DGIdb - VORINOSTAT Drug Record

VORINOSTAT chembl:CHEMBL98 ApprovedAntineoplasticImmunotherapy

Alternate Names:

MK0683
VORINOSTAT
MK-0683
ZOLINZA
OCTANEDIOIC ACID HYDROXYAMIDE PHENYLAMIDE
SHH
SUBEROYLANILIDE HYDROXAMIC ACID
SAHA
SUBERANILOHYDROXAMIC ACID
pubchem.compound:5311
chembl:CHEMBL98
chemidplus:149647-78-9
drugbank:02546
rxcui:194337

Drug Info:

Drug Categories	therapeutic uses
Drug Categories	qtc-prolonging agents (indeterminate risk and risk modifying)
Drug Categories	pharmacologic actions
Drug Categories	organic chemicals
Drug Categories	myelosuppressive agents
Drug Categories	molecular mechanisms of pharmacological action
Drug Categories	hyperglycemia-associated agents
Drug Categories	hydroxylamines
Drug Categories	hydroxy acids
Drug Categories	histone deacetylase inhibitors
Drug Categories	fluorine radioisotopes
Drug Categories	enzyme inhibitors
Drug Categories	chemical actions and uses
Drug Categories	carboxylic acids
Drug Categories	antineoplastic and immunomodulating agents
Drug Categories	antineoplastic agents
Drug Categories	amines
Drug Groups	investigational
Drug Groups	approved
Drug Type	small molecule
Year of Approval	2006
Drug Class	antineoplastic agents
FDA Approval	Cutaneous T-cell lymphoma
Drug Class	Small molecule inhibitor
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent
Drug Categories	qtc prolonging agents
Drug Categories	potential qtc-prolonging agents
Drug Categories	narrow therapeutic index drugs
Drug Categories	immunosuppressive agents
Drug Categories	hydroxamic acids
Drug Categories	aniline compounds
Drug Categories	anilides
Drug Categories	amides

(12 More Sources)

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett
Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol
Yang W et al., 2015, Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors., Bioorg Med Chem
Daniel KB et al., 2015, Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release., J Med Chem
Neelarapu R et al., 2011, Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes., J Med Chem
Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
Dallavalle S et al., 2009, Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors., Eur J Med Chem
Guerrant W et al., 2012, Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors., J Med Chem
Grolla AA et al., 2009, Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases., J Med Chem
Pérez-Balado C et al., 2007, Bispyridinium dienes: histone deacetylase inhibitors with selective activities., J Med Chem
Li X et al., 2014, Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity., J Med Chem
Olson DE et al., 2013, Discovery of the first histone deacetylase 6/8 dual inhibitors., J Med Chem
Xu et al., 2007, Histone deacetylase inhibitors: molecular mechanisms of action., Oncogene
Day JA et al., 2013, Investigating the selectivity of metalloenzyme inhibitors., J Med Chem
Dalgard et al., 2008, Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma., Clin. Cancer Res.
Rushlow et al., 2013, Characterisation of retinoblastomas without RB1 mutations: genomic, gene expression, and clinical studies., Lancet Oncol.
Landreville et al., 2012, Histone deacetylase inhibitors induce growth arrest and differentiation in uveal melanoma., Clin. Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Mai A et al., 2008, Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities., Bioorg Med Chem Lett
He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov
Lee HY et al., 2014, Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells., J Med Chem
Kemp MM et al., 2011, A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold., Bioorg Med Chem Lett
Moffat D et al., 2010, Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor., J Med Chem
Sodji QH et al., 2013, Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors., J Med Chem
Yao Y et al., 2015, Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities., J Med Chem
Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget
Kerl et al., 2013, The histone deacetylase inhibitor SAHA acts in synergism with fenretinide and doxorubicin to control growth of rhabdoid tumor cells., BMC Cancer
Fu et al., 2015, Phase I study of pazopanib and vorinostat: a therapeutic approach for inhibiting mutant p53-mediated angiogenesis and facilitating mutant p53 degradation., Ann. Oncol.
Alexandrova et al., 2015, Improving survival by exploiting tumour dependence on stabilized mutant p53 for treatment., Nature
New et al., 2016, TLR Adaptor Protein MYD88 Mediates Sensitivity to HDAC Inhibitors via a Cytokine-Dependent Mechanism., Cancer Res.
Xu et al., 2005, The histone deacetylase inhibitor suberoylanilide hydroxamic acid down-regulates expression levels of Bcr-abl, c-Myc and HDAC3 in chronic myeloid leukemia cell lines., Int. J. Mol. Med.
Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
Geeleher P et al., 2015, Predicting Response to Histone Deacetylase Inhibitors Using High-Throughput Genomics., J Natl Cancer Inst
Vlietstra et al., 1998, Frequent inactivation of PTEN in prostate cancer cell lines and xenografts., Cancer Res.
Qian et al., 2012, Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling., Clin. Cancer Res.
Garcia et al., 2016, Selective Toxicity of Investigational Ixazomib for Human Leukemia Cells Expressing Mutant Cytoplasmic NPM1: Role of Reactive Oxygen Species., Clin. Cancer Res.
Kulp et al., 2006, Antitumor effects of a novel phenylbutyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer., Clin. Cancer Res.
Kim GH et al., 2019, IDH1<sup>R132H</sup> Causes Resistance to HDAC Inhibitors by Increasing NANOG in Glioblastoma Cells., Int J Mol Sci

VORINOSTAT HDAC8

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Yang W et al., 2015, Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors., Bioorg Med Chem

VORINOSTAT HDAC3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Pérez-Balado C et al., 2007, Bispyridinium dienes: histone deacetylase inhibitors with selective activities., J Med Chem

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

VORINOSTAT HDAC7

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Yang W et al., 2015, Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors., Bioorg Med Chem

VORINOSTAT HDAC2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Yang W et al., 2015, Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors., Bioorg Med Chem

VORINOSTAT HDAC11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Yang W et al., 2015, Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors., Bioorg Med Chem

VORINOSTAT HDAC1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Xu et al., 2007, Histone deacetylase inhibitors: molecular mechanisms of action., Oncogene

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

VORINOSTAT HDAC10

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Neelarapu R et al., 2011, Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes., J Med Chem

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Dallavalle S et al., 2009, Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors., Eur J Med Chem

VORINOSTAT HDAC9

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? False

Endogenous Drug? False

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Yang W et al., 2015, Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors., Bioorg Med Chem

VORINOSTAT HDAC4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Publications:

Mai A et al., 2008, Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities., Bioorg Med Chem Lett

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

VORINOSTAT HDAC6

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Merck

Novel drug target Established target

Mechanism of Interaction Histone deacetylase 6 inhibitor

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Lee HY et al., 2014, Azaindolylsulfonamides, with a more selective inhibitory effect on histone deacetylase 6 activity, exhibit antitumor activity in colorectal cancer HCT116 cells., J Med Chem

VORINOSTAT HDAC5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Yang W et al., 2015, Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors., Bioorg Med Chem

VORINOSTAT RB1

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type retinoblastoma

Response Type sensitive

Approval Status Preclinical - Cell culture

Publications:

Dalgard et al., 2008, Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma., Clin. Cancer Res.

Rushlow et al., 2013, Characterisation of retinoblastomas without RB1 mutations: genomic, gene expression, and clinical studies., Lancet Oncol.

VORINOSTAT FBXW7

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type head and neck squamous cell carcinoma

Response Type sensitive

Approval Status Preclinical

Publications:

He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov
VORINOSTAT EZH2

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Approval Status Preclinical

Publications:

Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget
VORINOSTAT SMARCB1

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fenretinide + Vorinostat

Indication/Tumor Type rhabdoid cancer

Response Type sensitive

Publications:

Kerl et al., 2013, The histone deacetylase inhibitor SAHA acts in synergism with fenretinide and doxorubicin to control growth of rhabdoid tumor cells., BMC Cancer

VORINOSTAT TP53

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pazopanib + Vorinostat

Indication/Tumor Type Advanced Solid Tumor

Response Type decreased response

Publications:

Fu et al., 2015, Phase I study of pazopanib and vorinostat: a therapeutic approach for inhibiting mutant p53-mediated angiogenesis and facilitating mutant p53 degradation., Ann. Oncol.

Alexandrova et al., 2015, Improving survival by exploiting tumour dependence on stabilized mutant p53 for treatment., Nature

VORINOSTAT MYD88

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Approval Status Preclinical - Cell culture

Publications:

New et al., 2016, TLR Adaptor Protein MYD88 Mediates Sensitivity to HDAC Inhibitors via a Cytokine-Dependent Mechanism., Cancer Res.

VORINOSTAT BRAF

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol

VORINOSTAT PTEN

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0941 + vorinostat

Indication/Tumor Type prostate cancer

Response Type sensitive

Publications:

Vlietstra et al., 1998, Frequent inactivation of PTEN in prostate cancer cell lines and xenografts., Cancer Res.

Qian et al., 2012, Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling., Clin. Cancer Res.

VORINOSTAT NPM1

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type sensitive

combination therapy Ixazomib + Vorinostat

Indication/Tumor Type acute myeloid leukemia

Publications:

Garcia et al., 2016, Selective Toxicity of Investigational Ixazomib for Human Leukemia Cells Expressing Mutant Cytoplasmic NPM1: Role of Reactive Oxygen Species., Clin. Cancer Res.
VORINOSTAT IDH1

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type predicted - sensitive

combination therapy AGI-5198 + Vorinostat

Evidence Type Actionable

Publications:

Kim GH et al., 2019, IDH1<sup>R132H</sup> Causes Resistance to HDAC Inhibitors by Increasing NANOG in Glioblastoma Cells., Int J Mol Sci
VORINOSTAT GNA11

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family HDAC inhibitor

Alteration GNA11:Q209L,Q209P

Publications:
VORINOSTAT TUBA3D

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBB3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBB

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT BAP1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Landreville et al., 2012, Histone deacetylase inhibitors induce growth arrest and differentiation in uveal melanoma., Clin. Cancer Res.
VORINOSTAT TUBA1B

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBB1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBA3E

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBA1C

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT ACE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Day JA et al., 2013, Investigating the selectivity of metalloenzyme inhibitors., J Med Chem

VORINOSTAT MYC

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Xu et al., 2005, The histone deacetylase inhibitor suberoylanilide hydroxamic acid down-regulates expression levels of Bcr-abl, c-Myc and HDAC3 in chronic myeloid leukemia cell lines., Int. J. Mol. Med.

VORINOSTAT TUBB8

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBA4A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT CHD4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Geeleher P et al., 2015, Predicting Response to Histone Deacetylase Inhibitors Using High-Throughput Genomics., J Natl Cancer Inst
VORINOSTAT TUBB2B

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBB4A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBB4B

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT BIRC5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kulp et al., 2006, Antitumor effects of a novel phenylbutyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer., Clin. Cancer Res.
VORINOSTAT TUBB6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT TUBB2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT CFTR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol
VORINOSTAT TUBA3C

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
VORINOSTAT NFE2L2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
VORINOSTAT GMNN

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
VORINOSTAT NR0B1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
VORINOSTAT PAX8

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

DrugBank: DB02546
- Version: 5.1.7
Alternate Names:

VORINOSTAT DrugBank Drug Name

149647-78-9 CAS Number

Zolinza Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Xu et al., 2007, Histone deacetylase inhibitors: molecular mechanisms of action., Oncogene

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
TEND: VORINOSTAT
- Version: 01-August-2011
Alternate Names:

VORINOSTAT Primary Drug Name

Drug Info:

Drug Class antineoplastic agents

Year of Approval 2006

Publications:
MyCancerGenome: VORINOSTAT
- Version: 20-Jun-2017
Alternate Names:

ZOLINZA Trade Name

Drug Info:

Drug Class Small molecule inhibitor

FDA Approval Cutaneous T-cell lymphoma

Publications:
TdgClinicalTrial: VORINOSTAT
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

DTC: VORINOSTAT

Version: 02-September-2020

Alternate Names:

CHEMBL98 ChEMBL Drug ID

Drug Info:

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Grolla AA et al., 2009, Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases., J Med Chem

Guerrant W et al., 2012, Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors., J Med Chem

NCI: SAHA

Version: 14-September-2017

Alternate Names:

C1796 NCI drug code

Drug Info:

Publications:

Xu et al., 2005, The histone deacetylase inhibitor suberoylanilide hydroxamic acid down-regulates expression levels of Bcr-abl, c-Myc and HDAC3 in chronic myeloid leukemia cell lines., Int. J. Mol. Med.

Kulp et al., 2006, Antitumor effects of a novel phenylbutyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer., Clin. Cancer Res.

PharmGKB: vorinostat
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Geeleher P et al., 2015, Predicting Response to Histone Deacetylase Inhibitors Using High-Throughput Genomics., J Natl Cancer Inst

JAX-CKB: Vorinostat

Version: 15-September-2020

Alternate Names:

Drug Info:

Publications:

Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol

He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov

Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget

GuideToPharmacologyInteractions: 178103458
- Version: 20-July-2020
Alternate Names:

VORINOSTAT GuideToPharmacology Ligand Name

Drug Info:

Publications:
TALC: VORINOSTAT
- Version: 12-May-2016
Alternate Names:

VORINOSTAT Primary Drug Name

VORINOSTAT Drug Generic Name

ZOLINZA Drug Trade Name

Drug Info:

Publications:
TTD: Vorinostat
- Version: 2020.06.01
Alternate Names:

D0E7PQ TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL98
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: VORINOSTAT
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL98
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: VORINOSTAT
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
CGI: Vorinostat
- Version: 14-September-2020
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

Notes
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	Merck
Novel drug target	Established target
Mechanism of Interaction	Histone deacetylase 6 inhibitor

Indication/Tumor Type	retinoblastoma
Response Type	sensitive
Approval Status	Preclinical - Cell culture

Indication/Tumor Type	head and neck squamous cell carcinoma
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	diffuse large B-cell lymphoma
Response Type	sensitive
Approval Status	Preclinical

combination therapy	Fenretinide + Vorinostat
Indication/Tumor Type	rhabdoid cancer
Response Type	sensitive

combination therapy	Pazopanib + Vorinostat
Indication/Tumor Type	Advanced Solid Tumor
Response Type	decreased response

Evidence Type	Actionable
Approval Status	Preclinical - Cell line xenograft
Response Type	sensitive

combination therapy	GDC-0941 + vorinostat
Indication/Tumor Type	prostate cancer
Response Type	sensitive

Response Type	predicted - sensitive
combination therapy	AGI-5198 + Vorinostat
Evidence Type	Actionable

VORINOSTAT	DrugBank Drug Name
149647-78-9	CAS Number
Zolinza	Drug Brand

VORINOSTAT	Primary Drug Name
VORINOSTAT	Drug Generic Name
ZOLINZA	Drug Trade Name

VORINOSTAT Drug Record

VORINOSTAT chembl:CHEMBL98 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

Publications: Xu et al., 2007, Histone deacetylase inhibitors: molecular mechanisms of action., Oncogene Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res. Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Direct Interaction? False Endogenous Drug? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Merck Novel drug target Established target Mechanism of Interaction Histone deacetylase 6 inhibitor

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type retinoblastoma Response Type sensitive Approval Status Preclinical - Cell culture

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type head and neck squamous cell carcinoma Response Type sensitive Approval Status Preclinical

Publications: He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type diffuse large B-cell lymphoma Response Type sensitive Approval Status Preclinical

Publications: Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Fenretinide + Vorinostat Indication/Tumor Type rhabdoid cancer Response Type sensitive

Publications: Kerl et al., 2013, The histone deacetylase inhibitor SAHA acts in synergism with fenretinide and doxorubicin to control growth of rhabdoid tumor cells., BMC Cancer

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Pazopanib + Vorinostat Indication/Tumor Type Advanced Solid Tumor Response Type decreased response

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type diffuse large B-cell lymphoma Response Type sensitive Approval Status Preclinical - Cell culture

Publications: New et al., 2016, TLR Adaptor Protein MYD88 Mediates Sensitivity to HDAC Inhibitors via a Cytokine-Dependent Mechanism., Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell line xenograft Response Type sensitive

Publications: Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol

Interaction Types & Directionality: n/a

Interaction Info: combination therapy GDC-0941 + vorinostat Indication/Tumor Type prostate cancer Response Type sensitive

Interaction Types & Directionality: n/a

Interaction Info: Response Type sensitive combination therapy Ixazomib + Vorinostat Indication/Tumor Type acute myeloid leukemia

Publications: Garcia et al., 2016, Selective Toxicity of Investigational Ixazomib for Human Leukemia Cells Expressing Mutant Cytoplasmic NPM1: Role of Reactive Oxygen Species., Clin. Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info: Response Type predicted - sensitive combination therapy AGI-5198 + Vorinostat Evidence Type Actionable

Publications: Kim GH et al., 2019, IDH1<sup>R132H</sup> Causes Resistance to HDAC Inhibitors by Increasing NANOG in Glioblastoma Cells., Int J Mol Sci

Interaction Types & Directionality: n/a

Interaction Info: Drug family HDAC inhibitor Alteration GNA11:Q209L,Q209P

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Landreville et al., 2012, Histone deacetylase inhibitors induce growth arrest and differentiation in uveal melanoma., Clin. Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality: n/a

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Xu et al., 2007, Histone deacetylase inhibitors: molecular mechanisms of action., Oncogene

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? False

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Merck

Novel drug target Established target

Mechanism of Interaction Histone deacetylase 6 inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type retinoblastoma

Response Type sensitive

Approval Status Preclinical - Cell culture

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type head and neck squamous cell carcinoma

Response Type sensitive

Approval Status Preclinical

Publications:

He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Approval Status Preclinical

Publications:

Johnson et al., 2015, HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphoma., Oncotarget

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Fenretinide + Vorinostat

Indication/Tumor Type rhabdoid cancer

Response Type sensitive

Publications:

Kerl et al., 2013, The histone deacetylase inhibitor SAHA acts in synergism with fenretinide and doxorubicin to control growth of rhabdoid tumor cells., BMC Cancer

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Pazopanib + Vorinostat

Indication/Tumor Type Advanced Solid Tumor

Response Type decreased response

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type diffuse large B-cell lymphoma

Response Type sensitive

Approval Status Preclinical - Cell culture

Publications:

New et al., 2016, TLR Adaptor Protein MYD88 Mediates Sensitivity to HDAC Inhibitors via a Cytokine-Dependent Mechanism., Cancer Res.

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell line xenograft

Response Type sensitive

Publications:

Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0941 + vorinostat

Indication/Tumor Type prostate cancer

Response Type sensitive

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type sensitive

combination therapy Ixazomib + Vorinostat

Indication/Tumor Type acute myeloid leukemia

Publications:

Garcia et al., 2016, Selective Toxicity of Investigational Ixazomib for Human Leukemia Cells Expressing Mutant Cytoplasmic NPM1: Role of Reactive Oxygen Species., Clin. Cancer Res.

Interaction Types & Directionality:

n/a

Interaction Info:

Response Type predicted - sensitive

combination therapy AGI-5198 + Vorinostat

Evidence Type Actionable

Publications:

Kim GH et al., 2019, IDH1<sup>R132H</sup> Causes Resistance to HDAC Inhibitors by Increasing NANOG in Glioblastoma Cells., Int J Mol Sci

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family HDAC inhibitor

Alteration GNA11:Q209L,Q209P

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Landreville et al., 2012, Histone deacetylase inhibitors induce growth arrest and differentiation in uveal melanoma., Clin. Cancer Res.

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Day JA et al., 2013, Investigating the selectivity of metalloenzyme inhibitors., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Xu et al., 2005, The histone deacetylase inhibitor suberoylanilide hydroxamic acid down-regulates expression levels of Bcr-abl, c-Myc and HDAC3 in chronic myeloid leukemia cell lines., Int. J. Mol. Med.

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Geeleher P et al., 2015, Predicting Response to Histone Deacetylase Inhibitors Using High-Throughput Genomics., J Natl Cancer Inst

Interaction Types & Directionality:

n/a

Publications:

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem