Page last updated: 2024-12-11

romidepsin

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Description

depsipeptide : A natural or synthetic compound having a sequence of amino and hydroxy carboxylic acid residues (usually alpha-amino and alpha-hydroxy acids), commonly but not necessarily regularly alternating. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5352062
CHEMBL ID343448
CHEBI ID61080
SCHEMBL ID677497
MeSH IDM0519758

Synonyms (81)

Synonym
AB01273968-01
romidepsinum
(1s,4s,7z,10s,16e,21r)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
romidepsine
romidepsina
oxa-12,8,20,23-tetrazabicyclo[8.7.6]tricosane, cyclic peptide deriv.
l-valine,3-didehydro-2-aminobutanoyl-,.xi.-lactone, cyclic (1.fwdarw.2)-disulfide
NSC630176 ,
(e)-(1s,10s,21r)-7-[(z)-ethylidene]-4,21-diisopropyl-2- oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
depsipeptide
nsc-630176
fk228
antibiotic fr 901228
fr 901228
fk-228
istodax
fk-901228
fr-901228
HDINHIB_000006 ,
romidepsin (jan/usan/inn)
istodax (tn)
D06637
PROBES1_000153
PROBES2_000337
l-valine, n-(3-hydroxy-7-mercapto-1-oxo-4-heptenyl)-d-valyl-d-cysteinyl-(z)-2,3-didehydro-2-aminobutanoyl-, xi-lactone, cyclic (1-2)-disulfide, (s-(e))-
(1s,4s,7z,10s,16e,21r)-7-ethylidene-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo(8.7.6)tricos-16-ene-3,6,9,19,22-pentone
nsc 630176
fk 228
c24h36n4o6s2
l-valine, n-((3s,4e)-3-hydroxy-7-mercapto-1-oxo-4-heptenyl)-d-valyl-d-cysteinyl-(2z)-2-amino-2-butenoxyl-, (4-1)-lactone, cyclic (1-2)-disulfide
chromadax
fr901228
bdbm19151
(1s,4s,7z,10s,16e,21r)-7-ethylidene-4,21-bis(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
chembl343448 ,
chebi:61080 ,
(1s,4s,7z,10s,16e,21r)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
api0005301
nsc-754143
(e)-(1s,10s,21r)-7-[(z)-ethylidene]-4,21-diisopropyl-2- oxa-12,13-dithia-5,8,20,23- tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
l-valine,3-didehydro-2- aminobutanoyl-,.xi.-lactone, cyclic (1.fwdarw.2)-disulfide
nsc754143
dtxcid8028505
cyclo((2z)-2-amino-2-butenoyl-l-valyl-(3s,4e)-3-hydroxy-7-mercapto-4-heptenoyl-d-valyl-d-cysteinyl), cyclic (3->5)-disulfide
unii-cx3t89xqbk
cx3t89xqbk ,
HY-15149
CS-0985
romidepsin [who-dd]
romidepsin [orange book]
romidepsin [mi]
romidepsin [mart.]
romidepsin [usan]
romidepsin [jan]
depsipeptide [who-dd]
romidepsin [vandf]
cyclo((2z)-2-amino-2-butenoyl-l-valyl-(3s,4e)-3-hydroxy-7-mercapto-4-heptenoyl-d-valyl-d-cysteinyl), cyclic (3->5)-disulphide
(1s,4s,7z,10s,16e,21r)-7-ethylidene-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
romidepsin [inn]
S3020
gtpl7006
SCHEMBL677497
cyclo[(2z)-2-amino-2-butenoyl-l-valyl-(3s,4e)-3-hydroxy-7-mercapto-4-heptenoyl-d-valyl-d-cysteinyl], cyclic (3-5) disulfide
HB1386
cyclo[(2z)-2-amino-2-butenoyl-l-val yl-(3s,4e)-3-hydroxy-7-mercapto-4-heptenoyl-d-valy l-d-cysteinyl], cyclic (3-5) disulfide
DB06176
SR-01000941579-1
sr-01000941579
romidepsin, >=98% (hplc)
mfcd18433404
(1s,4s,7z,10s,16e,21r)-7- ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23- tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
(1s,4s,7z,10s,16e,21r)-7-ethylidene-4,21-bis(1methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16ene-3,6,9,19,22-pentone
romidepsin (fk228 ,depsipeptide)
Q7363205
romidepsin; fk-228
EN300-22844947
romidepsin (fk228)
(1s,4s,10s,16e,21r)-7-((2z)-ethylidene)-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo(8.7.6)tricos-16-ene-3,6,9,19,22-pentone
l01xx39
(1s,4s,7z,10s,16e,21r)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo(8.7.6)tricos-16-ene-3,6,9,19,22-pentone
romidepsin (mart.)

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
EC 3.5.1.98 (histone deacetylase) inhibitorAn EC 3.5.1.* (non-peptide linear amide C-N hydrolase) inhibitor that interferes with the function of histone deacetylase (EC 3.5.1.98).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
cyclodepsipeptideA depsipeptide in which the amino and hydroxy carboxylic acid residues are connected in a ring.
organic disulfideCompounds of structure RSSR in which R and R' are organic groups.
heterocyclic antibiotic
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 3Homo sapiens (human)IC50 (µMol)0.05890.00040.619610.0000AID1188979; AID1250642; AID1275076; AID303347; AID331898; AID331899; AID620939; AID620945; AID620946; AID620947; AID673992; AID721448
Histone deacetylase 3Homo sapiens (human)Ki0.00840.00020.42378.1900AID331899; AID496803; AID765391
Bromodomain-containing protein 4Homo sapiens (human)IC50 (µMol)0.03600.00040.40329.0500AID1462230
Nuclear receptor corepressor 1Homo sapiens (human)Ki0.00020.00020.01240.0250AID765391
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)0.01800.00040.908610.0000AID620939
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.03900.00031.38338.4000AID620946
Histone deacetylase 4Homo sapiens (human)IC50 (µMol)6.47480.00061.052610.0000AID1119930; AID1188980; AID1250644; AID1275076; AID303347; AID331898; AID620940; AID695594; AID721448; AID90698; AID90700
Histone deacetylase 4Homo sapiens (human)Ki0.02050.00021.62559.1242AID496804; AID765389
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.02000.00010.54948.4000AID620945
Histone deacetylase 1Homo sapiens (human)IC50 (µMol)0.44890.00010.55439.9000AID1077074; AID1119929; AID1182191; AID1188977; AID1250640; AID1254047; AID1275076; AID1275077; AID1797826; AID303347; AID303348; AID331898; AID620937; AID673990; AID695592; AID695593; AID721448; AID721452; AID90669; AID90670
Histone deacetylase 1Homo sapiens (human)Ki0.00000.00000.49888.1900AID496801; AID765393
Histone deacetylase 7Homo sapiens (human)IC50 (µMol)10.06260.00071.02609.9000AID1250646; AID1275076; AID303347; AID331898; AID620942; AID721448
Histone deacetylase 7Homo sapiens (human)Ki1.25000.00022.00059.5000AID496807; AID765387
Histone deacetylase 2Homo sapiens (human)IC50 (µMol)0.88830.00010.72219.9700AID1188978; AID1250641; AID1275076; AID303347; AID331898; AID620938; AID673991; AID721448; AID90686
Histone deacetylase 2Homo sapiens (human)Ki0.00000.00000.47098.1900AID496802; AID765392
Polyamine deacetylase HDAC10Homo sapiens (human)IC50 (µMol)0.06460.00050.72459.9000AID1188985; AID1250649; AID1275076; AID303347; AID331898; AID721448
Histone deacetylase 11 Homo sapiens (human)IC50 (µMol)1.72930.00030.92989.9000AID1188986; AID1250650; AID1275076; AID303347; AID331898; AID721448
Histone deacetylase 8Homo sapiens (human)IC50 (µMol)8.63080.00070.99479.9000AID1250643; AID1254049; AID1275076; AID303347; AID331898; AID620943; AID721448
Histone deacetylase 8Homo sapiens (human)Ki0.00020.00020.75258.1900AID496808; AID765390
Histone deacetylase 6Homo sapiens (human)IC50 (µMol)35.45530.00000.53769.9000AID1119931; AID1250648; AID1254048; AID1275076; AID1275078; AID303347; AID303349; AID331898; AID331900; AID620941; AID673993; AID695596; AID695597; AID721448; AID90704
Histone deacetylase 6Homo sapiens (human)Ki0.10650.00010.41568.1900AID331900; AID496806; AID765385
Histone deacetylase 9Homo sapiens (human)IC50 (µMol)10.06260.00050.94139.9000AID1250647; AID1275076; AID303347; AID331898; AID620944; AID721448
Histone deacetylase 9Homo sapiens (human)Ki1.10000.00021.85209.0000AID496809; AID765386
Histone deacetylase 5Homo sapiens (human)IC50 (µMol)2.07520.00070.961010.0000AID1250645; AID1275076; AID303347; AID331898; AID721448
Histone deacetylase 5Homo sapiens (human)Ki0.55000.00021.29939.5000AID496805; AID765388
Nuclear receptor corepressor 2Homo sapiens (human)IC50 (µMol)1.05850.00170.59528.0000AID331899; AID620937; AID620938; AID620939; AID620945; AID620946; AID620947; AID673992
Nuclear receptor corepressor 2Homo sapiens (human)Ki0.02490.00030.33253.2000AID331899
Histone deacetylase 6Mus musculus (house mouse)IC50 (µMol)0.31430.00060.20660.7870AID1077073; AID1182193; AID1797826; AID721451
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 1Homo sapiens (human)EC50 (µMol)36.00000.03001.98776.7000AID90679
Histone deacetylase 6Homo sapiens (human)EC50 (µMol)14,000.00000.00521.59986.7000AID90836
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 3Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 4Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 1Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 7Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 2Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Polyamine deacetylase HDAC10Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 11 Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 8Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 6Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 9Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
Histone deacetylase 5Homo sapiens (human)INH0.02440.02440.24340.5720AID603218
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (199)

Processvia Protein(s)Taxonomy
negative regulation of myotube differentiationHistone deacetylase 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
establishment of mitotic spindle orientationHistone deacetylase 3Homo sapiens (human)
in utero embryonic developmentHistone deacetylase 3Homo sapiens (human)
positive regulation of protein phosphorylationHistone deacetylase 3Homo sapiens (human)
chromatin organizationHistone deacetylase 3Homo sapiens (human)
transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
protein deacetylationHistone deacetylase 3Homo sapiens (human)
regulation of mitotic cell cycleHistone deacetylase 3Homo sapiens (human)
positive regulation of protein ubiquitinationHistone deacetylase 3Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 3Homo sapiens (human)
positive regulation of TOR signalingHistone deacetylase 3Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of multicellular organism growthHistone deacetylase 3Homo sapiens (human)
positive regulation of protein import into nucleusHistone deacetylase 3Homo sapiens (human)
regulation of circadian rhythmHistone deacetylase 3Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
negative regulation of JNK cascadeHistone deacetylase 3Homo sapiens (human)
spindle assemblyHistone deacetylase 3Homo sapiens (human)
establishment of skin barrierHistone deacetylase 3Homo sapiens (human)
cellular response to fluid shear stressHistone deacetylase 3Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone deacetylase 3Homo sapiens (human)
DNA repair-dependent chromatin remodelingHistone deacetylase 3Homo sapiens (human)
cornified envelope assemblyHistone deacetylase 3Homo sapiens (human)
negative regulation of cardiac muscle cell differentiationHistone deacetylase 3Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
chromatin organizationBromodomain-containing protein 4Homo sapiens (human)
DNA damage responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
regulation of inflammatory responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of T-helper 17 cell lineage commitmentBromodomain-containing protein 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor corepressor 1Homo sapiens (human)
chromatin organizationNuclear receptor corepressor 1Homo sapiens (human)
locomotor rhythmNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of glycolytic processNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of fatty acid metabolic processNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of JNK cascadeNuclear receptor corepressor 1Homo sapiens (human)
spindle assemblyNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of miRNA transcriptionNuclear receptor corepressor 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
chromatin remodelingHistone deacetylase 4Homo sapiens (human)
protein deacetylationHistone deacetylase 4Homo sapiens (human)
inflammatory responseHistone deacetylase 4Homo sapiens (human)
nervous system developmentHistone deacetylase 4Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 4Homo sapiens (human)
response to denervation involved in regulation of muscle adaptationHistone deacetylase 4Homo sapiens (human)
cardiac muscle hypertrophy in response to stressHistone deacetylase 4Homo sapiens (human)
protein sumoylationHistone deacetylase 4Homo sapiens (human)
B cell differentiationHistone deacetylase 4Homo sapiens (human)
positive regulation of protein sumoylationHistone deacetylase 4Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 4Homo sapiens (human)
B cell activationHistone deacetylase 4Homo sapiens (human)
regulation of protein bindingHistone deacetylase 4Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 4Homo sapiens (human)
negative regulation of glycolytic processHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
type I interferon-mediated signaling pathwayHistone deacetylase 4Homo sapiens (human)
response to interleukin-1Histone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 7Homo sapiens (human)
vasculogenesisHistone deacetylase 7Homo sapiens (human)
chromatin remodelingHistone deacetylase 7Homo sapiens (human)
protein deacetylationHistone deacetylase 7Homo sapiens (human)
cell-cell junction assemblyHistone deacetylase 7Homo sapiens (human)
protein sumoylationHistone deacetylase 7Homo sapiens (human)
negative regulation of interleukin-2 productionHistone deacetylase 7Homo sapiens (human)
negative regulation of osteoblast differentiationHistone deacetylase 7Homo sapiens (human)
regulation of mRNA processingHistone deacetylase 7Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 7Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionHistone deacetylase 7Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
response to amphetamineHistone deacetylase 2Homo sapiens (human)
cardiac muscle hypertrophyHistone deacetylase 2Homo sapiens (human)
chromatin remodelingHistone deacetylase 2Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 2Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 2Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 2Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 2Homo sapiens (human)
negative regulation of neuron projection developmentHistone deacetylase 2Homo sapiens (human)
dendrite developmentHistone deacetylase 2Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 2Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 2Homo sapiens (human)
response to caffeineHistone deacetylase 2Homo sapiens (human)
heterochromatin formationHistone deacetylase 2Homo sapiens (human)
response to lipopolysaccharideHistone deacetylase 2Homo sapiens (human)
positive regulation of interleukin-1 productionHistone deacetylase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionHistone deacetylase 2Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 2Homo sapiens (human)
positive regulation of collagen biosynthetic processHistone deacetylase 2Homo sapiens (human)
cellular response to heatHistone deacetylase 2Homo sapiens (human)
response to nicotineHistone deacetylase 2Homo sapiens (human)
protein modification processHistone deacetylase 2Homo sapiens (human)
response to cocaineHistone deacetylase 2Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinHistone deacetylase 2Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 2Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 2Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of MHC class II biosynthetic processHistone deacetylase 2Homo sapiens (human)
positive regulation of proteolysisHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
behavioral response to ethanolHistone deacetylase 2Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 2Homo sapiens (human)
response to hyperoxiaHistone deacetylase 2Homo sapiens (human)
hair follicle placode formationHistone deacetylase 2Homo sapiens (human)
negative regulation of dendritic spine developmentHistone deacetylase 2Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 2Homo sapiens (human)
fungiform papilla formationHistone deacetylase 2Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 2Homo sapiens (human)
cellular response to retinoic acidHistone deacetylase 2Homo sapiens (human)
cellular response to transforming growth factor beta stimulusHistone deacetylase 2Homo sapiens (human)
positive regulation of male mating behaviorHistone deacetylase 2Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
cellular response to dopamineHistone deacetylase 2Homo sapiens (human)
response to amyloid-betaHistone deacetylase 2Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 2Homo sapiens (human)
negative regulation of peptidyl-lysine acetylationHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolyamine deacetylase HDAC10Homo sapiens (human)
DNA repairPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationPolyamine deacetylase HDAC10Homo sapiens (human)
regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
macroautophagyPolyamine deacetylase HDAC10Homo sapiens (human)
positive regulation of mismatch repairPolyamine deacetylase HDAC10Homo sapiens (human)
homologous recombinationPolyamine deacetylase HDAC10Homo sapiens (human)
negative regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
polyamine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
spermidine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
epigenetic regulation of gene expressionPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationHistone deacetylase 11 Homo sapiens (human)
oligodendrocyte developmentHistone deacetylase 11 Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 11 Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 8Homo sapiens (human)
chromatin organizationHistone deacetylase 8Homo sapiens (human)
mitotic sister chromatid cohesionHistone deacetylase 8Homo sapiens (human)
negative regulation of protein ubiquitinationHistone deacetylase 8Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 8Homo sapiens (human)
regulation of telomere maintenanceHistone deacetylase 8Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 8Homo sapiens (human)
polyamine deacetylationHistone deacetylase 6Homo sapiens (human)
spermidine deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 6Homo sapiens (human)
protein polyubiquitinationHistone deacetylase 6Homo sapiens (human)
response to amphetamineHistone deacetylase 6Homo sapiens (human)
protein deacetylationHistone deacetylase 6Homo sapiens (human)
protein quality control for misfolded or incompletely synthesized proteinsHistone deacetylase 6Homo sapiens (human)
intracellular protein transportHistone deacetylase 6Homo sapiens (human)
autophagyHistone deacetylase 6Homo sapiens (human)
actin filament organizationHistone deacetylase 6Homo sapiens (human)
negative regulation of microtubule depolymerizationHistone deacetylase 6Homo sapiens (human)
regulation of autophagyHistone deacetylase 6Homo sapiens (human)
positive regulation of epithelial cell migrationHistone deacetylase 6Homo sapiens (human)
negative regulation of hydrogen peroxide metabolic processHistone deacetylase 6Homo sapiens (human)
regulation of macroautophagyHistone deacetylase 6Homo sapiens (human)
axonal transport of mitochondrionHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex assemblyHistone deacetylase 6Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 6Homo sapiens (human)
protein destabilizationHistone deacetylase 6Homo sapiens (human)
lysosome localizationHistone deacetylase 6Homo sapiens (human)
protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationHistone deacetylase 6Homo sapiens (human)
cellular response to heatHistone deacetylase 6Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 6Homo sapiens (human)
response to immobilization stressHistone deacetylase 6Homo sapiens (human)
cellular response to topologically incorrect proteinHistone deacetylase 6Homo sapiens (human)
erythrocyte enucleationHistone deacetylase 6Homo sapiens (human)
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathwayHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
regulation of fat cell differentiationHistone deacetylase 6Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 6Homo sapiens (human)
negative regulation of proteolysisHistone deacetylase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 6Homo sapiens (human)
collateral sproutingHistone deacetylase 6Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceHistone deacetylase 6Homo sapiens (human)
positive regulation of dendrite morphogenesisHistone deacetylase 6Homo sapiens (human)
negative regulation of oxidoreductase activityHistone deacetylase 6Homo sapiens (human)
response to corticosteroneHistone deacetylase 6Homo sapiens (human)
response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHistone deacetylase 6Homo sapiens (human)
cilium assemblyHistone deacetylase 6Homo sapiens (human)
regulation of microtubule-based movementHistone deacetylase 6Homo sapiens (human)
regulation of androgen receptor signaling pathwayHistone deacetylase 6Homo sapiens (human)
dendritic spine morphogenesisHistone deacetylase 6Homo sapiens (human)
cilium disassemblyHistone deacetylase 6Homo sapiens (human)
parkin-mediated stimulation of mitophagy in response to mitochondrial depolarizationHistone deacetylase 6Homo sapiens (human)
regulation of establishment of protein localizationHistone deacetylase 6Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 6Homo sapiens (human)
aggresome assemblyHistone deacetylase 6Homo sapiens (human)
polyubiquitinated misfolded protein transportHistone deacetylase 6Homo sapiens (human)
response to growth factorHistone deacetylase 6Homo sapiens (human)
cellular response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
cellular response to parathyroid hormone stimulusHistone deacetylase 6Homo sapiens (human)
response to dexamethasoneHistone deacetylase 6Homo sapiens (human)
tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of cellular response to oxidative stressHistone deacetylase 6Homo sapiens (human)
negative regulation of protein acetylationHistone deacetylase 6Homo sapiens (human)
regulation of autophagy of mitochondrionHistone deacetylase 6Homo sapiens (human)
positive regulation of cholangiocyte proliferationHistone deacetylase 6Homo sapiens (human)
negative regulation of aggrephagyHistone deacetylase 6Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of cytokine productionHistone deacetylase 9Homo sapiens (human)
response to amphetamineHistone deacetylase 9Homo sapiens (human)
inflammatory responseHistone deacetylase 9Homo sapiens (human)
heart developmentHistone deacetylase 9Homo sapiens (human)
neuron differentiationHistone deacetylase 9Homo sapiens (human)
B cell differentiationHistone deacetylase 9Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 9Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 9Homo sapiens (human)
B cell activationHistone deacetylase 9Homo sapiens (human)
cholesterol homeostasisHistone deacetylase 9Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 9Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 9Homo sapiens (human)
regulation of skeletal muscle fiber developmentHistone deacetylase 9Homo sapiens (human)
regulation of striated muscle cell differentiationHistone deacetylase 9Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
inflammatory responseHistone deacetylase 5Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 5Homo sapiens (human)
regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
response to activityHistone deacetylase 5Homo sapiens (human)
neuron differentiationHistone deacetylase 5Homo sapiens (human)
B cell differentiationHistone deacetylase 5Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 5Homo sapiens (human)
B cell activationHistone deacetylase 5Homo sapiens (human)
response to cocaineHistone deacetylase 5Homo sapiens (human)
regulation of protein bindingHistone deacetylase 5Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 5Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 5Homo sapiens (human)
cellular response to lipopolysaccharideHistone deacetylase 5Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor corepressor 2Homo sapiens (human)
lactationNuclear receptor corepressor 2Homo sapiens (human)
response to organonitrogen compoundNuclear receptor corepressor 2Homo sapiens (human)
regulation of cellular ketone metabolic processNuclear receptor corepressor 2Homo sapiens (human)
cerebellum developmentNuclear receptor corepressor 2Homo sapiens (human)
response to estradiolNuclear receptor corepressor 2Homo sapiens (human)
estrous cycleNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of miRNA transcriptionNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (71)

Processvia Protein(s)Taxonomy
transcription corepressor bindingHistone deacetylase 3Homo sapiens (human)
chromatin bindingHistone deacetylase 3Homo sapiens (human)
transcription corepressor activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase activityHistone deacetylase 3Homo sapiens (human)
protein bindingHistone deacetylase 3Homo sapiens (human)
enzyme bindingHistone deacetylase 3Homo sapiens (human)
cyclin bindingHistone deacetylase 3Homo sapiens (human)
chromatin DNA bindingHistone deacetylase 3Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 3Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 3Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 3Homo sapiens (human)
protein decrotonylase activityHistone deacetylase 3Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 3Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 3Homo sapiens (human)
transcription cis-regulatory region bindingBromodomain-containing protein 4Homo sapiens (human)
p53 bindingBromodomain-containing protein 4Homo sapiens (human)
chromatin bindingBromodomain-containing protein 4Homo sapiens (human)
transcription coregulator activityBromodomain-containing protein 4Homo sapiens (human)
transcription coactivator activityBromodomain-containing protein 4Homo sapiens (human)
protein bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityBromodomain-containing protein 4Homo sapiens (human)
enzyme bindingBromodomain-containing protein 4Homo sapiens (human)
lysine-acetylated histone bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II C-terminal domain bindingBromodomain-containing protein 4Homo sapiens (human)
P-TEFb complex bindingBromodomain-containing protein 4Homo sapiens (human)
histone reader activityBromodomain-containing protein 4Homo sapiens (human)
transcription cis-regulatory region bindingNuclear receptor corepressor 1Homo sapiens (human)
transcription corepressor activityNuclear receptor corepressor 1Homo sapiens (human)
protein bindingNuclear receptor corepressor 1Homo sapiens (human)
nuclear receptor bindingNuclear receptor corepressor 1Homo sapiens (human)
histone deacetylase bindingNuclear receptor corepressor 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingNuclear receptor corepressor 1Homo sapiens (human)
nuclear thyroid hormone receptor bindingNuclear receptor corepressor 1Homo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 4Homo sapiens (human)
histone bindingHistone deacetylase 4Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase activityHistone deacetylase 4Homo sapiens (human)
protein bindingHistone deacetylase 4Homo sapiens (human)
zinc ion bindingHistone deacetylase 4Homo sapiens (human)
SUMO transferase activityHistone deacetylase 4Homo sapiens (human)
potassium ion bindingHistone deacetylase 4Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 4Homo sapiens (human)
identical protein bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 4Homo sapiens (human)
molecular adaptor activityHistone deacetylase 4Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo sapiens (human)
chromatin bindingHistone deacetylase 7Homo sapiens (human)
transcription corepressor activityHistone deacetylase 7Homo sapiens (human)
histone deacetylase activityHistone deacetylase 7Homo sapiens (human)
protein kinase C bindingHistone deacetylase 7Homo sapiens (human)
protein bindingHistone deacetylase 7Homo sapiens (human)
SUMO transferase activityHistone deacetylase 7Homo sapiens (human)
protein kinase bindingHistone deacetylase 7Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 7Homo sapiens (human)
metal ion bindingHistone deacetylase 7Homo sapiens (human)
14-3-3 protein bindingHistone deacetylase 7Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 7Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 2Homo sapiens (human)
chromatin bindingHistone deacetylase 2Homo sapiens (human)
RNA bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 2Homo sapiens (human)
protein bindingHistone deacetylase 2Homo sapiens (human)
enzyme bindingHistone deacetylase 2Homo sapiens (human)
heat shock protein bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 2Homo sapiens (human)
histone bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 2Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 2Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 2Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 2Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 2Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
protein bindingPolyamine deacetylase HDAC10Homo sapiens (human)
zinc ion bindingPolyamine deacetylase HDAC10Homo sapiens (human)
deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
enzyme bindingPolyamine deacetylase HDAC10Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase bindingPolyamine deacetylase HDAC10Homo sapiens (human)
acetylputrescine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
acetylspermidine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityHistone deacetylase 11 Homo sapiens (human)
protein bindingHistone deacetylase 11 Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 11 Homo sapiens (human)
histone deacetylase activityHistone deacetylase 8Homo sapiens (human)
protein bindingHistone deacetylase 8Homo sapiens (human)
Hsp70 protein bindingHistone deacetylase 8Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 8Homo sapiens (human)
metal ion bindingHistone deacetylase 8Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 8Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 8Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 8Homo sapiens (human)
acetylspermidine deacetylase activityHistone deacetylase 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 6Homo sapiens (human)
actin bindingHistone deacetylase 6Homo sapiens (human)
histone deacetylase activityHistone deacetylase 6Homo sapiens (human)
protein bindingHistone deacetylase 6Homo sapiens (human)
beta-catenin bindingHistone deacetylase 6Homo sapiens (human)
microtubule bindingHistone deacetylase 6Homo sapiens (human)
zinc ion bindingHistone deacetylase 6Homo sapiens (human)
enzyme bindingHistone deacetylase 6Homo sapiens (human)
polyubiquitin modification-dependent protein bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin protein ligase bindingHistone deacetylase 6Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 6Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 6Homo sapiens (human)
tubulin deacetylase activityHistone deacetylase 6Homo sapiens (human)
alpha-tubulin bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin bindingHistone deacetylase 6Homo sapiens (human)
tau protein bindingHistone deacetylase 6Homo sapiens (human)
beta-tubulin bindingHistone deacetylase 6Homo sapiens (human)
misfolded protein bindingHistone deacetylase 6Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 6Homo sapiens (human)
dynein complex bindingHistone deacetylase 6Homo sapiens (human)
transcription factor bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein kinase C bindingHistone deacetylase 9Homo sapiens (human)
protein bindingHistone deacetylase 9Homo sapiens (human)
histone H3K14 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H3K9 deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H4K16 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 9Homo sapiens (human)
metal ion bindingHistone deacetylase 9Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 5Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 5Homo sapiens (human)
chromatin bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase activityHistone deacetylase 5Homo sapiens (human)
protein kinase C bindingHistone deacetylase 5Homo sapiens (human)
protein bindingHistone deacetylase 5Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 5Homo sapiens (human)
identical protein bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 5Homo sapiens (human)
metal ion bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA bindingNuclear receptor corepressor 2Homo sapiens (human)
chromatin bindingNuclear receptor corepressor 2Homo sapiens (human)
transcription corepressor activityNuclear receptor corepressor 2Homo sapiens (human)
Notch bindingNuclear receptor corepressor 2Homo sapiens (human)
protein bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear glucocorticoid receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
histone deacetylase bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear retinoid X receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (40)

Processvia Protein(s)Taxonomy
nucleusHistone deacetylase 3Homo sapiens (human)
nucleoplasmHistone deacetylase 3Homo sapiens (human)
cytoplasmHistone deacetylase 3Homo sapiens (human)
Golgi apparatusHistone deacetylase 3Homo sapiens (human)
cytosolHistone deacetylase 3Homo sapiens (human)
plasma membraneHistone deacetylase 3Homo sapiens (human)
mitotic spindleHistone deacetylase 3Homo sapiens (human)
histone deacetylase complexHistone deacetylase 3Homo sapiens (human)
transcription repressor complexHistone deacetylase 3Homo sapiens (human)
nucleusHistone deacetylase 3Homo sapiens (human)
condensed nuclear chromosomeBromodomain-containing protein 4Homo sapiens (human)
nucleusBromodomain-containing protein 4Homo sapiens (human)
nucleoplasmBromodomain-containing protein 4Homo sapiens (human)
nucleusNuclear receptor corepressor 1Homo sapiens (human)
nucleoplasmNuclear receptor corepressor 1Homo sapiens (human)
cytosolNuclear receptor corepressor 1Homo sapiens (human)
membraneNuclear receptor corepressor 1Homo sapiens (human)
mitotic spindleNuclear receptor corepressor 1Homo sapiens (human)
histone deacetylase complexNuclear receptor corepressor 1Homo sapiens (human)
chromatinNuclear receptor corepressor 1Homo sapiens (human)
transcription repressor complexNuclear receptor corepressor 1Homo sapiens (human)
nucleusHistone deacetylase 4Homo sapiens (human)
nucleoplasmHistone deacetylase 4Homo sapiens (human)
cytoplasmHistone deacetylase 4Homo sapiens (human)
cytosolHistone deacetylase 4Homo sapiens (human)
nuclear speckHistone deacetylase 4Homo sapiens (human)
histone deacetylase complexHistone deacetylase 4Homo sapiens (human)
chromatinHistone deacetylase 4Homo sapiens (human)
transcription repressor complexHistone deacetylase 4Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 7Homo sapiens (human)
nucleoplasmHistone deacetylase 7Homo sapiens (human)
cytoplasmHistone deacetylase 7Homo sapiens (human)
cytosolHistone deacetylase 7Homo sapiens (human)
chromosome, telomeric regionHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleoplasmHistone deacetylase 2Homo sapiens (human)
cytoplasmHistone deacetylase 2Homo sapiens (human)
NuRD complexHistone deacetylase 2Homo sapiens (human)
Sin3-type complexHistone deacetylase 2Homo sapiens (human)
histone deacetylase complexHistone deacetylase 2Homo sapiens (human)
chromatinHistone deacetylase 2Homo sapiens (human)
protein-containing complexHistone deacetylase 2Homo sapiens (human)
ESC/E(Z) complexHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleusPolyamine deacetylase HDAC10Homo sapiens (human)
nucleoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytosolPolyamine deacetylase HDAC10Homo sapiens (human)
intracellular membrane-bounded organellePolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase complexPolyamine deacetylase HDAC10Homo sapiens (human)
nucleusHistone deacetylase 11 Homo sapiens (human)
plasma membraneHistone deacetylase 11 Homo sapiens (human)
histone deacetylase complexHistone deacetylase 11 Homo sapiens (human)
nuclear chromosomeHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleoplasmHistone deacetylase 8Homo sapiens (human)
cytoplasmHistone deacetylase 8Homo sapiens (human)
histone deacetylase complexHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 6Homo sapiens (human)
nucleoplasmHistone deacetylase 6Homo sapiens (human)
cytoplasmHistone deacetylase 6Homo sapiens (human)
multivesicular bodyHistone deacetylase 6Homo sapiens (human)
centrosomeHistone deacetylase 6Homo sapiens (human)
cytosolHistone deacetylase 6Homo sapiens (human)
microtubuleHistone deacetylase 6Homo sapiens (human)
caveolaHistone deacetylase 6Homo sapiens (human)
inclusion bodyHistone deacetylase 6Homo sapiens (human)
aggresomeHistone deacetylase 6Homo sapiens (human)
axonHistone deacetylase 6Homo sapiens (human)
dendriteHistone deacetylase 6Homo sapiens (human)
cell leading edgeHistone deacetylase 6Homo sapiens (human)
ciliary basal bodyHistone deacetylase 6Homo sapiens (human)
perikaryonHistone deacetylase 6Homo sapiens (human)
perinuclear region of cytoplasmHistone deacetylase 6Homo sapiens (human)
axon cytoplasmHistone deacetylase 6Homo sapiens (human)
histone deacetylase complexHistone deacetylase 6Homo sapiens (human)
microtubule associated complexHistone deacetylase 6Homo sapiens (human)
nucleusHistone deacetylase 9Homo sapiens (human)
nucleoplasmHistone deacetylase 9Homo sapiens (human)
cytoplasmHistone deacetylase 9Homo sapiens (human)
histone deacetylase complexHistone deacetylase 9Homo sapiens (human)
transcription regulator complexHistone deacetylase 9Homo sapiens (human)
histone methyltransferase complexHistone deacetylase 9Homo sapiens (human)
nucleusHistone deacetylase 5Homo sapiens (human)
nucleoplasmHistone deacetylase 5Homo sapiens (human)
cytoplasmHistone deacetylase 5Homo sapiens (human)
Golgi apparatusHistone deacetylase 5Homo sapiens (human)
cytosolHistone deacetylase 5Homo sapiens (human)
nuclear speckHistone deacetylase 5Homo sapiens (human)
histone deacetylase complexHistone deacetylase 5Homo sapiens (human)
nucleusNuclear receptor corepressor 2Homo sapiens (human)
nucleoplasmNuclear receptor corepressor 2Homo sapiens (human)
membraneNuclear receptor corepressor 2Homo sapiens (human)
nuclear matrixNuclear receptor corepressor 2Homo sapiens (human)
nuclear bodyNuclear receptor corepressor 2Homo sapiens (human)
chromatinNuclear receptor corepressor 2Homo sapiens (human)
transcription repressor complexNuclear receptor corepressor 2Homo sapiens (human)
cytosolHistone deacetylase 6Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (253)

Assay IDTitleYearJournalArticle
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID721607Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1188993Inhibition of HDAC5 (unknown origin) at 1 uM incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID1462230Inhibition of BRD4 (unknown origin)2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
AID721454Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077033Cytotoxicity against human DU145 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID496803Inhibition of human HDAC32010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID721589Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID623373Cytotoxicity against human A498 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1250650Inhibition of recombinant human HDAC11 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID331900Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID623365Cytotoxicity against human UO31 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623412Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID90670Inhibitory concentration against human Histone deacetylase 1 (C151S)2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID721593Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1188980Inhibition of HDAC4 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID1250655Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID673993Inhibition of recombinant HDAC6 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1275078Inhibition of recombinant human HDAC62016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.
AID721451Inhibition of mouse HDAC6 using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1182193Inhibition of mouse HDAC6 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader in presence of 0.1 mM dithiothreitol2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID623408Antitumor activity against human NCI-H522 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077040Cytotoxicity against human ACHN cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID620963Selectivity ratio of IC50 for recombinant human HDAC1/N-CoR2 to IC50 for recombinant human HDAC3/N-CoR22011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID1188994Inhibition of HDAC7 (unknown origin) at 1 uM incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID1119933Selectivity ratio of IC50 for human recombinant HDAC6 to IC50 for human recombinant HDAC12012MedChemComm, Aug-01, Volume: 3, Issue:8
Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from
AID623376Cytotoxicity against human Caki1 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID765387Inhibition of recombinant human HDAC7 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID721452Inhibition of human HDAC1 using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077074Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID721592Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID620964Selectivity ratio of IC50 for recombinant human HDAC2/N-CoR2 to IC50 for recombinant human HDAC3/N-CoR22011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID721586Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1250649Inhibition of recombinant human HDAC10 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1077065Cytotoxicity against human U251 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID620944Inhibition of recombinant human HDAC9 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID623402Antitumor activity against human COLO205 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623407Antitumor activity against human NCI-H23 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID673991Inhibition of recombinant HDAC2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID623377Cytotoxicity against human SN12C cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID765386Inhibition of recombinant human HDAC9 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID721448Inhibition of class 1 HDAC (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077053Cytotoxicity against human NCI-H522 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID230221Inhibitory concentration against HDAC6/HDAC12003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID496806Inhibition of human HDAC62010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID90698Inhibitory concentration against human Histone deacetylase 42003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1077056Cytotoxicity against human HCT15 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623367Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1188995Inhibition of HDAC8 (unknown origin) at 1 uM incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID721613Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID765388Inhibition of recombinant human HDAC5 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID623400Antitumor activity against human SF295 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID721601Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID765392Inhibition of recombinant human HDAC2 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1254044Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID1250640Inhibition of recombinant human HDAC1 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID695593Inhibition of HDAC1 by fluorimetric assay in presence of DTT2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID623405Antitumor activity against human MDA-MB-435 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623375Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623401Antitumor activity against human U251 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID721597Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077051Cytotoxicity against human A549 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623410Antitumor activity against human OVCAR5 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID496801Inhibition of human HDAC12010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID765391Inhibition of GST-tagged recombinant human HDAC3/NcoR1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID623399Antitumor activity against human MDA-MB-231 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1188997Inhibition of HDAC6 (unknown origin) at 1 uM incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID1073051Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.
AID1188986Inhibition of HDAC11 (unknown origin) incubated for 3 hrs in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID620937Inhibition of recombinant human HDAC1/NCOR2 using Boc-L-Lys(epsilon-acetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID1073050Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis relative to SAHA-treated control2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.
AID1119931Inhibition of human recombinant HDAC6 after 1 hr by luminescence assay2012MedChemComm, Aug-01, Volume: 3, Issue:8
Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from
AID496805Inhibition of human HDAC52010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1188987Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID1077048Cytotoxicity against human DMS273 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID765385Inhibition of recombinant human HDAC6 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID765384Inhibition of recombinant human HDAC10 enzyme using tetrapeptide Ac-ArgThr-Lys(Ac)Lys(Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID721614Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID765383Inhibition of recombinant human HDAC11 enzyme using Ac-LeuGlyLys(Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1250644Inhibition of recombinant human HDAC4 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1182195Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID623404Antitumor activity against human LOXIMVI cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077066Cytotoxicity against human MDA-MB-231 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623444Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077072Selectivity index, ratio of IC50 for mouse HDAC6 to IC50 for human HDAC12014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1077068Cytotoxicity against human MCF7 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623416Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID721453Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID623371Cytotoxicity against human U251 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1250657Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1119929Inhibition of human recombinant HDAC1 after 1 hr by luminescence assay2012MedChemComm, Aug-01, Volume: 3, Issue:8
Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from
AID721594Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077032Cytotoxicity against human PC3 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID765389Inhibition of recombinant human HDAC4 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1077059Cytotoxicity against human SNB78 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID695595Inhibition of HDAC4 by fluorimetric assay in presence of DTT2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID695597Inhibition of HDAC6 by fluorimetric assay in presence of DTT2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID1077044Cytotoxicity against human OVCAR5 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623378Cytotoxicity against human NCI60 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID90704Inhibitory concentration against human Histone deacetylase 62003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID721600Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077070Cytotoxicity against human HBC4 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1250666Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1077055Cytotoxicity against human HCT116 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1250645Inhibition of recombinant human HDAC5 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID620945Inhibition of recombinant human HDAC3/N-CoR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay in presence of 0.2 mM H2O2 (Rvb = 0.018 uM)2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID623369Cytotoxicity against human COLO205 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623403Antitumor activity against human SW620 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID721459Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID721455Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID721587Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID620947Inhibition of recombinant human HDAC3/N-CoR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay in presence of 1 mM H2O2 (Rvb = 0.018 uM)2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID496807Inhibition of human HDAC72010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1250658Selectivity ratio of GI50 for human DU145 cells to GI50 for human HLF cells2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1077069Cytotoxicity against human BSY1 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1119932Selectivity ratio of IC50 for human recombinant HDAC4 to IC50 for human recombinant HDAC12012MedChemComm, Aug-01, Volume: 3, Issue:8
Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from
AID623374Cytotoxicity against human SF295 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1250648Inhibition of recombinant human HDAC6 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID90836Tested for inhibition of Histone deacetylase 6 induced acetylated tubulin in mammalian cells.2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID695594Inhibition of HDAC4 by fluorimetric assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID1077050Cytotoxicity against human NCI-H460 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID90679Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells.2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1188985Inhibition of HDAC10 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID623406Antitumor activity against human UACC62 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077054Cytotoxicity against human NCI-H23 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID721583Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1250642Inhibition of recombinant human HDAC3 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID623372Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID721603Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID331899Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID721584Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID765390Inhibition of recombinant human HDAC8 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1250653Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1254049Inhibition of HDAC8 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID721456Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID721596Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID623366Cytotoxicity against human ACHN cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623411Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID620942Inhibition of recombinant human HDAC7 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID623418Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077046Cytotoxicity against human OVCAR3 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID721449Selectivity index, ratio of IC50 for mouse HDAC6 to IC50 for human HDAC12013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077037Cytotoxicity against human MKN28 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623409Antitumor activity against human OVRAC3 cells implanted subcutaneously in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID620939Inhibition of recombinant human HDAC3/NCOR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID721602Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID721605Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077052Cytotoxicity against human NCI-H226 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID673990Inhibition of recombinant HDAC1 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID1254046Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID721585Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1250654Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID721608Growth inhibition of human U251 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID695592Inhibition of HDAC1 by fluorimetric assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID496802Inhibition of human HDAC22010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID620940Inhibition of recombinant human HDAC4 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID1250656Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1077039Cytotoxicity against human St-4 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID90686Inhibitory concentration against human Histone deacetylase 22003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1275076Inhibition of HDAC in human HeLa nuclear extract2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.
AID1250643Inhibition of recombinant human HDAC8 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID303346Growth inhibition of MCF7 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID303347Inhibition of HDAC in HeLa nuclear extract in presence of DTT2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID303349Inhibition of HDAC6 in presence of DTT2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID1077060Cytotoxicity against human HCC2998 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID496809Inhibition of human HDAC92010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1275077Inhibition of recombinant human HDAC12016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.
AID721611Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID721598Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID603218Inhibition of HDAC in human HeLa cell extracts assessed as conversion of dithiothreitol to dithiol after 1 hr by Flour-de-Lys assay2011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.
AID721599Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID721604Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077067Cytotoxicity against human HBC5 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID721588Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID714187Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells2012European journal of medicinal chemistry, Mar, Volume: 49Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
AID1254047Inhibition of HDAC1 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID1250647Inhibition of recombinant human HDAC9 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1077047Cytotoxicity against human LOXIMVI cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1077034Cytotoxicity against human MKN45 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623417Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623441Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077045Cytotoxicity against human OVCAR4 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1182194Ratio of IC50 for mouse HDAC6 to IC50 for human HDAC1 in presence of 0.1 mM dithiothreitol2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID1077061Cytotoxicity against human SNB75 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID721591Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077042Cytotoxicity against human SKOV3 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1077041Cytotoxicity against human RXF631L cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623442Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1182191Inhibition of human HDAC1 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader in presence of 0.1 mM dithiothreitol2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID620943Inhibition of recombinant human HDAC8 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID695596Inhibition of HDAC6 by fluorimetric assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID623370Cytotoxicity against human UACC257 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID721590Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1254045Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID721606Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID496808Activity of human HDAC82010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID620941Inhibition of recombinant human HDAC6 using Boc-L-Lys(epsilon-acetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID496804Inhibition of human HDAC42010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1077057Cytotoxicity against human HT-29 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID721610Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1188977Inhibition of HDAC1 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID1077035Cytotoxicity against human MKN74 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1250646Inhibition of recombinant human HDAC7 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID90700Inhibition of Histone deacetylase 4 in mammalian cells.2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1188979Inhibition of HDAC3 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID1077036Cytotoxicity against human MKN7 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1119930Inhibition of human recombinant HDAC4 after 1 hr by luminescence assay2012MedChemComm, Aug-01, Volume: 3, Issue:8
Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from
AID721595Growth inhibition of human A549 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID721457Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077064Cytotoxicity against human SF268 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1077073Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID721609Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID1077049Cytotoxicity against human DMS114 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID673992Inhibition of recombinant HDAC3/NCoR2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
AID620938Inhibition of recombinant human HDAC2/NCOR2 using Boc-L-Lys(epsilon-acetyl)-AMC as substrate by two-step fluorogenic assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID1182192Inhibition of human HDAC4 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader in presence of 0.1 mM dithiothreitol2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID721612Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID331898Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from HDAC in human HeLa nuclear cell extract by fluorescence p2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1254048Inhibition of HDAC6 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID623413Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID90669Inhibitory concentration against human Histone deacetylase 12003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1077063Cytotoxicity against human SF539 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID695598Inhibition of HDAC assessed as induction of p21 promoter expression by cell-based assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID303348Inhibition of HDAC1 in presence of DTT2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID623415Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID623368Cytotoxicity against human RXF393 cells after 6 days by MTT assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID765393Inhibition of recombinant human HDAC1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
AID1077038Cytotoxicity against human MKN1 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID620946Inhibition of recombinant human HDAC3/N-CoR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay in presence of 0.4 mM H2O2 (Rvb = 0.018 uM)2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Thailandepsins: bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activities.
AID1077043Cytotoxicity against human OVCAR8 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID623414Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077062Cytotoxicity against human SF295 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1188978Inhibition of HDAC2 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1250641Inhibition of recombinant human HDAC2 after 60 mins by fluorescence assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
AID1188996Inhibition of HDAC9 (unknown origin) at 1 uM incubated for 30 mins in presence of BSA and DTT by fluorescence assay2014ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
AID721458Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method2013European journal of medicinal chemistry, Feb, Volume: 60Total synthesis of bicyclic depsipeptides spiruchostatins C and D and investigation of their histone deacetylase inhibitory and antiproliferative activities.
AID623443Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Histone deacetylase inhibitors from Burkholderia thailandensis.
AID1077058Cytotoxicity against human KM12 cells by SRB assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
AID1346032Human histone deacetylase 6 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346077Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346131Human histone deacetylase 7 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346104Human histone deacetylase 4 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346068Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346082Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346066Human histone deacetylase 5 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346134Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346090Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1797826HDAC Enzyme Activity Assay from Article 10.1021/jm0703800: \\The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor.\\2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
The first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitor.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (20.83)29.6817
2010's18 (75.00)24.3611
2020's1 (4.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.43

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index56.43 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index4.92 (4.65)
Search Engine Demand Index87.98 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other21 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (100)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Pilot Study of a Novel Multimodality Immuno-Chemotherapy Platform for Patients With Advanced Cutaneous T Cell Lymphoma [NCT02061449]Phase 13 participants (Actual)Interventional2014-03-31Terminated(stopped due to Low Accrual)
Phase I/IIA Study of the Novel Antifolate Agent Pralatrexate in Combination With the Histone Deacetylase Inhibitor Romidepsin for the Treatment of Patients With Peripheral T-cell Lymphoma [NCT01947140]Phase 1/Phase 257 participants (Actual)Interventional2013-09-09Completed
An Open Label, Phase I/II Study to Evaluate the Safety and Efficacy of Tenalisib (RP6530), a Novel PI3K δ/γ Dual Inhibitor Given in Combination With a Histone Deacetylase (HDAC) Inhibitor, Romidepsin in Adult Patients With Relapsed/Refractory T-cell Lymph [NCT03770000]Phase 1/Phase 233 participants (Actual)Interventional2019-03-12Completed
ISTODAX® for Intravenous Infusion 10mg Drug Use Results Survey - Relapsed or Refractory Peripheral T-Cell Lymphoma [NCT03742921]150 participants (Actual)Observational2019-02-04Completed
A Phase IB/II Study of Escalating Doses of Romidepsin (Istodax®) in Association With CHOP (Ro-CHOP) in the Treatment of Peripheral T-Cell Lymphomas [NCT01280526]Phase 1/Phase 237 participants (Actual)Interventional2011-01-31Completed
A Phase 2a, Randomized Study of Romidepsin With or Without 3BNC117 to Evaluate the Effects on the HIV-1 Reservoir (ROADMAP) [NCT02850016]Phase 248 participants (Actual)Interventional2017-01-06Completed
An Open Label, Single-Arm Rollover Study for Subjects Who Participated In Other Romidepsin Protocols [NCT01353664]Phase 219 participants (Actual)Interventional2011-05-01Completed
Phase I/II Study of Ixazomib and Romidepsin in Relapsed/ Refractory Peripheral T-cell Lymphoma (PTCL) [NCT03547700]Phase 1/Phase 211 participants (Actual)Interventional2018-09-26Active, not recruiting
A Multicenter Phase I Dose-finding and Preliminary Efficacy Study of the Histone Deacetylase Inhibitor Romidepsin (Istodax) in Combination With Gemcitabine (Gemzar), Oxaliplatin (Eloxatin), and Dexamethasone for the Treatment of Adults With Relapsed/Refra [NCT02181218]Phase 124 participants (Actual)Interventional2015-02-04Completed
Pilot Safety and Feasibility Study of an In Vivo Sensitivity Screen Using a Direct Tumor Microinjection Technique and FDG-PET [NCT03432741]Phase 139 participants (Anticipated)Interventional2018-03-27Suspended(stopped due to funding - sponsor filing of Chapter 11 bankruptcy)
Romidepsin in Combination With CHOEP as First Line Treatment Before Hematopoietic Stem Cell Transplantation in Young Patients With Nodal Peripheral T-cell Lymphomas: a Phase I-II Study [NCT02223208]Phase 1/Phase 289 participants (Actual)Interventional2014-09-30Active, not recruiting
A Phase 2 Study of Venetoclax and Romidepsin With Safety Lead-In for Treatment of Relapsed/Refractory Mature T-Cell Lymphomas [NCT03534180]Phase 212 participants (Actual)Interventional2018-08-21Completed
Phase II Study of Romidepsin Plus Lenalidomide for Patients With Previously Untreated PTCL [NCT02232516]Phase 235 participants (Actual)Interventional2015-06-30Active, not recruiting
A Phase 1 Study of Romidepsin, CC-486 (5-azacitidine), Dexamethasone, and Lenalidomide (RAdR) for Relapsed/Refractory T-cell Malignancies [NCT04447027]Phase 130 participants (Anticipated)Interventional2020-12-17Recruiting
Retrospective and Prospective Study of Long-term Use of Romidepsin in Patients [NCT02296398]47 participants (Actual)Observational2015-01-31Completed
Phase 3 Multi-center Randomized Study to Compare Efficacy and Safety of Romidepsin CHOP (Ro-CHOP) Versus CHOP in Patients With Previously Untreated Peripheral T-cell Lymphoma [NCT01796002]Phase 3421 participants (Actual)Interventional2013-01-31Completed
A Phase II Study of Single Agent Depsipeptide (FK228) in Radioiodine (RAI)-Refractory Metastatic Non-medullary (Papillary, Follicular, and Hurthle Cell Variants) Thyroid Carcinoma [NCT00098813]Phase 220 participants (Actual)Interventional2004-10-31Completed
Phase II Trial of Depsipeptide in Patients With Cutaneous T-Cell Lymphoma and Relapsed Peripheral T-Cell Lymphoma [NCT00007345]Phase 2131 participants (Actual)Interventional2001-03-08Completed
A Phase Ib/IIa Study of Romidepsin in Combination With Lenalidomide in Adults With Relapsed or Refractory Lymphomas and Myeloma [NCT01755975]Phase 1/Phase 262 participants (Actual)Interventional2012-12-31Completed
Randomized Phase 3 Study Evaluating the Efficacy and the Safety of Oral Azacitidine (CC-486) Compared to Investigator's Choice Therapy in Patient With Relapsed or Refractory Angioimmunoblastic T Cell Lymphoma [NCT03593018]Phase 386 participants (Actual)Interventional2018-11-09Active, not recruiting
Randomized Study of Romidepsin Versus the Combination of Romidepsin Plus Pralatrexate in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (PTCL) [NCT03355768]Phase 30 participants (Actual)Interventional2018-09-01Withdrawn(stopped due to Study was never opened due to lack of funding)
Phase I/II Study of Cisplatin Plus Romidepsin and Nivolumab in Metastatic Triple Negative Breast Cancer or BRCA Mutation-Associated Locally Recurrent or Metastatic Breast Cancer [NCT02393794]Phase 1/Phase 251 participants (Actual)Interventional2015-07-17Active, not recruiting
A Phase I Study of Romidepsin, Gemcitabine, Dexamethasone and Cisplatin Combination Therapy in the Treatment of Peripheral T-Cell and Diffuse Large B-Cell Lymphoma [NCT01846390]Phase 121 participants (Actual)Interventional2013-10-01Completed
A Phase I/II Trial of Romidepsin, Rituximab and Lenalidomide (R3) in Relapsed/Refractory B Cell Lymphomas Including Transformed Follicular Lymphoma [NCT02281279]Phase 1/Phase 20 participants (Actual)Interventional2016-10-31Withdrawn
Early Administration of Latency Reversing Therapy and Broadly Neutralizing Antibodies to Limit the Establishment of the HIV-1 Reservoir During Initiation of Antiretroviral Treatment - a Randomized Controlled Trial [NCT03041012]Phase 260 participants (Actual)Interventional2017-01-20Active, not recruiting
A Phase I Trial of Volasertib Plus Romidepsin in Patients With Relapsed/Refractory Peripheral T Cell and Cutaneous T Cell Lymphoma [NCT02757248]Phase 10 participants (Actual)Interventional2016-11-30Withdrawn(stopped due to Boehringer Ingelheim is discontinuing their volasertib development program)
Phase I/II Study to Determine the Maximum Tolerated Dose and Activity of the Combination of Romidepsin and Carfilzomib in Relapsed or Refractory Peripheral T-cell Lymphoma [NCT03141203]Phase 1/Phase 250 participants (Actual)Interventional2015-07-13Completed
A Phase II Study of Single Agent Depsipeptide (FK228) in Metastatic or Unresectable Soft Tissue Sarcomas [NCT00112463]Phase 240 participants (Actual)Interventional2005-01-07Completed
A Phase II Trial of Romidepsin and Bortezomib for Multiple Myeloma Patients With Relapsed or Refractory Disease [NCT00765102]Phase 232 participants (Actual)Interventional2008-09-01Terminated(stopped due to There was a change in the Sponsor's research strategy; safety concerns were not a factor.)
Phase I Trial of a Four Hour Infusion of Depsipeptide (NSC630176) Given on Days 1 and 5 of a 21 Day Cycle in Patients With Refractory Neoplasms [NCT00019318]Phase 10 participants Interventional1997-08-31Completed
Phase I/IIa Study of the Oral 5-Azacitidine in Combination With the Histone Deacetylase Inhibitor Romidepsin for the Treatment of Patients With Relapsed and Refractory Lymphoid Malignancies [NCT01998035]Phase 1/Phase 252 participants (Actual)Interventional2013-11-30Terminated(stopped due to PI left institution)
Phase I Study of Bortezomib and Romidepsin in Patients With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma, Indolent B-Cell Lymphoma, Peripheral T-Cell Lymphoma or Cutaneous T-Cell Lymphoma [NCT00963274]Phase 118 participants (Actual)Interventional2010-04-26Completed
A Phase I/II Study of Romidepsin (Depsipeptide) in Combination With Gemcitabine in Patients With Pancreatic and Other Advanced Solid Tumors. [NCT00379639]Phase 136 participants (Actual)Interventional2006-07-01Completed
An Open Label Phase I Trial to Evaluate the Safety and Effect of HIVconsv Vaccines in Combination With Histone Deacetylase Inhibitor Romidepsin on the Viral Rebound Kinetic After Treatment Interruption in Early Treated HIV-1 Infected Individuals (BCN02-Ro [NCT02616874]Phase 115 participants (Actual)Interventional2016-02-29Completed
Romidepsin Therapy in Conditioning and Maintenance in Patients With T-Cell Malignancies Receiving Allogeneic Stem Cell Transplant [NCT02512497]Phase 110 participants (Anticipated)Interventional2017-12-08Recruiting
A Multicenter Phase I Dose-finding and Preliminary Efficacy Study of the Histone Deacetylase Inhibitor Romidepsin (Istodax®) in Combination With Doxorubicin HCl Liposomal (Doxil®) for the Treatment of Adults With Relapsed or Refractory Cutaneous T-cell Ly [NCT01902225]Phase 124 participants (Actual)Interventional2014-03-04Completed
A Pilot Study of Romidepsin in Relapsed or Refractory Extranodal NK/T-cell [NCT01913119]Early Phase 116 participants (Actual)Interventional2013-07-31Completed
A Phase II, Multicenter, Open-Label Trial Evaluating The Activity And Tolerability Of Romidepsin (Depsipeptide, FK228) In Progressive Or Relapsed Peripheral T-Cell Lymphoma Following Prior Systemic Therapy (GPI-06-0002) [NCT00426764]Phase 2131 participants (Actual)Interventional2007-06-19Completed
A Phase I Trial of Duvelisib in Combination With Either Romidepsin or Bortezomib in Relapsed/Refractory T-cell Lymphomas [NCT02783625]Phase 1114 participants (Actual)Interventional2016-05-31Active, not recruiting
A Phase 2 Multicenter Study of High Dose Chemotherapy With Autologous Stem Cell Transplant Followed by Maintenance Therapy With Romidepsin for the Treatment of T Cell Non-Hodgkin Lymphoma [NCT01908777]Phase 247 participants (Actual)Interventional2013-07-16Active, not recruiting
A Phase I Open-label, 2-period Study to Evaluate the Influence of Multiple Oral Doses of Ketoconazole on the Single Dose Pharmacokinetics of Romidepsin in Subjects With Advanced Cancer [NCT01324310]Phase 115 participants (Actual)Interventional2011-04-01Completed
A Phase I Open-label, 2-period Study to Evaluate the Influence of Multiple Oral Doses of Rifampin on the Single Dose Pharmacokinetics of Romidepsin in Subjects With Advanced Cancer [NCT01324323]Phase 114 participants (Actual)Interventional2011-04-01Completed
Phase Ib/IIa Study of Combination Therapy With Carfilzomib, Romidepsin, Lenalidomide in Patients With Relapsed or Refractory B- and T-cell Lymphomas [NCT02341014]Phase 1/Phase 231 participants (Anticipated)Interventional2015-01-02Completed
Phase 1B Study of the PI3K Inhibitor Copanlisib in Combination With Romidepsin in the Treatment of Patients With Relapsed or Refractory Mature T-cell Lymphoma [NCT04233697]Phase 10 participants (Actual)Interventional2020-02-29Withdrawn(stopped due to Investigator left institution)
A Phase II Study of Single Agent Depsipeptide (FK228) (NSC 630176; IND 51,810) in Relapsed Small Cell Lung Cancer [NCT00086827]Phase 236 participants (Actual)Interventional2004-05-31Completed
A Phase II Study of Depsipeptide (NSC-630176) In Patients With Advanced Transitional Cell Carcinoma Of The Urinary Tract Who Have Progressed After Receiving One Prior Chemotherapy Regimen For Advanced Disease [NCT00087295]Phase 26 participants (Actual)Interventional2004-06-30Terminated(stopped due to Permanently Closed Due to Poor Accrual)
A Phase II Study Of Single Agent Depsipeptide (FK228) In Recurrent, Platinum Sensitive Adeno-Carcinoma Of The Ovary Or Peritoneum [NCT00091195]Phase 251 participants (Actual)Interventional2004-09-30Terminated(stopped due to Administratively complete.)
Phase I Study of Sequential Depsipeptide/Flavopiridol Infusion for Malignancies Involving Lungs, Esophagus, Pleura, Thymus or Mediastinum [NCT00094978]Phase 123 participants (Actual)Interventional2004-10-25Terminated
A Phase II Study Of Depsipeptide In Patients With Relapsed Or Refractory Ovarian Carcinoma [NCT00085527]Phase 20 participants (Actual)Interventional2005-05-31Withdrawn
A Phase I/II Trial of Romidepsin (Depsipeptide) and Bortezomib in Patients With Relapsed Myeloma [NCT00431990]Phase 1/Phase 240 participants (Anticipated)Interventional2006-11-30Recruiting
A Pilot Open Label Phase I Trial to Evaluate the Safety and the Tolerability of a Combination of Two HIV-1 Inducers in HIV+ Sub-type B Patients Under cART With Undetectable Viral Load [NCT05230368]Phase 115 participants (Anticipated)Interventional2022-12-14Recruiting
Randomized Phase 3 Study Evaluation the Efficacy and Safety of Oral Azacitidine(CC-486) Compared to Investigator's Choice Therapy in Patients With Relapsed or Refractory Angioimmunoblastic T Cell Lymphoma [NCT03703375]Phase 322 participants (Actual)Interventional2018-11-06Active, not recruiting
A Phase II Study Of Single Agent Depsipeptide (FK228) In Breast Cancer [NCT00098397]Phase 237 participants (Actual)Interventional2005-02-28Completed
A Phase 2 Study of Depsipeptide in Relapsed/Refractory Multiple Myeloma [NCT00066638]Phase 250 participants (Actual)Interventional2003-06-30Completed
Phase II Study of Depsipeptide in Metastatic Neuroendocrine Tumors [NCT00084461]Phase 225 participants (Actual)Interventional2004-03-31Terminated
A Multicenter, Open-Label Continuation Trial Evaluating the Tolerability and Activity of FK228 in Patients That Have Completed a Prior Clinical Study With FK228 [NCT00106301]Phase 22 participants (Actual)Interventional2004-04-01Completed
An Exploratory Phase II, Multicenter, Open-label Trial Evaluating the Activity and Tolerability of FK228 in Androgen Independent Metastatic Prostate Cancer Patients With Rising PSA [NCT00106418]Phase 235 participants (Actual)Interventional2003-05-07Completed
An Exploratory Phase II, Multicenter, Open-label Trial Evaluating the Activity and Tolerability of FK228 in Patients With Metastatic Renal Cell Carcinoma That is Progressive Following or During Immunotherapy [NCT00106613]Phase 230 participants (Actual)Interventional2003-05-01Completed
A Phase I Study of 5-AZA-2'-Deoxycytidine and Depsipeptide in Patients With Relapsed/Refractory Leukemia, Myelodysplastic Syndromes, or Myeloproliferative Disease [NCT00114257]Phase 136 participants (Actual)Interventional2005-05-31Completed
A Randomized, Phase IIB, Multicenter, Trial of Oral Azacytidine Plus Romidepsin Versus Investigator's Choice in Patients With Relapse or Refractory Peripheral T-cell Lymphoma (PTCL) [NCT04747236]Phase 250 participants (Anticipated)Interventional2021-02-19Recruiting
Phase I Trial of Oral 5-azacitidine With Romidepsin in Advanced Solid Tumors, With an Expansion Cohort in Virally Mediated Cancers and Liposarcoma [NCT01537744]Phase 118 participants (Actual)Interventional2012-02-29Completed
A Phase 2 Study of Single Agent Depsipeptide (FK228) in Gastric and Esophageal Cancers [NCT00098527]Phase 220 participants (Actual)Interventional2004-10-31Terminated
Phase I Trial of Romidepsin Given on Days One, Three, and Five in Patients With Thyroid and Other Advanced Cancers [NCT00048334]Phase 128 participants (Actual)Interventional2002-10-26Completed
A Phase II Study Of Depsipeptide, A Histone Deacetylase Inhibitor, In Relapsed Or Refractory Mantle Cell Or Diffuse Large Cell Non-Hodgkin's Lymphoma [NCT00077194]Phase 235 participants (Actual)Interventional2004-01-31Completed
Phase II Study of FR901228 in Patients With Refractory or Progressive Small Cell or Non-Small Cell Lung Cancer [NCT00020202]Phase 20 participants Interventional2000-06-30Completed
A Phase I Study of Depsipeptide in Selected Hematologic Malignancies (NSC 630176) [NCT00024180]Phase 10 participants Interventional2002-01-31Completed
Phase I Study of Gene Induction Mediated by Sequential Decitabine/Depsipeptide Infusion With or Without Concurrent Celecoxib in Subjects With Pulmonary and Pleural Malignancies [NCT00037817]Phase 134 participants (Actual)Interventional2002-05-17Completed
Phase II Trial of Depsipeptide (NSC-630176) in Colorectal Cancer Patients Who Have Received Either One or Two Prior Chemotherapy Regimens for Metastatic or Locally Advanced, Unresectable Disease [NCT00077337]Phase 20 participants Interventional2004-04-30Completed
A Phase II Study of Single Agent Depsipeptide (NSC 630176) Followed by a Phase I Study of Rituximab/Fludarabine Combination With an Escalating Dose of Depsipeptide in Relapsed or Refractory Low Grade B Cell Lymphomas [NCT00079443]Phase 260 participants (Actual)Interventional2004-01-31Terminated
A Pilot Study Of FR901228, Or Depsipeptide (NSC #630176) For Adult Patients With Advanced Hematologic Cancers [NCT00042822]Phase 20 participants Interventional2002-05-31Completed
A PHASE I STUDY OF DEPSIPEPTIDE (NSC#630176, IND# 51810) IN PEDIATRIC PATIENTS WITH REFRACTORY SOLID TUMORS AND LEUKEMIAS [NCT00053963]Phase 130 participants (Actual)Interventional2002-09-30Completed
A Phase 2 Study of Depsipeptide in Patients With Relapsed or Refractory AML [NCT00062075]Phase 247 participants (Anticipated)Interventional2003-05-31Completed
A Phase I Study of Romidepsin in Combination With Parsaclisib in Relapsed and Refractory T-Cell Lymphomas [NCT04774068]Phase 120 participants (Anticipated)Interventional2021-09-01Recruiting
A Pilot Study of Romidepsin for Therapy of Graft-versus-Host Disease [NCT02203578]1 participants (Actual)Interventional2014-11-30Terminated(stopped due to slow accrual)
A Phase 1 Trial of MLN8237 Plus Romidepsin for Relapsed/Refractory Aggressive B-Cell and T-Cell Lymphomas [NCT01897012]Phase 126 participants (Actual)Interventional2013-07-17Completed
[NCT00299351]Phase 28 participants InterventionalNot yet recruiting
A Multicenter, Phase I/II Study of Sequential Epigenetic and Immune Targeting in Combination With Nab-Paclitaxel/Gemcitabine in Patients With Advanced Pancreatic Ductal Adenocarcinoma. [NCT04257448]Phase 1/Phase 275 participants (Anticipated)Interventional2020-05-25Active, not recruiting
A Study of Using Epigenetic Modulators to Enhance Response to MK-3475 in Microsatellite Stable Advanced Colorectal Cancer [NCT02512172]Phase 127 participants (Actual)Interventional2016-02-19Completed
An Open Label, International, Multi-centre, Phase I/IIa Study of Lenalidomide (Revlimid) and Romidepsin (Istodax) for Relapsed /Refractory Hodgkin Lymphoma, Mature T-cell Lymphoma and Multiple Myeloma. (RId Study) [NCT01742793]Phase 112 participants (Actual)Interventional2012-10-31Terminated(stopped due to The study was terminated due to withdrawal of institutional support, Phase II never began.)
Phase IIa Study on the Role of Gemcitabine Plus Romidepsin (GEMRO Regimen) in the Treatment of Relapsed/Refractory Peripheral T-cell Lymphoma Patients. [NCT01822886]Phase 220 participants (Actual)Interventional2013-01-31Completed
Phase I Study of Topical Romidepsin (Depsipeptide) in Early Stage Cutaneous T-Cell Lymphoma [NCT01445340]Phase 16 participants (Actual)Interventional2007-04-21Terminated
A Phase 1 Study of Doxorubicin, CC-486 (5-azacitidine), Romidepsin, and Duvelisib (hARD) for T-cell Lymphoma [NCT04639843]Phase 10 participants (Actual)Interventional2022-11-03Withdrawn(stopped due to Safety issues with PI3 kinase inhibitors)
Phase I Study of Romidepsin (ISTODAX®) Plus ICE for Patients With Relapsed or Refractory Peripheral T-Cell Lymphoma [NCT01590732]Phase 122 participants (Actual)Interventional2012-10-29Completed
A Phase I/II Study of Erlotinib and Romidepsin in Advanced Non-Small Cell Lung Cancer [NCT01302808]Phase 117 participants (Actual)Interventional2009-09-30Completed
A Phase I/II Study of Romidepsin in HIV-Infected Adults With Suppressed Viremia on Antiretroviral Therapy to Assess Safety, Tolerability, and Activation of HIV-1 Expression [NCT01933594]Phase 1/Phase 259 participants (Actual)Interventional2014-05-05Completed
An Open Phase I/IIa Study to Evaluate the Safety and Effect of Therapeutic HIV-1 Immunization Using Vacc-4x + rhuGM-CSF and HIV-1 Reactivation Using Romidepsin on the Viral Reservoir in Virologically Suppressed HIV-1 Infected Adults on cART [NCT02092116]Phase 1/Phase 226 participants (Actual)Interventional2014-03-31Completed
A Phase I/II Study of Romidepsin in Combination With Abraxane in Patients With Metastatic Inflammatory Breast Cancer [NCT01938833]Phase 1/Phase 29 participants (Actual)Interventional2014-04-30Terminated(stopped due to Closed by Sponsor)
A Phase I-II Trial of Depsipeptide in Patients With Recurrent High-Grade Gliomas [NCT00085540]Phase 1/Phase 250 participants (Actual)Interventional2005-01-31Completed
A Phase I/II Study of Pomalidomide (CC-4047®), Dexamethasone and Romidepsin in Patients With Relapsed or Refractory Multiple Myeloma (Romi Poma) [NCT01979276]Phase 1/Phase 24 participants (Actual)Interventional2013-11-30Terminated(stopped due to this study was terminated due to losing financial support, and enrollment challenges)
Phase II Trial of Depsipeptide (NSC 630176) in Advanced Malignant Melanoma [NCT00104884]Phase 24 participants (Actual)Interventional2005-10-04Terminated(stopped due to The study was terminated on May 17, 2006 due to slow accrual.)
A Phase II Study of Depsipeptide, a Histone Deacetylase Inhibitor, in Relapsed or Refractory Mantle Cell or Diffuse Large Cell Non-Hodgkin's Lymphoma [NCT00383565]Phase 29 participants (Actual)Interventional2006-09-30Terminated
A Japanese Phase 1/2, Multicenter, Open-label Study to Assess the Efficacy, Tolerability, Safety and Pharmacokinetics of Romidepsin in Subjects With the Progressive or Relapsed Peripheral T-cell Lymphoma [NCT01456039]Phase 1/Phase 251 participants (Actual)Interventional2011-12-01Completed
A Phase I Trial Assessing the Feasibility of Romidepsin Combined With Brentuximab Vedotin for Patients Requiring Systemic Therapy for Cutaneous T-cell Lymphoma [NCT02616965]Phase 116 participants (Actual)Interventional2017-02-22Active, not recruiting
A Phase II Study of Single Agent Depsipeptide (FK228; NSC 630176; IND 51,810) in Patients With Unresectable Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck [NCT00084682]Phase 214 participants (Actual)Interventional2005-06-30Completed
A Phase I/II Study of Pembrolizumab (MK-3475) in Combination With Romidepsin in Patients With Relapsed or Refractory Peripheral T-Cell Lymphoma [NCT03278782]Phase 1/Phase 239 participants (Actual)Interventional2017-11-14Active, not recruiting
Phase 1/2a Study of Anti-PD-L1 Monoclonal Antibody Durvalumab in Combination With Pralatrexate and Romidepsin, Oral 5-Aza and Romidepsin, Romidepsin Alone, or Oral 5-Azacitidine for Treatment of Patients With Relapsed and Refractory PTCL [NCT03161223]Phase 1/Phase 2148 participants (Anticipated)Interventional2018-05-30Recruiting
A Phase 1 and Pharmacokinetic Single Agent Study of Romidepsin in Patients With, Lymphomas, Chronic Lymphocytic Leukemia, and Select Solid Tumors and Varying Degrees of Liver Dysfunction [NCT01638533]Phase 137 participants (Actual)Interventional2012-06-12Active, not recruiting
A Phase 3, Randomized, Two-Arm, Open-Label, Multicenter, International Trial of Alisertib (MLN8237) or Investigator's Choice (Selected Single Agent) in Patients With Relapsed or Refractory Peripheral T-Cell Lymphoma [NCT01482962]Phase 3271 participants (Actual)Interventional2012-06-11Completed
A Single Agent Phase II Study of Depsipeptide (FK228) in the Treatment of Cutaneous T-cell Lymphoma [NCT00106431]Phase 2102 participants (Actual)Interventional2005-01-01Completed
A Randomized Phase I Dose-Escalation Trial of Carfilzomib With and Without Romidepsin in Cutaneous T-Cell Lymphoma [NCT01738594]Phase 17 participants (Actual)Interventional2013-03-22Terminated(stopped due to Slow accrual)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00007345 (7) [back to overview]Fold Change in Histone Acetylation
NCT00007345 (7) [back to overview]Number of Participants With Adverse Events
NCT00007345 (7) [back to overview]Time to Progression
NCT00007345 (7) [back to overview]Duration of Response (DOR)
NCT00007345 (7) [back to overview]Number of Participants With a Response
NCT00007345 (7) [back to overview]Multidrug Resistance Protein 1 (MDR1) or ATP-binding Cassette Sub-family B Member 1 (ABCB1) Gene Expression
NCT00007345 (7) [back to overview]Median Number of Cycles of Depsipeptide Administered
NCT00084682 (1) [back to overview]Disease Control (i.e., Achievement of Complete Response, Partial Response, or Stable Disease)
NCT00085540 (3) [back to overview]Response Rate Associated With Depsipeptide Therapy (Phase II)
NCT00085540 (3) [back to overview]Number of Participants With Dose-limiting Toxicities Due to Romidepsin Graded According to the NCI Common Toxicity Criteria (CTCAE Version 3.0) (Phase I)
NCT00085540 (3) [back to overview]6 Months Progression-free Survival (Phase II)
NCT00098813 (1) [back to overview]Tumor Major Response Rate (Including Stable Disease) as Measured by RECIST Criteria
NCT00104884 (1) [back to overview]Proportion of Patients With Response to Depsipeptide
NCT00106431 (7) [back to overview]Time to Objective Disease Response
NCT00106431 (7) [back to overview]Time to Disease Progression
NCT00106431 (7) [back to overview]The Percent of Patients (Pts) With Objective Disease Response
NCT00106431 (7) [back to overview]Percent of Pts With Objective Disease Control
NCT00106431 (7) [back to overview]Duration of Objective Disease Response
NCT00106431 (7) [back to overview]Duration of Objective Disease Control (ODC)
NCT00106431 (7) [back to overview]Decrease in Pruritus Visual Analogue Scale (VAS) Score of ≥30 mm or a Score of 0 for at Least 2 Consecutive Cycles.
NCT00112463 (4) [back to overview]Time to Progression
NCT00112463 (4) [back to overview]Objective Tumor Response (Complete and Partial)
NCT00112463 (4) [back to overview]Survival
NCT00112463 (4) [back to overview]Toxicity as Assessed Using the Expanded Common Toxicity Criteria Version 3
NCT00379639 (3) [back to overview]Number of Participants With a Dose-limiting Toxicity (DLT)
NCT00379639 (3) [back to overview]Number of Participants With Adverse Events (AEs)
NCT00379639 (3) [back to overview]Best Overall Response
NCT00383565 (3) [back to overview]Median Overall Survival
NCT00383565 (3) [back to overview]Overall Objective Response Rate (Complete Response [CR] and Partial Response [PR]) After 6 Courses of Treatment
NCT00383565 (3) [back to overview]Median Progression Free-survival (PFS)
NCT00426764 (7) [back to overview]Percentage of Participants With Objective Disease Response
NCT00426764 (7) [back to overview]Percentage of Participants With a Complete Response According to the International Workshop Response Criteria (IWC) for Non-Hodgkin's Lymphomas (NHL) Assessed by an Independent Review Committee
NCT00426764 (7) [back to overview]Duration of Objective Disease Response
NCT00426764 (7) [back to overview]Duration of Complete Disease Response
NCT00426764 (7) [back to overview]Time to Disease Progression
NCT00426764 (7) [back to overview]Change in Eastern Cooperative Oncology Group (ECOG) Performance Status
NCT00426764 (7) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT00765102 (7) [back to overview]Total Volume of Distribution (Vz)
NCT00765102 (7) [back to overview]Participants With Treatment-emergent Adverse Events (TEAEs)
NCT00765102 (7) [back to overview]Maximum Observed Concentration (Cmax)
NCT00765102 (7) [back to overview]Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-∞)
NCT00765102 (7) [back to overview]Terminal Half-life (t1/2)
NCT00765102 (7) [back to overview]Time to Maximum Observed Concentration (Tmax)
NCT00765102 (7) [back to overview]Total Clearance (CL)
NCT01302808 (2) [back to overview]Area Under the Concentration-time Curve (AUC0 t) of Romidepsin in Combination With Erlotinib
NCT01302808 (2) [back to overview]Number of Participants With Dose Limiting Toxicities and Maximum Tolerated Dose (MTD)
NCT01324310 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t)of Romidepsin
NCT01324310 (9) [back to overview]Estimate of the Terminal Elimination Half-life in Plasma (t1/2)
NCT01324310 (9) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT01324310 (9) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax)
NCT01324310 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time 0 Extrapolated to Infinity (AUC0-∞)
NCT01324310 (9) [back to overview]Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT01324310 (9) [back to overview]Apparent Total Plasma Clearance (CL)
NCT01324310 (9) [back to overview]Apparent Total Volume of Distribution (Vz)
NCT01324310 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time 0 to 24-hour (AUC 0-24)
NCT01324323 (9) [back to overview]Apparent Total Volume of Distribution (Vz).
NCT01324323 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time 0 to 24-hour (AUC0-24) for Romidepsin
NCT01324323 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t)of Romidepsin
NCT01324323 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time Zero Extrapolated to Infinity (AUC0-∞).
NCT01324323 (9) [back to overview]Clearance (CL): Apparent Total Plasma Clearance.
NCT01324323 (9) [back to overview]Estimate of the Terminal Elimination Half-life in Plasma (t1/2)
NCT01324323 (9) [back to overview]Maximum Observed Plasma Concentration (Cmax)of Romidepsin
NCT01324323 (9) [back to overview]Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT01324323 (9) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax)
NCT01353664 (1) [back to overview]Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT01456039 (24) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC∞) of Romidepsin in Phase 1
NCT01456039 (24) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of Romidepsin in Phase 1
NCT01456039 (24) [back to overview]AUC0-t, Accumulation Ratio of Romidepsin in Phase 1, Cycle 1
NCT01456039 (24) [back to overview]AUC0-t, at Steady State (ss) of Romidepsin in Phase 1 at Cycle 1, Day 15
NCT01456039 (24) [back to overview]Cmax Accumulation Ratio of Romidepsin in Phase 1, Cycle 1
NCT01456039 (24) [back to overview]Cmax, ss of Romidepsin in Phase 1 at Cycle 1, Day 15
NCT01456039 (24) [back to overview]Kaplan Meier (K-M) Estimate of Time to Progression (TTP) in PTCL Participants Based on the Modified 2007 IWC as Assessed by IER
NCT01456039 (24) [back to overview]Kaplan Meier Estimate of Duration of Response (DOR) for PTCL Responders Based on the Modified 1999 IWC as Assessed by the IER.
NCT01456039 (24) [back to overview]Kaplan Meier Estimate of Duration of Response (DOR) for PTCL Responders Based on the Modified 2007 IWC as Assessed by the IER.
NCT01456039 (24) [back to overview]Kaplan Meier Estimate of Time to Progression (TTP) in PTCL Participants Based on the 1999 IWC as Assessed by IER
NCT01456039 (24) [back to overview]Maximum Plasma Concentration (Cmax) of Romidepsin in Phase 1
NCT01456039 (24) [back to overview]Number of Participants With Dose-limiting Toxicity (DLT) in Accordance With National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0 as Determined by the Efficacy and Safety Evaluation Committee (ESEC)
NCT01456039 (24) [back to overview]Percentage of PTCL Participants With an Overall Best Response in Accordance With a Modified International Workshop Response Criteria (IWC) 1999 in Phase 2
NCT01456039 (24) [back to overview]Percentage of PTCL Participants With the Best Response in Accordance With the Modified 2007 International Workshop Response Criteria as Assessed by IER
NCT01456039 (24) [back to overview]Terminal Phase Half-life of Romidepsin (t½) in Phase 1
NCT01456039 (24) [back to overview]Terminal Phase Half-life of Romidepsin (t½) in Phase 1 at Cycle 1, Day 15
NCT01456039 (24) [back to overview]Time to Maximum Plasma Concentration of Romidepsin (Tmax) in Phase 1
NCT01456039 (24) [back to overview]Time to Response (TTR) for PTCL Participants With at Least a PR Based on the Modified 1999 IWC as Assessed by IER
NCT01456039 (24) [back to overview]Time to Response (TTR) for PTCL Participants With at Least a PR Based on the Modified 2007 IWC as Assessed by IER
NCT01456039 (24) [back to overview]Tmax,ss of Romidepsin in Phase 1 at Cycle 1, Day 15
NCT01456039 (24) [back to overview]Participants With Treatment-Emergent Adverse Events (TEAEs) Associated With Romidepsin
NCT01456039 (24) [back to overview]The Percentage of Participants With Abnormal Q-wave and T Wave Intervals
NCT01456039 (24) [back to overview]Apparent Total Clearance of Romidepsin (CL/F) of Romidepsin in Phase 1
NCT01456039 (24) [back to overview]Apparent Volume of Distribution (Vz/F) of Romidepsin in Phase 1
NCT01482962 (12) [back to overview]Time to Response
NCT01482962 (12) [back to overview]Time to Disease Progression (TTP)
NCT01482962 (12) [back to overview]Overall Response Rate (ORR) Based on Independent Review Committee (IRC) Assessment
NCT01482962 (12) [back to overview]Duration of Response (DOR)
NCT01482962 (12) [back to overview]Complete Response (CR) Rate
NCT01482962 (12) [back to overview]Number of Participants With Clinically Important Abnormal Laboratory Values Reported as AEs
NCT01482962 (12) [back to overview]Progression-Free Survival (PFS) Based on IRC Assessment
NCT01482962 (12) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT01482962 (12) [back to overview]Number of Participants With Clinically Important Vital Sign Measurements Reported as AEs
NCT01482962 (12) [back to overview]Change Form Baseline in Reported Symptoms and Quality of Life (QoL) Assessment Per Functional Assessment of Cancer Therapy-Lymphoma (FACT-LYM) for Functioning and Symptoms
NCT01482962 (12) [back to overview]Time to Subsequent Antineoplastic Therapy
NCT01482962 (12) [back to overview]Overall Survival (OS)
NCT01738594 (1) [back to overview]Number of Patients With Dose Limiting Toxicities (DLTs)
NCT01822886 (5) [back to overview]Overall Response Rate (ORR)
NCT01822886 (5) [back to overview]Complete Remission (CR) Rate
NCT01822886 (5) [back to overview]Overall Survival is Measured From the Date of Study Entry to the Date of Patient's Death
NCT01822886 (5) [back to overview]Percentage of Participants With Progression-Free Survival
NCT01822886 (5) [back to overview]Safety - Frequency of Toxicities Grade 3 and 4
NCT01933594 (40) [back to overview]PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Dolutegravir or Raltegravi) in Cohort 4
NCT01933594 (40) [back to overview]PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3
NCT01933594 (40) [back to overview]PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Dolutegravir or Raltegravi) in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Histone Acetylation (Median FITC Ac-Histone) in CD3+ Cells in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Cell-associated HIV-1 RNA Levels in Resting CD4 T-cells in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Cell-associated HIV-1 RNA Levels in Resting CD4 T Cells in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Cell-associated HIV-1 RNA Levels in PBMCs in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD4+ T-cells) in Cohort 4
NCT01933594 (40) [back to overview]PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3
NCT01933594 (40) [back to overview]PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3
NCT01933594 (40) [back to overview]PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3
NCT01933594 (40) [back to overview]HIV-1 RNA Levels in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Cell-associated HIV-1 RNA Levels in PBMCs in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in CD4+ T Cell Percent in Cohort 4
NCT01933594 (40) [back to overview]Proportion of Participants With Grade 3 or Higher Adverse Events (AEs) in Cohorts 1-3 Romidepsin Arms
NCT01933594 (40) [back to overview]Proportion of Participants With Grade 3 or Higher Adverse Events (AEs) in Cohort 4 Romidepsin Arm
NCT01933594 (40) [back to overview]Number of Participants With Reported Grade 2-4 AEs in Cohorts 1-3
NCT01933594 (40) [back to overview]Number of Participants With Reported Grade 2-4 AEs in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD4+ T-cells) in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD8+ T-cells) in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD8+ T-cells) in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD4+ T-cells) in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD4+ T-cells) in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD8+ T-cells) in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD8+ T-cells) in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Histone Acetylation in (Median FITC Ac-histone) in CD3+ Cells in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Percentage of CD4+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Percentage of CD4+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Percentage of CD8+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Percentage of CD8+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in PTEF-b Phosphorylation (pNFKB+% and pS175%) in CD4+ T-cells in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in PTEF-b Phosphorylation (pNFKB+% and pS175%) in CD8+ T-cells in Cohorts 1-3
NCT01933594 (40) [back to overview]Change From Baseline in PTEF-b Phosphorylation (pNFKB+%) in CD4+ T-cells in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in PTEF-b Phosphorylation (pS175+%) in CD4+ T-cells in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Total HIV-1 DNA in PBMCs in Cohort 4
NCT01933594 (40) [back to overview]Change From Baseline in Total HIV-1 DNA in Resting or Total CD4 T Cells in Cohorts 1-3
NCT01979276 (1) [back to overview]Time to Disease Progression (Progression Free Survival)
NCT02092116 (5) [back to overview]Part A: Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT02092116 (5) [back to overview]Part A: Changes From Baseline in HIV-1 Reservoir (Total HIV-1DNA; Integrated HIV-1 DNA in Unfractionated CD4+ T Cells and Replication Competent Provirus. Estimates of Change From Baseline of the Size of the Latent HIV-1 Reservoir in CD4+ Cells.
NCT02092116 (5) [back to overview]Part B: Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT02092116 (5) [back to overview]Part B: Level of HIV-1 Transcription.
NCT02092116 (5) [back to overview]Part B: Changes From Baseline in HIV-1 Reservoir (Total HIV-1DNA; Integrated HIV-1 DNA in Unfractionated CD4+ T Cells and Replication Competent Provirus.
NCT02203578 (9) [back to overview]Total Duration of Immunosuppressive Therapy
NCT02203578 (9) [back to overview]Rate of Documented Infection
NCT02203578 (9) [back to overview]Incidence of cGVHD
NCT02203578 (9) [back to overview]Incidence of aGVHD
NCT02203578 (9) [back to overview]Incidence of cGVHD
NCT02203578 (9) [back to overview]Incidence of cGVHD
NCT02203578 (9) [back to overview]T Cell Kinetics - Reconstitution
NCT02203578 (9) [back to overview]Incidence of cGVHD
NCT02203578 (9) [back to overview]Incidence of cGVHD
NCT02850016 (5) [back to overview]Change in the Size of the Proviral HIV-1 Reservoir
NCT02850016 (5) [back to overview]Days to Viral Rebound During Analytical Treatment Interruption (ATI)
NCT02850016 (5) [back to overview]HIV-1 Transcriptional Activity as Determined by Unspliced HIV-1 RNA (CA usHIV-1 RNA) in Circulating Total CD4+ T Cells.
NCT02850016 (5) [back to overview]Plasma HIV-1 RNA
NCT02850016 (5) [back to overview]Number of of Adverse Events (AE), Serious Adverse Events (SAE), and Serious Unexpected Serious Adverse Reactions (SUSAR).
NCT03534180 (2) [back to overview]Number of Patients With Grade 3 or Above Toxicities
NCT03534180 (2) [back to overview]Overall Survival at 100 Days
NCT03770000 (3) [back to overview]Overall Response Rate (ORR) With Tenalisib and Romidepsin Combination
NCT03770000 (3) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT03770000 (3) [back to overview]Duration of Response (DoR) With Tenalisib and Romidepsin Combination

Fold Change in Histone Acetylation

Fold change is calculated by dividing the level of histone acetylation in a treated sample (at 4, 24, and 48 hours) measured as intensity on a dot blot immunoassay, divided by the intensity in the pre-treatment sample. We considered a ≥ 2-fold change a measurable difference, and indicative of successful HDAC inhibition by romidepsin (depsipeptide). (NCT00007345)
Timeframe: 4 hours, 24 hours, and 48 hours after Romidepsin

,
InterventionFold change (Median)
4 hours24 hours48 hours
Cutaneous T-cell Lymphoma (CTCL)3.001.781.67
Peripheral T-cell Lymphoma (PTCL)2.991.970.62

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Number of Participants With Adverse Events

Here is the number of participants with adverse events. For a detailed list of adverse events, see the adverse event module. (NCT00007345)
Timeframe: 147 months and 5 days

Interventionparticipants (Number)
Peripheral T-cell Lymphoma (PTCL)47
Cutaneous T-cell Lymphoma (CTCL)84

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Time to Progression

Time to progression is defined from the first day of therapy until documentation of progressive disease. Progressive disease (PD) is at least a 20% increase in the sum of the target lesions, or the appearance of one or more new lesions. Lymph node disease was assessed bi-dimensionally using the International Working Group (IWG) criteria. Bone marrow involvement, as recommended by IWG criteria, and presence of circulating malignant T-cells ascertained by flow cytometry. (NCT00007345)
Timeframe: Until disease progression, or 30 days following off study date

InterventionMonths (Median)
Peripheral T-cell Lymphoma (PTCL)4.8
Cutaneous T-cell Lymphoma (CTCL)6.4

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Duration of Response (DOR)

DOR is defined as the date response was noted until disease was no longer considered to be responding. Response was assessed by the Response Evaluation Criteria in Solid Tumors (RECIST) criteria and the International Working Group Criteria (IWG).Complete response (CR) required clearing of all known disease sites. Partial response (PR) required documented response in skin (≥ 30% per RECIST) or lymph nodes (≥ 50% per the International Working Group (IWG) criteria, with response in both compartments for a determination of PR, IWG guidelines. Stable disease (SD) is neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD. Progressive disease (PD) is at least a 20% increase in the sum of the target lesions, or the appearance of one or more new lesions. Lymph node disease was assessed bi-dimensionally using the IWG criteria. Bone marrow involvement, as recommended by IWG criteria, and presence of circulating malignant T-cells ascertained by flow cytometry. (NCT00007345)
Timeframe: up to 127 months

,
InterventionMonths (Median)
Complete Response/Partial ResponseComplete Response
Cutaneous T-cell Lymphoma (CTCL)13.819.3
Peripheral T-cell Lymphoma (PTCL)974

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Number of Participants With a Response

A rigorous composite assessment was employed with uni-dimensional measurements of skin and visceral disease sites assessed by the Response Evaluation Criteria in Solid Tumors (RECIST). Complete response (CR) required clearing of all known disease sites. Partial response (PR) required documented response in skin (≥ 30% per RECIST) or lymph nodes (≥ 50% per the International Working Group (IWG) criteria, with response in both compartments for a determination of PR, IWG guidelines. Stable disease (SD) is neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD. Progressive disease (PD) is at least a 20% increase in the sum of the target lesions, or the appearance of one or more new lesions. Lymph node disease was assessed bi-dimensionally using the IWG criteria. Bone marrow involvement, as recommended by IWG criteria, and presence of circulating malignant T-cells ascertained by flow cytometry. (NCT00007345)
Timeframe: up to 56.5 days

,
Interventionparticipants (Number)
Complete Response + Partial ResponseComplete ResponsePartial ResponseStable DiseaseProgressive diseaseNot Evaluable
Cutaneous T-cell Lymphoma (CTCL)2852332186
Peripheral T-cell Lymphoma (PTCL)17895185

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Multidrug Resistance Protein 1 (MDR1) or ATP-binding Cassette Sub-family B Member 1 (ABCB1) Gene Expression

Total ribonucleic acid (RNA) was isolated from peripheral blood mononuclear cells or patient tissue biopsies and analyzed by quantitative polymerase chain reaction (qPCR). Expression of MDR-1/ABCB1 was determined by qPCR relative to an RNA standard, then normalized to ribosomal RNA (rRNA). Fold change is calculated by dividing the level of MDR-1 in a treated sample (at 4, 24, and 48 hours) measured by qPCR, divided by MDR-1 in the pre-treatment sample. We considered a ≥ 2-fold change a measurable difference, and indicative of successful HDAC inhibition by romidepsin (depsipeptide). (NCT00007345)
Timeframe: 4 hours, 24 hours, and 48 hours after Romidepsin

,
InterventionFold change (Median)
4 hours24 hours48 hours
Cutaneous T-cell Lymphoma (CTCL)1.781.531.205
Peripheral T-cell Lymphoma (PTCL)2.741.50.545

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Median Number of Cycles of Depsipeptide Administered

Participants were administered Depsipeptide and cycles (each cycle is 21 days) were monitored from the prescribed dose or higher to determine reductions (if needed) to maintain tolerability. (NCT00007345)
Timeframe: 83 cycles (i.e., each cycle is 21 days)

InterventionCycles per patient (Median)
Peripheral T-cell Lymphoma (PTCL)3
Cutaneous T-cell Lymphoma (CTCL)4.5

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Disease Control (i.e., Achievement of Complete Response, Partial Response, or Stable Disease)

Tumor response was assessed every eight weeks per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions as assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR. Stable disease (SD) was defined as having no evidence of response (CR or PR) as best response to therapy, and no evidence of disease progression (appearance of new lesions or >/= 30% increase in target lesions) at 8 weeks. (NCT00084682)
Timeframe: Up to 2 years

Interventionparticipants (Number)
Stable DiseaseDisease progressionSymptomatic deterioration
Treatment (Romidepsin)292

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Response Rate Associated With Depsipeptide Therapy (Phase II)

"RECIST Complete Response (CR): Complete disappearance of all measurable and evaluable disease. No new lesions. No evidence of non-evaluable disease. Patients must be on no steroids.~Partial Response (PR): Greater than or equal to 50% decrease under baseline in the sum of products of perpendicular diameters of all measurable lesions. No progression of evaluable disease. No new lesions.~Stable/No Response: Does not qualify for CR, PR, or progression. The designation of Stable/No Response requires a minimum of 8 weeks duration.~Progression: 25% increase in the sum of products of all measurable lesions over smallest sum observed (over baseline if no decrease) OR clear worsening of any evaluable disease, OR appearance of any new lesion/site, OR clear clinical worsening or failure to return for evaluation due to death or deteriorating condition" (NCT00085540)
Timeframe: Up to 2 years

Interventionparticipants (Number)
Phase 2 Dose From Phase 1 - Romidepsin0

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Number of Participants With Dose-limiting Toxicities Due to Romidepsin Graded According to the NCI Common Toxicity Criteria (CTCAE Version 3.0) (Phase I)

"dose limiting toxicity defined as: ANC /= 3X ULN and T. Bili >/= 1.5 ULN~grade 3 Nausea, vomiting, fatigue and asymptomatic hypocalcemia (treatment may continue after discuss with PI)" (NCT00085540)
Timeframe: First 4 weeks of treatment

Interventionparticipants (Number)
Phase 1 Dose Escalation - Romidepsin0

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6 Months Progression-free Survival (Phase II)

evaluated patients with glioblastoma (GBM (35 patients) (NCT00085540)
Timeframe: At 6 months

Interventionpercentage of participants (Number)
Phase 2 Dose From Phase 1 - Romidepsin3

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Tumor Major Response Rate (Including Stable Disease) as Measured by RECIST Criteria

(NCT00098813)
Timeframe: From start of treatment to 8 weeks

Interventionparticipants (Number)
Stable DiseaseProgression of Disease
Treatment (Romidepsin)101

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Proportion of Patients With Response to Depsipeptide

"Response is evaluated using Solid Tumor Response Criteria (RECIST) and defined as either complete repose (CR) or partial response (PR).~Per RECIST criteria, CR = disappearance of all target and nontarget lesions; PR = at least 30% decrease in the sum of the longest diameters of target lesions from baseline, and persistence of one or more non-target lesion(s) and/or the maintenance of tumor marker level above the normal limits." (NCT00104884)
Timeframe: Assessed every 3 months if patient is < 2 years from study entry; every 6 months if patient is 2 - 3 years from study entry, up to 3 years

Interventionpercentage of participants (Number)
DepsipeptideNA

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Time to Objective Disease Response

Time to Objective Response was defined as the time in months from first dose date to the first date of objective disease response (later confirmed) and time to CCR was defined as the time in months from first dose date to the first date of CCR (later confirmed). (NCT00106431)
Timeframe: Up to 10 months

InterventionMonths (Median)
Romidepsin1.87

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Time to Disease Progression

Time To Progression was defined as the duration from the date of the first study drug dose to the date of progression (PD). In this analysis, pts who did not progress were censored at their last evaluation with an OPDREC assessment. (NCT00106431)
Timeframe: Up to 10 months; median duration of follow up was 6.1 months

InterventionMonths (Median)
Romidepsin8.28

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The Percent of Patients (Pts) With Objective Disease Response

The percent of pts with confirmed Objective Disease Response (confirmed best responses of complete response [CR], clinical complete response [CCR], or partial response [PR]). Responses were evaluated according to a composite assessment (Objective Primary Disease Response Evaluation Criteria - OPDREC). (NCT00106431)
Timeframe: 6 months

InterventionPercent of participants (Number)
Romidepsin34

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Percent of Pts With Objective Disease Control

The percent of pts with confirmed ODC (CR, CCR, PR and SD90) based on OPDREC was summarized. (NCT00106431)
Timeframe: Up to 10 months

InterventionPercent of participants (Number)
Romidepsin64

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Duration of Objective Disease Response

Duration of Objective Response was defined as the number of months from the date of the first disease response (clinical complete response [CCR], or partial response [PR]) (later confirmed) until the date of progression and was determined using Kaplan-Meier product-limit estimates. In this analysis, pts who did not progress were censored as of their last evaluation with an OPDREC assessment. (NCT00106431)
Timeframe: Up to 10 months; median duration of follow up was 5.1 months

InterventionMonths (Median)
Romidepsin14.91

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Duration of Objective Disease Control (ODC)

For pts with confirmed ODC (pts with CR, CCR, PR, SD90 [stable disease for 90 days]) based on OPDREC, duration of ODC was summarized with descriptive statistics, including number of censored observations, and 25th, 50th, 75th percentiles of distribution, based on Kaplan-Meier product limit estimates. For pts with confirmed progressive disease (PD), duration of ODC was calculated from first date of study drug to first date of diagnosis of confirmed PD. For pts without confirmed PD, duration of ODC was calculated from first date of study drug to date of the last visit with any OPDREC data. (NCT00106431)
Timeframe: Up to 10 months; median duration of follow up was 6.0 months

InterventionMonths (Median)
Romidepsin17.67

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Decrease in Pruritus Visual Analogue Scale (VAS) Score of ≥30 mm or a Score of 0 for at Least 2 Consecutive Cycles.

Pruritus was reported monthly by pts using a 0 (no itching) to 100 (unbearable itching) mm visual analog scale (VAS). Pts were considered to have significant pruritus if the baseline VAS score was ≥ 30 mm. Clinically meaningful reduction in pruritus was defined as a decrease in VAS score of ≥ 30 mm or a score of 0 for at least 2 consecutive cycles. (NCT00106431)
Timeframe: Up to 10 months

Interventionparticipants (Number)
Romidepsin25

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Time to Progression

Progressive disease is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameters (LD) of target lesions, taking as reference the smallest sum LD recorded since treatment started, or a measurable increase in a non-target lesion, or the appearance of new lesions. Time to progression is the number of months from first treatment until the date of progression. (NCT00112463)
Timeframe: Until disease progression - max of 48 months

Interventionmonths (Median)
Treatment (Single-agent Depsipeptide)1.9

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Objective Tumor Response (Complete and Partial)

Objective tumor response was evaluated using the criteria proposed by the Response Evaluation Criteria In Solid Tumors (RECIST) Committee (JNCI 92(3):205-216,2000). Changes in only the largest diameter (unidimensional measurement) of the target lesions are used. A sum of the longest diameter (LD) for all target lesions was calculated and reported as the baseline sum LD. The baseline sum LD was used as reference by which to characterize the objective tumor response. Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions, taking as reference the baseline sum LD; Overall Response (OR) = CR + PR (NCT00112463)
Timeframe: While on treatment - max of 16 months

InterventionParticipants (Count of Participants)
Treatment (Single-agent Depsipeptide)2

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Survival

Months from first treatment until death or the last date of contact (NCT00112463)
Timeframe: Max of 98 months

Interventionmonths (Median)
Treatment (Single-agent Depsipeptide)12.2

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Toxicity as Assessed Using the Expanded Common Toxicity Criteria Version 3

"The outcome reported here is the number (%) of participants who experienced grade 3 or greater toxicity while on study.~A summary of the individual toxicities can be found in the AE/SAE results." (NCT00112463)
Timeframe: During treatment (max of 16 months) and for 1 month following treatment

InterventionParticipants (Count of Participants)
Treatment (Single-agent Depsipeptide)13

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Number of Participants With a Dose-limiting Toxicity (DLT)

"Toxicities were assessed according to the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE), V 3.0. A DLT was one of the following, if considered at least possibly related to study treatment:~Grade 4 neutropenia for ≥5 days or febrile neutropenia; Grade 4 thrombocytopenia or need for a platelet transfusion; ≥ Grade 3 nausea and/or emesis despite using optimal antiemetic therapy; ≥ Grade 3 diarrhea despite using maximal supportive therapy; Any clinically significant Grade 3 or 4 nonhematologic toxicity; Inability to administer all doses in cycle 1." (NCT00379639)
Timeframe: 28 days

Interventionparticipants (Number)
Dose Level 13
Dose Level 21
Dose Level 50
Dose Level 62
Dose Level 80

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Number of Participants With Adverse Events (AEs)

"AEs were graded for severity according to the National Cancer Institute Common Terminology Criteria (NCI CTCAE), V 3.0: Grade 1: Mild; Grade 2: Moderate; Grade 3: Severe (prevents normal everyday activities); Grade 4: Life-threatening or disabling; Grade 5: Death.~A serious AE is associated with events that pose a threat to a patient's life or functioning, require hospitalization, is a congenital anomaly/birth defect or is an important medical event or condition that may jeopardize the patient and may require medical or surgical intervention to prevent one of the above outcomes." (NCT00379639)
Timeframe: From the date of first dose to 30 days after last dose (up to 236 days).

,,,,
Interventionparticipants (Number)
Any adverse event≥Grade 3 adverse eventGrade 4 adverse eventSerious adverse eventAdverse event leading to discontinuationAdverse event leading to death
Dose Level 1771300
Dose Level 2752200
Dose Level 51053410
Dose Level 6642100
Dose Level 8631211

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Best Overall Response

"Disease response was determined by the Investigator according to Response Evaluation Criteria in Solid Tumors (RECIST) criteria using computed tomography or magnetic resonance imaging:~Complete Response (CR): Disappearance of all target lesions; Partial Response (PR): At least a 30% decrease in the sum of the longest diameter (LD) of target lesions; Progressive Disease (PD): At least a 20% increase in the sum of the LD of target lesions or the appearance of ≥1 new lesions; Stable Disease (SD): Neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD." (NCT00379639)
Timeframe: Disease assessments were performed within 4 weeks of first dose and every 8 weeks thereafter (up to 236 days).

,,,,
Interventionparticipants (Number)
Complete ResponsePartial ResponseStable diseaseProgressive disease
Dose Level 10051
Dose Level 20142
Dose Level 50034
Dose Level 60013
Dose Level 80111

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Median Overall Survival

Survival time is defined as the time from registration to death due to any cause, measured in months. The distribution of survival time estimated using the method of Kaplan-Meier. (NCT00383565)
Timeframe: 5 Years

Interventionmonths (Median)
FR90122820

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Overall Objective Response Rate (Complete Response [CR] and Partial Response [PR]) After 6 Courses of Treatment

International Working Group response for non- Hodgkin's lymphoma: Complete Response (CR) - disappearance all detectable clinical/radiographic evidence of disease and disappearance of all disease-related symptoms (present before therapy) and normalization of those biochemical abnormalities; Partial Response (PR) - ≥50% decrease in sum products of greatest diameters (SPD) of 6 largest dominant nodes or nodal masses, selected by clearly measurable in at least two perpendicular dimensions, from disparate regions of body and no decrease in size of other nodes, liver, or spleen. (NCT00383565)
Timeframe: 24 weeks (6 courses of 4 week cycles)

Interventionparticipants (Number)
Complete ResponsePartial Response
FR90122801

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Median Progression Free-survival (PFS)

Time to disease progression is defined as the time from registration to documentation of disease progression. (NCT00383565)
Timeframe: 2 Years

Interventionmonths (Median)
FR9012284

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Percentage of Participants With Objective Disease Response

Objective disease response was defined as patients with a Complete Response, Unconfirmed Complete Response or a Partial Response (PR) according to the IWC 1999 assessed by an independent review committee: CR, Cru defined above, PR defined as ≥50% decrease in size of 6 largest dominant nodes and/or nodal masses & extranodal index lesions and no increase of non-index lesions, liver, or spleen; no new sites of disease evident; skin lesions decreased by ≥50%. (NCT00426764)
Timeframe: Response was assessed after every 2 cycles of treatment and at completion of therapy, up until 30 September 2012 (data cutoff for analysis). Maximum duration on study was 1931 days.

Interventionpercentage of participants (Number)
Romidepsin26.2

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Percentage of Participants With a Complete Response According to the International Workshop Response Criteria (IWC) for Non-Hodgkin's Lymphomas (NHL) Assessed by an Independent Review Committee

Complete Response (CR): >75% decrease in size aggregate of nodal index lesions (large and small), complete disappearance of extranodal and non-index lesions; total disappearance of clinical disease including skin involvement; disease-related signs and symptoms, normalization of biochemical abnormalities and reduction in size of spleen or liver so no longer palpable. Unconfirmed CR: all above criteria except all nodal index lesions must have regressed >75% in the sum of the product diameters (SPD) from baseline. Individual nodes previously confluent must have regressed by >75% in their SPD. (NCT00426764)
Timeframe: Response was assessed after every 2 cycles of treatment and at completion of therapy, up until 30 September 2012 (data cutoff for analysis). Maximum duration on study was 1931 days.

Interventionpercentage of participants (Number)
Romidepsin15.4

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Duration of Objective Disease Response

Duration of response was defined as the number of days from the date of the first disease response (Complete, Unconfirmed Complete or Partial Response) until the date of progression and was determined using Kaplan-Meier product-limit estimates. Progression was defined as: a ≥50% increase from the nadir in the individual sum of the products of the diameters of any index lesion; the reappearance of pathology, enlargement of liver/spleen, or unequivocal progression of non-measurable disease or appearance of any new lesions. (NCT00426764)
Timeframe: Response was assessed after every 2 cycles of treatment and at completion of therapy, up until 30 September 2012 (data cutoff for analysis). Maximum duration on study was 1931 days.

Interventiondays (Median)
RomidepsinNA

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Duration of Complete Disease Response

Duration of response was defined as the number of days from the date of the first disease response (Complete or Unconfirmed Complete) until the date of progression and was determined using Kaplan-Meier product-limit estimates. Progression was defined as: a ≥50% increase from the nadir in the individual sum of the products of the diameters of any index lesion; the reappearance of pathology, enlargement of liver/spleen, or unequivocal progression of non-measurable disease or appearance of any new lesions. (NCT00426764)
Timeframe: Response was assessed after every 2 cycles of treatment and at completion of therapy, up until 30 September 2012 (data cutoff for analysis). Maximum duration on study was 1931 days.

Interventiondays (Median)
RomidepsinNA

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Time to Disease Progression

Time to progression (≥50% increase from the nadir in the individual sum of the products of the diameters of any index lesion; the reappearance of pathology, enlargement of liver/spleen, or unequivocal progression of non-measurable disease or appearance of any new lesions) was defined as the duration from the date of the first study drug dose to the date of relapse or progression as reported by the independent review committee and was determined using Kaplan-Meier product-limit estimates. (NCT00426764)
Timeframe: Response was assessed after every 2 cycles of treatment and at completion of therapy, up until 30 September 2012 (data cutoff for analysis). Maximum duration on study was 1931 days.

Interventiondays (Median)
Romidepsin182

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Change in Eastern Cooperative Oncology Group (ECOG) Performance Status

The ECOG scale is as follows: Grade 0: Fully active, able to perform all pre-disease activities without restriction; Grade 1: Restricted in physically strenuous activity, ambulatory, able to carry out light work; Grade 2: Ambulatory and capable of all self-care but unable to work. Up and about more than 50% of waking hours; Grade 3: Capable of only limited self-care, confined to bed or chair > 50% of waking hours; Grade 4: Completely disabled. Cannot carry on any self-care. Confined to bed or chair. Data reported is the shift from Baseline ECOG score to best on-study assessment score. (NCT00426764)
Timeframe: From Baseline up until 30 September 2012 (data cutoff for analysis). Maximum duration on study was 1931 days.

,,,,,
Interventionparticipants (Number)
Missing Baseline ECOG ScoreBaseline ECOG Score = 0Baseline ECOG Score = 1Baseline ECOG Score = 2Baseline ECOG Score = 3Baseline ECOG Score = 4
Best ECOG = 002613100
Best ECOG = 101635600
Best ECOG = 20112600
Best ECOG = 3004200
Best ECOG = 4012100
Missing121100

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

An adverse event or experience (AE) is defined as any untoward medical occurrence, which does not necessarily have to have a causal relationship with this treatment. A serious AE is any untoward medical occurrence that at any dose: results in death; is life-threatening; requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; is an important medical event or condition. Related AEs are defined as those considered by the Investigator to have a possible, probable, or very likely/certain relationship to the study drug. AEs were graded as mild (1), moderate (2), severe (3), lifethreatening (4), or death (5). TEAEs occurred from the first dose of study medication through the end of the study (30 days post last dose) or any event that was present at baseline but worsened in intensity or was subsequently considered drug-related by the Investigator through end of study. (NCT00426764)
Timeframe: From first dose of study treatment until the final study visit, which occurred 30 days after receiving the last dose. Mean duration of treatment up until 30 September 2012 (data cutoff for analysis) was 169 days.

InterventionParticipants (Count of Participants)
TEAE≥ Grade 3 TEAE≥ Grade 4 TEAESerious TEAETEAE Leading to DiscontinuationDeaths within 30 days of Last Dose
Romidepsin128892761258

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Total Volume of Distribution (Vz)

Total volume of distribution of Romidepsin (NCT00765102)
Timeframe: Day 1 (cycle 1): 1 hour prior to romidepsin administration, 0.25, 0.5, 1, 2, 3, 4, 6, and 24 hours after initiation of romidepsin infusion

InterventionL (Geometric Mean)
Romidepsin 8 mg/m^2 + Bortezomib66.5
Romidepsin 10 mg/m^2 + Bortezomib85.9

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Participants With Treatment-emergent Adverse Events (TEAEs)

Counts of participants with TEAEs, and subset by relation to drug, grade of severity, serious, TEAEs leading to discontinuation or leading to death. AEs were graded for severity according to the National Cancer Institute Common Terminology Criteria (NCI CTCAE), V 3.0: Grade 1: Mild; Grade 2: Moderate; Grade 3: Severe (prevents normal everyday activities); Grade 4: Life-threatening or disabling; Grade 5: Death. (NCT00765102)
Timeframe: up to 9 months

Interventionparticipants (Number)
At least 1 TEAEAt least 1 drug-related TEAEAt least 1 Romidepsin-related TEAEAt least 1 Bortezomib-related TEAEAt least 1 >=Grade 3 TEAEAt least 1 Grade 4 TEAEAt least 1 serious TEAEAt least 1 TEAE leading to discontinuationAt least 1 TEAE leading to death
Romidepsin + Bortezomib323028302851462

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Maximum Observed Concentration (Cmax)

Maximum observed concentration of Romidepsin (NCT00765102)
Timeframe: Day 1 (cycle 1): 1 hour prior to romidepsin administration, 0.25, 0.5, 1, 2, 3, 4, 6, and 24 hours after initiation of romidepsin infusion

Interventionng/mL (Geometric Mean)
Romidepsin 8 mg/m^2 + Bortezomib913.9
Romidepsin 10 mg/m^2 + Bortezomib1002.7

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Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-∞)

AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞) of Romidepsin based on plasma samples. (NCT00765102)
Timeframe: Day 1 (cycle 1): 1 hour prior to romidepsin administration, 0.25, 0.5, 1, 2, 3, 4, 6, and 24 hours after initiation of romidepsin infusion

Interventionng*hr/mL (Geometric Mean)
Romidepsin 8 mg/m^2 + Bortezomib1209.1
Romidepsin 10 mg/m^2 + Bortezomib1149.5

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Terminal Half-life (t1/2)

Terminal half-life of Romidepsin (NCT00765102)
Timeframe: Day 1 (cycle 1): 1 hour prior to romidepsin administration, 0.25, 0.5, 1, 2, 3, 4, 6, and 24 hours after initiation of romidepsin infusion

Interventionhr (Geometric Mean)
Romidepsin 8 mg/m^2 + Bortezomib4.1
Romidepsin 10 mg/m^2 + Bortezomib3.6

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Time to Maximum Observed Concentration (Tmax)

Time to maximum observed concentration of Romidepsin (NCT00765102)
Timeframe: Day 1 (cycle 1): 1 hour prior to romidepsin administration, 0.25, 0.5, 1, 2, 3, 4, 6, and 24 hours after initiation of romidepsin infusion

Interventionhr (Median)
Romidepsin 8 mg/m^2 + Bortezomib1.04
Romidepsin 10 mg/m^2 + Bortezomib0.58

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Total Clearance (CL)

Total clearance of Romidepsin (NCT00765102)
Timeframe: Day 1 (cycle 1): 1 hour prior to romidepsin administration, 0.25, 0.5, 1, 2, 3, 4, 6, and 24 hours after initiation of romidepsin infusion

InterventionL/hr (Geometric Mean)
Romidepsin 8 mg/m^2 + Bortezomib11.3
Romidepsin 10 mg/m^2 + Bortezomib16.4

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Area Under the Concentration-time Curve (AUC0 t) of Romidepsin in Combination With Erlotinib

AUC0 t was measured in the time interval from 0 to time (t) when the last blood sample is collected with a concentration above the limit of quantification. (NCT01302808)
Timeframe: 0, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72 hours post-dose on Days 1 and 8

,
Interventionng*h/ml (Mean)
Dosing day / Day 1Dosing day / Day 8
Cohort 2 (10mg/m2) +Cohort 3 ( Modified Prophylaxis @ 10 mg/m2)2185.521851.84
Erlotinib Plus Romidepsin Cohort 1 (8mg/m2) + Cohort 4 (Modified Prophylaxis @ 8 mg/m2)1207.00989.19

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Number of Participants With Dose Limiting Toxicities and Maximum Tolerated Dose (MTD)

Dose limiting toxicities per Protocol definition using (CTCAE), Version 3.0 (NCT01302808)
Timeframe: 12 months

InterventionParticipants (Count of Participants)
Cohort 1 (Erlotinib Plus Romidepsin (8 mg/m^2))0
Cohort 2 (Erlotinib Plus Romidepsin (10 mg/m^2))2
Cohort 3 (Erlotinib Plus Romidepsin (10 mg/m^2)) + Antiemetic Prophylaxis0
Cohort 4 (Erlotinib Plus Romidepsin (8 mg/m^2)) + Antiemetic Prophylaxis0

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Area Under the Plasma Concentration Time-curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t)of Romidepsin

AUC0-t: area under the plasma concentration time-curve from Time 0 to the time of the last quantifiable concentration (Ct), calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing. For AUC0-t, an analysis of variance (ANOVA) model was used to estimate the ratio of geometric means and its 90% CI between romidepsin alone and romidepsin in the presence to ketoconazole. (NCT01324310)
Timeframe: Days 1 and 8; at 0 (pre-dose) 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 1911.0
Romidepsin and Ketoconazole Day 81020.7

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Estimate of the Terminal Elimination Half-life in Plasma (t1/2)

Terminal elimination half-life (t1/2) in plasma, was calculated as [(ln 2)/λz] (NCT01324310)
Timeframe: Days 1 and 8; at 0 (pre-dose),1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionhours (Geometric Mean)
Romidepsin Day 19.69
Romidepsin and Ketoconazole Day 810.171

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Maximum Observed Plasma Concentration (Cmax)

Cmax: maximum observed plasma concentration, obtained directly from the observed concentration versus time data; for Cmax, an analysis of variance (ANOVA) model was used to estimate the ratio of geometric means and its 90% confidence interval (CI) between romidepsin alone and romidepsin in the presence of ketoconazole (NCT01324310)
Timeframe: Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng/mL (Geometric Mean)
Romidepsin Day 1229.05
Romidepsin and Ketoconazole Day 8224.79

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Time to Maximum Observed Plasma Concentration (Tmax)

Tmax: time to maximum observed Tmax, obtained directly from the observed concentration versus time data (NCT01324310)
Timeframe: Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionhours (Median)
Romidepsin Day 13.257
Romidepsin and Ketoconazole Day 82.992

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Area Under the Plasma Concentration Time-curve From Time 0 Extrapolated to Infinity (AUC0-∞)

AUC0-∞: area under the plasma concentration time-curve from Time 0 extrapolated to infinity, calculated as [AUCt + Ct/λz]. (NCT01324310)
Timeframe: Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 1915.3
Romidepsin and Ketoconazole Day 81027.6

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Summary of Participants With Treatment Emergent Adverse Events (TEAEs)

All 15 subjects in the safety population received at least 1 dose of romidepsin. AEs were considered related if assessed by the Investigator as possibly, probably or definitely related to study drug. Serious AEs (SAEs) are those that resulted in death, were life-threatening, required or prolonged inpatient hospitalization, resulted in persistent or significant disability/incapacity, congenital anomaly, or resulted in an important medical event that may have jeopardized the patient or required medical or surgical intervention to prevent one of the outcomes listed above. (NCT01324310)
Timeframe: Day 1 up to Day 36 (28 days after last treatment)

Interventionparticipants (Number)
= > 1 TEAE= > 1 TEAE related to any study drug= > 1 TEAE related to Romidepsin= > 1 TEAE related to Ketoconazole= > 1 Serious TEAE= > 1 Serious TEAE related to any drug= > 1 Serious TEAE related to Romidepsin= > 1 Serious TEAE related to Ketoconazole= > 1 TEAE leading to discontinuation= > 1 TEAE related discontinuation due to any drug= > 1 Romidepsin related TEAE discontinuation= > 1 Ketoconazole related TEAE discontinuationParticipants who died
Romidepsin Plus Ketoconazole1514144411010003

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Apparent Total Plasma Clearance (CL)

Apparent total plasma clearance, (CL) calculated as [Dose/AUC 0-∞]. (NCT01324310)
Timeframe: Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

InterventionL/hr (Geometric Mean)
Romidepsin Day 116.922
Romidepsin and Ketoconazole Day 814.84

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Apparent Total Volume of Distribution (Vz)

Vz: apparent total volume of distribution, calculated as [(CL)/λz]. (NCT01324310)
Timeframe: Days 1 and 8, At 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

InterventionLiter (Geometric Mean)
Romidepsin Day 1236.4
Romidepsin and Ketoconazole Day 8217.78

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Area Under the Plasma Concentration Time-curve From Time 0 to 24-hour (AUC 0-24)

AUC 0-24: area under the plasma concentration time-curve from Time 0 to 24 hours, calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing; for AUC 0-24 an analysis of variance (ANOVA) model was used to estimate the ratio of geometric means and its 90% confidence interval (CI) between romidepsin alone and romidepsin in the presence of ketoconazole (NCT01324310)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 1900.1
Romidepsin and Ketoconazole Day 81002.2

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Apparent Total Volume of Distribution (Vz).

Apparent total volume of distribution (Vz) was calculated as [(CL)/λz] for Romidepsin and co-administered with Rifampin. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

InterventionLiters (Geometric Mean)
Romidepsin Day 1161.48
Romidepsin and Rifampin Day 877.6

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Area Under the Plasma Concentration Time-curve From Time 0 to 24-hour (AUC0-24) for Romidepsin

Individual and mean romidepsin plasma concentrations by treatment and scheduled time data were collected. AUC0-24: area under the plasma concentration time-curve from Time 0 to 24 hours, calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing. (NCT01324323)
Timeframe: Day 1 and Day 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 12204.2
Romidepsin and Rifampin Day 83903.9

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Area Under the Plasma Concentration Time-curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t)of Romidepsin

AUC0-t: area under the plasma concentration time-curve from Time 0 to the time of the last quantifiable concentration (Ct), calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 12225.1
Romidepsin and Rifampin Day 83966.3

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Area Under the Plasma Concentration Time-curve From Time Zero Extrapolated to Infinity (AUC0-∞).

AUC0-∞: area under the plasma concentration time-curve from Time 0 extrapolated to infinity, calculated as [AUCt + Ct/λz]. λz is the apparent terminal rate constant. No AUC extrapolation was performed with unreliable λz. If the percentage of AUC extrapolated is ≥ 25%, AUC0-∞ will not be reported. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 12229.8
Romidepsin and Rifampin Day 83980.7

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Clearance (CL): Apparent Total Plasma Clearance.

The apparent total plasma clearance (CL) was calculated as [Dose/AUC0-∞] for Romidepsin alone and co-administered with rifampin plasma concentrations. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

InterventionL/hr (Geometric Mean)
Romidepsin Day 111.59
Romidepsin and Rifampin Day 86.45

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Estimate of the Terminal Elimination Half-life in Plasma (t1/2)

The terminal elimination half-life (t1/2) in plasma, was calculated as [(ln 2)/λz]. This was only calculated when a reliable estimate for λz could be obtained. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionhours (Geometric Mean)
Romidepsin Day 19.666
Romidepsin and Rifampin Day 88.341

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Maximum Observed Plasma Concentration (Cmax)of Romidepsin

Maximum observed plasma concentration (Cmax)was obtained directly from the observed concentration versus time data. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng/mL (Geometric Mean)
Romidepsin Day 1571.2
Romidepsin and Rifampin Day 8900.1

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Summary of Participants With Treatment Emergent Adverse Events (TEAEs)

AEs were considered related if assessed by the Investigator as possibly, probably or definitely related to study drug. Serious AEs (SAEs) are those that resulted in death, were life-threatening, required or prolonged inpatient hospitalization, resulted in persistent or significant disability/incapacity, congenital anomaly, or resulted in an important medical event that may have jeopardized the patient or required medical or surgical intervention to prevent one of the outcomes listed above. (NCT01324323)
Timeframe: Day 1 up to Day 36 (28 days after the last treatment)

Interventionparticipants (Number)
= > 1 TEAE= > 1 TEAE related to any study drug= > 1 TEAE related to Romidepsin= > 1 TEAE related to Rifampin= > 1 Serious TEAE= > 1 Serious TEAE related to any drug= > 1 Serious TEAE related to Romidepsin= > 1 Serious TEAE related to Rifampin= > 1 TEAE leading to discontinuation= > 1 TEAE related discontinuation to any drug= > 1 Romidepsin related TEAE discontinuation= > 1 Rifampin related TEAE discontinuationParticipants who died
Romidepsin Plus Rifampin1313132211100000

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Time to Maximum Observed Plasma Concentration (Tmax)

Time to maximum observed plasma concentration (Tmax) was obtained directly from the observed concentration versus time data. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionhours (Median)
Romidepsin Day 13.0
Romidepsin and Rifampin Day 83.00

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Summary of Participants With Treatment Emergent Adverse Events (TEAEs)

An adverse event (AE) is any noxious, unintended, or untoward medical occurrence that may appear or worsen in a participant during the course of a study. Adverse events were assessed using National Cancer Institute, Common Terminology Criteria for Adverse Events (NCI CTCAE), Version 4: On the following is the scale: Grade 1 = Mild AE, Grade 2 = Moderate AE, Grade 3 = Severe and Undesirable AE, Grade 4 = Life-threatening or Disabling AE, and Grade 5 = Death. Serious AEs (SAEs) are those that resulted in death, were life-threatening, required or prolonged inpatient hospitalization, resulted in persistent or significant disability/incapacity, congenital anomaly, or resulted in an important medical event that may have jeopardized the patient or required medical or surgical intervention. A TEAE is defined as any AE occurring or worsening on or after the first dose of study drug and within 28 days after the last dose of study drug. (NCT01353664)
Timeframe: All AEs were recorded by the Investigator from the time the participant signed the informed consent to 28 days after the last dose of study drug; maximum drug exposure was 231 days

InterventionParticipants (Number)
≥ 1 Adverse Event (AE)≥ 1 AE related to study drug≥ 1 NCI CTCAE Grade 3 AE≥ 1 NCI CTCAE Grade 4-5 AE≥ 1 NCI CTCAE Grade 3 AE related to study drug≥ 1 NCI CTCAE Grade 4-5 AE related to study drug≥ 1 Serious Adverse Event (SAE)≥ 1 SAE related to study drug≥ 1 AE leading to discontinuation≥ 1 AE leading to stopping the study drug≥ 1 AE leading to dose reduction/interruption≥1 AE dose reduction related to study drug
ROMI 4181411060611074

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Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC∞) of Romidepsin in Phase 1

Area under the plasma concentration-time curve from time zero extrapolated to infinity (AUC∞) of romidepsin on Day 1; if possible the area under the concentration-time curve from time zero to infinity, calculated by the linear trapezoidal rule and extrapolated to infinity was calculated according to the following equation: AUC∞ = AUCt + (Ct/ λz ), where Ct is the last quantifiable concentration. (NCT01456039)
Timeframe: Day 1 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionng*h/mL (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^21027.08
Phase 1: Cohort 2: Romidepsin 14mg/m^22330.91

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Area Under the Plasma Concentration-time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of Romidepsin in Phase 1

Area under the plasma concentration-time curve from time zero to the last quantifiable time point, calculated by the linear trapezoidal rule when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing. (NCT01456039)
Timeframe: Day 1 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionng*h/mL (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^21023.76
Phase 1: Cohort 2: Romidepsin 14mg/m^22325.55

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AUC0-t, Accumulation Ratio of Romidepsin in Phase 1, Cycle 1

Area under the plasma concentration-time curve from time zero to the last quantifiable time point; accumulation ratio calculated as AUC (0-t),ss/AUC (0-t) (NCT01456039)
Timeframe: Day 1 and Day 15 in Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionratio (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^21.00
Phase 1: Cohort 2: Romidepsin 14mg/m^20.83

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AUC0-t, at Steady State (ss) of Romidepsin in Phase 1 at Cycle 1, Day 15

Area under the plasma concentration-time curve from time zero to the last quantifiable time point at steady state, calculated by the linear trapezoidal rule when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing (NCT01456039)
Timeframe: Day 15 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionng*h/mL (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^21024.66
Phase 1: Cohort 2: Romidepsin 14mg/m^21825.74

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Cmax Accumulation Ratio of Romidepsin in Phase 1, Cycle 1

Cmax of Romidepsin: accumulation ratio based on Cmax calculated as Cmax,ss/Cmax (NCT01456039)
Timeframe: Day 1 and Day 15 in Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at end of administration) hours after the start of administration, 0.25, 0.5, 1, 2, 4, 6, 20, and 44 hours after the end of administration. Day 8, Cycle 1, samples collected at 0 hour

Interventionratio (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^20.93
Phase 1: Cohort 2: Romidepsin 14mg/m^20.86

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Cmax, ss of Romidepsin in Phase 1 at Cycle 1, Day 15

Maximum observed concentration in plasma at steady state (NCT01456039)
Timeframe: Day 15 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionng/mL (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^2250.05
Phase 1: Cohort 2: Romidepsin 14mg/m^2489.47

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Kaplan Meier (K-M) Estimate of Time to Progression (TTP) in PTCL Participants Based on the Modified 2007 IWC as Assessed by IER

Time to progression (≥50% increase from the nadir in the individual sum of the products of the diameters of any index lesion; the reappearance of pathology, enlargement of liver/spleen, or unequivocal progression of non-measurable disease or appearance of any new lesions) was defined as the duration from the date of the first study drug dose to the date of relapse or progression (NCT01456039)
Timeframe: Median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventiondays (Median)
Phase 1: Cohort 1: Romidepsin 9mg/m^2NA
Phase 1: Cohort 2: Romidepsin 14mg/m^2899.00
Phase 2: Romidepsin 14mg/m^2179.00
Total: Romidepsin 14mg/m^2179.00

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Kaplan Meier Estimate of Duration of Response (DOR) for PTCL Responders Based on the Modified 1999 IWC as Assessed by the IER.

DOR was defined as the number of days from the date of the first disease response (Complete, Unconfirmed Complete or Partial Response) until the date of progression, analyzed using Kaplan-Meier methods. (NCT01456039)
Timeframe: Median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventiondays (Median)
Phase 1: Cohort 2: Romidepsin 14mg/m^2106.00
Phase 2: Romidepsin 14mg/m^2337.00
Total: Romidepsin 14mg/m^2337.00

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Kaplan Meier Estimate of Duration of Response (DOR) for PTCL Responders Based on the Modified 2007 IWC as Assessed by the IER.

DOR was defined as the number of days from the date of the first disease response (Complete, Unconfirmed Complete or Partial Response) until the date of progression, analyzed using Kaplan-Meier methods. (NCT01456039)
Timeframe: Median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventiondays (Median)
Phase 1: Cohort 2: Romidepsin 14mg/m^2163.00
Phase 2: Romidepsin 14mg/m^2337.00
Total: Romidepsin 14mg/m^2163.00

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Kaplan Meier Estimate of Time to Progression (TTP) in PTCL Participants Based on the 1999 IWC as Assessed by IER

Time to progression (≥50% increase from the nadir in the individual sum of the products of the diameters of any index lesion; the reappearance of pathology, enlargement of liver/spleen, or unequivocal progression of non-measurable disease or appearance of any new lesions) was defined as the duration from the date of the first study drug dose to the date of relapse or progression (NCT01456039)
Timeframe: Median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventiondays (Median)
Phase 1: Cohort 1: Romidepsin 9mg/m^2114.00
Phase 1: Cohort 2: Romidepsin 14mg/m^2899.00
Phase 2: Romidepsin 14mg/m^2170.00
Total: Romidepsin 14mg/m^2179.00

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Maximum Plasma Concentration (Cmax) of Romidepsin in Phase 1

The maximum observed plasma concentration of romidepsin (Cmax) obtained directly from the observed concentration versus time data (NCT01456039)
Timeframe: Day 1 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionng/mL (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^2269.75
Phase 1: Cohort 2: Romidepsin 14mg/m^2593.47

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Number of Participants With Dose-limiting Toxicity (DLT) in Accordance With National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0 as Determined by the Efficacy and Safety Evaluation Committee (ESEC)

DLT was defined as an adverse event (AE) occurring in Cycle 1 in Phase 1 and judged that the causal relationship to the investigational product could not be denied. The severity of all AEs was graded based upon the NCI CTCAE version 3.0. DLTs were defined as: • Grade 4 Hemoglobin <6.5 g/dL • Grade 4 Neutrophil <500/μL continuing for at least 5 days • Febrile neutropenia (Grade 4 neutropenia caused by fever and ≥ 38.5° C for more than 1 hour) • Grade 4 thrombocyte (< 25,000/μL), or thrombocytopenia with hemorrhage requiring platelet transfusion • Nausea, vomiting, or diarrhea at > grade 3 in spite of treatment • Grade 3 ALT (alanine aminotransferase) or AST (aspartate aminotransferase) values continued for 7 days. • Grade 4 ALT or AST • Grade 2 arrhythmia • Grade 4 non-hematological AEs • Other grade 3 non-hematological AEs except transient fatigue, anorexia, hyponatremia, and tumor lysis syndrome • Other AEs leading to discontinuation of administration (NCT01456039)
Timeframe: Up to Day 28; Cycle 1

Interventionparticipants (Number)
Phase 1: Cohort 1: Romidepsin 9mg/m^20
Phase 1: Cohort 2: Romidepsin 14mg/m^20

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Percentage of PTCL Participants With an Overall Best Response in Accordance With a Modified International Workshop Response Criteria (IWC) 1999 in Phase 2

Objective disease response in PTCL was defined as patients with a complete response (CR), unconfirmed complete response (CRu) or a partial response (PR) according to modified IWC 1999 criteria and assessed by an independent efficacy reviewer. A CR is >75% decrease in size of maximum 6 largest target within nodal and extranodal lesions, complete disappearance of other nodal and extranodal; total disappearance of clinical disease; disease-related signs and symptoms, normalization of biochemical abnormalities, disappearance of spleen, liver, or kidney enlargement; no bone marrow (BM) involvement, no new sites of disease. CRu: all above criteria fulfilled except for BM involvement is indeterminate. PR: a ≥50% decrease in size of 6 largest target lesions and no increase other nodal and extranodal; no progression of clinical disease; disease-related signs and symptoms, normalization or biochemical abnormalities, no progression in size of liver, spleen, or kidney; and no new sites of disease (NCT01456039)
Timeframe: Tumor assessments performed every 2 months; median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventionpercentage of participants (Number)
Phase 1: Romidepsin 9mg/m^20
Phase 1: Romidepsin 14mg/m^266.7
Phase 2: Romidepsin 14mg/m^242.5
Total: Romidepsin 14mg/m^245.7

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Percentage of PTCL Participants With the Best Response in Accordance With the Modified 2007 International Workshop Response Criteria as Assessed by IER

Objective disease response in PTCL was defined as achieving a CR or PR based on the Modified 2007 IWC. A CR = a complete disappearance of all disease; lymph node mass regression to normal size on computerized tomography (CT) scan or negative on positron emission tomography (PET); non-palpable splenic and disappearance of liver nodules; infiltrate cleared on repeat bone marrow (BM), immunohistochemistry negative. PR = a reduction of measurable lesions; ≥ 50% decrease in sum of the products of the greatest diameters (SPD) of up to 6 largest dominant masses, no enlargement in size of other nodes; ≥ 50% decrease in SPD and no increase in liver or spleen. (NCT01456039)
Timeframe: Tumor assessments performed every 2 months; median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventionpercentage of participants (Number)
Phase 1: Cohort 1: Romidepsin 9mg/m^20
Phase 1: Cohort 2: Romidepsin 14mg/m^216.7
Phase 2: Romidepsin 14mg/m^242.5
Total: Romidepsin 14mg/m^239.1

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Terminal Phase Half-life of Romidepsin (t½) in Phase 1

The terminal phase half-life of romidepsin after a single dose on Day 1, calculated according to the following equation: t½ = 0.693/λz, where λz is the terminal phase rate constant. (NCT01456039)
Timeframe: Day 1 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration.

Interventionhours (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^29.52
Phase 1: Cohort 2: Romidepsin 14mg/m^29.12

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Terminal Phase Half-life of Romidepsin (t½) in Phase 1 at Cycle 1, Day 15

The terminal phase half-life of romidepsin after a single dose on Day 15, calculated according to the following equation: t½ = 0.693/λz, where λz is the terminal phase rate constant. (NCT01456039)
Timeframe: Day 15 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration.

Interventionhours (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^28.77
Phase 1: Cohort 2: Romidepsin 14mg/m^29.01

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Time to Maximum Plasma Concentration of Romidepsin (Tmax) in Phase 1

The time to first maximum observed plasma concentration of romidepsin after a single dose on Day 1. (NCT01456039)
Timeframe: Day 1 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionhours (Median)
Phase 1: Cohort 1: Romidepsin 9mg/m^24.02
Phase 1: Cohort 2: Romidepsin 14mg/m^22.00

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Time to Response (TTR) for PTCL Participants With at Least a PR Based on the Modified 1999 IWC as Assessed by IER

TTR for PTCL was defined as the time in days from first dose date to the first date of objective disease response. (NCT01456039)
Timeframe: Median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventiondays (Median)
Phase 1: Romidepsin 14mg/m^2109.0
Phase 2: Romidepsin 14mg/m^256.0
Total: Romidepsin 14mg/m^256.0

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Time to Response (TTR) for PTCL Participants With at Least a PR Based on the Modified 2007 IWC as Assessed by IER

TTR for PTCL was defined as the time in days from first dose date to the first date of objective disease response. (NCT01456039)
Timeframe: Median follow-up time was 100 days; up to the data cut-off of 28 July 2015

Interventiondays (Median)
Phase 1: Romidepsin 14mg/m^2737.0
Phase 2: Romidepsin 14mg/m^256.0
Total: Romidepsin 14mg/m^256.0

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Tmax,ss of Romidepsin in Phase 1 at Cycle 1, Day 15

Observed time to first maximum plasma concentration at steady state (NCT01456039)
Timeframe: Day 15 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

Interventionhours (Median)
Phase 1: Cohort 1: Romidepsin 9mg/m^21.95
Phase 1: Cohort 2: Romidepsin 14mg/m^22.94

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Participants With Treatment-Emergent Adverse Events (TEAEs) Associated With Romidepsin

An adverse event (AE) is any noxious, unintended, or untoward medical occurrence that may appear or worsen during the course of a study. An AE that resulted in any of the outcomes was defined as a serious (SAE): • Death • Life-threatening event • An inpatient hospitalization or prolongation of existing hospitalization • Persistent or significant disability or incapacity; • Congenital anomaly or birth defect • Other important medical event The investigator judged the relationship of an AE to study drug based on the timing of the AE relative to drug administration and whether or not other drugs, therapeutic interventions, or underlying conditions could provide an explanation for the event. The severity of an AE was evaluated by the investigator according to Common Terminology Criteria for Adverse Events (CTCAE Version 3.0), Japanese Clinical Oncology Group (JCOG) where Grade 1 = Mild, Grade 2 = Moderate, Grade 3 = Severe, Grade 4 = Life-threatening and Grade 5 = Death. (NCT01456039)
Timeframe: Day 1 of study drug through 30 days after the last dose of study drug or discontinuation date; Up to data cut-off of 28 July 2015; maximum follow up time was 184.3 weeks

,,,
Interventionparticipants (Number)
Any 1 TEAETEAE related to any study drugTEAE with CTCAE Grade 3 or greaterTEAE with CTCAE ≥Grade 3 related to study drug≥ 1 serious TEAESerious TEAE related to study drugTEAE leading to discontinuation of study drugTEAE related leading to discontinuation of drugTEAE leading to dose held of study drugRelated TEAE leading to dose held of study drugTEAE leading to dose reduction of study drugRelated TEAE leading to dose reduction of drugTEAE leading to dose interruption of study drugRelated TEAE leading to dose interruption of drugAt least one TEAE with NCI CTCAE Grade 5
Phase 1: Romidepsin 14mg/m^2776644334344430
Phase 1: Romidepsin 9mg/m^2333310001100110
Phase 2: Romidepsin 14mg/m^2404037371061092422171723222
Total: Romidepsin 14mg/m^247474343141013122825212127252

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The Percentage of Participants With Abnormal Q-wave and T Wave Intervals

The time from the start of the Q-wave to the end of the T-wave QTc intervals greater than 450 msec post-baseline performed by centralized reviewer. The Bazett's (QTcB) and Fridericia (QTcF) correction were used as the standard clinical correction for calculating the heart rate-corrected QTc interval (NCT01456039)
Timeframe: Median follow-up: 100 days; up to data cut-off of 28 July 2015

,,,
Interventionpercentage of participants (Number)
QTcB >450 msecQTcB >480 msecQTcB >500 msecQTcB increase from predose >30 msecQTcB increase from predose >60 msecQTcF >450 msecQTcF >480 msecQTcF >500 msecQTcF increase from predose >30 msecQTcF increase from predose >60 msec
Phase 1: Romidepsin 14mg/m^257.128.614.357.128.614.314.314.357.114.3
Phase 1: Romidepsin 9mg/m^210066.733.366.733.333.333.333.366.733.3
Phase 2: Romidepsin 14mg/m^255.00.00.010.00.010.00.00.010.00.0
Total: Romidepsin 14mg/m^255.34.32.117.04.310.62.12.117.02.1

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Apparent Total Clearance of Romidepsin (CL/F) of Romidepsin in Phase 1

The apparent total clearance of romidepsin after a single dose on Day 1, calculated as dose/AUC0-infinity. (NCT01456039)
Timeframe: Day 1 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration.

InterventionL/h (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^214.29
Phase 1: Cohort 2: Romidepsin 14mg/m^29.31

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Apparent Volume of Distribution (Vz/F) of Romidepsin in Phase 1

Apparent volume of distribution, was calculated according to the equation: Vd/F = (CL/F)/λz (NCT01456039)
Timeframe: Day 1 at Cycle 1; collected at 0 (pre-dose), 1, 2, 3, and 4 (at the end of administration) hours after the start of administration, 0.25 (15 minutes), 0.5 (30 minutes), 1, 2, 4, 6, 20, and 44 hours after the end of administration

InterventionLiters (Geometric Mean)
Phase 1: Cohort 1: Romidepsin 9mg/m^2196.24
Phase 1: Cohort 2: Romidepsin 14mg/m^2122.47

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Time to Response

Time to Response is defined as the time from the date of randomization to the date of first documentation of PR or better. (NCT01482962)
Timeframe: At the end of every 8 weeks from date of first dose treatment; every 12 weeks after 40 week assessment; at end of treatment visit until progressive disease. Duration is approximately 3 years

Interventiondays (Median)
Alisertib62
Pralatrexate, or Romidepsin, or Gemcitabine64

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Time to Disease Progression (TTP)

Time to Progression (TTP) was defined as the time from the date of randomization to the date of first documentation of PD/relapse. (NCT01482962)
Timeframe: At the end of every 8 weeks from date of first dose treatment; every 12 weeks after 40 week assessment; at end of treatment visit until progressive disease. Duration is approximately 3 years

Interventiondays (Median)
Alisertib162
Pralatrexate, or Romidepsin, or Gemcitabine116

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Overall Response Rate (ORR) Based on Independent Review Committee (IRC) Assessment

ORR was defined as the percentage of participants who achieve Complete Response (CR) or Partial Response (PR) as assessed by the IRC using International Working Group (IWG) criteria. CR=Disappearance of all evidence of disease and PR=Regression of measurable disease and no new sites. (NCT01482962)
Timeframe: Every 8 weeks from date of first dose treatment; every 12 weeks after 40 week assessment; at end of treatment visit until progressive disease. Duration is approximately 3 years

Interventionpercentage of participants (Number)
Alisertib33
Pralatrexate, or Romidepsin, or Gemcitabine45

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Duration of Response (DOR)

DOR was defined as the time from the date of first documentation of a PR or better to the date of first documentation of progressive disease (PD)/relapse for responders as assessed by the IRC using IWG criteria. Responders without documentation of PD/relapse were censored at the date of last response assessment that was stable disease (SD) or better. (NCT01482962)
Timeframe: At the end of every 8 weeks from date of first dose treatment; every 12 weeks after 40 week assessment; at end of treatment visit until progressive disease. Duration is approximately 3 years

Interventiondays (Median)
Alisertib225
Pralatrexate, or Romidepsin, or Gemcitabine172

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Complete Response (CR) Rate

Complete Response (CR) rate is defined as the percentage of participants with CR as assessed by the IRC using IWG criteria (2007 Cheson). CR= Disappearance of all evidence of disease. (NCT01482962)
Timeframe: At the end of every 8 weeks from date of first dose treatment; every 12 weeks after 40 week assessment; at end of treatment visit until PD (approximately 3 years)

Interventionpercentage of participants (Number)
Alisertib18
Pralatrexate, or Romidepsin, or Gemcitabine27

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Number of Participants With Clinically Important Abnormal Laboratory Values Reported as AEs

Clinical laboratory tests included chemistry, hematology and urinalysis test. Clinically significant treatment-emergent laboratory abnormalities were reported by the investigator as TEAEs. (NCT01482962)
Timeframe: First dose to 30 days after last dose of study drug or comparator (Up to 152 Weeks)

,
Interventionparticipants (Number)
Neutrophil Count DecreasedWhite Blood Cell Count DecreasedLymphocyte Count DecreasedMonocyte Count DecreasedLymphocyte Count IncreasedMonocyte Count IncreasedWhite Blood Cell Count IncreasedPlatelet Count DecreasedAlanine Aminotransferase IncreasedAspartate Aminotransferase IncreasedGamma-glutamyltransferase IncreasedBlood Bilirubin IncreasedHepatic Enzyme IncreasedLiver Function Test AbnormalTransaminases IncreasedBlood Alkaline Phosphatase IncreasedBlood Lactate Dehydrogenase IncreasedBlood Creatinine IncreasedBlood Creatinine DecreasedBlood Urea IncreasedBlood Potassium DecreasedBlood Magnesium DecreasedBlood Bicarbonate DecreasedBlood Calcium DecreasedBlood Calcium IncreasedBlood Phosphorus DecreasedCalcium Ionised IncreasedHaemoglobin DecreasedHaematocrit IncreasedHaematocrit DecreasedCoagulation Factor XIII Level DecreasedInternational Normalised Ratio IncreasedBlood Albumin DecreasedMyocardial Necrosis Marker IncreasedTroponin IncreasedBlood Glucose IncreasedImmunoglobulins IncreasedBlood Uric Acid IncreasedEnterovirus Test Positive
Alisertib181762111158562200953011100101111110100110
Pralatrexate, or Romidepsin, or Gemcitabine14105100022111131011717104211010320002011001

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Progression-Free Survival (PFS) Based on IRC Assessment

PFS was defined as the time from the date of randomization to the date of first documentation of progressive disease (PD) or death due to any cause, whichever occurred first. (NCT01482962)
Timeframe: Every 8 weeks from date of first dose treatment; every 12 weeks after 40 week assessment; at end of treatment visit until progressive disease. Duration is approximately 3 years

Interventiondays (Median)
Alisertib115
Pralatrexate, or Romidepsin, or Gemcitabine104

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. A TEAE is defined as an adverse event with an onset that occurs after receiving study drug. A SAE is any untoward medical occurrence that at any dose: results in death, is life-threatening, requires inpatient hospitalization or prolongation of an existing hospitalization, results in persistent or significant disability or incapacity, is a congenital anomaly/ birth defect or is a medically important event. (NCT01482962)
Timeframe: First dose to 30 days after last dose of study drug or comparator (Up to 152 Weeks)

,
Interventionparticipants (Number)
TEAESAE
Alisertib13675
Pralatrexate, or Romidepsin, or Gemcitabine12669

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Number of Participants With Clinically Important Vital Sign Measurements Reported as AEs

Vital signs included blood pressure, heart rate and temperature. Individual clinically significant changes in vital signs were reported by the investigator as TEAEs. (NCT01482962)
Timeframe: First dose to 30 days after last dose of study drug or comparator (Up to 152 Weeks)

,
Interventionparticipants (Number)
Heart Rate IncreasedBody Temperature IncreasedHypotensionOrthostatic HypotensionHypertensionPyrexia
Alisertib1042548
Pralatrexate, or Romidepsin, or Gemcitabine0161740

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Change Form Baseline in Reported Symptoms and Quality of Life (QoL) Assessment Per Functional Assessment of Cancer Therapy-Lymphoma (FACT-LYM) for Functioning and Symptoms

The FACT-LYM includes the Functional Assessment of Cancer Therapy General Scale (FACT-G) and a 15-item lymphoma-specific subscale (LYM) over the past week. The FACT-G has 27 items that incorporate 4 scales including physical well-being (PWB; 7 items), social/family well-being (SWB, 7 items), emotional well-being (EWB; 6 items), and functional well-being (FWB; 7 items). The combined FACT-LYM instrument consists of a total of a 42 item questionnaire. Each question is answered on a 5- point scale of 0 (not at all) to 4 (very much) for a total possible score of 168. Higher scores indicate better well-being and a positive change from Baseline indicates improvement. (NCT01482962)
Timeframe: Baseline and End of Treatment (EOT) (Up to 152 Weeks)

,
Interventionscore on a scale (Mean)
Physical Well-Being, EOTSocial/Family Well-Being, EOTEmotional Well-Being, EOTFunctional Well-Being, EOT
Alisertib-2.4-0.3-1.4-2.4
Pralatrexate, or Romidepsin, or Gemcitabine-1.30.0-0.8-0.3

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Time to Subsequent Antineoplastic Therapy

Time to subsequent antineoplastic therapy was defined as the time from randomization to the first date of subsequent antineoplastic therapy (excluding transplant). Participants without subsequent antineoplastic therapy were censored at the date of death or last known to be alive. (NCT01482962)
Timeframe: From date of last study drug to date of subsequent antineoplastic therapy, if required; approximately 3 years

Interventiondays (Median)
Alisertib336
Pralatrexate, or Romidepsin, or Gemcitabine233

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Overall Survival (OS)

OS was defined as the time from the date of randomization to the date of death. Participants without documentation of death were censored at the date last known to be alive. (NCT01482962)
Timeframe: Participants were followed for survival for 2 years from date of last participant off study treatment, or death, whichever occurs first. Contacts were every 4 months (Median follow-up 519 days in the alisertib arm and 586 days in the comparative arm)

Interventiondays (Median)
Alisertib415
Pralatrexate, or Romidepsin, or Gemcitabine367

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Number of Patients With Dose Limiting Toxicities (DLTs)

"To determine the maximum tolerated dose (MTD) by assessing the adverse events experienced by patients of both carfilzomib alone and when taken with romidepsin for dose limiting toxicities (DLT) on days 1 and 15 of the first 28 days of treatment. Toxicities will be assessed according to the NCI Common Terminology Criteria for Adverse Events (CTCAE) v 4.0.~DLT is defined as any of the following:~Grade ≥ 2 neuropathy with pain Grade ≥ 3 non-hematologic toxicity Grade ≥ 3 nausea, vomiting, or diarrhea not controlled Grade ≥ 4 fatigue persisting for > 7 days Grade 4 neutropenia (ANC < 500/mm3) occurring for >7 days Febrile neutropenia [ANC < 1000/mm3 with fever Grade ≥ 3 thrombocytopenia persisting for > 7 days Grade ≥ 3 thrombocytopenia associated with bleeding Any toxicity requiring a dose reduction within Cycle 1 Inability to receive Cycle 2, Day 1 dose due to drug related toxicity persisting from Cycle 1 or drug-related toxicity newly encountered on Cycle 2, Day 1" (NCT01738594)
Timeframe: During the first 28 days (1 cycle=28 days) of treatment.

InterventionParticipants (Count of Participants)
Arm A, Cohort 1 (Carfilzomib)0
Arm B Cohort -1 (Carfilzomib + Romidepsin)0
Arm B Cohort 1 (Carfilzomib + Romidepsin2

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Overall Response Rate (ORR)

"ORR the proportion of patients who achieve CR (complete response), CRu (complete remission unconfirmed) or PR (partial response) relative to the per-protocol population. Disease response and progression will be evaluated according to the Revised Response Criteria for malignant lymphoma (Cheson et al. 2007)." (NCT01822886)
Timeframe: 24 months

InterventionParticipants (Count of Participants)
Romidepsin, Gemcitabine6

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Complete Remission (CR) Rate

"Complete Remission is disappearance of all target lesions per the Revised Response Criteria for Malignant Lymphoma (Cheson et al. 2007)" (NCT01822886)
Timeframe: 18 months

InterventionParticipants (Count of Participants)
Romidepsin, Gemcitabine3

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Overall Survival is Measured From the Date of Study Entry to the Date of Patient's Death

OS (overall survival) is measured from the date of study entry to the date of patient's death. If the patient is alive or his vital status is unknown, the date of death will be censored at the date that the patient is last known to be alive. (NCT01822886)
Timeframe: 24 months

Interventionpercentage of partecipants (Number)
Romidepsin, Gemcitabine50

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Percentage of Participants With Progression-Free Survival

The time from start of study treatment to first documentation of objective tumor progression or to death due to any cause, whichever comes first. PFS (progression-free survival) data will be censored on the day following the date of the last radiological assessment of measured lesions documenting absence of progressive disease for patients who do not have objective tumor progression and are still on study at the time of an analysis, are given antitumor treatment other than the study treatment or stem cell transplant, or are removed from study prior to documentation of objective tumor progression. Patients lacking an evaluation of tumor response after their first dose will have their event time censored at 1 day. Percentage of participants is an estimate based on Kaplan-Meier method. (NCT01822886)
Timeframe: 24 months

Interventionpercentage of partecipants (Number)
Romidepsin, Gemcitabine11.2

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Safety - Frequency of Toxicities Grade 3 and 4

Frequency of toxicities was reported by type and grade according to the National Cancer Institute Common Terminology Criteria for Adverse Events (version 4.0). (NCT01822886)
Timeframe: 24 months

Interventionevents (Number)
Romidepsin, Gemcitabine29

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PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Dolutegravir or Raltegravi) in Cohort 4

"PK concentration (ng/mL) for Romidepsin pre and post the third and fourth administrations of Romidepsin or placebo.~PK concentration (ng/mL) for co-administered antiretroviral drugs (Dolutegravir [DTG], or Raltegravir [RAL]) 24 hours after the third and fourth administrations of Romidepsin or placebo." (NCT01933594)
Timeframe: Pre, post and 24 hours after the third and fourth administrations of Romidepsin or placebo (at days 28 and 42)

Interventionng/mL (Median)
RMD PK concentration pre infusion 3RMD PK concentration post infusion 3RMD PK concentration pre infusion 4RMD PK concentration post infusion 4RAL PK concentration 24 hours post infusion 3RAL PK concentration 24 hours post infusion 4DTG PK concentration 24 hours post infusion 3DTG PK concentration 24 hours post infusion 4
Cohort 4-Arm 4A (Romidepsin)20769NA13490656721241568

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PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3

"Hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Hour 4 is at the completion of Romidepsin or placebo administration. Hours 6, 12 and 24 are 2, 8 and 20 hours after the completion of Romidepsin or placebo administration.~PK concentration (ng/mL) for Romidepsin at hours 0, 4, 6, 12 and 24. PK concentration (ng/mL) for co-administered antiretroviral drugs (Efavirenz [EFV], Dolutegravir [DTG], or Raltegravir [RAL]) at hours 0 and 24." (NCT01933594)
Timeframe: At hours 0, 4, 6, 12 and 24

Interventionng/mL (Median)
RMD PK concentration at Hour 0RMD PK concentration at Hour 4RMD PK concentration at Hour 6RMD PK concentration at Hour 12RMD PK concentration at Hour 24EFV PK concentration at Hour 0EFV PK concentration at Hour 24RAL PK concentration at Hour 0RAL PK concentration at Hour 24DTG PK concentration at Hour 0DTG PK concentration at Hour 24
Cohort 2-Arm 2A (Romidepsin)NA75.22.7NANA2560187091039840352190

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PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Dolutegravir or Raltegravi) in Cohort 4

"PK concentration (ng/mL) for Romidepsin pre and post the third and fourth administrations of Romidepsin or placebo.~PK concentration (ng/mL) for co-administered antiretroviral drugs (Dolutegravir [DTG], or Raltegravir [RAL]) 24 hours after the third and fourth administrations of Romidepsin or placebo." (NCT01933594)
Timeframe: Pre, post and 24 hours after the third and fourth administrations of Romidepsin or placebo (at days 28 and 42)

Interventionng/mL (Median)
DTG PK concentration 24 hours post infusion 3DTG PK concentration 24 hours post infusion 4
Cohort 4-Arm 4B (Placebo for Romidepsin)913833

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Change From Baseline in Histone Acetylation (Median FITC Ac-Histone) in CD3+ Cells in Cohorts 1-3

"Baseline is defined as the value at Hour 0, right before the single administration of Romidepsin or placebo.~Change was calculated as the value at 24 hours after administration of Romidepsin or placebo (at entry) minus the value at baseline.~Median Fluorescent Intensity (MFI) data describes a shift in the expression of a fluorescently labeled marker on a population of cells. The reported MFI is an arbitrary value dependent on the voltage applied to the corresponding flow cytometer detector." (NCT01933594)
Timeframe: Hour 0 and 24 hours after the single administration of RMD or placebo (at entry)

Interventionarbitrary units (Median)
Cohorts 1-3 (Romidepsin)-7
Cohorts 1-3 (Placebo for Romidepsin)-194

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Change From Baseline in Cell-associated HIV-1 RNA Levels in Resting CD4 T-cells in Cohorts 1-3

Baseline is defined as the pre-entry value. Change was calculated as the value at 24 hours after administration of Romidepsin or placebo (at entry) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry and 24 hours after the single administration of Romidepsin or placebo (at entry)

Interventionlog10 (copies/10^6 resting CD4 cells) (Median)
Cohorts 1-3 (Romidepsin)-.009
Cohorts 1-3 (Placebo for Romidepsin)0

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Change From Baseline in Cell-associated HIV-1 RNA Levels in Resting CD4 T Cells in Cohorts 1-3

Baseline is defined as the pre-entry value. Change was calculated as the value at 14 days after administration of Romidepsin or placebo (at entry) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry and 14 days after the administration of RMD or placebo (at entry)

Interventionlog10 copies/mL (Median)
Cohorts 1-3 (Romidepsin)0.02
Cohorts 1-3 (Placebo for Romidepsin)-0.05

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Change From Baseline in Cell-associated HIV-1 RNA Levels in PBMCs in Cohort 4

Baseline is defined as the pre-entry value. Change was calculated as the value at 72 hours after the second administration of Romidepsin or placebo (at day 14) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry and 72 hours after the second administration of Romidepsin or placebo (at day 14)

Interventionlog10 copies/mL (Median)
Cohort 4-Arm 4A (Romidepsin)-0.26
Cohort 4-Arm 4B (Placebo for Romidepsin)-0.16

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Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohort 4

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 72 hours after the second administration of Romidepsin or placebo (at day 14) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, entry and 72 hours after the second administration of Romidepsin or placebo (at day 14)

Interventionlog10 copies/mL (Median)
Cohort 4-Arm 4A (Romidepsin)0
Cohort 4-Arm 4B (Placebo for Romidepsin)0.82

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Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD4+ T-cells) in Cohort 4

Baseline is defined as the average of the two pre-entry values. Change was calculated as the value at 24 hours post first and fourth administration of Romidepsin or placebo (at entry and day 42) and 10 weeks post the fourth administration (at day 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours after the first and fourth administration of Romidepsin or placebo (at entry and day 42), and 10 weeks after the fourth administration (at day 42)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 4Change from baseline to 10 weeks post infusion 4
Cohort 4-Arm 4A (Romidepsin)0.210.4
Cohort 4-Arm 4B (Placebo for Romidepsin)0.520.7

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PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3

"Hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Hour 4 is at the completion of Romidepsin or placebo administration. Hours 6, 12 and 24 are 2, 8 and 20 hours after the completion of Romidepsin or placebo administration.~PK concentration (ng/mL) for Romidepsin at hours 0, 4, 6, 12 and 24. PK concentration (ng/mL) for co-administered antiretroviral drugs (Efavirenz [EFV], Dolutegravir [DTG], or Raltegravir [RAL]) at hours 0 and 24." (NCT01933594)
Timeframe: At hours 0, 4, 6, 12 and 24

Interventionng/mL (Median)
EFV PK concentration at Hour 0EFV PK concentration at Hour 24RAL PK concentration at Hour 0RAL PK concentration at Hour 24
Cohorts 1-3 (Placebo for Romidepsin)25201600401142

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PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3

"Hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Hour 4 is at the completion of Romidepsin or placebo administration. Hours 6, 12 and 24 are 2, 8 and 20 hours after the completion of Romidepsin or placebo administration.~PK concentration (ng/mL) for Romidepsin at hours 0, 4, 6, 12 and 24. PK concentration (ng/mL) for co-administered antiretroviral drugs (Efavirenz [EFV], Dolutegravir [DTG], or Raltegravir [RAL]) at hours 0 and 24." (NCT01933594)
Timeframe: At hours 0, 4, 6, 12 and 24

Interventionng/mL (Median)
RMD PK concentration at Hour 0RMD PK concentration at Hour 4RMD PK concentration at Hour 6RMD PK concentration at Hour 12RMD PK concentration at Hour 24EFV PK concentration at Hour 0EFV PK concentration at Hour 24DTG PK concentration at Hour 0DTG PK concentration at Hour 24
Cohort 3-Arm 3A (Romidepsin)NA892.6NANA2612288629882399

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PK Parameters for Romidepsin and Co-administered Antiretroviral Drugs (Efavirenz, Dolutegravir, or Raltegravir) in Cohorts 1-3

"Hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Hour 4 is at the completion of Romidepsin or placebo administration. Hours 6, 12 and 24 are 2, 8 and 20 hours after the completion of Romidepsin or placebo administration.~PK concentration (ng/mL) for Romidepsin at hours 0, 4, 6, 12 and 24. PK concentration (ng/mL) for co-administered antiretroviral drugs (Efavirenz [EFV], Dolutegravir [DTG], or Raltegravir [RAL]) at hours 0 and 24." (NCT01933594)
Timeframe: At hours 0, 4, 6, 12 and 24

Interventionng/mL (Median)
RMD PK concentration at Hour 0RMD PK concentration at Hour 4RMD PK concentration at Hour 6RMD PK concentration at Hour 12RMD PK concentration at Hour 24EFV PK concentration at Hour 0EFV PK concentration at Hour 24RAL PK concentration at Hour 0RAL PK concentration at Hour 24
Cohort 1-Arm 1A (Romidepsin)NA123.2NANA203021057771234

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HIV-1 RNA Levels in Cohort 4

HIV-1 RNA levels at 7 days after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) (NCT01933594)
Timeframe: 7 days after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42)

InterventionParticipants (Count of Participants)
HIV-1 RNA level at day 7 post infusion 171941744HIV-1 RNA level at day 7 post infusion 171941745HIV-1 RNA level at day 7 post infusion 271941745HIV-1 RNA level at day 7 post infusion 271941744HIV-1 RNA level at day 7 post infusion 371941744HIV-1 RNA level at day 7 post infusion 371941745HIV-1 RNA level at day 7 post infusion 471941744HIV-1 RNA level at day 7 post infusion 471941745
40 - 199 copies/mL< 40 copies/mL
Cohort 4-Arm 4A (Romidepsin)13
Cohort 4-Arm 4B (Placebo for Romidepsin)2
Cohort 4-Arm 4B (Placebo for Romidepsin)0
Cohort 4-Arm 4A (Romidepsin)8
Cohort 4-Arm 4A (Romidepsin)0
Cohort 4-Arm 4A (Romidepsin)11
Cohort 4-Arm 4B (Placebo for Romidepsin)3

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Change From Baseline in Cell-associated HIV-1 RNA Levels in PBMCs in Cohort 4

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, entry and 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42)

,
Interventionlog10 (copies/10^6 PBMCs) (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 2Change from baseline to 24 hours post infusion 3Change from baseline to 24 hours post infusion 4
Cohort 4-Arm 4A (Romidepsin)-0.06-0.07-0.44-0.05
Cohort 4-Arm 4B (Placebo for Romidepsin)-0.16-0.52-0.02-0.3

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Change From Baseline in CD4+ T Cell Percent in Cohort 4

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 24 hours post each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 2, 5, 10 and 18 weeks post the fourth administration minus the value at baseline (NCT01933594)
Timeframe: Pre-entry, entry, 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42), and 2, 5, 10 and 18 weeks after the fourth administration (at day 42)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 2Change from baseline to 24 hours post infusion 3Change from baseline to 24 hours post infusion 4Change from baseline to 2 weeks post infusion 4Change from baseline to 5 weeks post infusion 4Change from baseline to 10 weeks post infusion 4Change from baseline to 18 weeks post infusion 4
Cohort 4-Arm 4A (Romidepsin)-2.5-4.5-3.5-4.5-0.5-1.8-2.8-0.5
Cohort 4-Arm 4B (Placebo for Romidepsin)-20.510.5-0.50-0.5-2.5

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Proportion of Participants With Grade 3 or Higher Adverse Events (AEs) in Cohorts 1-3 Romidepsin Arms

Proportion of participants with Grade 3 or higher adverse events (AEs) in Cohorts 1-3 Romidepsin Arms, including signs/symptoms, lab toxicities, and /or clinical events probably, possibly, or definitely related to study treatment (as judged by the core team, blinded to treatment arm). The DAIDS AE Grading Table (Version 1.0) was used. (NCT01933594)
Timeframe: Measured from the time of Romidepsin administration (at entry) until 28 days after the administration

Interventionproportion of participants (Number)
Cohorts 1-3 (Romidepsin)0

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Proportion of Participants With Grade 3 or Higher Adverse Events (AEs) in Cohort 4 Romidepsin Arm

Proportion of participants with Grade 3 or Higher Adverse Events (AEs) in Cohort 4 Romidepsin Arm, including signs/symptoms, lab toxicities, and /or clinical events probably, possibly, or definitely related to study treatment (as judged by the core team, blinded to treatment arm). The DAIDS AE Grading Table (Version 1.0) was used. (NCT01933594)
Timeframe: Measured from the time of the first Romidepsin administration through 28 days after the last administration (at day 42)

Interventionproportion of participants (Number)
Cohort 4-Arm 4A (Romidepsin)0.077

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Number of Participants With Reported Grade 2-4 AEs in Cohorts 1-3

Number of participants with reported grade 2-4 adverse events including signs/symptoms, lab toxicities, and clinical events that are at least possibly related to study treatment. The DAIDS AE Grading Table (Version 1.0) was used. (NCT01933594)
Timeframe: Measured from study entry to off study

InterventionParticipants (Count of Participants)
Cohort 1-Arm 1A (Romidepsin)4
Cohort 2-Arm 2A (Romidepsin)2
Cohort 3-Arm 3A (Romidepsin)1
Cohorts 1-3 (Placebo for Romidepsin)1

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Number of Participants With Reported Grade 2-4 AEs in Cohort 4

Number of participants with reported grade 2-4 adverse events including signs/symptoms, lab toxicities, and clinical events that are at least possibly related to study treatment. The DAIDS AE Grading Table (Version 1.0) was used. (NCT01933594)
Timeframe: Measured from study entry to off study

InterventionParticipants (Count of Participants)
Cohort 4-Arm 4A (Romidepsin)5
Cohort 4-Arm 4B (Placebo for Romidepsin)0

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Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohorts 1-3

"Baseline is defined as the average of the pre-entry and entry values. Hour 24/48 is defined as the average of values at 24 and 48 hours after the single administration of Romidepsin or placebo (at study entry).~Change was calculated as the value at hour 24/48 minus the value at baseline." (NCT01933594)
Timeframe: Pre-entry, entry, 24 and 48 hours after the single administration of Romidepsin or placebo (at entry)

Interventionlog10 copies/mL (Median)
Cohorts 1-3 (Romidepsin)0.12
Cohorts 1-3 (Placebo for Romidepsin)0.12

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Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD4+ T-cells) in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 48 hours post infusionChange from baseline to 7 days post infusionChange from baseline to 28 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)0.4-1-1.4
Cohorts 1-3 (Romidepsin)0.511.2

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Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD8+ T-cells) in Cohort 4

Baseline is defined as the average of the two pre-entry values. Change was calculated as the value at 24 hours post first and fourth administration of Romidepsin or placebo (at entry and day 42) and 10 weeks post the fourth administration (at day 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours after the first and fourth administration of Romidepsin or placebo (at entry and day 42), and 10 weeks after the fourth administration (at day 42)

,
Interventionpercentage of CD8 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 4Change from baseline to 10 weeks post infusion 4
Cohort 4-Arm 4A (Romidepsin)0.61.1-0.3
Cohort 4-Arm 4B (Placebo for Romidepsin)0.21.12.8

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Change From Baseline in Cellular Markers of Immune Activation (CD38/HLA-DR Expression on CD8+ T-cells) in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD8 cells (Median)
Change from baseline to 48 hours post infusionChange from baseline to 7 days post infusionChange from baseline to 28 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)0.3-1.3-0.1
Cohorts 1-3 (Romidepsin)0.10.80.3

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Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD4+ T-cells) in Cohort 4

Baseline is defined as the average of the two pre-entry values. Change was calculated as the value at 24 hours post first and fourth administration of Romidepsin or placebo (at etnry and day 42) and 10 weeks post the fourth administration (at day 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours after the first and fourth administration of Romidepsin or placebo (at etnry and day 42), and 10 weeks after the fourth administration (at day 42)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 4Change from baseline to 10 weeks post infusion 4
Cohort 4-Arm 4A (Romidepsin)000
Cohort 4-Arm 4B (Placebo for Romidepsin)-0.1-0.1-0.1

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Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD4+ T-cells) in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 48 hours post infusionChange from baseline to 7 days post infusionChange from baseline to 28 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)000
Cohorts 1-3 (Romidepsin)000

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Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD8+ T-cells) in Cohort 4

Baseline is defined as the average of the two pre-entry values. Change was calculated as the value at 24 hours post first and fourth administration of Romidepsin or placebo (at etnry and day 42) and 10 weeks post the fourth administration (at day 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours after the first and fourth administration of Romidepsin or placebo (at etnry and day 42), and 10 weeks after the fourth administration (at day 42

,
Interventionpercentage of CD8 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 4Change from baseline to 10 weeks post infusion 4
Cohort 4-Arm 4A (Romidepsin)000
Cohort 4-Arm 4B (Placebo for Romidepsin)0-0.10

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Change From Baseline in Cellular Markers of Immune Activation (CD69/CD25 Expression on CD8+ T-cells) in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD8 cells (Median)
Change from baseline to 48 hours post infusionChange from baseline to 7 days post infusionChange from baseline to 28 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)000
Cohorts 1-3 (Romidepsin)000

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Change From Baseline in Histone Acetylation in (Median FITC Ac-histone) in CD3+ Cells in Cohort 4

"Baseline is defined as the value right before the first administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 72 hours after the second administration minus the value at baseline.~Median Fluorescent Intensity (MFI) data describes a shift in the expression of a fluorescently labeled marker on a population of cells. The reported MFI is an arbitrary value dependent on the voltage applied to the corresponding flow cytometer detector." (NCT01933594)
Timeframe: Entry, 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42), and 72 hours after the second administration (at day 14)

,
Interventionarbitrary units (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 2Change from baseline to 72 hours post infusion 2Change from baseline to 24 hours post infusion 3Change from baseline to 24 hours post infusion 4
Cohort 4-Arm 4A (Romidepsin)24022774474145224342
Cohort 4-Arm 4B (Placebo for Romidepsin)7498497474156652697

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Change From Baseline in Percentage of CD4+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohort 4

Baseline is defined as the average of the two pre-entry values. Change was calculated as the value at 24 hours post first and fourth administration of Romidepsin or placebo (at entry and day 42) and 10 weeks post the fourth administration (at day 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours after the first and fourth administration of Romidepsin or placebo (at entry and day 42), and 10 weeks after the fourth administration (at day 42)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 4Change from baseline to 10 weeks post infusion 4
Cohort 4-Arm 4A (Romidepsin)0.5-20.3
Cohort 4-Arm 4B (Placebo for Romidepsin)-1.40.90.1

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Change From Baseline in Percentage of CD4+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry) minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 48 hours post infusionChange from baseline to 7 days post infusionChange from baseline to 28 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)1.20-1.3
Cohorts 1-3 (Romidepsin)0.20.61.2

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Change From Baseline in Percentage of CD8+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohort 4

Baseline is defined as the average of the two pre-entry values. Change was calculated as the value at 24 hours post first and fourth administration of Romidepsin or placebo (at entry and day 42) and 10 weeks post the fourth administration (at day 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours after the first and fourth administration of Romidepsin or placebo (at entry and day 42), and 10 weeks after the fourth administration (at day 42)

,
Interventionpercentage of CD8 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 4Change from baseline to 10 weeks post infusion 4
Cohort 4-Arm 4A (Romidepsin)0.1-2.50.9
Cohort 4-Arm 4B (Placebo for Romidepsin)-4.1-.6-0.8

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Change From Baseline in Percentage of CD8+ T-cells Expressing Annexin V and/or 7 Amino-actinomycin D (7-AAD) in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry) minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 48 hours, 7 days and 28 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD8 cells (Median)
Change from baseline to 48 hours post infusionChange from baseline to 7 days post infusionChange from baseline to 28 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)1.8-1.1-1.9
Cohorts 1-3 (Romidepsin)-0.10.30.9

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Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohort 4

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, entry, 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42)

,
Interventionlog10 copies/mL (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 2Change from baseline to 24 hours post infusion 3Change from baseline to 24 hours post infusion 4
Cohort 4-Arm 4A (Romidepsin)00.030.30
Cohort 4-Arm 4B (Placebo for Romidepsin)-0.110.150.470.33

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Change From Baseline in Plasma HIV-1 RNA Levels as Detected by Single Copy Assay in Cohorts 1-3

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 6 hours, 12 hours, 7 days, 14 days and 28 days after administration of Romidepsin or placebo (at entry) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, entry, 6 hours, 12 hours, 7 days, 14 days and 28 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionlog10 copies/mL (Median)
Change from baseline to 6 hours post infusionChange from baseline to 12 hours post infusionChange from baseline to 7 days post infusionChange from baseline to 14 days post infusionChange from baseline to 28 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)0.140.270.27-0.13-0.08
Cohorts 1-3 (Romidepsin)-0.020000

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Change From Baseline in PTEF-b Phosphorylation (pNFKB+% and pS175%) in CD4+ T-cells in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 24 hours after the single administration of Romidepsin or placebo (at entry) minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 24 hours after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD4 cells (Median)
Change in pNFKB+% on CD4Change in pS175% on CD4
Cohorts 1-3 (Placebo for Romidepsin)19.36
Cohorts 1-3 (Romidepsin)2018.1

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Change From Baseline in PTEF-b Phosphorylation (pNFKB+% and pS175%) in CD8+ T-cells in Cohorts 1-3

"Baseline is defined as the value at hour 0, where hour 0 is right before the single administration of Romidepsin or placebo (at entry).~Change was calculated as the value at 24 hours after the single administration of Romidepsin or placebo (at entry) minus the value at baseline." (NCT01933594)
Timeframe: Hour 0 and 24 hours after the single administration of Romidepsin or placebo (at entry)

,
Interventionpercentage of CD8 cells (Median)
Change in pNFKB+% on CD8Change in pS175% on CD8
Cohorts 1-3 (Placebo for Romidepsin)3.825.3
Cohorts 1-3 (Romidepsin)16.526.5

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Change From Baseline in PTEF-b Phosphorylation (pNFKB+%) in CD4+ T-cells in Cohort 4

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 72 hours after the second administration (at day 14) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, entry, 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 72 hours after the second administration (at day 14)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 2Change from baseline to 72 hours post infusion 2Change from baseline to 24 hours post infusion 3Change from baseline to 24 hours post infusion 4
Cohort 4-Arm 4A (Romidepsin)5.048.786.395.789.63
Cohort 4-Arm 4B (Placebo for Romidepsin)0.010000

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Change From Baseline in PTEF-b Phosphorylation (pS175+%) in CD4+ T-cells in Cohort 4

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 72 hours after the second administration (at day 14) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, entry, 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 72 hours after the second administration (at day 14)

,
Interventionpercentage of CD4 cells (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 2Change from baseline to 72 hours post infusion 2Change from baseline to 24 hours post infusion 3Change from baseline to 24 hours post infusion 4
Cohort 4-Arm 4A (Romidepsin)9.93171114.8516.52
Cohort 4-Arm 4B (Placebo for Romidepsin)-0.01-0.01-0.0100.01

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Change From Baseline in Total HIV-1 DNA in PBMCs in Cohort 4

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value at 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 72 hours after the second administration minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours after each administration of Romidepsin or placebo (at entry, and days 14, 28 and 42) and 72 hours after the second administration (at day 14)

,
Interventionlog10 (copies/10^6 PBMCs) (Median)
Change from baseline to 24 hours post infusion 1Change from baseline to 24 hours post infusion 2Change from baseline to 72 hours post infusion 2Change from baseline to 24 hours post infusion 3Change from baseline to 24 hours post infusion 4
Cohort 4-Arm 4A (Romidepsin)-0.06-0.13-0.13-0.06-0.14
Cohort 4-Arm 4B (Placebo for Romidepsin)-0.04-0.11-0.07-0.13-0.07

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Change From Baseline in Total HIV-1 DNA in Resting or Total CD4 T Cells in Cohorts 1-3

Baseline is defined as the pre-entry value. Change was calculated as the value at 24 hours and 14 days after administration of Romidepsin or placebo (at entry) minus the value at baseline. (NCT01933594)
Timeframe: Pre-entry, 24 hours and 14 days after the single administration of Romidepsin or placebo (at entry)

,
Interventionlog10 (copies/10^6 resting CD4 cells) (Median)
Change from baseline to 24 hours post infusionChange from baseline to 14 days post infusion
Cohorts 1-3 (Placebo for Romidepsin)0.05-0.05
Cohorts 1-3 (Romidepsin)-0.04-0.01

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Time to Disease Progression (Progression Free Survival)

(NCT01979276)
Timeframe: From start of treatment, to date of disease progression (on average, ten 28-day cycles)

Interventioncycles (defined as 28 days) (Mean)
ALL Patients9.5

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Part A: Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)

Safety and tolerability evaluation as measured by adverse events (AE) and serious adverse events (SAE). (NCT02092116)
Timeframe: 3 weeks

Interventionparticipants (Number)
Treatment emergent adverse eventsAdverse reactions, grade 1Adverse reactions, grade 2Related to RomidepsinNot related
Part A66163

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Part A: Changes From Baseline in HIV-1 Reservoir (Total HIV-1DNA; Integrated HIV-1 DNA in Unfractionated CD4+ T Cells and Replication Competent Provirus. Estimates of Change From Baseline of the Size of the Latent HIV-1 Reservoir in CD4+ Cells.

"Total HIV-1 DNA and integrated HIV-1 DNA were analysed by MMRM analysis (copies/10^6 CD4+ T cells). To estimate the frequency of infectious units per 10^6 resting memory CD4+ T cells a quantitative viral outgrowth assay (qVOA) was used.~Total HIV-1 DNA was measured at Day 84" (NCT02092116)
Timeframe: Day 56/84

Interventioncopies/10^6 CD4+ T cells (Mean)
Total HIV-1 DNA, BaslineTotal HIV-1 DNA, Day 84Integrated HIV-1 DNA, BaselineIntegrated HIV-1 DNA, Day 84Replication competent provirus, BaselineReplication competent provirus, Day 56
Part A791.7718.82825.64846.90.390.43

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Part B: Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)

Safety and tolerability evaluation of romidepsin and Vacc-4x in combination with GM-CSF as measured by adverse events (AE) and serious adverse events (SAE). (NCT02092116)
Timeframe: 287 days

Interventionparticipants (Number)
Non-treatment emergent adverse eventsTreatment emergent adverse eventsSerious adverse eventAdverse reaction, grade 1Adverse reaction, grade 2Adverse reaction, grade 3Related to Vacc-4x and GM-CSFRelated to RomidepsinNot related
Part B12012051191716

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Part B: Level of HIV-1 Transcription.

At day 105, 112 and 119 patients receive romidepsin and 4 hours after each administration HIV transcription is measured as unspliced HIV-1 RNA. (NCT02092116)
Timeframe: Day 105, 112 and 119

Interventioncopies/10^6 CD4+ T cells (Mean)
Day 105, before romidepsinDay 105, 4 hours post romidepsinDay 112, 4 hours post romidepsinDay 119, 4 hours post romidepsin
Part B6.9512.7722.9825.91

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Part B: Changes From Baseline in HIV-1 Reservoir (Total HIV-1DNA; Integrated HIV-1 DNA in Unfractionated CD4+ T Cells and Replication Competent Provirus.

"Total HIV-1 DNA and integrated HIV-1 DNA were analysed by MMRM analysis (copies/10^6 CD4+ T cells). To estimate the frequency of infectious units per 10^6 resting memory CD4+ T cells a quantitative viral outgrowth assay (qVOA) was used.~Blood samples were obtained at Day 0, Day 105 and Day 161." (NCT02092116)
Timeframe: Day 161/175

InterventionEstimated % change from baseline (Mean)
Total HIV-1 DNA, day 161Integrated HIV-1 DNA, day 175Replication competent provirus, day 161
Part B-39.71-19.21-38

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Total Duration of Immunosuppressive Therapy

(NCT02203578)
Timeframe: Up to 12 months after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Rate of Documented Infection

(NCT02203578)
Timeframe: Up to 12 months after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Incidence of cGVHD

(NCT02203578)
Timeframe: At 9 months after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Incidence of aGVHD

(NCT02203578)
Timeframe: At 28 days after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Incidence of cGVHD

(NCT02203578)
Timeframe: At 6 months after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Incidence of cGVHD

(NCT02203578)
Timeframe: At 3 months after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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T Cell Kinetics - Reconstitution

(NCT02203578)
Timeframe: Up to 12 months after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Incidence of cGVHD

(NCT02203578)
Timeframe: At 12 months after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Incidence of cGVHD

(NCT02203578)
Timeframe: At 1 month after initiation of romidepsin

Intervention ()
Supportive Care (Romidepsin)0

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Change in the Size of the Proviral HIV-1 Reservoir

Determined by total HIV-1 DNA and episomal HIV-1 DNA (2-LTR) in circulating total CD4+ T cells at baseline and prior to the ATI period (week 24). (NCT02850016)
Timeframe: baseline and week 24

InterventionHIV-1 DNA per million CD4+ T cells (Median)
Group A58
Group B46

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Days to Viral Rebound During Analytical Treatment Interruption (ATI)

"Viral rebound is defined as HIV-1 RNA ≥ 200 copies/mL on 2 consecutive measurements during ATI. If viral rebound occurs, the date of the first measurement of HIV-1 RNA ≥ 200 copies/mL will be defined as date of viral rebound" (NCT02850016)
Timeframe: Week 24 to Week 36

Interventiondays (Median)
Group A18
Group B28

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HIV-1 Transcriptional Activity as Determined by Unspliced HIV-1 RNA (CA usHIV-1 RNA) in Circulating Total CD4+ T Cells.

The median fold-change in cell-associated unspliced HIV-1 RNA concentrations after romidepsin administration across all infusions (NCT02850016)
Timeframe: baseline and week 24

InterventionCA-us HIV-1 RNA per million CD4 T cells (Median)
Group A9
Group B11

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Plasma HIV-1 RNA

As measured by a routine clinical assay (Cobas Taqman; detection limit 20 copies/mL), a transcription mediated amplification (TMA)-based assay (detection limit 12 copies/ml) and/or a single copy assay (detection limit 1-2 copies/mL) (NCT02850016)
Timeframe: 48 weeks

InterventionParticipants (Count of Participants)
Group A4
Group B4

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Number of of Adverse Events (AE), Serious Adverse Events (SAE), and Serious Unexpected Serious Adverse Reactions (SUSAR).

The occurrence of adverse events was assessed during each follow up visit. Adverse events of grades 1 or higher were reported. (NCT02850016)
Timeframe: 48 weeks

,
Interventionevents (Number)
All Adverse events related to RomidepsinAll Adverse events related to 3BNC117Grade 2 or higher Adverse Events Related to RomidepsinGrade 2 or higher Adverse Events Related to 3BNC117
Group A1124291
Group B66050

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Number of Patients With Grade 3 or Above Toxicities

Graded according to Common Terminology Criteria for Adverse Events (CTCAE) version (v.) 5.0. During the first 2 cycles, all grades of toxicity will be collected. After cycle 2, only the highest grade of any toxicity will be collected for each cycle during protocol treatment and for the period of safety follow-up after end of treatment. (NCT03534180)
Timeframe: Up to 30 days post-treatment, an average of 4 months.

InterventionParticipants (Count of Participants)
Treatment (Venetoclax, Romidepsin)9

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Overall Survival at 100 Days

Overall survival (OS) was measured from start of the study treatment to death from any cause. OS to be estimated using the product-limit method of Kaplan- Meier with the Greenwood estimator of standard error. (NCT03534180)
Timeframe: From the start of study treatment up to 100 days

Interventionpercent probability (Number)
Treatment (Venetoclax, Romidepsin)63

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Overall Response Rate (ORR) With Tenalisib and Romidepsin Combination

Overall response (ORR) = CR + PR) was assessed according to the Lugano classification with PTCL and according to the modified Severity Weighted Assessment Tool (mSWAT)/Global assessment in patients with CTCL. (NCT03770000)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Dose escalation_Cohort 12
Dose escalation_Cohort 22
Dose escalation_Cohort 30
Dose expansion_Group 1 (PTCL)7
Dose expansion_Group 2 (CTCL)6

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Maximum Observed Plasma Concentration (Cmax)

Assessment of Cmax in subjects treated with Tenalisib and Romidepsin combination. Blood samples for measurement of RP6530 plasma concentrations were collected pre-dose and at 0.5, 1, 2, 3, 4, 6, 8, 10, and 11 hours after dosing on Day 8 of the first cycle. Maximum (peak) drug concentration (Cmax in nanograms/milliliter) was estimated using Single-Dose data. (NCT03770000)
Timeframe: 8 days

Interventionnanogram/millilitre (Mean)
Dose escalation_Cohort 11544.42
Dose escalation_Cohort 22152.17
Dose escalation_Cohort 35791.11

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Duration of Response (DoR) With Tenalisib and Romidepsin Combination

The time period from the response achieved in patient until the disease progression (NCT03770000)
Timeframe: 28 weeks

Interventiondays (Median)
Dose escalation_Cohort 1151
Dose escalation_Cohort 2151
Dose expansion_Group1 (PTCL Patients)151
Dose expansion_Group2 (CTCL Patients)114

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