 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19410459	Inhibitor 8228	57.0 nM [IC50]
Histone deacetylase 6 27 Target ID: CHEMBL1865 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25734520	Inhibitor 8228	1.0 µM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cutaneous T-cell lymphoma 9 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021991s002lbl.pdf	Primary		Approved 8360	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 1.16000634E12

C_max

Value	Dose	Analyte	Population
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
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:

AUC

Value	Dose	Analyte	Population
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
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:

T_1/2

Value	Dose	Analyte	Population
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
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:

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) n = 5 Health Status: unhealthy Condition: advanced multiple myeloma Age Group: 63 years (range: 38 - 74 years) Population Size: 5 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 (starting) 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) n = 12 Health Status: unhealthy Condition: cutaneous Tcell lymphoma Age Group: 69 years (range: 26.0 - 80.0 years) Sex: M+F Population Size: 12 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 1579 inducer 768 supressor 21	inhibitor 1752 inducer 383	inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP 110 P-gp 1437 CYP1A2 1509 CYP2B6 799 CYP2C8 901 CYP2C19 1463	CYP 266 P-gp 1527 UGT1A1 418 UGT1A3 422 UGT1A7 236 UGT1A8 283 UGT1A9 380 UGT2B7 389 UGT2B17 213	CYP1A2 689 CYP2B6 538 CYP2C19 290

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
P-gp 1626	inhibitor 3240 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 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 79.8 uM]
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6, 25, 26	no [IC50 >100 uM]
CYP 146	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf Page: 9.0	no
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 25.0	yes
CYP2B6 985	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP2C19 1537	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP3A4 1909	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 26.0	yes
CYP3A4 1909	supressor 155 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 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4, 6, 27	inconclusive
CYP 266	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 6.0	no
UGT1A1 418	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A3 422	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A7 236	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A8 283	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 3.0	yes
UGT1A9 380	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4.0	yes
UGT2B17 213	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021991s000_Zolinza_ClinPharmR.pdf Page: 4.0	yes
UGT2B7 389	substrate 3326 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 1632	inhibitor 1613 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
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
eMolecules	1989084	https://www.emolecules.com/cgi-bin/more?vid=1989084

PubMed

Title	Date	PubMed
The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces differentiation of human breast cancer cells.	2001 Dec 1	11731433
Histone deacetylase inhibitors induce caspase-dependent apoptosis and downregulation of daxx in acute promyelocytic leukaemia with t(15;17).	2001 Nov	11703323
Synergistic induction of mitochondrial damage and apoptosis in human leukemia cells by flavopiridol and the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA).	2002 Jul	12094258
Suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor, suppresses the growth of carcinogen-induced mammary tumors.	2002 May-Jun	12168829
Histone deacetylase inhibitors promote STI571-mediated apoptosis in STI571-sensitive and -resistant Bcr/Abl+ human myeloid leukemia cells.	2003 May 1	12727828
Susceptibility of multidrug resistance tumor cells to apoptosis induction by histone deacetylase inhibitors.	2003 May 1	12594812
Inhibition of histone deacetylase increases cytotoxicity to anticancer drugs targeting DNA.	2003 Nov 1	14612526
The proteasome inhibitor bortezomib interacts synergistically with histone deacetylase inhibitors to induce apoptosis in Bcr/Abl+ cells sensitive and resistant to STI571.	2003 Nov 15	12893773
Microarray profiling of the effects of histone deacetylase inhibitors on gene expression in cancer cell lines.	2004 Apr	15010814
Combined histone deacetylase and NF-kappaB inhibition sensitizes non-small cell lung cancer to cell death.	2004 Aug	15300209
Histone deacetylase inhibitors up-regulate the expression of tight junction proteins.	2004 Dec	15634758
The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces apoptosis via induction of 15-lipoxygenase-1 in colorectal cancer cells.	2004 Dec 1	15574791
Restoration of transforming growth factor-beta signaling through receptor RI induction by histone deacetylase activity inhibition in breast cancer cells.	2004 Jul 30	15155736
Enhancement of radiation sensitivity of human squamous carcinoma cells by histone deacetylase inhibitors.	2004 Jun	15161353
Synergistic induction of oxidative injury and apoptosis in human multiple myeloma cells by the proteasome inhibitor bortezomib and histone deacetylase inhibitors.	2004 Jun 1	15173093
Role of oxidative enzymatic treatments on enzymatic hydrolysis of softwood.	2004 Jun 5	15129438
Sequence-specific potentiation of topoisomerase II inhibitors by the histone deacetylase inhibitor suberoylanilide hydroxamic acid.	2004 May 15	15108350
Proteasome inhibition sensitizes non-small cell lung cancer to histone deacetylase inhibitor-induced apoptosis through the generation of reactive oxygen species.	2004 Nov	15514602
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
Histone deacetylase inhibitors in programmed cell death and cancer therapy.	2005 Apr	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 Apr	15625278
Suberoylanilide hydroxamic acid combined with gemcitabine enhances apoptosis in non-small cell lung cancer.	2005 Aug	16153448
Synergistic apoptosis induction by proteasome and histone deacetylase inhibitors is dependent on protein synthesis.	2005 Aug	16133866
It's about time: scheduling alters effect of histone deacetylase inhibitors on camptothecin-treated cells.	2005 Aug 1	16061681
Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates.	2005 Feb 24	15715470
Histone deacetylase inhibitors profoundly decrease proliferation of human lymphoid cancer cell lines.	2005 Jan	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 Jan	15583844
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.	2005 Jan 17	15603949
Effect of inhibitors of histone deacetylase on the induction of cell differentiation in murine and human erythroleukemia cell lines.	2005 Jul	15930892
Design and synthesis of non-hydroxamate histone deacetylase inhibitors: identification of a selective histone acetylating agent.	2005 Jul 1	15927839
The histone-deacetylase inhibitor SAHA potentiates proapoptotic effects of 5-fluorouracil and irinotecan in hepatoma cells.	2005 Jun	15754201
Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer.	2005 Jun 10	15897550
Drug insight: Histone deacetylase inhibitors--development of the new targeted anticancer agent suberoylanilide hydroxamic acid.	2005 Mar	16264908
4-Hydroxybenzoyl derivative from the aqueous extract of the hydroid Campanularia sp.	2005 Mar	15787459
Histone deacetylase inhibitors interact synergistically with tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) to induce apoptosis in carcinoma cell lines.	2005 Mar	15744585
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 Mar 1	15713371
[Histone deacetylase inhibitors as a new generation of anti-cancer agents].	2005 Mar 11	15928589
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 Mar 15	15781658
Suberoylanilide hydroxamic acid (SAHA) has potent anti-glioma properties in vitro, ex vivo and in vivo.	2005 May	15857402
Modulation of radiation response by histone deacetylase inhibition.	2005 May 1	15850925
The role of histone acetylation in SMN gene expression.	2005 May 1	15772088
Novel histone deacetylase inhibitors in the treatment of thyroid cancer.	2005 May 15	15897598
Suberoylanilide hydroxamic acid enhances gap junctional intercellular communication via acetylation of histone containing connexin 43 gene locus.	2005 Nov 1	16266998
Activity of suberoylanilide hydroxamic Acid against human breast cancer cells with amplification of her-2.	2005 Sep 1	16144943
Histone deacetylase inhibitors suppress the induction of c-Jun and its target genes including COX-2.	2005 Sep 23	15994313
Histone deacetylase inhibitors reduce VEGF production and induce growth suppression and apoptosis in human mantle cell lymphoma.	2006 Jan	16343270
SAHA, a HDAC inhibitor, has profound anti-growth activity against non-small cell lung cancer cells.	2006 Jan	16328054
Clinical experience with intravenous and oral formulations of the novel histone deacetylase inhibitor suberoylanilide hydroxamic acid in patients with advanced hematologic malignancies.	2006 Jan 1	16330674
Suberoylanilide hydroxamic acid potentiates apoptosis, inhibits invasion, and abolishes osteoclastogenesis by suppressing nuclear factor-kappaB activation.	2006 Mar 3	16377638
Carbonyl- and sulfur-containing analogs of suberoylanilide hydroxamic acid: Potent inhibition of histone deacetylases.	2006 May 15	16434199

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 `Thu Jul 06 21:20:17 UTC 2023` Edited by `admin` on `Thu Jul 06 21:20:17 UTC 2023`
Record UNII	58IFB293JI
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

VORINOSTAT

Official Name

English

VORINOSTAT [MI]

Common Name

English

NSC-759852

Code

English

VORINOSTAT [ORANGE BOOK]

Common Name

English

NSC-701852

Code

English

N-HYDROXY-N'-PHENYLOCTANEDIAMIDE

Systematic Name

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