Page last updated: 2024-12-05

vinblastine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Vinblastine is a natural alkaloid, extracted from the Madagascar periwinkle plant (Catharanthus roseus). It acts as an anti-cancer agent, specifically targeting microtubules. The compound inhibits the polymerization of tubulin, a protein that forms microtubules, which are essential for cell division. This disruption of microtubule function leads to cell cycle arrest and ultimately, cell death. Vinblastine is particularly effective against various cancers, including Hodgkin's lymphoma, non-Hodgkin's lymphoma, and testicular cancer. Its importance lies in its ability to provide significant clinical benefit to patients with these diseases. Continued research on vinblastine focuses on understanding its mechanism of action, optimizing its therapeutic efficacy, and exploring its potential for combination therapies. Studies also investigate its potential use in other diseases, such as autoimmune disorders and viral infections.'

sobrerol: RN given is for parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
VincagenusA plant genus of the family Apocynaceae.[MeSH]ApocynaceaeThe dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters.[MeSH]
VincagenusA plant genus of the family Apocynaceae.[MeSH]ApocynaceaeThe dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters.[MeSH]

Cross-References

ID SourceID
PubMed CID91463
CHEMBL ID2228862
CHEBI ID134802
SCHEMBL ID1649171
MeSH IDM0022672
PubMed CID13342
CHEMBL ID159
SCHEMBL ID3628
MeSH IDM0022672

Synonyms (112)

Synonym
p-menth-6-ene-2,8-diol, ( )-
3-cyclohexene-1-methanol, 5-hydroxy-.alpha.,.alpha.,4-trimethyl-, trans-( )-
OPREA1_276529
nsc43652
nsc-43652
NCIOPEN2_000885
sobrerol
nsc74541
nsc-74541
nsc-408849
nsc408849
ai3-23138
3-cyclohexene-1-methanol, 5-hydroxy-alpha,alpha,4-trimethyl-, (+/-)
einecs 207-868-1
soberol
5-hydroxy-alpha,alpha,4-trimethylcyclohex-3-ene-1-methanol
ccris 7135
CHEBI:134802
(1s)-5-(2-hydroxypropan-2-yl)-2-methylcyclohex-2-en-1-ol
sobrepin (tn)
D08520
mucoflux (tn)
cyclidrol
498-71-5
5-(2-hydroxypropan-2-yl)-2-methylcyclohex-2-en-1-ol
AKOS006230491
42370-41-2
pinol hydrate
6,8-carvomenthendiol
FT-0630625
CHEMBL2228862
SCHEMBL1649171
5-(2-hydroxypropan-2-yl)-2-methylcyclohex-2-enol
pinolhydrat
6,8-carvomenthenedioll-p-methene-6,8-diolpinol hydrate
5-hydroxy-.alpha.,.alpha.,4-trimethyl-3-cyclohexene-1-methanol
3-cyclohexene-1-methanol, 5-hydroxy-.alpha.,.alpha.,4-trimethyl-
(+/-)-1-hydroxyisodihydrocarveol
6,8-carvomenthenediol; nsc 408849; pinol hydrate; sobrepin
d,l-trans-sobrerol; dl-sobrerol; trans-6-hydroxy-alpha-terpineol
1,2-cyclohexanediol, 1-methyl-4-(1-methylethenyl)-, (1alpha,2alpha,4beta)- (9ci); 1,2-cyclohexanediol, 1-methyl-4-(1-methylethenyl)-, (1alpha,2alpha,4beta)-(+/-)-
DTXSID90871701
BIDD:PXR0201
vinblastinum
vinblastina
unii-5v9klz54cy
5v9klz54cy ,
BRD-K01188359-065-02-5
nsc 49842
velban
vincaleukoblastine
vinblastin
ndc 0002-1452-01
vincoblastine
einecs 212-734-0
nci-c04842
rozevin
vinblastine [inn:ban]
vr-8
vinblastina [dcit]
vincaleucoblastin
hsdb 3263
(3ar-(3aalpha,4beta,5beta,5abeta,9(3r*,5s*,7r*,9s*),10br*,13aalpha))-methyl 4-(acetyloxy)-3a-ethyl-9-(5-ethyl-1,4,5,6,7,8,9,10-octahydro-5-hydroxy-9-(methoxycarbonyl)-2h-3,7-methanoazacycloundecino(5,4-b)indol-9-yl)-3a,4,5,5a,6,11,12,13a-octahydro-5-hydro
nincaluicolflastine
vinblastinum [inn-latin]
nsc 47842
1h-indolizino(8,1-cd)carbazole-5-carboxylic acid, 4-(acetyloxy)-3a-ethyl-9-(5-ethyl-1,4,5,6,7,8,9,10-octahydro-5-hydroxy-9-(methoxycarbonyl)-2h-3,7-methanoazacycloundecino(5,4-b)indol-9-yl)-3a,4,5,5a,6,11,12,13a-octahydro-5-hydroxy-8-methoxy-6-methyl-, me
ccris 9002
(2alpha,2'beta,3beta,4alpha,5beta)-vincaleukoblastine
VLB ,
1Z2B
DB00570
BSPBIO_001228
NCGC00022585-04
[3h]-vinblastine
nsc-47842
CHEMBL159 ,
bdbm50012278
(2alpha,2''''beta,3beta,4alpha,5beta)-vincaleukoblastine
cid_5388983
NCGC00022585-05
AKOS015965500
HY-17418
CS-1336
gtpl6851
vinblastine [mi]
vinblastine [inn]
vincristine sulfate impurity h [ep impurity]
vinblastine [hsdb]
vindesine sulfate impurity b [ep impurity]
vinblastine [vandf]
vinblastine [who-dd]
SCHEMBL3628
JXLYSJRDGCGARV-CFWMRBGOSA-N
AC-24191
DTXSID8021430 ,
vbl
methyl (3ar,3a1r,4r,5s,5ar,10br)-4-acetoxy-3a-ethyl-9-((5s,7r,9s)-5-ethyl-5-hydroxy-9-(methoxycarbonyl)-1,4,5,6,7,8,9,10-octahydro-2h-3,7-methano[1]azacycloundecino[5,4-b]indol-9-yl)-5-hydroxy-8-methoxy-6-methyl-3a,3a1,4,5,5a,6,11,12-octahydro-1h-indolizi
NCGC00485975-02
BRD-K01188359-001-02-0
(2alpha,2'beta,3alpha,5beta,19beta)-vincaleukoblastine
methyl (1r,9r,10s,11r,12r,19r)-11-acetyloxy-12-ethyl-4-[(13s,15r,17s)-17-ethyl-17-hydroxy-13-methoxycarbonyl-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraen-13-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.01
132142-72-4
AS-15821
EN300-19874057
methyl (1r,9r,10s,11r,12r,19r)-11-(acetyloxy)-12-ethyl-4-[(13s,15r,17s)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0^{4,12}.0^{5,10}]nonadeca-4(12),5(10),6,8-tetraen-13-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.
nsc816570
nsc-816570
l01ca01
dtxcid801430
vinblastinum (inn-latin)
(3ar-(3aalpha,4beta,5beta,5abeta,9(3r*,5s*,7r*,9s*),10br*,13aalpha))-methyl 4-(acetyloxy)-3a-ethyl-9-(5-ethyl-1,4,5,6,7,8,9,10-octahydro-5-hydroxy-9- (methoxycarbonyl)-2h-3,7-methanoazacycloundecino(5,4-b)indol-9-yl)- 3a,4,5,5a,6,11,12,13a-octahydro-5-hyd

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Treatment with sobrerol was well tolerated but two patients treated with placebo reported adverse reactions (stomach pain and cutaneous rash)."( Evaluation of the efficacy and safety of sobrerol granules in patients suffering from chronic rhinosinusitis.
Bellussi, L; Buccella, MG; Cacchi, R; Manini, G,
)
0.13

Pharmacokinetics

ExcerptReferenceRelevance
"The pharmacokinetic profile of Sobrerol, a mucolytic drug, has been studied in patients with acute exacerbations of chronic bronchitis and dense sputum."( Pharmacokinetics of Sobrerol in chronic bronchitis. Comparison of serum and bronchial mucus levels.
Allegra, L; Bossi, R; Braga, PC; De Angelis, L; Fraschini, F; Scaglione, F; Scarpazza, G, 1983
)
0.27
"The reversal effect of itraconazole on P-glycoprotein (P-gp)-mediated resistance of vinblastine, daunorubicin and doxorubicin was analyzed from a cellular pharmacokinetic point of view, namely by [3H]azidopine photoaffinity labeling, intracellular accumulation and transcellular transport experiments."( Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
Komada, F; Nishiguchi, K; Okumura, K; Sakaeda, T; Takara, K; Tanigawara, Y, 1999
)
0.53
"The mechanisms of pharmacokinetic interactions of a novel anti-human immunodeficiency virus (anti-HIV-1) antagonist of chemokine receptor 5 (CCR5) [2-(R)-[N-methyl-N-(1-(R)-3-(S)-((4-(3-benzyl-1-ethyl-(1H)-pyrazol-5-yl)piperidin-1-yl)methyl)-4-(S)-(3-fluorophenyl)cyclopent-1-yl)amino]-3-methylbutanoic acid (MRK-1)] with ritonavir were evaluated in rats and monkeys."( Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.
Baillie, TA; Chen, Q; Chiu, SH; Didolkar, V; Franklin, RB; Iliff, SA; Kumar, S; Kwei, GY; Lin, JH; Pearson, PG; Poon, GK; Wang, RW; Wang, Y; Yamazaki, M, 2003
)
0.32
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33
" 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
" Furthermore, the pharmacokinetic profile of the sesquiterpene lactones was investigated using computational methods."( Sesquiterpene lactones from Anthemis melanolepis and their antibacterial and cytotoxic activities. Prediction of their pharmacokinetic profile.
Dimas, K; Karioti, A; Koukoulitsa, C; Rancic, A; Saroglou, V; Skaltsa, H; Zervou, M, 2010
)
0.36

Compound-Compound Interactions

ExcerptReferenceRelevance
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
" Although the systemic pharmacokinetics of MRK-1 in rats and monkeys were linear, the oral bioavailability increased with an increase in dose from 2 to 10 mg/kg."( Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.
Baillie, TA; Chen, Q; Chiu, SH; Didolkar, V; Franklin, RB; Iliff, SA; Kumar, S; Kwei, GY; Lin, JH; Pearson, PG; Poon, GK; Wang, RW; Wang, Y; Yamazaki, M, 2003
)
0.32
" Aniline 6 is orally bioavailable and is 250-fold more potent than noscapine in reducing cell proliferation in rapidly dividing cells."( Identification of novel and improved antimitotic agents derived from noscapine.
Anderson, JT; Bennani, YL; Boozer, S; Brunden, KR; Crumrine, C; Danzig, J; Dent, T; Faga, L; Harrington, JJ; Hodnick, WF; Murphy, SM; Pawlowski, G; Perry, R; Raber, A; Rundlett, SE; Stricker-Krongrad, A; Ting, AE; Wang, J, 2005
)
0.33
" Previously described THQ PFTIs had limitations of poor oral bioavailability and rapid clearance from the circulation of rodents."( Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.
Ankala, S; Barrett, LK; Bauer, KD; Bendale, P; Buckner, FS; Chakrabarti, D; Floyd, D; Gelb, MH; Hamilton, AD; Hornéy, C; Hucke, O; Lombardo, LJ; Nallan, L; Rivas, KL; Smart, BP; Strickland, C; Van Voorhis, WC; Verlinde, CL; Williams, DK; Yokoyama, K, 2007
)
0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" We targeted oral bioavailability and efficacy against multidrug resistant (MDR) tumors for further work."( Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
Carlson, EM; Cheng, H; Condon, K; Du, H; Eckley, S; Hu, Y; Jiang, Y; Kumar, V; Lewis, BM; Littlefield, BA; Narayan, S; Saxton, P; Schuck, E; Seletsky, BM; Tendyke, K; Towle, MJ; Yu, MJ; Zhang, H; Zheng, W, 2011
)
0.37
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" However, PB-93 was rapidly cleared, and dosing every 12 h failed to cure the rats."( Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.
Ankala, S; Barrett, LK; Bauer, KD; Bendale, P; Buckner, FS; Chakrabarti, D; Floyd, D; Gelb, MH; Hamilton, AD; Hornéy, C; Hucke, O; Lombardo, LJ; Nallan, L; Rivas, KL; Smart, BP; Strickland, C; Van Voorhis, WC; Verlinde, CL; Williams, DK; Yokoyama, K, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
p-menthane monoterpenoid
[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 (41)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)88.35000.11007.190310.0000AID681139; AID681155
Tubulin alpha-1A chainSus scrofa (pig)IC50 (µMol)1.10000.00672.160310.0000AID1244335; AID160673; AID551268
Tubulin beta chainSus scrofa (pig)IC50 (µMol)1.10000.00672.137410.0000AID1244335; AID160673; AID551268
Tubulin beta-4A chainHomo sapiens (human)IC50 (µMol)0.82330.00051.968010.0000AID1194487; AID214333; AID281715
CholinesteraseHomo sapiens (human)IC50 (µMol)2.10000.00001.559910.0000AID1194487
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)8.00000.06404.012610.0000AID150754; AID681128
Tubulin beta chainHomo sapiens (human)IC50 (µMol)0.82330.00052.052910.0000AID1194487; AID214333; AID281715
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)25.25710.00022.318510.0000AID150618; AID150752; AID150755; AID310120; AID310122; AID681122; AID681126; AID681127; AID681131; AID681381
ATP-dependent translocase ABCB1Homo sapiens (human)Ki32.50000.02002.35948.5900AID150616; AID150735; AID680140; AID681356; AID681383; AID681611
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)26.00000.00011.753610.0000AID54923
Tubulin alpha-3C chainHomo sapiens (human)IC50 (µMol)0.82330.00051.955510.0000AID1194487; AID214333; AID281715
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)0.60000.00002.015110.0000AID1203389
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC50 (µMol)5.03700.11003.26419.0330AID625146
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)2.10000.00031.09147.7625AID1194487
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)50.00000.20004.713010.0000AID150753; AID681119
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)2.10000.00031.09147.7625AID1194487
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)2.10000.00031.06917.7625AID1194487
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)1.87000.00091.230410.0000AID625229
Multidrug resistance-associated protein 1 Homo sapiens (human)IC50 (µMol)30.00000.00153.71109.6600AID679011
Amine oxidase [flavin-containing] BBos taurus (cattle)Ki77.00000.05401.83906.0000AID126507; AID358162
Tubulin alpha-1B chainHomo sapiens (human)IC50 (µMol)0.82330.00051.955510.0000AID1194487; AID214333; AID281715
Tubulin alpha-4A chainHomo sapiens (human)IC50 (µMol)0.82330.00051.955510.0000AID1194487; AID214333; AID281715
Tubulin beta-4B chainHomo sapiens (human)IC50 (µMol)0.82330.00051.968010.0000AID1194487; AID214333; AID281715
Tubulin beta-3 chainHomo sapiens (human)IC50 (µMol)0.82330.00051.894510.0000AID1194487; AID214333; AID281715
Tubulin beta-2A chainHomo sapiens (human)IC50 (µMol)0.82330.00051.968010.0000AID1194487; AID214333; AID281715
Beta-tubulin Leishmania donovaniIC50 (µMol)1.00001.00001.38002.0000AID247822
Tubulin beta-8 chainHomo sapiens (human)IC50 (µMol)0.82330.00051.968010.0000AID1194487; AID214333; AID281715
Tubulin beta-2B chainBos taurus (cattle)IC50 (µMol)0.65000.25001.88388.7000AID1203389; AID214009
Tubulin beta-2B chainBos taurus (cattle)Ki100.00000.14001.34003.2000AID213853
Tubulin alpha-3E chainHomo sapiens (human)IC50 (µMol)0.82330.00051.955510.0000AID1194487; AID214333; AID281715
Tubulin alpha-1A chainHomo sapiens (human)IC50 (µMol)0.82330.00051.955510.0000AID1194487; AID214333; AID281715
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)0.65000.25001.87798.7000AID1203389; AID214009
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)0.65000.25001.86568.7000AID1203389; AID214009
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)21.00002.41006.343310.0000AID681370
Tubulin alpha-1C chainHomo sapiens (human)IC50 (µMol)0.82330.00051.955510.0000AID1194487; AID214333; AID281715
Tubulin beta-6 chainHomo sapiens (human)IC50 (µMol)0.82330.00051.968010.0000AID1194487; AID214333; AID281715
Tubulin beta-2B chainHomo sapiens (human)IC50 (µMol)0.82330.00051.968010.0000AID1194487; AID214333; AID281715
Tubulin beta-1 chainHomo sapiens (human)IC50 (µMol)0.82330.00051.987010.0000AID1194487; AID214333; AID281715
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC50 (µMol)43.50000.10472.71957.0795AID1197747
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki18.60000.08002.46889.8000AID1197747
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC50 (µMol)46.80000.05002.37979.7000AID1197744
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki10.20000.04401.36305.0000AID1197744
[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)
Tubulin beta-4A chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
ATP-dependent translocase ABCB1Homo sapiens (human)EC50 (µMol)24.30000.01600.67863.1000AID678838; AID679466
ATP-dependent translocase ABCB1Homo sapiens (human)Kd3.00000.07305.798110.0000AID680155
Tubulin alpha-3C chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin alpha-1B chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin alpha-4A chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta-4B chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta-3 chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta-2A chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta-8 chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin alpha-3E chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin alpha-1A chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin alpha-1C chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta-6 chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta-2B chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
Tubulin beta-1 chainHomo sapiens (human)EC50 (µMol)0.20000.00900.36851.2300AID282705
[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)
interferon gamma precursorHomo sapiens (human)AC500.16000.128015.173038.6100AID1259420
ATP-dependent translocase ABCB1Homo sapiens (human)Activity15.90000.02001.67004.5000AID386358; AID386359; AID386360
ATP-dependent translocase ABCB1Homo sapiens (human)Km75.54000.01403.717210.0000AID679236; AID679260; AID681163; AID681164; AID681613
Non-lysosomal glucosylceramidaseMus musculus (house mouse)Activity1.20001.20001.20001.2000AID386360
Canalicular multispecific organic anion transporter 1Homo sapiens (human)Km137.30007.20008.30009.4000AID680782
Bile salt export pumpMus musculus (house mouse)Km38.30005.70005.70005.7000AID681566
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (150)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
negative regulation of microtubule polymerizationTubulin beta-4A chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-4A chainHomo sapiens (human)
mitotic cell cycleTubulin beta-4A chainHomo sapiens (human)
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
odontoblast differentiationTubulin beta chainHomo sapiens (human)
microtubule-based processTubulin beta chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin beta chainHomo sapiens (human)
natural killer cell mediated cytotoxicityTubulin beta chainHomo sapiens (human)
regulation of synapse organizationTubulin beta chainHomo sapiens (human)
spindle assemblyTubulin beta chainHomo sapiens (human)
cell divisionTubulin beta chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta chainHomo sapiens (human)
mitotic cell cycleTubulin beta chainHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-3C chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-3C chainHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo sapiens (human)
leukotriene metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
response to xenobiotic stimulusMultidrug resistance-associated protein 1 Homo sapiens (human)
cobalamin transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid biosynthetic processMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to oxidative stressMultidrug resistance-associated protein 1 Homo sapiens (human)
heme catabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transportMultidrug resistance-associated protein 1 Homo sapiens (human)
phospholipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
positive regulation of inflammatory responseMultidrug resistance-associated protein 1 Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cell chemotaxisMultidrug resistance-associated protein 1 Homo sapiens (human)
transepithelial transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cyclic nucleotide transportMultidrug resistance-associated protein 1 Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 1 Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to amyloid-betaMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-1B chainHomo sapiens (human)
microtubule-based processTubulin alpha-1B chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin alpha-1B chainHomo sapiens (human)
cell divisionTubulin alpha-1B chainHomo sapiens (human)
cellular response to interleukin-4Tubulin alpha-1B chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-1B chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-4A chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-4A chainHomo sapiens (human)
natural killer cell mediated cytotoxicityTubulin beta-4B chainHomo sapiens (human)
mitotic cell cycleTubulin beta-4B chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-4B chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-3 chainHomo sapiens (human)
axon guidanceTubulin beta-3 chainHomo sapiens (human)
netrin-activated signaling pathwayTubulin beta-3 chainHomo sapiens (human)
dorsal root ganglion developmentTubulin beta-3 chainHomo sapiens (human)
mitotic cell cycleTubulin beta-3 chainHomo sapiens (human)
cerebral cortex developmentTubulin beta-2A chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-2A chainHomo sapiens (human)
mitotic cell cycleTubulin beta-2A chainHomo sapiens (human)
oocyte maturationTubulin beta-8 chainHomo sapiens (human)
spindle assembly involved in female meiosisTubulin beta-8 chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-8 chainHomo sapiens (human)
mitotic cell cycleTubulin beta-8 chainHomo sapiens (human)
microtubule-based processTubulin beta-2B chainBos taurus (cattle)
nervous system developmentTubulin beta-2B chainBos taurus (cattle)
positive regulation of axon guidanceTubulin beta-2B chainBos taurus (cattle)
biological_processTubulin alpha-3E chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-3E chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-3E chainHomo sapiens (human)
neuron migrationTubulin alpha-1A chainHomo sapiens (human)
startle responseTubulin alpha-1A chainHomo sapiens (human)
intracellular protein transportTubulin alpha-1A chainHomo sapiens (human)
microtubule-based processTubulin alpha-1A chainHomo sapiens (human)
centrosome cycleTubulin alpha-1A chainHomo sapiens (human)
smoothened signaling pathwayTubulin alpha-1A chainHomo sapiens (human)
memoryTubulin alpha-1A chainHomo sapiens (human)
adult locomotory behaviorTubulin alpha-1A chainHomo sapiens (human)
visual learningTubulin alpha-1A chainHomo sapiens (human)
response to mechanical stimulusTubulin alpha-1A chainHomo sapiens (human)
glial cell differentiationTubulin alpha-1A chainHomo sapiens (human)
gene expressionTubulin alpha-1A chainHomo sapiens (human)
dentate gyrus developmentTubulin alpha-1A chainHomo sapiens (human)
cerebellar cortex morphogenesisTubulin alpha-1A chainHomo sapiens (human)
pyramidal neuron differentiationTubulin alpha-1A chainHomo sapiens (human)
cerebral cortex developmentTubulin alpha-1A chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin alpha-1A chainHomo sapiens (human)
response to tumor necrosis factorTubulin alpha-1A chainHomo sapiens (human)
locomotory exploration behaviorTubulin alpha-1A chainHomo sapiens (human)
microtubule polymerizationTubulin alpha-1A chainHomo sapiens (human)
forebrain morphogenesisTubulin alpha-1A chainHomo sapiens (human)
homeostasis of number of cells within a tissueTubulin alpha-1A chainHomo sapiens (human)
regulation of synapse organizationTubulin alpha-1A chainHomo sapiens (human)
synapse organizationTubulin alpha-1A chainHomo sapiens (human)
cell divisionTubulin alpha-1A chainHomo sapiens (human)
neuron apoptotic processTubulin alpha-1A chainHomo sapiens (human)
motor behaviorTubulin alpha-1A chainHomo sapiens (human)
cellular response to calcium ionTubulin alpha-1A chainHomo sapiens (human)
organelle transport along microtubuleTubulin alpha-1A chainHomo sapiens (human)
neuron projection arborizationTubulin alpha-1A chainHomo sapiens (human)
response to L-glutamateTubulin alpha-1A chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-1A chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-1A chainHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
microtubule-based processTubulin alpha-1C chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin alpha-1C chainHomo sapiens (human)
cell divisionTubulin alpha-1C chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-1C chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-1C chainHomo sapiens (human)
mitotic cell cycleTubulin beta-6 chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-6 chainHomo sapiens (human)
neuron migrationTubulin beta-2B chainHomo sapiens (human)
microtubule-based processTubulin beta-2B chainHomo sapiens (human)
cerebral cortex developmentTubulin beta-2B chainHomo sapiens (human)
modulation of chemical synaptic transmissionTubulin beta-2B chainHomo sapiens (human)
positive regulation of axon guidanceTubulin beta-2B chainHomo sapiens (human)
embryonic brain developmentTubulin beta-2B chainHomo sapiens (human)
mitotic cell cycleTubulin beta-2B chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-2B chainHomo sapiens (human)
platelet formationTubulin beta-1 chainHomo sapiens (human)
thyroid gland developmentTubulin beta-1 chainHomo sapiens (human)
microtubule polymerizationTubulin beta-1 chainHomo sapiens (human)
spindle assemblyTubulin beta-1 chainHomo sapiens (human)
thyroid hormone transportTubulin beta-1 chainHomo sapiens (human)
platelet aggregationTubulin beta-1 chainHomo sapiens (human)
mitotic cell cycleTubulin beta-1 chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-1 chainHomo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (86)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
GTPase activityTubulin beta-4A chainHomo sapiens (human)
calcium ion bindingTubulin beta-4A chainHomo sapiens (human)
protein bindingTubulin beta-4A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-4A chainHomo sapiens (human)
GTP bindingTubulin beta-4A chainHomo sapiens (human)
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
GTPase activityTubulin beta chainHomo sapiens (human)
structural molecule activityTubulin beta chainHomo sapiens (human)
protein bindingTubulin beta chainHomo sapiens (human)
protein domain specific bindingTubulin beta chainHomo sapiens (human)
ubiquitin protein ligase bindingTubulin beta chainHomo sapiens (human)
GTPase activating protein bindingTubulin beta chainHomo sapiens (human)
MHC class I protein bindingTubulin beta chainHomo sapiens (human)
protein-containing complex bindingTubulin beta chainHomo sapiens (human)
metal ion bindingTubulin beta chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta chainHomo sapiens (human)
GTP bindingTubulin beta chainHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
hydrolase activityTubulin alpha-3C chainHomo sapiens (human)
metal ion bindingTubulin alpha-3C chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-3C chainHomo sapiens (human)
GTP bindingTubulin alpha-3C chainHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Mus musculus (house mouse)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type vitamin B12 transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled lipid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BBos taurus (cattle)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BBos taurus (cattle)
monoamine oxidase activityAmine oxidase [flavin-containing] BBos taurus (cattle)
double-stranded RNA bindingTubulin alpha-1B chainHomo sapiens (human)
GTPase activityTubulin alpha-1B chainHomo sapiens (human)
structural molecule activityTubulin alpha-1B chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-1B chainHomo sapiens (human)
protein bindingTubulin alpha-1B chainHomo sapiens (human)
GTP bindingTubulin alpha-1B chainHomo sapiens (human)
ubiquitin protein ligase bindingTubulin alpha-1B chainHomo sapiens (human)
protein bindingTubulin alpha-4A chainHomo sapiens (human)
hydrolase activityTubulin alpha-4A chainHomo sapiens (human)
protein kinase bindingTubulin alpha-4A chainHomo sapiens (human)
metal ion bindingTubulin alpha-4A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-4A chainHomo sapiens (human)
GTP bindingTubulin alpha-4A chainHomo sapiens (human)
double-stranded RNA bindingTubulin beta-4B chainHomo sapiens (human)
GTPase activityTubulin beta-4B chainHomo sapiens (human)
protein bindingTubulin beta-4B chainHomo sapiens (human)
MHC class I protein bindingTubulin beta-4B chainHomo sapiens (human)
metal ion bindingTubulin beta-4B chainHomo sapiens (human)
unfolded protein bindingTubulin beta-4B chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-4B chainHomo sapiens (human)
GTP bindingTubulin beta-4B chainHomo sapiens (human)
GTPase activityTubulin beta-3 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-3 chainHomo sapiens (human)
protein bindingTubulin beta-3 chainHomo sapiens (human)
GTP bindingTubulin beta-3 chainHomo sapiens (human)
peptide bindingTubulin beta-3 chainHomo sapiens (human)
metal ion bindingTubulin beta-3 chainHomo sapiens (human)
netrin receptor bindingTubulin beta-3 chainHomo sapiens (human)
GTPase activityTubulin beta-2A chainHomo sapiens (human)
protein bindingTubulin beta-2A chainHomo sapiens (human)
metal ion bindingTubulin beta-2A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-2A chainHomo sapiens (human)
GTP bindingTubulin beta-2A chainHomo sapiens (human)
molecular_functionTubulin beta-8 chainHomo sapiens (human)
GTPase activityTubulin beta-8 chainHomo sapiens (human)
metal ion bindingTubulin beta-8 chainHomo sapiens (human)
GTP bindingTubulin beta-8 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-8 chainHomo sapiens (human)
GTPase activityTubulin beta-2B chainBos taurus (cattle)
metal ion bindingTubulin beta-2B chainBos taurus (cattle)
protein heterodimerization activityTubulin beta-2B chainBos taurus (cattle)
molecular_functionTubulin alpha-3E chainHomo sapiens (human)
protein bindingTubulin alpha-3E chainHomo sapiens (human)
hydrolase activityTubulin alpha-3E chainHomo sapiens (human)
metal ion bindingTubulin alpha-3E chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-3E chainHomo sapiens (human)
GTP bindingTubulin alpha-3E chainHomo sapiens (human)
structural molecule activityTubulin alpha-1A chainHomo sapiens (human)
protein bindingTubulin alpha-1A chainHomo sapiens (human)
hydrolase activityTubulin alpha-1A chainHomo sapiens (human)
identical protein bindingTubulin alpha-1A chainHomo sapiens (human)
protein-containing complex bindingTubulin alpha-1A chainHomo sapiens (human)
metal ion bindingTubulin alpha-1A chainHomo sapiens (human)
protein heterodimerization activityTubulin alpha-1A chainHomo sapiens (human)
GTP bindingTubulin alpha-1A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-1A chainHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
structural molecule activityTubulin alpha-1C chainHomo sapiens (human)
protein bindingTubulin alpha-1C chainHomo sapiens (human)
hydrolase activityTubulin alpha-1C chainHomo sapiens (human)
metal ion bindingTubulin alpha-1C chainHomo sapiens (human)
GTP bindingTubulin alpha-1C chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-1C chainHomo sapiens (human)
molecular_functionTubulin beta-6 chainHomo sapiens (human)
GTPase activityTubulin beta-6 chainHomo sapiens (human)
protein bindingTubulin beta-6 chainHomo sapiens (human)
metal ion bindingTubulin beta-6 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-6 chainHomo sapiens (human)
GTP bindingTubulin beta-6 chainHomo sapiens (human)
GTPase activityTubulin beta-2B chainHomo sapiens (human)
protein bindingTubulin beta-2B chainHomo sapiens (human)
metal ion bindingTubulin beta-2B chainHomo sapiens (human)
protein heterodimerization activityTubulin beta-2B chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-2B chainHomo sapiens (human)
GTP bindingTubulin beta-2B chainHomo sapiens (human)
GTPase activityTubulin beta-1 chainHomo sapiens (human)
metal ion bindingTubulin beta-1 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-1 chainHomo sapiens (human)
GTP bindingTubulin beta-1 chainHomo sapiens (human)
serine-type endopeptidase inhibitor activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (56)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
nucleusTubulin beta-4A chainHomo sapiens (human)
cytosolTubulin beta-4A chainHomo sapiens (human)
microtubuleTubulin beta-4A chainHomo sapiens (human)
axonemeTubulin beta-4A chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-4A chainHomo sapiens (human)
internode region of axonTubulin beta-4A chainHomo sapiens (human)
neuronal cell bodyTubulin beta-4A chainHomo sapiens (human)
myelin sheathTubulin beta-4A chainHomo sapiens (human)
intercellular bridgeTubulin beta-4A chainHomo sapiens (human)
extracellular exosomeTubulin beta-4A chainHomo sapiens (human)
mitotic spindleTubulin beta-4A chainHomo sapiens (human)
microtubuleTubulin beta-4A chainHomo sapiens (human)
cytoplasmTubulin beta-4A chainHomo sapiens (human)
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
extracellular regionTubulin beta chainHomo sapiens (human)
nucleusTubulin beta chainHomo sapiens (human)
nuclear envelope lumenTubulin beta chainHomo sapiens (human)
cytoplasmTubulin beta chainHomo sapiens (human)
cytosolTubulin beta chainHomo sapiens (human)
cytoskeletonTubulin beta chainHomo sapiens (human)
microtubuleTubulin beta chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta chainHomo sapiens (human)
azurophil granule lumenTubulin beta chainHomo sapiens (human)
cytoplasmic ribonucleoprotein granuleTubulin beta chainHomo sapiens (human)
cell bodyTubulin beta chainHomo sapiens (human)
membrane raftTubulin beta chainHomo sapiens (human)
intercellular bridgeTubulin beta chainHomo sapiens (human)
extracellular exosomeTubulin beta chainHomo sapiens (human)
mitotic spindleTubulin beta chainHomo sapiens (human)
protein-containing complexTubulin beta chainHomo sapiens (human)
cytoplasmTubulin beta chainHomo sapiens (human)
microtubuleTubulin beta chainHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
nucleusTubulin alpha-3C chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-3C chainHomo sapiens (human)
microtubuleTubulin alpha-3C chainHomo sapiens (human)
cytoplasmTubulin alpha-3C chainHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Mus musculus (house mouse)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basal plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
lateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
extracellular exosomeMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BBos taurus (cattle)
mitochondrial outer membraneAmine oxidase [flavin-containing] BBos taurus (cattle)
microtubule cytoskeletonTubulin alpha-1B chainHomo sapiens (human)
microtubuleTubulin alpha-1B chainHomo sapiens (human)
cytoplasmic microtubuleTubulin alpha-1B chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-1B chainHomo sapiens (human)
microtubuleTubulin alpha-1B chainHomo sapiens (human)
cytoplasmTubulin alpha-1B chainHomo sapiens (human)
extracellular regionTubulin alpha-4A chainHomo sapiens (human)
cytosolTubulin alpha-4A chainHomo sapiens (human)
cytoskeletonTubulin alpha-4A chainHomo sapiens (human)
microtubuleTubulin alpha-4A chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-4A chainHomo sapiens (human)
extracellular exosomeTubulin alpha-4A chainHomo sapiens (human)
cytoplasmTubulin alpha-4A chainHomo sapiens (human)
microtubuleTubulin alpha-4A chainHomo sapiens (human)
extracellular regionTubulin beta-4B chainHomo sapiens (human)
nucleusTubulin beta-4B chainHomo sapiens (human)
cytosolTubulin beta-4B chainHomo sapiens (human)
cytoskeletonTubulin beta-4B chainHomo sapiens (human)
microtubuleTubulin beta-4B chainHomo sapiens (human)
axonemal microtubuleTubulin beta-4B chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-4B chainHomo sapiens (human)
azurophil granule lumenTubulin beta-4B chainHomo sapiens (human)
intercellular bridgeTubulin beta-4B chainHomo sapiens (human)
extracellular exosomeTubulin beta-4B chainHomo sapiens (human)
mitotic spindleTubulin beta-4B chainHomo sapiens (human)
extracellular vesicleTubulin beta-4B chainHomo sapiens (human)
microtubuleTubulin beta-4B chainHomo sapiens (human)
cytoplasmTubulin beta-4B chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-3 chainHomo sapiens (human)
nucleusTubulin beta-3 chainHomo sapiens (human)
microtubuleTubulin beta-3 chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-3 chainHomo sapiens (human)
lamellipodiumTubulin beta-3 chainHomo sapiens (human)
filopodiumTubulin beta-3 chainHomo sapiens (human)
axonTubulin beta-3 chainHomo sapiens (human)
dendriteTubulin beta-3 chainHomo sapiens (human)
growth coneTubulin beta-3 chainHomo sapiens (human)
neuronal cell bodyTubulin beta-3 chainHomo sapiens (human)
intercellular bridgeTubulin beta-3 chainHomo sapiens (human)
extracellular exosomeTubulin beta-3 chainHomo sapiens (human)
cell peripheryTubulin beta-3 chainHomo sapiens (human)
mitotic spindleTubulin beta-3 chainHomo sapiens (human)
microtubuleTubulin beta-3 chainHomo sapiens (human)
cytoplasmTubulin beta-3 chainHomo sapiens (human)
nucleusTubulin beta-2A chainHomo sapiens (human)
microtubuleTubulin beta-2A chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-2A chainHomo sapiens (human)
intercellular bridgeTubulin beta-2A chainHomo sapiens (human)
extracellular exosomeTubulin beta-2A chainHomo sapiens (human)
mitotic spindleTubulin beta-2A chainHomo sapiens (human)
extracellular vesicleTubulin beta-2A chainHomo sapiens (human)
cytoplasmTubulin beta-2A chainHomo sapiens (human)
microtubuleTubulin beta-2A chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-8 chainHomo sapiens (human)
intercellular bridgeTubulin beta-8 chainHomo sapiens (human)
extracellular exosomeTubulin beta-8 chainHomo sapiens (human)
mitotic spindleTubulin beta-8 chainHomo sapiens (human)
meiotic spindleTubulin beta-8 chainHomo sapiens (human)
microtubuleTubulin beta-8 chainHomo sapiens (human)
cytoplasmTubulin beta-8 chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-2B chainBos taurus (cattle)
nucleusTubulin alpha-3E chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-3E chainHomo sapiens (human)
microtubuleTubulin alpha-3E chainHomo sapiens (human)
cytoplasmTubulin alpha-3E chainHomo sapiens (human)
condensed chromosomeTubulin alpha-1A chainHomo sapiens (human)
nucleusTubulin alpha-1A chainHomo sapiens (human)
cytosolTubulin alpha-1A chainHomo sapiens (human)
microtubuleTubulin alpha-1A chainHomo sapiens (human)
axonemal microtubuleTubulin alpha-1A chainHomo sapiens (human)
plasma membraneTubulin alpha-1A chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-1A chainHomo sapiens (human)
neuromuscular junctionTubulin alpha-1A chainHomo sapiens (human)
cytoplasmic ribonucleoprotein granuleTubulin alpha-1A chainHomo sapiens (human)
recycling endosomeTubulin alpha-1A chainHomo sapiens (human)
extracellular exosomeTubulin alpha-1A chainHomo sapiens (human)
microtubuleTubulin alpha-1A chainHomo sapiens (human)
cytoplasmTubulin alpha-1A chainHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleusTubulin alpha-1C chainHomo sapiens (human)
microtubuleTubulin alpha-1C chainHomo sapiens (human)
cytoplasmic microtubuleTubulin alpha-1C chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-1C chainHomo sapiens (human)
vesicleTubulin alpha-1C chainHomo sapiens (human)
membrane raftTubulin alpha-1C chainHomo sapiens (human)
microtubuleTubulin alpha-1C chainHomo sapiens (human)
cytoplasmTubulin alpha-1C chainHomo sapiens (human)
nucleusTubulin beta-6 chainHomo sapiens (human)
microtubuleTubulin beta-6 chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-6 chainHomo sapiens (human)
intercellular bridgeTubulin beta-6 chainHomo sapiens (human)
extracellular exosomeTubulin beta-6 chainHomo sapiens (human)
mitotic spindleTubulin beta-6 chainHomo sapiens (human)
cytoplasmTubulin beta-6 chainHomo sapiens (human)
microtubuleTubulin beta-6 chainHomo sapiens (human)
nucleusTubulin beta-2B chainHomo sapiens (human)
microtubuleTubulin beta-2B chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-2B chainHomo sapiens (human)
intercellular bridgeTubulin beta-2B chainHomo sapiens (human)
mitotic spindleTubulin beta-2B chainHomo sapiens (human)
Schaffer collateral - CA1 synapseTubulin beta-2B chainHomo sapiens (human)
microtubuleTubulin beta-2B chainHomo sapiens (human)
cytoplasmTubulin beta-2B chainHomo sapiens (human)
cytoplasmTubulin beta-1 chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-1 chainHomo sapiens (human)
intercellular bridgeTubulin beta-1 chainHomo sapiens (human)
extracellular exosomeTubulin beta-1 chainHomo sapiens (human)
mitotic spindleTubulin beta-1 chainHomo sapiens (human)
microtubuleTubulin beta-1 chainHomo sapiens (human)
cytoplasmTubulin beta-1 chainHomo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1010)

Assay IDTitleYearJournalArticle
AID1080459Antifeedant activity against apterous adult stage of Lipaphis erysimi (mustard aphids) in compound pre-treated cabbage leaves assessed as antifeedant ratio measured after 48 hr2008Journal of agricultural and food chemistry, Dec-10, Volume: 56, Issue:23
Quantitative structure-activity relationship of terpenoid aphid antifeedants.
AID357339Cytotoxicity against mouse B16 cells by MTT assay2001Journal of natural products, Aug, Volume: 64, Issue:8
New jatrophane diterpenoid esters from Euphorbia turczaninowii.
AID272491Antiproliferative activity against multidrug resistant MDA435/LCC6 cells by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID319346Resistant ratio, IC50 for multidrug resistant human HepG2 cells to IC50 for human HepG2 cells2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID551863Antiangiogenic activity against FGF2-induced HUVEC assessed as inhibition of cell proliferation at 10'-5 uM after 24 hrs2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis, in vitro and in vivo preliminary evaluation of anti-angiogenic properties of some pyrroloazaflavones.
AID150368Compound was tested in vitro for growth inhibition of murine leukemic P388 cells1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Novel antineoplastic agents with efficacy against multidrug resistant tumor cells.
AID1203387Cytotoxicity against human NCI60 cells2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID319347Growth inhibition of human K562 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID266298Antiproliferative activity against human vinblastine resistant CCRF-CEM cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity.
AID273255Antiproliferative activity against HeLa-mdr1 cells overexpressing P-glycoprotein in presence of verapamil by SRB assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis, structure-activity relationships, and antitumor studies of 2-benzoxazolyl hydrazones derived from alpha-(N)-acyl heteroaromatics.
AID124265In vivo activity against transplanted colon-26 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID132719Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intravenously at a dose of 6 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID607675Effect on bovine brain microtubule depolymerization assessed as decrease in absorbance at wavelength 340 nm after 15 mins2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
2-Amino-4-methyl-5-phenylethyl substituted-7-N-benzyl-pyrrolo[2,3-d]pyrimidines as novel antitumor antimitotic agents that also reverse tumor resistance.
AID367772Cytotoxicity against vinblastine-resistant human CCRF-CEM cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Novel DNA-directed alkylating agents: design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker.
AID1154192Cytotoxicity against human CEM/VBL100 cells assessed as growth inhibition after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and biological evaluation of arylcinnamide hybrid derivatives as novel anticancer agents.
AID154246Compound was tested for T/C range at optimal dose of 3.0 mg/kg for antitumor activity against P388 leukemia cells in mice; value ranges from 157-2031991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
New alpha-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity.
AID1197745Inhibition of human OATP1B3-mediated [3H]CCK-8 at 100 uM after 5 mins relative to control2015European journal of medicinal chemistry, Mar-06, Volume: 92Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID155864In vitro cytotoxic activity (growth inhibition) of compound against PC-12 human cancer cell line was determined2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity.
AID40597The ratio of survival time for treated divided by survival time of control x 100 at a dose of 0.2 mg/kg in B16 melanoma cells1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Chalcones: a new class of antimitotic agents.
AID404109Cytotoxicity against human OVCAR-3 cells after 48 hrs by SRB assay2005Journal of natural products, Sep, Volume: 68, Issue:9
Sesquiterpene lactones from Centaurea spinosa and their antibacterial and cytotoxic activities.
AID1237725Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID762138Cytotoxicity against human HCT116 cells after 72 hrs by resazurin assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and biological evaluation of a new series of highly functionalized 7'-homo-anhydrovinblastine derivatives.
AID551505Cytotoxicity against human MRC5 cells assessed as metabolic active cells at 100 uM after 72 hrs by XTT assay relative to control2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones.
AID319342Growth inhibition of human KB V1 cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID379779Cytotoxicity against human KB cells1999Journal of natural products, May, Volume: 62, Issue:5
A new bistetrahydrofuran acetogenin from the roots of Annona salzmanii.
AID375830Growth inhibition of human HCT116 cells after 48 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2: Structure-activity relationships of the 4-, 5-, 6-, 7- and 8-positions.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID404105Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2005Journal of natural products, Sep, Volume: 68, Issue:9
Sesquiterpene lactones from Centaurea spinosa and their antibacterial and cytotoxic activities.
AID681611TP_TRANSPORTER: transepithelial transport of digoxin (basal to apical) in Caco-2 cells2003Pharmaceutical research, Feb, Volume: 20, Issue:2
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID271729Inhibition of ATPase measured as ATP availability in Caco-2 cells at 20 nM after 120 mins relative to control2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
AID319344Growth inhibition of human HepG2 cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID1197744Inhibition of human OATP1B1-mediated [3H]estrone 3-sulfate at after 5 mins by Dixon plot method2015European journal of medicinal chemistry, Mar-06, Volume: 92Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID599279Cytotoxicity against human MRC5 cells assessed as cell viability at 0.12 uM after 72 hrs by XTT proliferation assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria.
AID101911Cytotoxic activity was evaluated against MCF-7/ADR cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID777495Ratio of IC50 for vinblastine-resistant human HCT116/VM46 cells overexpressing P-gp to IC50 for vinblastine-sensitive human HCT116 cells by phosphatase assay
AID1154393Inhibition of sheep brain tubulin assembly by UV-spectrophotometry2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
One-pot synthesis of vinca alkaloids-phomopsin hybrids.
AID607291Antiproliferative activity against human vinblastine-resistant CEM/VBL100 cells overexpressing P-gp assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID288696Growth inhibition of human MCF7 cells after 48 hrs2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Alkylation potency and protein specificity of aromatic urea derivatives and bioisosteres as potential irreversible antagonists of the colchicine-binding site.
AID272515Antiproliferative activity against adriamycin resistant P388 cells in presence of 5 uM verapamil by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID266301Antiproliferative activity against human MX1 cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity.
AID1236004Downregulation of Mcl-1 protein expression in human A549 cells at 100 nM after 24 hrs by Western blot analysis2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID627399Antiproliferative activity against human B16F0 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID1205824Displacement of colchicine from tubulin (unknown origin) preincubated for 30 mins followed by colchicine addition measured after 30 mins by fluorescence assay2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Synthesis and Structure-Activity Relationship Study of 1-Phenyl-1-(quinazolin-4-yl)ethanols as Anticancer Agents.
AID1236003Downregulation of Bcl-XL protein expression in human A549 cells at 100 nM after 24 hrs by Western blot analysis2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID605763Antiproliferative activity against mouse P388D1 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID248840Concentration required for growth inhibition of vinblastine resistant human lymphoblastic leukemic cell line (CCRF-CEM/VBL) was determined2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Potent antitumor N-mustard derivatives of 9-anilinoacridine, synthesis and antitumor evaluation.
AID338007Cytotoxicity against human SK-MEL-2 cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID124260In vivo activity against transplanted Mam-17/Adr tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID680782TP_TRANSPORTER: transepithelial transport (basal to apical) in the presence of PSC-833 in MRP2-expressing MDCK cells2002Pharmaceutical research, Jun, Volume: 19, Issue:6
Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa?
AID103084Compound was tested in vitro for growth inhibition of MCF-7/ADR cells that exhibit MDR phenotype.1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Novel antineoplastic agents with efficacy against multidrug resistant tumor cells.
AID669245Cytotoxicity against human SBcl2 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID430795Cytotoxicity against human HCT116 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12.
AID280075Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID404107Cytotoxicity against human H460 cells after 48 hrs by SRB assay2005Journal of natural products, Sep, Volume: 68, Issue:9
Sesquiterpene lactones from Centaurea spinosa and their antibacterial and cytotoxic activities.
AID526944Cytotoxicity against human multidrug-resistant MDA-MB-435/LCCMDR1 cells after 48 hrs by sulforhodamine B assay2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents.
AID1203384Antiproliferative activity in sea urchin embryo assessed as antimitotic activity by measuring cleavage arrest exposed for 8 to 20 mins after fertilization and 45 to 55 mins before first mitotic cycle completion measured 2.5 to 5.5 hrs after fertilization2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID137658Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 2 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID280073Antiproliferative activity against drug resistant Messa/DX5 cell line expressing MDR1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1221976Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko1432011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1221975Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko1432011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID680269TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Vinblastine: 70 uM) in MDR1-expressing NIH-3T3 cells2004Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4
Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.
AID132376Percent increase in life span at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID310120Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID681155TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID375833Induction of apoptosis in human HCT116 cells measured after 48 hrs by cell and caspase based HTS assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2: Structure-activity relationships of the 4-, 5-, 6-, 7- and 8-positions.
AID777504Growth inhibition of human LNCaP-FGC cells after 72 hrs by MTS assay
AID681610TP_TRANSPORTER: increase in brain concentration in mdr1a(-/-) mouse2001The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3
In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results.
AID626622Antiproliferative activity against human multidrug-resistant CEM/VLB cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID721883Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTT assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID679268TP_TRANSPORTER: transepithelial transport (apical to basal) of Vinblastine at a concentration of 22.5 nM in MDR1-expressing LLC-PK1 cells2001Pharmaceutical research, Dec, Volume: 18, Issue:12
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.
AID327678Antiproliferative activity against human HT29 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Antiproliferative limonoids of a Malleastrum sp. from the Madagascar rainforest.
AID1169460Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by MTT assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
11H-Pyrido[3',2':4,5]pyrrolo[3,2-c]cinnoline and pyrido[3',2':4,5]pyrrolo[1,2-c][1,2,3]benzotriazine: two new ring systems with antitumor activity.
AID715432Apparent permeability from basolateral to apical side in MDCK2 cells expressing MDR1 by gamma counting2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Radiofluorinated histamine H₃ receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.
AID551319Cytotoxicity against vinblastine-resistant human CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis, and biological evaluation of novel water-soluble N-mustards as potential anticancer agents.
AID767265Growth inhibition of human doxorubicin-resistant MES-SA/Dx5 cells after 48 hrs by MTT assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exploring natural product chemistry and biology with multicomponent reactions. 5. Discovery of a novel tubulin-targeting scaffold derived from the rigidin family of marine alkaloids.
AID1221965Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID605767Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID248807Concentration required for growth inhibition of taxol resistant human lymphoblastic leukemic cell line (CCRF-CEM/taxol) was determined2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Potent antitumor N-mustard derivatives of 9-anilinoacridine, synthesis and antitumor evaluation.
AID78567Approximate percentage for level of inhibition of cell growth in presence and absence of inhibitor (Value of drug + alpha Tochoferol / Value of drug)2004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID679302TP_TRANSPORTER: transcellular transport in MRP2-expressing MDCKII cells2007Neuropharmacology, Feb, Volume: 52, Issue:2
Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.
AID464061Cytotoxicity against human SF268 cells after 48 hrs by SRB assay2010Journal of natural products, Feb-26, Volume: 73, Issue:2
Sesquiterpene lactones from Anthemis melanolepis and their antibacterial and cytotoxic activities. Prediction of their pharmacokinetic profile.
AID1203430Cytotoxicity against human OVCAR8 cells2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID280519Cytotoxicity against drug-sensitive CCRF-CEM cells after 72 hrs2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Total structure and inhibition of tumor cell proliferation of laxaphycins.
AID392698Cytotoxicity against human MCF7 cells2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
Synthesis and SAR of vinca alkaloid analogues.
AID247795Intrinsic cytotoxic activity against wild type HCT116 cell line2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Multidrug resistance reversal activity of permethyl ningalin B amide derivatives.
AID272510Antiproliferative activity against multidrug resistant MDA435/LCC6 cells in presence of 5 uM 1,13-bis[4'-((5,7-dihydroxy)-4H-chromen-4-on-2-yl)phenyl]-1,4,7,10,13-pentaoxatridecane by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID553042Cytotoxicity against human MDA435 cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID1203420Cytotoxicity against human MDA-MB-435 cells2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID137820Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intravenously at a dose of 5 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID487886Binding affinity to P-gp at 0.05 uM after 30 mins by spectrophotometry2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Targeting efflux pumps-In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation.
AID669244Cytotoxicity against human HCT116 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID132539Percent increase in life span at dose 8 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID629605Antiproliferative activity against human vinblastine-resistant CEM/VBL100 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID616994Antiproliferative activity against MDR-1 overexpressing human 786-0 cells in presence of MDR1 inhibitor verapamil2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID737103Cytotoxicity against human CEM/VBL100 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID588980Substrates of transporters of clinical importance in the absorption and disposition of drugs, MDR32010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1183717Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by CellTitre-Glo assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID43547Tested for the inhibitory concentration against cell growth of human leukemic cell line CCRF-CEM2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID51924Effect on cross resistance of chinese hamster cells resistant to Actinomycin D.1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID375829Growth inhibition of human T47D cells after 48 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2: Structure-activity relationships of the 4-, 5-, 6-, 7- and 8-positions.
AID1237727Induction of apoptosis in human HeLa cells at 20 nM after 24 hrs by propidium iodide/annexin V-FITC staining-based cytofluorometric analysis2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID200620Cytotoxicity against human small-cell lung cancer (SCLC)1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
Design of antineoplastic agents on the basis of the "2-phenylnaphthalene-type" structural pattern. 2. Synthesis and biological activity studies of benzo]b]naphtho[2,3-d]furan-6,11-dione derivatives.
AID1177868Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach.
AID681128TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID386358Inhibition of cross-linking of human Pgp TM3T199R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot2007The Journal of biological chemistry, Nov-02, Volume: 282, Issue:44
Suppressor mutations in the transmembrane segments of P-glycoprotein promote maturation of processing mutants and disrupt a subset of drug-binding sites.
AID462943Cytotoxicity against human H1299 cells after 72 hrs by alamar blue assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID132382Percent increase in life span at dose 5 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID150753Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID263821Cytotoxicity against human Colo320DM cells by clonogenic assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID681126TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29140Apparent value (pKa) calculated with ACD/pKa (experimental pKa value)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID679580TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical)(Digoxin: 0.1uM, Vinblastine: 20 uM) in MDR1-expressing LLC-PK1 cells1992The Journal of pharmacology and experimental therapeutics, Nov, Volume: 263, Issue:2
Transport of digoxin by human P-glycoprotein expressed in a porcine kidney epithelial cell line (LLC-PK1).
AID1221962Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID762137Cytotoxicity against human K562 cells after 72 hrs by resazurin assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and biological evaluation of a new series of highly functionalized 7'-homo-anhydrovinblastine derivatives.
AID579983Cytotoxicity against human DLD1 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID551321Selectivity ratio of IC50 for vinblastine-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis, and biological evaluation of novel water-soluble N-mustards as potential anticancer agents.
AID124267In vivo activity against transplanted colon-51 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID736269Cytotoxicity against human H522-T1 cells after 96 hrs by CellTiter-Glo assay2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Mycoleptodiscins A and B, cytotoxic alkaloids from the endophytic fungus Mycoleptodiscus sp. F0194.
AID1200321Antiproliferative activity against human GBM 031810 cells assessed as reduction in cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Activity of 2-aryl-2-(3-indolyl)acetohydroxamates against drug-resistant cancer cells.
AID629602Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID576507Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.
AID624622Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID624629Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID430793Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12.
AID777500Growth inhibition of human SW403 cells after 72 hrs by MTS assay
AID15472Bullaticin index relates the IC50 values by normalizing to the value of bullatacin for easy comparison.1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of diverse Annonaceous acetogenins against multidrug resistant human mammary adenocarcinoma (MCF-7/Adr) cells.
AID430797Cytotoxicity against human HL60 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID400581Ratio of IC50 for VM46-resistant human HCT116 cells overexpressing P-gp to IC50 for human HCT116 cells2004Journal of natural products, Mar, Volume: 67, Issue:3
Scleritodermin A, a cytotoxic cyclic peptide from the lithistid sponge Scleritoderma nodosum.
AID689656Antiproliferative activity against human MDA-MB-435 cells assessed as cell viability at 1 ng/ml after 96 hrs2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Minutissamides E-L, antiproliferative cyclic lipodecapeptides from the cultured freshwater cyanobacterium cf. Anabaena sp.
AID298667Effect on apoptosis in Jurkat cells assessed as cleavage of procaspase 3 to active enzyme at 1 uM2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Discovery and investigation of antiproliferative and apoptosis-inducing properties of new heterocyclic podophyllotoxin analogues accessible by a one-step multicomponent synthesis.
AID1237723Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 48 hrs by SRB assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID1221964Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID82851Tested for the inhibitory concentration against cell growth of HL60 acute myeloid leukemia using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID137651Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intravenously at a dose of 9 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID78580Percentage inhibition of cell growth in the presence of compound and in the absence of GG198 in H69/LX4 cells with clofazimine MDR inhibitor2004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID280077Antiproliferative activity against drug resistant H69AR cell line expressing MRP1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID366386Cytotoxicity against mouse P388 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID704739Antitumor activity against human HCT116 cells xenografted in mouse assessed as mouse survival at 0.5 mg/kg2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
10'-Fluorovinblastine and 10'-Fluorovincristine: Synthesis of a Key Series of Modified Vinca Alkaloids.
AID462939Selectivity ratio of IC50 for taxol-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID403547Cytotoxicity against human multi drug-resistant CEM/VBL100 cells1998Journal of natural products, Dec, Volume: 61, Issue:12
New cyclic peptides from the ascidian Lissoclinum patella.
AID137486Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 3 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID708919Cytotoxicity against human HL60R cells overexpressing Pgp incubated for 72 hrs by MTS assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Flavaglines as potent anticancer and cytoprotective agents.
AID602936Cytotoxicity against human vinblastine-resistant CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates.
AID322939Inhibition of bovine neuronal tubulin polymerization for 60 mins2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents.
AID1203431Cytotoxicity against human NCI-ADR-RES cells2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID774535Inhibition of tubulin polymerization (unknown origin) after 90 mins2013European journal of medicinal chemistry, Jul, Volume: 65Elaboration of thorough simplified vinca alkaloids as antimitotic agents based on pharmacophore similarity.
AID674217Antiproliferative activity against human vinblastine-resistant CEM/VBL100 cells overexpressing P-gp assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID607672Resistance factor, ratio of IC50 for Pgp-deficient human MCF7/VP cells expressing MRP1 in absence of vinblastin to IC50 for drug sensitive human MCF7 cells in presence of 50 nM vinblastin2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
2-Amino-4-methyl-5-phenylethyl substituted-7-N-benzyl-pyrrolo[2,3-d]pyrimidines as novel antitumor antimitotic agents that also reverse tumor resistance.
AID45285Efflux in Caco-2 cells; yes2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.
AID551872Antiangiogenic activity against FGF2-induced in HUVEC cells assessed as inhibition of capillary-like formation at 10'-5 uM after 18 hrs by Matrigel assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis, in vitro and in vivo preliminary evaluation of anti-angiogenic properties of some pyrroloazaflavones.
AID115823Evaluation of Survival of mice upon intraperitoneal injection of VBL at a concentration of 0.2 mg/kg1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes.
AID282705Inhibition of tubulin polymerization2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Identification of novel and improved antimitotic agents derived from noscapine.
AID681370TP_TRANSPORTER: inhibition of calcein-AM efflux in MRP2-expressing MDCK cells2005Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 33, Issue:4
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.
AID137632Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intravenously at a dose of 3 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID154146Cytotoxic activity was evaluated against P388D1/ADR cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID124254In vivo activity against iv transplanted Leukemia L1210 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID406181Growth inhibition of multidrug resistant human HepG2/Dox cells after 72 hrs by SRB assay2008Journal of natural products, Jun, Volume: 71, Issue:6
Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID15625Statistical significance of IC 50 values; Expressed as R value1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of diverse Annonaceous acetogenins against multidrug resistant human mammary adenocarcinoma (MCF-7/Adr) cells.
AID448004Growth inhibition of human HeLa cells after 72 hrs by XTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID322938Inhibition of bovine neuronal tubulin polymerization for 20 mins2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents.
AID1154396Antiproliferative activity against human K562 cells after 72 hrs2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
One-pot synthesis of vinca alkaloids-phomopsin hybrids.
AID46881Inhibitory concentration against human T-cell leukemic cell line (CRFF-CEM) in vitro1989Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
In vitro metabolic transformations of vinblastine: oxidations catalyzed by peroxidase.
AID408353Cytotoxicity against human MX1 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage.
AID766783Inhibition of tubulin polymerization in human NCI-H522 cells assessed as beta-tubulin accumulation in cytoskeletal fraction at 100 nM after 24 hrs by Western blot analysis2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design, synthesis, and mechanism of action of 2-(3-hydroxy-5-methoxyphenyl)-6-pyrrolidinylquinolin-4-one as a potent anticancer lead.
AID551391Cytotoxicity against human U87 cells after 72 hrs by Alamar blue assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID105490Tested for the inhibitory concentration against cell growth of Tcell leukemic cell line MOLT-4 using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID342499Inhibition of nuclear translocation of thioredoxin 1 in human M21 cells at 0.1 uM after 18 hrs by immunocytochemistry2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression.
AID626623Ratio of IC50 for human multidrug-resistant CEM/VLB cells to IC50 for human CEM cells2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID736173Antiproliferative activity against human HeLa cells assessed as median dose after 24 hrs2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID263813Cytotoxicity against human MCF7 cells by clonogenic assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID427909Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents.
AID137662Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 6 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID678991TP_TRANSPORTER: Northern blot from primary hepatocytes2001Toxicology letters, Mar-31, Volume: 120, Issue:1-3
Up-regulation of transporters of the MRP family by drugs and toxins.
AID681164TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells2001Pharmaceutical research, Dec, Volume: 18, Issue:12
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.
AID464055Cytotoxicity against human H460 cells after 48 hrs by SRB assay2010Journal of natural products, Feb-26, Volume: 73, Issue:2
Sesquiterpene lactones from Anthemis melanolepis and their antibacterial and cytotoxic activities. Prediction of their pharmacokinetic profile.
AID777508Growth inhibition of human HCC1143 cells after 72 hrs by MTS assay
AID1194491Cytotoxicity against human U87 cells assessed as inhibition of cell proliferation after 72 hrs2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives.
AID399158Cytotoxicity against mouse P388 cells
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID405928Cytotoxicity against human HeLa cells after 72 hrs2008Journal of natural products, Jun, Volume: 71, Issue:6
Inhibitors of bacterial multidrug efflux pumps from the resin glycosides of Ipomoea murucoides.
AID663860Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antitumor evaluation of novel benzo[d]pyrrolo[2,1-b]thiazole derivatives.
AID322933Cytotoxicity against human MDA-MB-231 cells2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents.
AID609240Cytotoxic activity against drug-resistant MDR1-deficient human NCI/ADR cells expressing Pgp after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
2-Amino-4-methyl-5-phenylethyl substituted-7-N-benzyl-pyrrolo[2,3-d]pyrimidines as novel antitumor antimitotic agents that also reverse tumor resistance.
AID681566TP_TRANSPORTER: intracellular accumulation in Bsep-expressing LLC-PK1 cells2000Molecular pharmacology, Jan, Volume: 57, Issue:1
Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein.
AID1183745Cell cycle arrest in human PC3 cells at 500 to 2000 nM incubated for 24 hrs followed by compound washout measured after 24 hrs2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID627397Antiproliferative activity against mouse L1210 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID618986Resistance factor, ratio of IC50 for human NCI-ADR-RES cells to IC50 for drug-sensitive human OVCAR8 cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents.
AID96186Cytotoxic activity against human epidermoid carcinoma cells (KB)2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Synthesis, spectroscopy, and cytotoxicity of glycosylated acetogenin derivatives as promising molecules for cancer therapy.
AID310119Cytotoxicity against human A2780 cells after 72 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID1237735Cytotoxicity against human RD cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID729108Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties.
AID150736Fraction of high affinity at binding site of human P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID736653Inhibition of microtubule (unknown origin) GTPase activity using GTP as substrate assessed as reduction of inorganic phosphate release at 2 uM incubated for 10 mins prior to substrate addition measured after 10 mins by ammonium molybdate malachite green a2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID607292Antiproliferative activity against human taxol-resistant A549-T12 cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1235988Cytotoxicity against human A549 cells assessed as induction of cell death by microscopic analysis2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID80245In vitro cytotoxic activity (growth inhibition) of compound against HCT 116 cancer cell line was determined2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity.
AID355585Antiproliferative activity against mouse P388 cells at 0.1 ug after 48 hrs by two-layer agar-diffusion method
AID328774Disruption of tubulin network in human A549 cells assessed as disaggregation of microtubules at 1 uM after 24 hrs2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Isoindolo[2,1-a]quinoxaline derivatives, novel potent antitumor agents with dual inhibition of tubulin polymerization and topoisomerase I.
AID150758P-gp activity was measured by a direct transport assay, using polarized LLC-PK1 epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1177869Resistance factor, ratio of IC50 for vinblastine-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2014European journal of medicinal chemistry, Apr-09, Volume: 76Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach.
AID124256In vivo activity against transplanted Mam-16/C/ Taxol tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID1252758Cytotoxicity against human MES-SA/Dx5 cells assessed as growth inhibition incubated for 48 hrs by MTT assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Wittig derivatization of sesquiterpenoid polygodial leads to cytostatic agents with activity against drug resistant cancer cells and capable of pyrrolylation of primary amines.
AID335771Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 100 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID663889Ratio of IC50 for human taxol-resistant CCRF-CEM cells to IC50 for human CCRF-CEM cells2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antitumor evaluation of novel benzo[d]pyrrolo[2,1-b]thiazole derivatives.
AID272513Relative fold, IC50 in absence to presence of verapamil in multidrug resistant MDA435/LCC6 cells2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID679023TP_TRANSPORTER: inhibition of LTC4 uptake (LTC4: 0.01 uM, Vinblastine: 100 uM) in liver plasma membrane vesicles of Wistar rat1990The Journal of biological chemistry, Nov-05, Volume: 265, Issue:31
ATP-dependent primary active transport of cysteinyl leukotrienes across liver canalicular membrane. Role of the ATP-dependent transport system for glutathione S-conjugates.
AID94826Tested for the inhibitory concentration against cell growth of K562 chronic myeloid leukemia using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID681163TP_TRANSPORTER: ATP hydrolysis in reconstituted proteoliposomes1996The Journal of biological chemistry, Feb-09, Volume: 271, Issue:6
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.
AID519608Selectivity index, ratio of TC50 for hepatocytes to IC50 for Plasmodium yoelii 2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
New active drugs against liver stages of Plasmodium predicted by molecular topology.
AID551390Cytotoxicity against human OECM1 cells after 72 hrs by Alamar blue assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID137998Number of survivors on 30th day at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID350784Permeability from basolateral to apical side in human Caco-2 cells2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.
AID1203437Cytotoxicity against human RXF393 cells2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID91040Tested for the concentration required to reduce the viability of leukemia cells by 50% against cell growth of HuT78 T lymphoma using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID669243Cytotoxicity against human U251 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID45286Secretory Transport in Caco-2 cells in comparison to metoprolol2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.
AID551392Cytotoxicity against human H1299 cells after 72 hrs by Alamar blue assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID431440Displacement of fluorescein-labeled colchicine from bovine brain tubulin2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.
AID1121886Inhibition of tubulin polymerization (unknown origin) at 5 uM after 1 hr
AID135634Number of survivors on 60th day at dose 10 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID138165Number of survivors on 30th day at dose 9 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 4/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID427907Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents.
AID386356Inhibition of cross-linking of human Pgp TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot2007The Journal of biological chemistry, Nov-02, Volume: 282, Issue:44
Suppressor mutations in the transmembrane segments of P-glycoprotein promote maturation of processing mutants and disrupt a subset of drug-binding sites.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID579982Fold resistant ratio of IC50 for human MES-SA cells to IC50 for MES-SA/Dx5-Rx1 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID673735Inhibition of pig brain tubulin polymerization at 5 uM measured every min for 60 mins by spectrophotometry2012ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1
Identification of Simple Compounds with Microtubule-Binding Activity That Inhibit Cancer Cell Growth with High Potency.
AID1183738Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT method2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID355580Antiproliferative activity against human HT-29 cells at 1 ug after 48 hrs by two-layer agar-diffusion method
AID1121891Induction of beta tubulin de-stabilization in human PC3 cells at 10 nM after 24 hrs by DAPI-staining based immunofluorescence assay
AID137660Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 3 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID132715Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intravenously at a dose of 5 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID717147Antiproliferative activity against human vinblastine-resistant CEM/VBL100 cells overexpressing P-glycoprotein after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID708920Cytotoxicity against human HL60 cells incubated for 72 hrs by MTS assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Flavaglines as potent anticancer and cytoprotective agents.
AID124261In vivo activity against transplanted Mel-B16 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID342494Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID551862Growth inhibition of HUVEC cells after 20 hrs by MTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis, in vitro and in vivo preliminary evaluation of anti-angiogenic properties of some pyrroloazaflavones.
AID138006Number of survivors on 30th day at dose 5 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0 /101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID154149Cytotoxic Activity was evaluated against P388D1 cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID135665Number of survivors on 60th day at dose 3 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID137488Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 6 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1183740Cell cycle arrest in human RD cells assessed as accumulation at G2/M phase at 500 nM after 24 hrs by propidium iodide staining-based flow cytometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
AID335773Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 4 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID682080TP_TRANSPORTER: Northern blot from MCF-7 cells2001Toxicology letters, Mar-31, Volume: 120, Issue:1-3
Up-regulation of transporters of the MRP family by drugs and toxins.
AID281700Induction of apoptosis in human DLD1 cells assessed as caspase activation after 24 hrs2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.
AID367773Ratio of IC50 for taxol-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Novel DNA-directed alkylating agents: design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker.
AID106134Inhibitory concentration against the growth of HET-SR-2SC-LNM cell line after 72 hr of drug exposure by MTT test2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Effects of isoprenoid analogues of SDB-ethylenediamine on multidrug resistant tumor cells alone and in combination with chemotherapeutic drugs.
AID396713Inhibition of tubulin polymerization2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Antimitotic activity of two macrocyclic bis(bibenzyls), isoplagiochins A and B from the Liverwort Plagiochila fruticosa.
AID693021Genotoxicity in human lymphocytes assessed as micronucleated binucleate cells level at 0.03 ug/mL incubated for 24 hrs measured under no recovery condition in absence of rat liver S9 fraction (Rvb = 0.50%)2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.
AID1237730Cell cycle arrest in human HeLa cells assessed as accumulation at sub-G1 phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID291496Growth inhibition of Pgp deficient MCF7/VP cells expressing MRP12007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
AID551270Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline.
AID736649Inhibition of microtubule (unknown origin) GTPase activity using GTP as substrate assessed as reduction of inorganic phosphate release at 0.5 uM incubated for 10 mins prior to substrate addition measured after 10 mins by ammonium molybdate malachite green2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID337998Cytotoxicity against human A431 cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID1177861Cytotoxicity against human CCRF-CEM cells assessed as growth inhibition after 72 hrs by Alamar Blue assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach.
AID355578Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID54923Inhibition of human cytochrome P450 3A42003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID101632Inhibition of the growth of MDA-MB 231 human breast cancer cells1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1183703Growth inhibition of human CEM/VBL100 cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID135672Number of survivors on 60th day at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line for 1st scheduled day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID137649Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intravenously at a dose of 7 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID121100In vivo evaluation for the inhibitory activity against drug sensitive P388 cells (P388/S) cells bearing mice at dose 0.2 mg/kg1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes.
AID673732Inhibition of microtubule polymerization in human HT1080 cells at 100 nM for 4 hrs by immunocytochemistry analysis2012ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1
Identification of Simple Compounds with Microtubule-Binding Activity That Inhibit Cancer Cell Growth with High Potency.
AID43872Tested for the inhibitory concentration against cell growth of Tcell leukemic cell line CCRF-CEM using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID91042Tested for the inhibitory concentration against cell growth of HuT78 T lymphoma using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID392699Cytotoxicity against human HeLa cells2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
Synthesis and SAR of vinca alkaloid analogues.
AID367775Cytotoxicity against human MX1 cells after 72 hrs by SRB assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Novel DNA-directed alkylating agents: design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker.
AID400580Cytotoxicity against human SKBR3 cells after 72 hrs by MTS assay2004Journal of natural products, Mar, Volume: 67, Issue:3
Scleritodermin A, a cytotoxic cyclic peptide from the lithistid sponge Scleritoderma nodosum.
AID263818Cytotoxicity against human PA1 cells by MTT assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID551268Inhibition of porcine brain tubulin polymerization by microtubule assembly assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline.
AID777507Growth inhibition of vinblastine-sensitive human HCT116 cells after 72 hrs by MTS assay
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID121099In vivo evaluation for the inhibitory activity against drug sensitive P388 cells (P388/ADR) cells bearing mice at a concentration of 0.2 mg/kg1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes.
AID527876Cytotoxicity against vinblastine-resistant human HCT116 cells after 72 hrs2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Catharanthine C16 substituent effects on the biomimetic coupling with vindoline: preparation and evaluation of a key series of vinblastine analogues.
AID1235987Cytostatic activity against human A549 cells after 48 hrs by MTT assay2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID167216Tested for the inhibitory concentration against cell growth of RPM18226 multiple myeloma using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID150757P-gp activity was measured by a direct transport assay, using polarized LLC-MDR1 epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID681356TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells2002Pharmaceutical research, Jun, Volume: 19, Issue:6
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?
AID551396Ratio of IC50 for human CCRF-CEM cells to IC50 for vinblastine-resistant human CCRF-CEM cells2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1221969Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko1432011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID138148Number of survivors on 30th day at dose 7 mg/kg/day in 9 mice implanted with P388 leukemia cell line; 1 /91985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID408373Selectivity ratio of IC50 for vinblastine-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage.
AID627402Antiproliferative activity against human MDA-MB-231 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID272492Antiproliferative activity against MDA435/LCC6 cells by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID642113Induction apoptosis in human HeLa cells at 20 nM after 24 hrs by Annexin V-based flow cytometry analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID704749Cytotoxicity against mouse L1210 cells2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
10'-Fluorovinblastine and 10'-Fluorovincristine: Synthesis of a Key Series of Modified Vinca Alkaloids.
AID663861Cytotoxicity against human taxol-resistant CCRF-CEM cells after 72 hrs by XTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antitumor evaluation of novel benzo[d]pyrrolo[2,1-b]thiazole derivatives.
AID579805Fold resistance, ratio of IC50 for antiproliferative activity for human MES-SA cells to IC50 for antiproliferative activity for P-gp overexpressing human MES-SA/Dx5-Rx1cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID137827Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intravenously at a dose of 8 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1121895Growth inhibition of pig LLC-PK1 cells by Alamar Blue assay
AID1177867Cytotoxicity against human H1299 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach.
AID263814Cytotoxicity against human WRL68 cells by MTT assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID678838TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-CEM cells1996Anti-cancer drugs, Jul, Volume: 7, Issue:5
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.
AID1203414Cytotoxicity against human SF539 cells2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID487885Binding affinity to P-gp at 0.5 uM after 30 mins by spectrophotometry2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Targeting efflux pumps-In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation.
AID247560Inhibitory concentration against K562 cell line2004Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20
Antimitotic activity of 5-hydroxy-7-methoxy-2-phenyl-4-quinolones.
AID579981Cytotoxicity against human MES-SA/Dx5-Rx1 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID1176901Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay in presence of vinblastine2015Journal of natural products, Jan-23, Volume: 78, Issue:1
Jalapinoside, a macrocyclic bisdesmoside from the resin glycosides of Ipomea purga, as a modulator of multidrug resistance in human cancer cells.
AID579803Antiproliferative activity against human MES-SA cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID1154194Resistance ratio of IC50 for human CEM/VBL100 cells to IC50 for human CEM cells2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and biological evaluation of arylcinnamide hybrid derivatives as novel anticancer agents.
AID607444Fold resistance, ratio of IC50 for human vinblastine-resistant CEM/VBL100 cells overexpressing P-gp to IC50 for human CEM cells2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1183715Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID605774Antiproliferative activity against multidrug-resistant human CEM/VLB cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID338002Cytotoxicity against human KB cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID137487Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 4 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID288694Growth inhibition of human HT29 cells after 48 hrs2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Alkylation potency and protein specificity of aromatic urea derivatives and bioisosteres as potential irreversible antagonists of the colchicine-binding site.
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1063217Antiproliferative activity against human DG75 cells at 10 uM after 72 hrs by Alamar blue assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and antiproliferative action of a novel series of maprotiline analogues.
AID1177866Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach.
AID774563Cytotoxicity against KM mouse splenic lymphocytes assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Elaboration of thorough simplified vinca alkaloids as antimitotic agents based on pharmacophore similarity.
AID774536Antimitotic activity in human HepG2 cells assessed as cell morphological changes at 18 nM after 12 hrs by DAPI staining-based laser scanning confocal microscopic analysis2013European journal of medicinal chemistry, Jul, Volume: 65Elaboration of thorough simplified vinca alkaloids as antimitotic agents based on pharmacophore similarity.
AID282706Effect on cell growth in A549 cells by MTS assay2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Identification of novel and improved antimitotic agents derived from noscapine.
AID280520Cytotoxicity against vinblastine-resistant CEM/VLB100 cells after 72 hrs2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Total structure and inhibition of tumor cell proliferation of laxaphycins.
AID94823Tested for the concentration required to reduce the viability of leukemia cells by 50% against cell growth of K562 chronic myeloid leukemia using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID94652Tested for the inhibitory concentration against cell growth of human leukemic cell line K5622002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID1103247Growth inhibition of Mus musculus (mouse) P388 cells at 0.63 ug/ml after 24 hr by MTT assay2004Biological & pharmaceutical bulletin, Jun, Volume: 27, Issue:6
Biological activity of alpha-thujaplicin, the isomer of hinokitiol.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID401122Antitumor activity against mouse B16 cells xenografted in B6C3F1 mouse at 0.5 mg/kg relative to control
AID627400Antiproliferative activity against human DU145 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID150759P-gp activity was measured by a direct transport assay, using polarized LLC-mdr1a epithelial cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID135992Number of survivors on 60th day at dose 8 mg/kg/day in 9 mice implanted with P388 leukemia cell line; 0/91985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1203389Inhibition of bovine tubulin polymerization by turbidity assay2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID355921Cytotoxicity against african green monkey Vero cells after 24 hrs2003Journal of natural products, Jun, Volume: 66, Issue:6
Two unusual acetogenins from the roots of Annona salzmanii.
AID355582Antiproliferative activity against human HT-29 cells at 0.01 ug after 48 hrs by two-layer agar-diffusion method
AID78620Antiproliferative activity against the MDR positive human colon adenocarcinoma cell line HCT-152002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID480944Inhibition of human MDR1 expressed in MDCK cells assessed as fluorescence activity at 30 uM after 1.5 hrs by rhodamine 123 efflux test2010Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
Identification of serotonin 5-HT1A receptor partial agonists in ginger.
AID704748Cytotoxicity against human HCT116 cells2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
10'-Fluorovinblastine and 10'-Fluorovincristine: Synthesis of a Key Series of Modified Vinca Alkaloids.
AID579980Cytotoxicity against human MES-SA cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID426736Cytotoxicity against human vinblastine-resistant CCRF-CEM cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes.
AID462941Cytotoxicity against human MX1 cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID629604Antiproliferative activity against human CEM cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID579806Antiproliferative activity against human DLD1 cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID105285Tested for the inhibitory concentration against cell growth of human leukemic cell line MOLT-42002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID1235247Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell growth incubated for 72 hrs2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Cytotoxic Homoisoflavones from the Bulbs of Bellevalia eigii.
AID375834Induction of apoptosis in human SNU398 cells measured after 48 hrs by cell and caspase based HTS assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2: Structure-activity relationships of the 4-, 5-, 6-, 7- and 8-positions.
AID1221982Fraction absorbed in human2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID280523Ratio of IC50 for teniposide-resistant CEM/VM1 cells over IC50 for drug-sensitive CCRF-CEM cells2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Total structure and inhibition of tumor cell proliferation of laxaphycins.
AID397122Inhibition of HIV1 RT
AID642097Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 20 nM after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 0.10 %)2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID405926Cytotoxicity against human KB cells after 72 hrs2008Journal of natural products, Jun, Volume: 71, Issue:6
Inhibitors of bacterial multidrug efflux pumps from the resin glycosides of Ipomoea murucoides.
AID1221961Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID737104Cytotoxicity against human CEM cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID135675Number of survivors on 60th day at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 2/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1183739Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase at 500 nM after 24 hrs by propidium iodide staining-based flow cytometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID335776Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.032 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID153386Compound was tested in vitro for growth inhibition of murine leukemic P388/ADR cells that exhibit MDR phenotype.1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Novel antineoplastic agents with efficacy against multidrug resistant tumor cells.
AID1197743Inhibition of human OATP1B1-mediated [3H]estrone 3-sulfate at 100 uM after 5 mins relative to control2015European journal of medicinal chemistry, Mar-06, Volume: 92Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID367770Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Novel DNA-directed alkylating agents: design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker.
AID777501Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTS assay
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID270359Cytotoxicity against human MCF7 cells2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells.
AID408354Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage.
AID282707Effect on cell growth in A549 cells by colony-forming assay2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Identification of novel and improved antimitotic agents derived from noscapine.
AID605764Antiproliferative activity against mouse B16F0 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID160673Concentration of compound required to inhibit tubulin polymerization (Microtubule assembly) was determined by the turbidity formation after 20 min of incubation2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity.
AID124266In vivo activity against transplanted colon-38 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID137642Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intravenously at a dose of 5 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID579807Antiproliferative activity against human HCT15 cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID679983TP_TRANSPORTER: inhibition of apoptosis in hMRP1-expressing HEK293 cells2006Cell biology international, Mar, Volume: 30, Issue:3
Zoledronic acid is synergic with vinblastine to induce apoptosis in a multidrug resistance protein-1 dependent way: an in vitro study.
AID721880Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by MTT assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID150752Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID607288Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1183718Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by CellTitre-Glo assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID680149TP_TRANSPORTER: cell accumulation in P-gp transfected LNCaP cells2004The Prostate, Apr-01, Volume: 59, Issue:1
P-glycoprotein increases the efflux of the androgen dihydrotestosterone and reduces androgen responsive gene activity in prostate tumor cells.
AID327679Antiproliferative activity against human HS22T1 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Antiproliferative limonoids of a Malleastrum sp. from the Madagascar rainforest.
AID335778Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.00128 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID521208Antiproliferative activity against mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID386360Inhibition of cross-linking of human Pgp TM6 F343R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot2007The Journal of biological chemistry, Nov-02, Volume: 282, Issue:44
Suppressor mutations in the transmembrane segments of P-glycoprotein promote maturation of processing mutants and disrupt a subset of drug-binding sites.
AID681154TP_TRANSPORTER: cell accumulation in KB-3-1 and KB-V1 cells2001The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3
In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results.
AID94350Cytotoxic activity was evaluated against KB3-1 cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID496947Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
AID281699Induction of apoptosis in human H1299 cells assessed as caspase activation after 24 hrs2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.
AID1169469Resistance index, ratio of GI50 for human vinblastin-resistant CEM cells to GI50 for human CEM cells2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
11H-Pyrido[3',2':4,5]pyrrolo[3,2-c]cinnoline and pyrido[3',2':4,5]pyrrolo[1,2-c][1,2,3]benzotriazine: two new ring systems with antitumor activity.
AID681613TP_TRANSPORTER: intracellular accumulation in MDR1-expressing LLC-PK1 cells2000Molecular pharmacology, Jan, Volume: 57, Issue:1
Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein.
AID642061Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID679791TP_TRANSPORTER: increase in Glibenclamide intracellular accumulation (Glibenclamide: 0.0525 uM, Vinblastine: 100 uM) in CC531mdr+ cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
AID335777Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.0064 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID552974Cytotoxicity against human HL60R cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID319341Growth inhibition of human KB3-1 cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID688498Cytotoxicity against drug-sensitive human MCF7 cells after 72 hrs by SRB assay2012Journal of natural products, Sep-28, Volume: 75, Issue:9
Mammalian multidrug resistance lipopentasaccharide inhibitors from Ipomoea alba seeds.
AID679919TP_TRANSPORTER: inhibition of TBuMA transepithelial transport (basal to apical)(TBuMA: 10 uM, Vinblastine: 2 uM) in MDR1-expressing LLC-PK1 cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs.
AID43861Tested for the concentration required to reduce the viability of leukemia cells by 50% against cell growth of T cell leukemia cell line CCRF-CEM using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID669246Cytotoxicity against human WM35 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID270358Cytotoxicity against human HT29 cells2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells.
AID334033Cytotoxicity against human CCRF-CEM cells1997Journal of natural products, Nov, Volume: 60, Issue:11
Oxidations of vincristine catalyzed by peroxidase and ceruloplasmin.
AID406328Growth inhibition of human HepG2 cells after 72 hrs by SRB assay2008Journal of natural products, Jun, Volume: 71, Issue:6
Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells.
AID1183720Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 20 nM by propidium iodide staining-based flow cytometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID736652Inhibition of microtubule (unknown origin) GTPase activity using GTP as substrate assessed as reduction of inorganic phosphate release at 5 uM incubated for 10 mins prior to substrate addition measured after 10 mins by ammonium molybdate malachite green a2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID1221960Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID357845Binding affinity to calf thymus DNA assessed as reduction in DNA peak by pre-incubation method
AID358278Resistance index, ratio of IC50 for multidrug-resistant human KBV1 cells to IC50 for drug-sensitive human KB-3-1 cells2001Journal of natural products, Nov, Volume: 64, Issue:11
Leishmanicidal, antiplasmodial, and cytotoxic activity of novel diterpenoid 1,2-quinones from Perovskia abrotanoides: new source of tanshinones.
AID291516Induction of microtubule loss in rat A10 cells at 5 uM after 24 hrs2007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
AID327680Antiproliferative activity against human U937 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Antiproliferative limonoids of a Malleastrum sp. from the Madagascar rainforest.
AID553044Cytotoxicity against human PC3 cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID126507Inhibitory activity against Monoamine oxidase B isolated from beef liver mitochondria was determined1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Vinblastine and vincristine are inhibitors of monoamine oxidase B.
AID777498Growth inhibition of human T47D cells after 72 hrs by MTS assay
AID412798Inhibition of tubulin polymerisation by UV spectrophotometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Synthesis and biological evaluation of vinca alkaloids and phomopsin hybrids.
AID132722Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intravenously at a dose of 7 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID605715Antiproliferative activity against CHO cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID732664Cytotoxicity against human H460 cells after 96 hrs by CellTiter-Glo luminescent assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Structures and cytotoxic evaluation of new and known acyclic Ene-Ynes from an American Samoa Petrosia sp. Sponge.
AID681383TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells2001Pharmaceutical research, Feb, Volume: 18, Issue:2
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.
AID688499Cytotoxicity against vinblastine-reasistant human MCF7 cells after 72 hrs by SRB assay2012Journal of natural products, Sep-28, Volume: 75, Issue:9
Mammalian multidrug resistance lipopentasaccharide inhibitors from Ipomoea alba seeds.
AID150751Inhibition of P-glycoprotein using ATPase in MDR1 membranes2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID624628Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID135997Number of survivors on 60th day at dose 9 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID715431Apparent permeability from apical to basolateral side in MDCK2 cells expressing MDR1 by gamma counting2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Radiofluorinated histamine H₃ receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID263820Cytotoxicity against human Colo320DM cells by MTT assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID723116Displacement of [3H]Vinblastine from pig tubulin at 7.2 x 10'-5 M after 60 mins2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Total synthesis and evaluation of vinblastine analogues containing systematic deep-seated modifications in the vindoline subunit ring system: core redesign.
AID426740Cross-resistance, IC50 for human taxol-resistant CCRF-CEM cells to IC50 for human CCRF-CEM cells2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes.
AID291502Cell cycle arrest in HL60 cells assessed as accumulation in S phase at 80 nM2007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
AID150616Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID312972Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.
AID312971Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.
AID669242Cytotoxicity against human MDA-MB-231 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID310121Inhibition of P-glycoprotein expressed in MDCK-MDR1 cells by calcein AM assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID629603Antiproliferative activity against doxorubicin-resistant human LoVo cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID366387Cytotoxicity against adriamycin-resistant mouse P388 cells expressing p-glycoprotein2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity.
AID551395Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID629655Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID677620Antitrypanosomal activity against bloodstream form of Trypanosoma brucei 427 after 48 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Identification of selective tubulin inhibitors as potential anti-trypanosomal agents.
AID767266Growth inhibition of human MES-SA cells after 48 hrs by MTT assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exploring natural product chemistry and biology with multicomponent reactions. 5. Discovery of a novel tubulin-targeting scaffold derived from the rigidin family of marine alkaloids.
AID679993TP_TRANSPORTER: Western blot, MCF-7 cells2001Toxicology letters, Mar-31, Volume: 120, Issue:1-3
Up-regulation of transporters of the MRP family by drugs and toxins.
AID408372Selectivity ratio of IC50 for taxol-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage.
AID338001Cytotoxicity against human HT cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID132553Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intraperitoneally at a dose of 6 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID355584Antiproliferative activity against mouse P388 cells at 1 ug after 48 hrs by two-layer agar-diffusion method
AID400579Cytotoxicity against human A2780 cells after 72 hrs by MTS assay2004Journal of natural products, Mar, Volume: 67, Issue:3
Scleritodermin A, a cytotoxic cyclic peptide from the lithistid sponge Scleritoderma nodosum.
AID1203385Antiproliferative activity in sea urchin embryo assessed as destabilization of microtubule by measuring embryo spinning after 15 mins to 20 hrs2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID1157195Cytotoxicity against human CCRF-CEM cells after 72 hrs by AlamarBlue assay2014European journal of medicinal chemistry, Aug-18, Volume: 83The synthesis and biological evaluation of new DNA-directed alkylating agents, phenyl N-mustard-4-anilinoquinoline conjugates containing a urea linker.
AID681127TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID681381TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells2005Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 33, Issue:4
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.
AID1221958Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1252757Cytotoxicity against human MES-SA cells assessed as growth inhibition incubated for 48 hrs by MTT assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Wittig derivatization of sesquiterpenoid polygodial leads to cytostatic agents with activity against drug resistant cancer cells and capable of pyrrolylation of primary amines.
AID408352Cytotoxicity against vinblastine-resistant human CCRF-CEM cells after 72 hrs by XTT assay2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage.
AID272512Relative fold, IC50 in absence to presence of 1,13-bis[4'-((5,7-dihydroxy)-4H-chromen-4-on-2-yl)phenyl]-1,4,7,10,13-pentaoxatridecane in multidrug resistant MDA435/LCC6 cells2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID605765Antiproliferative activity against human DU145 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID379780Cytotoxicity against african green monkey Vero cells1999Journal of natural products, May, Volume: 62, Issue:5
A new bistetrahydrofuran acetogenin from the roots of Annona salzmanii.
AID1228084Cytotoxicity against human OVCAR3 cells assessed as cell viability after 72 hrs by commercial absorbance assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
17-Norpimaranes and (9βH)-17-Norpimaranes from the Tuber of Icacina trichantha.
AID1121893Resistance factor, ratio of GI50 for pig LLC-PK1 cells expressing MDR1 to GI50 for pig LLC-PK1 cells
AID280072Antiproliferative activity against drug sensitive Messa cell line by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID626621Ratio of IC50 for colchicine and vinblastine-resistant CHO-VV 3-2 cells to IC50 for CHO cells2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID395037Inhibition of P-gp ATPase activity in human DC-3F/ADX cells assessed as increase in basal activity measured by NADH level at 5 uM by spectrophotometric method2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Search for MDR modulators: design, syntheses and evaluations of N-substituted acridones for interactions with p-glycoprotein and Mg2+.
AID618908Anticancer activity against human OVCAR8 cells after 96 hrs by SRB assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents.
AID91039Tested for the inhibitory concentration against cell growth of human leukemic cell line HuT782002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID29139Calculated dissociation constant (pKa, calculated with ACD/pKa)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID124255In vivo activity against transplanted Mam-16/C tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID336714Inhibition of tubulin assembly1994Journal of natural products, Jul, Volume: 57, Issue:7
Antimitotic and cytotoxic flavonols from Zieridium pseudobtusifolium and Acronychia porteri.
AID263816Cytotoxicity against human KB cells by MTT assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID263815Cytotoxicity against human WRL68 cells by clonogenic assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID723113Cytotoxicity against human vinblastine-resistant HCT116/VM46 cells assessed as growth inhibition after 72 hrs by phosphatase assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Total synthesis and evaluation of vinblastine analogues containing systematic deep-seated modifications in the vindoline subunit ring system: core redesign.
AID1194487Inhibition of tubulin (unknown origin) polymerization2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives.
AID426742Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes.
AID624623Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID626619Ratio of IC50 for paclitaxel-resistant CHO-TAX 5-6 cells to IC50 for CHO cells2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID1176900Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay2015Journal of natural products, Jan-23, Volume: 78, Issue:1
Jalapinoside, a macrocyclic bisdesmoside from the resin glycosides of Ipomea purga, as a modulator of multidrug resistance in human cancer cells.
AID124253In vivo activity against iv transplanted AML Leukemia 1498 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID679292TP_TRANSPORTER: uptake (apical to cell) in OCT2-expressing NIH3T3 cells1999Toxicological sciences : an official journal of the Society of Toxicology, Feb, Volume: 47, Issue:2
A transfected cell model for the renal toxin transporter, rOCT2.
AID729102Competitive binding affinity to bovine brain tubulin after 1 hr by mass spectrometry binding assay in presence of colchicine2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties.
AID1183716Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID627401Antiproliferative activity against human HT1080 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID1221966Ratio of plasma AUC in po dosed mdr1 knock out mouse to plasma AUC in po dosed wild type mouse2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID338006Cytotoxicity against human Lu1 cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID1244335Inhibition of porcine brain tubulin polymerization assessed as microtubule assembly after 15 mins by DAPI staining2015European journal of medicinal chemistry, Aug-28, Volume: 1014-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.
AID404103Cytotoxicity against human SF268 cells after 48 hrs by SRB assay2005Journal of natural products, Sep, Volume: 68, Issue:9
Sesquiterpene lactones from Centaurea spinosa and their antibacterial and cytotoxic activities.
AID624626Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID272511Antiproliferative activity against multidrug resistant MDA435/LCC6 cells in presence of 5 uM verapamil by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID736268Cytotoxicity against human A2058 cells after 96 hrs by CellTiter-Glo assay2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Mycoleptodiscins A and B, cytotoxic alkaloids from the endophytic fungus Mycoleptodiscus sp. F0194.
AID412800Inhibition of beta tubulin nucleotide site assessed as inhibition of displacement of cold GDP by [alpha32P]GTP at 20 uM by rapid filtration technique2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Synthesis and biological evaluation of vinca alkaloids and phomopsin hybrids.
AID271728Inhibition of ATPase measured as ATP availability in Caco-2 cells at 20 nM after 90 mins relative to control2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
AID777509Growth inhibition of human NCI-H520 cells after 72 hrs by MTS assay
AID680102TP_TRANSPORTER: intracellular accumulation in P388/S and P388/ADR cells2000Clinical and experimental pharmacology & physiology, Aug, Volume: 27, Issue:8
Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo.
AID1235991Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 100 nM after 24 hrs by FITC-annexin V/propidium iodide staining-based flow cytometric analysis relative to control2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID464060Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2010Journal of natural products, Feb-26, Volume: 73, Issue:2
Sesquiterpene lactones from Anthemis melanolepis and their antibacterial and cytotoxic activities. Prediction of their pharmacokinetic profile.
AID134232Acute iv toxicity against NMRI strain of 100 mice after 7 doses of injection1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID338000Cytotoxicity against human Col2 cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID1169468Cytotoxicity against human vinblastin-resistant CEM cells assessed as growth inhibition after 72 hrs by MTT assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
11H-Pyrido[3',2':4,5]pyrrolo[3,2-c]cinnoline and pyrido[3',2':4,5]pyrrolo[1,2-c][1,2,3]benzotriazine: two new ring systems with antitumor activity.
AID679011TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.05 uM) in membrane vesicle from MRP1-expressing HeLa cells1996The Journal of biological chemistry, Apr-19, Volume: 271, Issue:16
ATP-dependent 17 beta-estradiol 17-(beta-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroids.
AID291498Cell cycle arrest in HL60 cells assessed as accumulation in G0/G1 phase at 80 nM2007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
AID496946Antiproliferative activity against human KB3-1 cells after 72 hrs by Alamar blue assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
AID448005Growth inhibition of human MCF7 cells after 72 hrs by XTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID762135Cytotoxicity against HUVEC after 72 hrs by resazurin assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and biological evaluation of a new series of highly functionalized 7'-homo-anhydrovinblastine derivatives.
AID1237728Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID607671Cytotoxic activity against Pgp-deficient human MCF7/VP cells expressing MRP1 after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
2-Amino-4-methyl-5-phenylethyl substituted-7-N-benzyl-pyrrolo[2,3-d]pyrimidines as novel antitumor antimitotic agents that also reverse tumor resistance.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID605773Resistant ratio of IC50 for paclitaxel-resistant CHO-VV 3-2 cells to IC50 for CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID537734Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID98513Tested for the inhibition of L1210 cell proliferation.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
New alpha-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity.
AID78577Approximate percentage for level of inhibition of cell growth in presence and absence of inhibitor (Value of drug + GG918 / Value of drug)2004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID1197747Inhibition of human OATP1B3-mediated [3H]CCK-8 after 5 mins by Dixon plot method2015European journal of medicinal chemistry, Mar-06, Volume: 92Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID551399Cytotoxicity against Taxol-resistant human CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID280521Cytotoxicity against teniposide-resistant CEM/VM1 cells after 72 hrs2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Total structure and inhibition of tumor cell proliferation of laxaphycins.
AID376733Resistance index, ratio of IC50 for human KBV1 cells to IC50 for human KB31 cells2000Journal of natural products, Nov, Volume: 63, Issue:11
Cytotoxic activity of some phenanthroindolizidine N-oxide alkaloids from Cynanchum vincetoxicum.
AID1237724Cytotoxicity against Pgp overexpressing human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID418797Inhibition of tubulin polymerization by DAPI fluorescence method2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers.
AID137833Number of survivors on 30th day at dose 10 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1235992Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 100 nM after 24 hrs by FITC-annexin V/propidium iodide staining-based flow cytometric analysis relative to control2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID1121900Growth inhibition of P-gp expressing docetaxel-resistant human PC3 cells after 72 hrs by Alamar Blue assay
AID280074Antiproliferative activity against drug resistant HCT15 cell line expressing MDR1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID552975Cytotoxicity against human KB cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID605717Antiproliferative activity against mouse L1210 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID605766Antiproliferative activity against human HT1080 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
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.
AID124259In vivo activity against transplanted Mam-17 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID94508Cytotoxic activity was evaluated against KBV-1 cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID605716Antiproliferative activity against human K562 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1121898Growth inhibition of human OVCAR8 cells by Alamar Blue assay
AID19468Partition coefficient (logP)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID263812Cytotoxicity against human MCF7 cells by MTT assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID681120TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1157196Cytotoxicity against human vinblastine-resistant CCRF-CEM cells after 72 hrs by AlamarBlue assay2014European journal of medicinal chemistry, Aug-18, Volume: 83The synthesis and biological evaluation of new DNA-directed alkylating agents, phenyl N-mustard-4-anilinoquinoline conjugates containing a urea linker.
AID247415Growth inhibitory concentration is the concentration that reduced K562 cell growth by 50%; c = not available2004Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20
Antimitotic activity of 5-hydroxy-7-methoxy-2-phenyl-4-quinolones.
AID124262In vivo activity against transplanted Panc-02 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID137654Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 0.33 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID214713Inhibition of colchicine binding to tubulin1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives.
AID736658Inhibition of goat brain tubulin polymerization incubated for 20 mins prior to GTP addition measured for 30 mins by 90 degree light scattering-based fluorescence spectrophotometric method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID132723Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intravenously at a dose of 8 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID777506Growth inhibition of human HCC70 cells after 72 hrs by MTS assay
AID400577Cytotoxicity against human HCT116 cells after 72 hrs by MTS assay2004Journal of natural products, Mar, Volume: 67, Issue:3
Scleritodermin A, a cytotoxic cyclic peptide from the lithistid sponge Scleritoderma nodosum.
AID1063215Induction of apoptosis in human MUTU-I cells assessed as accumulation at pre-G1 phase at 10 uM after 24 hrs using propidium iodide staining by FACS analysis2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and antiproliferative action of a novel series of maprotiline analogues.
AID1221967Ratio of intestine AUC in po dosed mdr1 knock out mouse to intestine AUC in po dosed wild type mouse2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID335775Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.16 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID132550Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intraperitoneally at a dose of 2 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID105481Tested for the concentration required to reduce the viability of leukemia cells by 50% against cell growth of T cell leukemia cell line MOLT-4 using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID745769Cytotoxicity against human H522-T1 cells assessed as growth inhibition after 96 hrs by CellTiter-Glo luminescence assay2013Journal of natural products, May-24, Volume: 76, Issue:5
Antiproliferative Homoisoflavonoids and Bufatrienolides from Urginea depressa.
AID680117TP_TRANSPORTER: transepithelial transport in MDR1-expressing LLC-PK1 cells2003The Journal of pharmacology and experimental therapeutics, Mar, Volume: 304, Issue:3
Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.
AID462944Cytotoxicity against human CL1-5 cells after 72 hrs by alamar blue assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID1183721Cell cycle arrest in human HeLa cells assessed as mitotic rounded-up phenotype at 20 nM by light microscopy2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID23271Partition coefficient (logD7.4)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID249990Ability to induce cells in S phase2004Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20
Antimitotic activity of 5-hydroxy-7-methoxy-2-phenyl-4-quinolones.
AID82833Tested for the inhibitory concentration against cell growth of human leukemic cell line HL602002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID266297Antiproliferative activity against human taxol resistant CCRF-CEM cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity.
AID1203427Cytotoxicity against human OVCAR3 cells2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID1154183Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and biological evaluation of arylcinnamide hybrid derivatives as novel anticancer agents.
AID766787Inhibition of porcine brain tubulin polymerization at 1 uM measured every 30 seconds for 30 mins2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design, synthesis, and mechanism of action of 2-(3-hydroxy-5-methoxyphenyl)-6-pyrrolidinylquinolin-4-one as a potent anticancer lead.
AID150755Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID135842Number of survivors on 60th day at dose 7 mg/kg/day in 9 mice implanted with P388 leukemia cell line;0/91985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID627403Antiproliferative activity against human SKOV3 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID774133Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Synthesis and bioconversions of formestane.
AID1154397Antiproliferative activity against human MCF7 cells after 72 hrs2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
One-pot synthesis of vinca alkaloids-phomopsin hybrids.
AID45288permeability in Caco-2 cells; yes2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.
AID552973Cytotoxicity against human HL60 cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID679236TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCK cells2002Pharmaceutical research, Jun, Volume: 19, Issue:6
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?
AID777511Displacement of [3H]-VBL from porcine tubulin after 60 mins relative to control
AID272494Antiproliferative activity against P388 cells by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID669241Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID327677Antiproliferative activity against human MDA-MB-435 cells after 96 hrs by CellTiter-Glo luminescent cell viability assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Antiproliferative limonoids of a Malleastrum sp. from the Madagascar rainforest.
AID629656Antiproliferative activity against human taxol-resistant A549-T12 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID86838In vitro antimitotic activity against HeLa cells after 6 hours exposure1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Chalcones: a new class of antimitotic agents.
AID408351Cytotoxicity against taxol-resistant human CCRF-CEM cells after 72 hrs by XTT assay2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage.
AID527875Cytotoxicity against human HCT116 cells after 72 hrs2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Catharanthine C16 substituent effects on the biomimetic coupling with vindoline: preparation and evaluation of a key series of vinblastine analogues.
AID94507Cytotoxic activity was evaluated against KBV-1 cells in presence of reserpine1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID579808Cytotoxicity against human IMR90 cells up to 1 uM2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID681471TP_TRANSPORTER: increase in Colchicine intracellular accumulation (Colchicine: 0.035 uM, Vinblastine: 100 uM) in CC531mdr+ cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
AID137826Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intravenously at a dose of 7 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID663862Cytotoxicity against human vinblastine-resistant CCRF-CEM cells after 72 hrs by XTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antitumor evaluation of novel benzo[d]pyrrolo[2,1-b]thiazole derivatives.
AID405927Cytotoxicity against human Hep2 cells after 72 hrs2008Journal of natural products, Jun, Volume: 71, Issue:6
Inhibitors of bacterial multidrug efflux pumps from the resin glycosides of Ipomoea murucoides.
AID678990TP_TRANSPORTER: Western blot, primary hepatocytes2001Toxicology letters, Mar-31, Volume: 120, Issue:1-3
Up-regulation of transporters of the MRP family by drugs and toxins.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID132724Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intravenously at a dose of 9 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID602934Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates.
AID106133Inhibitory concentration against the growth of 2SC/20 cell line after 72 hr of drug exposure by MTT test2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Effects of isoprenoid analogues of SDB-ethylenediamine on multidrug resistant tumor cells alone and in combination with chemotherapeutic drugs.
AID721760Displacement of [3H]-vinblastine from pig tubulin at 7.2 x 10'-5 M after 60 mins2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
A remarkable series of vinblastine analogues displaying enhanced activity and an unprecedented tubulin binding steric tolerance: C20' urea derivatives.
AID1221981Efflux ratio of permeability from apical to basolateral over basolateral to apical side of MDCK cells expressing BCRP2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1236006Upregulation of p53 protein expression in human A549 cells at 100 nM after 24 hrs by Western blot analysis2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID138158Number of survivors on 30th day at dose 8 mg/kg/day in 9 mice implanted with P388 leukemia cell line; 0 /91985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID272493Antiproliferative activity against adriamycin resistant P388 cells by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID135804Number of survivors on 60th day at dose 4 mg/kg/day in 7 mice implanted with P388 leukemia cell line for 1,8,15 acheduled days form Exp-2; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID448008Growth inhibition of human KYO1 cells after 72 hrs by XTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID729165Inhibition of pig brain tubulin polymerization measured every 1 min for 40 mins by microplate reader analysis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties.
AID298560Cytotoxicity against human U937 cells by MTS assay after 24 hrs2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
An investigation into the cytotoxicity and mode of action of some novel N-alkyl-substituted isatins.
AID682151TP_TRANSPORTER: increase in plasma concentration in mdr1a(-/-) mouse2001The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3
In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results.
AID213853Binding constant at colchicine site of bovine brain tubulin2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID322932Cytotoxicity against human Jurkat cells2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents.
AID448600Induction of apoptosis in human DU145 cells at interphase assessed as curly appearance of microtubules at 1 nM after 24 hrs by beta tubulin immunofluorescent staining2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Unsaturated genistein disaccharide glycoside as a novel agent affecting microtubules.
AID496949Antiproliferative activity against human KB3-1 cells after 72 hrs by Alamar blue assay in presence of zosuquidar2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
AID627404Antiproliferative activity against human CEM after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID609239Cytotoxic activity against drug-sensitive Pgp-, MRP1-deficient human MCF7 cells after 48 hrs by sulforhodamine B assay in presence of 50 nM vinblastin2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
2-Amino-4-methyl-5-phenylethyl substituted-7-N-benzyl-pyrrolo[2,3-d]pyrimidines as novel antitumor antimitotic agents that also reverse tumor resistance.
AID1183743Cell cycle arrest in human RD cells assessed as rounded cells at 500 nM after 24 hrs by propidium iodide staining-based flow cytometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID551397Cytotoxicity against vinblastine-resistant human CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID721876Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID280076Antiproliferative activity against drug sensitive NCI-H69 cell line by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID355581Antiproliferative activity against human HT-29 cells at 0.1 ug after 48 hrs by two-layer agar-diffusion method
AID736267Cytotoxicity against human PC3 cells after 96 hrs by CellTiter-Glo assay2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Mycoleptodiscins A and B, cytotoxic alkaloids from the endophytic fungus Mycoleptodiscus sp. F0194.
AID132351Percent increase in life span at dose 11 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID736175Inhibition of goat brain tubulin polymerization at 3 uM incubated for 20 mins prior to GTP addition measured for 30 mins by 90 degree light scattering-based fluorescence spectrophotometric method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID103092Cytotoxicity against MCF-7/Adr cells.1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of diverse Annonaceous acetogenins against multidrug resistant human mammary adenocarcinoma (MCF-7/Adr) cells.
AID1221977Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko1432011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID496948Drug resistant ratio of EC50 for human KBV1 cells overexpressing MDR1 to EC50 for KB3-1 cells2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
AID717117Resistance ratio of IC50 for human vinblastine-resistant CEM/VBL100 cells overexpressing P-glycoprotein to IC50 for human CEM cells2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID78578Approximate percentage for level of inhibition of cell growth in presence and absence of inhibitor (Value of drug + Verapamil / Value of drug)2004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID682086TP_TRANSPORTER: cell accumulation in CCRF-CEM and CEM/VLB100 cells1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
AID248484Concentration required for growth inhibition of human lymphoblastic leukemic cell line (CCRF-CEM) was determined2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Potent antitumor N-mustard derivatives of 9-anilinoacridine, synthesis and antitumor evaluation.
AID551320Selectivity ratio of IC50 for taxol-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis, and biological evaluation of novel water-soluble N-mustards as potential anticancer agents.
AID298561Cytotoxicity against human Jurkat cells by MTS assay after 24 hrs2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
An investigation into the cytotoxicity and mode of action of some novel N-alkyl-substituted isatins.
AID424441Inhibition of tubulin polymerization2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
Discovery of substituted N'-(2-oxoindolin-3-ylidene)benzohydrazides as new apoptosis inducers using a cell- and caspase-based HTS assay.
AID137811Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intravenously at a dose of 3 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1121901Growth inhibition of human PC3 cells after 72 hrs by Alamar Blue assay
AID680935TP_TRANSPORTER: inhibition of TBuMA transepithelial transport (basal to apical)(TBuMA: 10 uM, Vinblastine: 2 uM) in Mdr1b-expressing LLC-PK1 cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs.
AID319343Resistant ratio, IC50 for multidrug resistant human KB3-1 cells to IC50 for human KB3-1 cells2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID412797Inhibition of tubulin polymerization assessed as ratio of IC50 for compound to IC50 for vinblastin by UV spectrophotometry2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Synthesis and biological evaluation of vinca alkaloids and phomopsin hybrids.
AID355586Antiproliferative activity against mouse P388 cells at 0.01 ug after 48 hrs by two-layer agar-diffusion method
AID137997Number of survivors on 30th day at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0 /101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID723114Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 72 hrs by phosphatase assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Total synthesis and evaluation of vinblastine analogues containing systematic deep-seated modifications in the vindoline subunit ring system: core redesign.
AID375987Cytotoxicity against human KB cells after 72 hrs by SRB method2006Journal of natural products, Apr, Volume: 69, Issue:4
Resin glycosides from the flowers of Ipomoea murucoides.
AID551269Cytotoxicity against human HL60 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline.
AID551394Cytotoxicity against human MX1 cells after 72 hrs by SRB assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID132709Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intravenously at a dose of 4 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID777497Growth inhibition of human PA1 cells after 72 hrs by MTS assay
AID310118Cytotoxicity against human A2780/ADR cells after 72 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID404101Cytotoxicity against human DLD1 cells after 48 hrs by SRB assay2005Journal of natural products, Sep, Volume: 68, Issue:9
Sesquiterpene lactones from Centaurea spinosa and their antibacterial and cytotoxic activities.
AID462938Cytotoxicity against vinblastine-resistant human CCRF-CEM cells after 72 hrs by XTT assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID313987Growth inhibition of human RPMI8226 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Antimitotic quinoid triterpenes from Maytenus chuchuhuasca.
AID669249Cytotoxicity against human MRC5 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID551400Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID774653Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei 427 after 3 days by Alamar Blue assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Approaches to protozoan drug discovery: phenotypic screening.
AID124264In vivo activity against transplanted Squam lung-LC12 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID551868Inhibition of growth factor-induced angiogenesis in HUVEC cells assessed as inhibition of in cell migration at 10'-5 uM after 4 hrs by fluorescence microscopy2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis, in vitro and in vivo preliminary evaluation of anti-angiogenic properties of some pyrroloazaflavones.
AID137999Number of survivors on 30th day at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line;5/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID338232Cytotoxicity against human ZR-75-1 cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID167214Tested for the inhibitory concentration against cell growth of human leukemic cell line RPMI82262002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID427908Induction of apoptosis in human DLD1 cells assessed as caspase activation after 48 hrs2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents.
AID736648Inhibition of microtubule (unknown origin) GTPase activity using GTP as substrate assessed as reduction of inorganic phosphate release at 1 uM incubated for 10 mins prior to substrate addition measured after 10 mins by ammonium molybdate malachite green a2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID101910Cytotoxic activity was evaluated against MCF-7 cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID281715Inhibition of tubulin polymerization2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.
AID67259EBV-positive nasopharyngeal colony count obtained from the examination of uniform plate surface areas after a dose of 6.0 ug/mL1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Bis(bioreductive) alkylating agents: synthesis and biological activity in a nude mouse human carcinoma model.
AID777502Growth inhibition of human MCF7 cells after 72 hrs by MTS assay
AID496950Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
AID280522Ratio of IC50 for vinblastine-resistant CEM/VLB100 cells over IC50 for drug-sensitive CCRF-CEM cells2007Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6
Total structure and inhibition of tumor cell proliferation of laxaphycins.
AID679103TP_TRANSPORTER: transepithelial transport in the presence of of Vinblastine at 0.1 uM in Caco-2 cells2003Pharmaceutical research, Aug, Volume: 20, Issue:8
Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.
AID1183702Growth inhibition of human CEM cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1176902Cytotoxicity against vinblastin-sensitive human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay2015Journal of natural products, Jan-23, Volume: 78, Issue:1
Jalapinoside, a macrocyclic bisdesmoside from the resin glycosides of Ipomea purga, as a modulator of multidrug resistance in human cancer cells.
AID526945Cytotoxicity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents.
AID132377Percent increase in life span at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line for 1st scheduled day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID338003Cytotoxicity against human drug-resistant KBV1 cells by SRB assay in presence of vinblastine1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID354537Cytotoxicity against rat C6 cells after 3 days treated 4 hrs before db-cAMP challenge by MTT assay1996Journal of natural products, Dec, Volume: 59, Issue:12
Cell-based screen for identification of inhibitors of tubulin polymerization.
AID1154394Antiproliferative activity against human HCT116 cells after 72 hrs2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
One-pot synthesis of vinca alkaloids-phomopsin hybrids.
AID338230Cytotoxicity against mouse P388 cells after 48 hrs by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID459115Induction of apoptosis in human SNU398 cells assessed as caspase activation after 48 hrs by HTS assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 9-oxo-9H-fluorene ring.
AID1063218Antiproliferative activity against human MUTU-I cells at 10 uM after 24 hrs by Alamar blue assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and antiproliferative action of a novel series of maprotiline analogues.
AID629688Ratio of IC50 for vinblastine-resistant human CEM/VBL100 cells to IC50 for human CEM cells2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID681131TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID471347Cytotoxicity against human HL60 cells after 48 hrs by MTT assay2009Journal of natural products, Sep, Volume: 72, Issue:9
Biscarpamontamines A and B, an aspidosperma-iboga bisindole alkaloid and an aspidosperma-aspidosperma bisindole alkaloid, from Tabernaemontana sphaerocarpa.
AID184451Acute iv toxicity against rat after a dose of injection1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID135825Number of survivors on 60th day at dose 6 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID313986Inhibition of tubulin polymerization2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Antimitotic quinoid triterpenes from Maytenus chuchuhuasca.
AID135638Number of survivors on 60th day at dose 11 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1237736Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID355583Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1221968Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko1432011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID721765Cytotoxicity against human HCT116 cells after 72 hrs by phosphatase assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
A remarkable series of vinblastine analogues displaying enhanced activity and an unprecedented tubulin binding steric tolerance: C20' urea derivatives.
AID150754Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID263819Cytotoxicity against human PA1 cells by clonogenic assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID386357Inhibition of cross-linking of human Pgp TM1 L65R/TM6 L339C/TM7 F728 mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot2007The Journal of biological chemistry, Nov-02, Volume: 282, Issue:44
Suppressor mutations in the transmembrane segments of P-glycoprotein promote maturation of processing mutants and disrupt a subset of drug-binding sites.
AID1186751Cytotoxicity against human MDA-MB-435 cells assessed as cell viability at 1 nM after 72 hrs2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Greensporones: resorcylic acid lactones from an aquatic Halenospora sp.
AID138133Number of survivors on 30th day at dose 6 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0 /101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID777503Growth inhibition of human LS 174T cells after 72 hrs by MTS assay
AID732665Cytotoxicity against human IMR90 cells after 96 hrs by CellTiter-Glo luminescent assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Structures and cytotoxic evaluation of new and known acyclic Ene-Ynes from an American Samoa Petrosia sp. Sponge.
AID551271Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline.
AID642062Growth inhibition of doxorubicin-resistant human NCI-ADR-RES cells overexpressing P-glycoprotein after 96 hrs2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1183748Cell cycle arrest in human HepG2 cells at 500 to 2000 nM incubated for 24 hrs followed by compound washout measured after 24 hrs2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID137815Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intravenously at a dose of 4 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID367771Cytotoxicity against taxol-resistant human CCRF-CEM cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Novel DNA-directed alkylating agents: design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker.
AID354543Cytotoxicity against rat C6 cells assessed as cell release at 50 ug/mL to 2.5 mg/mL after 5 hrs by MTT assay in absence of db-cAMP1996Journal of natural products, Dec, Volume: 59, Issue:12
Cell-based screen for identification of inhibitors of tubulin polymerization.
AID82849Tested for the concentration required to reduce the viability of leukemia cells by 50% against cell growth of HL60 acute myeloid leukemia using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID537735Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1200319Antiproliferative activity against human MES-SA cells assessed as reduction in cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Activity of 2-aryl-2-(3-indolyl)acetohydroxamates against drug-resistant cancer cells.
AID669247Cytotoxicity against human WM9 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID737102Resistance index, ratio of IC50 for human CEM/VBL100 cells to IC50 for human CEM cells2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID1121897Growth inhibition of P-gp expressing human NCI-ADR-RES cells by Alamar Blue assay
AID1253986Inhibition of pig tubulin polymerization at 5 uM incubated for 20 mins at 37 degC by fluorescence based tubulin polymerization inhibition assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Synthesis of stereochemically diverse cyclic analogs of tubulysins.
AID732663Selectivity index, ratio of IC50 for human IMR90 cells to IC50 for human A2058 cells2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Structures and cytotoxic evaluation of new and known acyclic Ene-Ynes from an American Samoa Petrosia sp. Sponge.
AID1186752Cytotoxicity against human HT-29 cells assessed as cell viability at 10 nM after 72 hrs2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Greensporones: resorcylic acid lactones from an aquatic Halenospora sp.
AID375831Growth inhibition of human SNU398 cells after 48 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2: Structure-activity relationships of the 4-, 5-, 6-, 7- and 8-positions.
AID132379Percent increase in life span at dose 4 mg/kg/day in 7 mice implanted with P388 leukemia cell line for 1,8,15 scheduled day from Exp-21985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID386359Inhibition of cross-linking of human Pgp TM5 I306R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot2007The Journal of biological chemistry, Nov-02, Volume: 282, Issue:44
Suppressor mutations in the transmembrane segments of P-glycoprotein promote maturation of processing mutants and disrupt a subset of drug-binding sites.
AID418791Growth inhibition of human SNU398 cells after 48 hrs2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers.
AID200624Cytotoxicity against human SCLC cells resistant to cisplatin (SCLC/CDDP)1993Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25
Design of antineoplastic agents on the basis of the "2-phenylnaphthalene-type" structural pattern. 2. Synthesis and biological activity studies of benzo]b]naphtho[2,3-d]furan-6,11-dione derivatives.
AID553043Cytotoxicity against human SKOV3 cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID681089TP_TRANSPORTER: transepithelial transport (basal to apical) in MRP1-expressing LLC-PK1cell2002Pharmacology, , Volume: 64, Issue:3
Comparison of furosemide and vinblastine secretion from cell lines overexpressing multidrug resistance protein (P-glycoprotein) and multidrug resistance-associated proteins (MRP1 and MRP2).
AID1236005Downregulation of BimEL protein expression in human A549 cells at 100 nM after 24 hrs by Western blot analysis2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bisleuconothine A Induces Autophagosome Formation by Interfering with AKT-mTOR Signaling Pathway.
AID762140Inhibition of sheep brain tubulin polymerization by UV spectrophotometric analysis2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and biological evaluation of a new series of highly functionalized 7'-homo-anhydrovinblastine derivatives.
AID298562Cytotoxicity against human MCF7 cells by MTS assay after 24 hrs2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
An investigation into the cytotoxicity and mode of action of some novel N-alkyl-substituted isatins.
AID137637Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intravenously at a dose of 4 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID527874Cytotoxicity against mouse L1210 cells after 72 hrs2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Catharanthine C16 substituent effects on the biomimetic coupling with vindoline: preparation and evaluation of a key series of vinblastine analogues.
AID682247TP_TRANSPORTER: inhibition of photolabeling by IAARh123 (IAARh123: 1 uM, VBL: 1000 uM) in membranes from Mrp6-expressing P. pastoris2002Biochemistry, Jun-25, Volume: 41, Issue:25
Nucleotide binding and nucleotide hydrolysis properties of the ABC transporter MRP6 (ABCC6).
AID762136Cytotoxicity against human U87MG cells after 72 hrs by resazurin assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and biological evaluation of a new series of highly functionalized 7'-homo-anhydrovinblastine derivatives.
AID115821Evaluation of ILS percentage of mice upon intraperitoneal injection of VBL at a concentration of 0.2 mg/kg1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes.
AID551317Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis, and biological evaluation of novel water-soluble N-mustards as potential anticancer agents.
AID358162Inhibition of bovine liver MAOB1992Journal of natural products, Mar, Volume: 55, Issue:3
Metabolism of the Catharanthus alkaloids: from Streptomyces griseus to monoamine oxidase B.
AID551318Cytotoxicity against taxol-resistant human CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Design, synthesis, and biological evaluation of novel water-soluble N-mustards as potential anticancer agents.
AID679260TP_TRANSPORTER: transepithelial transport (basal to apical) in Caco-2 cells1993Pharmaceutical research, May, Volume: 10, Issue:5
Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers.
AID248302Concentration required for growth inhibition of human lung carcinoma cell line (CCRF-CEM) was determined2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Potent antitumor N-mustard derivatives of 9-anilinoacridine, synthesis and antitumor evaluation.
AID681119TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID607670Resistance factor, ratio of IC50 for drug-resistant MDR1-deficient human NCI/ADR cells expressing Pgp in absence of vinblastin to IC50 for drug-sensitive human MCF7 cells in presence of 50 nM vinblastin2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
2-Amino-4-methyl-5-phenylethyl substituted-7-N-benzyl-pyrrolo[2,3-d]pyrimidines as novel antitumor antimitotic agents that also reverse tumor resistance.
AID736615Induction of mitotic microtubule depolymerization in human MCF7 cells assessed as ratio of polymeric to soluble tubulin at 2 nM after 48 hrs by Western blot analysis (Rvb = 1.2)2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death.
AID338005Cytotoxicity against human LNCAP cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID132389Percent increase in life span at dose 6 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1154395Antiproliferative activity against human U87 cells after 72 hrs2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
One-pot synthesis of vinca alkaloids-phomopsin hybrids.
AID708917Cytotoxicity against human KB cells incubated for 72 hrs by MTS assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Flavaglines as potent anticancer and cytoprotective agents.
AID704747Cytotoxicity against human vinblastin-resistant HCT116/VM46 cells2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
10'-Fluorovinblastine and 10'-Fluorovincristine: Synthesis of a Key Series of Modified Vinca Alkaloids.
AID272514Antiproliferative activity against adriamycin resistant P388 cells in presence of 5 uM 1,13-bis[4'-((5,7-dihydroxy)-4H-chromen-4-on-2-yl)phenyl]-1,4,7,10,13-pentaoxatridecane by ELISA2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID679126TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2004European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Jan, Volume: 21, Issue:1
Exploring the quantitative relationship between the level of MDR1 transcript, protein and function using digoxin as a marker of MDR1-dependent drug efflux activity.
AID459114Induction of apoptosis in human HCT116 cells assessed as caspase activation after 48 hrs by HTS assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 9-oxo-9H-fluorene ring.
AID367776Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Novel DNA-directed alkylating agents: design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker.
AID605771Resistant ratio of IC50 for paclitaxel-resistant CHO-TAX 5-6 cells to IC50 for CHO cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1063216Antiproliferative activity against human PBMC at 10 uM after 24 hrs by Alamar blue assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and antiproliferative action of a novel series of maprotiline analogues.
AID266296Antiproliferative activity against human CCRF-CEM cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity.
AID150618Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID132534Percent increase in life span at dose 7 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
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.
AID342492Growth inhibition of human HT29 cells after 48 hrs by sulforhodamine B assay2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID319348Growth inhibition of doxorubicin-resistant human K562 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID448007Growth inhibition of human K562 cells after 72 hrs by XTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID521209Antiproliferative activity against mouse astrocyte cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID400578Cytotoxicity against VM46-resistant human HCT116 cells overexpressing P-gp after 72 hrs by MTS assay2004Journal of natural products, Mar, Volume: 67, Issue:3
Scleritodermin A, a cytotoxic cyclic peptide from the lithistid sponge Scleritoderma nodosum.
AID356743Antitumor activity against rat A10 cells assessed as total loss of cellular microtubule at 150 nM after 18 hrs by indirect immunofluorescence2001Journal of natural products, Jul, Volume: 64, Issue:7
Isolation of dolastatin 10 from the marine cyanobacterium Symploca species VP642 and total stereochemistry and biological evaluation of its analogue symplostatin 1.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID430796Cytotoxicity against human HCT15 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12.
AID150756Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID674216Antiproliferative activity against human CEM cells assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID153937Long-term survivors (LTS) for 60 days at optimal dose of 3.0 mg/kg for antitumor activity against P388 leukemia cells in 45 mice.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
New alpha-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity.
AID1237726Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID135673Number of survivors on 60th day at dose 4 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID271727Inhibition of ATPase measured as ATP availability in Caco-2 cells at 20 nM after 60 mins relative to control2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
AID137828Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intravenously at a dose of 9 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID266299Antiproliferative activity against human A549 cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity.
AID1121894Growth inhibition of pig LLC-PK1 cells expressing MDR1 by Alamar Blue assay
AID642111Induction apoptosis in human HeLa cells at 100 nM after 24 hrs by Annexin V-based flow cytometry analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID627405Antiproliferative activity against paclitaxel-resistant CHO-TAX 5-6 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID462940Selectivity ratio of IC50 for vinblastine-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID1228082Cytotoxicity against human MDA-MB-435 cells assessed as cell viability after 72 hrs by commercial absorbance assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
17-Norpimaranes and (9βH)-17-Norpimaranes from the Tuber of Icacina trichantha.
AID150735High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID1203386Antiproliferative activity in sea urchin embryo assessed as destabilization of microtubule by tuberculate eggs after 15 mins to 20 hrs2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID729164Resistance index, ratio of IC50 for human MDA-MB-435/LCC6 MDR1 cells to IC50 for human MDA-MB-435 cells2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID448006Growth inhibition of human Jurkat cells after 72 hrs by XTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID537736Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID721877Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID519607Cytotoxicity against Hepatocyte cells assessed as cell viability by MTT assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
New active drugs against liver stages of Plasmodium predicted by molecular topology.
AID418790Growth inhibition of human HCT116 cells after 48 hrs2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers.
AID627395Antiproliferative activity against human CHO after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID708918Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTS assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Flavaglines as potent anticancer and cytoprotective agents.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID642112Induction apoptosis in human HeLa cells at 10 nM after 24 hrs by Annexin V-based flow cytometry analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID683699Antimalarial activity against liver stages of Plasmodium yoelii yoelii2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Targeting the liver stage of malaria parasites: a yet unmet goal.
AID1203383Antiproliferative activity in sea urchin embryo assessed as antimitotic activity by measuring cleavage alteration exposed for 8 to 20 mins after fertilization and 45 to 55 mins before first mitotic cycle completion measured 2.5 to 5.5 hrs after fertilizat2015European journal of medicinal chemistry, Apr-13, Volume: 94A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines.
AID462945Cytotoxicity against human CL1-0 cells after 72 hrs by alamar blue assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID766784Inhibition of tubulin polymerization in human NCI-H522 cells assessed as alpha-tubulin accumulation in cytoskeletal fraction at 100 nM after 24 hrs by Western blot analysis2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design, synthesis, and mechanism of action of 2-(3-hydroxy-5-methoxyphenyl)-6-pyrrolidinylquinolin-4-one as a potent anticancer lead.
AID551398Ratio of IC50 for human CCRF-CEM cells to IC50 for Taxol-resistant human CCRF-CEM cells2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID717148Antiproliferative activity against human CEM cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID67121Percent colony reduction in cell growth in EBV-positive nasopharyngeal cell lines after administration of 6.0 ug/mL dose1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Bis(bioreductive) alkylating agents: synthesis and biological activity in a nude mouse human carcinoma model.
AID777496Growth inhibition of vinblastine-resistant human HCT116/VM46 cells overexpressing P-gp after 72 hrs by MTS assay
AID398654Inhibition of tubulin assembly into microtubules1995Journal of natural products, Aug, Volume: 58, Issue:8
An antimitotic and cytotoxic chalcone from Fissistigma lanuginosum.
AID607281Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID426741Cytotoxicity against human MX1 cells after 72 hrs by SRB assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes.
AID697007Induction of human MDR1 ATPase activity assessed as inorganic phosphate production2011Journal of natural products, Apr-25, Volume: 74, Issue:4
The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
AID395038Inhibition of P-gp ATPase activity in human DC-3F/ADX cells assessed as increase in basal activity measured by NADH level at 0.5 uM by spectrophotometric method2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Search for MDR modulators: design, syntheses and evaluations of N-substituted acridones for interactions with p-glycoprotein and Mg2+.
AID227414Relative inhibition (IC50) in presence and absence of reserpine2004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID642114Induction apoptosis in human HeLa cells assessed as caspase -3 activity at 100 nM after 24 hrs by single-cell immunofluorescence assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID351577Inhibition of tubulin polymerization by DAPI staining method2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the carboxamide group.
AID281698Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.
AID679061TP_TRANSPORTER: transepithelial transport of Vinblastine at a concentration of 0.1 uM in MDR1-expressing MDCK cells2003Pharmaceutical research, Aug, Volume: 20, Issue:8
Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.
AID537733Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1194490Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives.
AID1177863Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach.
AID723115Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by phosphatase assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Total synthesis and evaluation of vinblastine analogues containing systematic deep-seated modifications in the vindoline subunit ring system: core redesign.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID732667Cytotoxicity against human A2058 cells after 96 hrs by CellTiter-Glo luminescent assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Structures and cytotoxic evaluation of new and known acyclic Ene-Ynes from an American Samoa Petrosia sp. Sponge.
AID124257In vivo activity against transplanted Mam-16/C/Adr tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID337999Cytotoxicity against human BC1 cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID354541Inhibition of tubulin polymerization in rat C6 cells after 4 hrs1996Journal of natural products, Dec, Volume: 59, Issue:12
Cell-based screen for identification of inhibitors of tubulin polymerization.
AID777510Growth inhibition of human AU565 cells after 72 hrs by MTS assay
AID312974Growth inhibition of human T47D cells after 48 hrs2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.
AID679467TP_TRANSPORTER: efflux in MDR1-expressing LLC-PK1 cells2004Biochemical pharmacology, Jan-15, Volume: 67, Issue:2
Variable modulation of opioid brain uptake by P-glycoprotein in mice.
AID1221963Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID291506Cell cycle arrest in HL60 cells assessed as accumulation in G0/M phase at 80 nM2007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID518932Inhibition of tubulin in Acanthamoeba castellanii by alamar blue assay2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Molecular basis for resistance of acanthamoeba tubulins to all major classes of antitubulin compounds.
AID607289Antiproliferative activity against human doxorubicin-resistant LoVo cells overexpressing P-gp assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID333844Genotoxicity against CHO cells
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID715430Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in MDCK2 cells expressing MDR1 by gamma counting2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Radiofluorinated histamine H₃ receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.
AID679466TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-P388 cells1996Anti-cancer drugs, Jul, Volume: 7, Issue:5
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.
AID137661Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 4 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID298665Increase in caspase 3 activation in Jurkat cells at 1 uM2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Discovery and investigation of antiproliferative and apoptosis-inducing properties of new heterocyclic podophyllotoxin analogues accessible by a one-step multicomponent synthesis.
AID487884Binding affinity to P-gp at 5 uM after 30 mins by spectrophotometry2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Targeting efflux pumps-In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation.
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID1237734Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID357846Binding affinity to yeast tRNA assessed as reduction in tRNA peak by pre-incubation method
AID721875Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID462942Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID518931Inhibition of tubulin in Acanthamoeba polyphaga by alamar blue assay2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Molecular basis for resistance of acanthamoeba tubulins to all major classes of antitubulin compounds.
AID1183747Cell cycle arrest in human RD cells at 500 nM incubated for 24 hrs followed by compound washout measured after 24 hrs2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID679743TP_TRANSPORTER: increase in Colchicine intracellular accumulation (Colchicine: 0.0175 uM, Vinblastine: 100 uM) in CEM/VBL600 cells1999Pflugers Archiv : European journal of physiology, Apr, Volume: 437, Issue:5
P-glycoprotein inhibition by glibenclamide and related compounds.
AID1177862Cytotoxicity against vinblastine-resistant human CCRF-CEM cells assessed as growth inhibition after 72 hrs by Alamar Blue assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach.
AID135811Number of survivors on 60th day at dose 5 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID681139TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID680488TP_TRANSPORTER: inhibition of Ivermectin binding (IVM: 0.2 uM, Vinblastine: 300-fold molar excess) in plasma membranes from CEM/VLB1.0 cells1997Biochemical pharmacology, Jan-10, Volume: 53, Issue:1
Reversal of P-glycoprotein-associated multidrug resistance by ivermectin.
AID338223Cytotoxicity against vinblastine-resistant human KBV1 cells1993Journal of natural products, Apr, Volume: 56, Issue:4
Bisamides from Aglaia species: structure analysis and potential to reverse drug resistance with cultured cells.
AID272516Relative fold, IC50 in absence to presence of 1,13-bis[4'-((5,7-dihydroxy)-4H-chromen-4-on-2-yl)phenyl]-1,4,7,10,13-pentaoxatridecane in multidrug resistant P388 cells2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Flavonoid dimers as bivalent modulators for P-glycoprotein-based multidrug resistance: synthetic apigenin homodimers linked with defined-length poly(ethylene glycol) spacers increase drug retention and enhance chemosensitivity in resistant cancer cells.
AID1237732Inhibition of microtubule polymerization in human HeLa cells assessed as appearance of tubulin foci and/or small asters of short microtubule fragments at 20 nM after 24 hrs by immunofluorescence staining-based microscopic analysis2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID418789Growth inhibition of human T47D cells after 48 hrs2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers.
AID214333The compound tested for the inhibition of tubulin polymerization.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
New alpha-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity.
AID338231Cytotoxicity against human U373 cells by SRB assay1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID680140TP_TRANSPORTER: inhibition of ATPase activity (Verapamil) in membranes from CEM/VLB100 cells1998Biochemical pharmacology, Sep-15, Volume: 56, Issue:6
Effect of modulators on the ATPase activity and vanadate nucleotide trapping of human P-glycoprotein.
AID1228083Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by commercial absorbance assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
17-Norpimaranes and (9βH)-17-Norpimaranes from the Tuber of Icacina trichantha.
AID603118Ratio of IC50 for human vinblastine-resistant CCRF-CEM cells to IC50 for human CCRF-CEM cells2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates.
AID412799Cytotoxicity against human KB cells after 72 hrs2009Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
Synthesis and biological evaluation of vinca alkaloids and phomopsin hybrids.
AID1183737Cytotoxicity against human RD cells assessed as growth inhibition after 48 hrs by MTT method2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID399157Cytotoxicity against human 9KB cells
AID462946Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1221970Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko1432011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID627396Antiproliferative activity against human K562 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID310122Inhibition of P-glycoprotein by Hoechst assay2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
New functional assay of P-glycoprotein activity using Hoechst 33342.
AID375986Cytotoxicity against human Hep2 cells after 72 hrs by SRB method2006Journal of natural products, Apr, Volume: 69, Issue:4
Resin glycosides from the flowers of Ipomoea murucoides.
AID596502Cytotoxicity against human KB-3-1 cells after 5 days by MTT assay2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Marinoquinolines A-F, pyrroloquinolines from Ohtaekwangia kribbensis (Bacteroidetes).
AID137646Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intravenously at a dose of 6 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID132552Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intraperitoneally at a dose of 4 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID551272Cytotoxicity against human A549 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline.
AID688497Cytotoxicity against vinblastine-sensitive human MCF7 cells after 72 hrs by SRB assay2012Journal of natural products, Sep-28, Volume: 75, Issue:9
Mammalian multidrug resistance lipopentasaccharide inhibitors from Ipomoea alba seeds.
AID137481Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 0.33 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID358163Drug level in mouse liver mitochondria1992Journal of natural products, Mar, Volume: 55, Issue:3
Metabolism of the Catharanthus alkaloids: from Streptomyces griseus to monoamine oxidase B.
AID350783Permeability from apical to basolateral side in human Caco-2 cells2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.
AID99290The ratio of survival time for treated divided by survival time of control x 100 at a dose of 0.2 mg/kg in L1210 leukemia cells1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Chalcones: a new class of antimitotic agents.
AID137988Number of survivors on 30th day at dose 3 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0 /101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID167215Tested for the concentration required to reduce the viability of leukemia cells by 50% against cell growth of RPMI8226 multiple myeloma using MTT assay2002Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
AID732666Cytotoxicity against human H522-T1 cells after 96 hrs by CellTiter-Glo luminescent assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Structures and cytotoxic evaluation of new and known acyclic Ene-Ynes from an American Samoa Petrosia sp. Sponge.
AID1235248Cytotoxicity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Cytotoxic Homoisoflavones from the Bulbs of Bellevalia eigii.
AID351382Inhibition of tubulin polymerization2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Novel carbazole and acyl-indole antimitotics.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1231622Inhibition of alpha-tubulin formation in human A549 cells at 50 nM after 24 hrs by TRITC/Hoechst 33258 staining-based immunofluorescence microscopic analysis2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of thiabendazole derivatives as anti-angiogenesis and vascular disrupting agents.
AID459122Growth inhibition of human T47D cells after 48 hrs2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 9-oxo-9H-fluorene ring.
AID1157201Ratio of IC50 for human vinblastine-resistant CCRF-CEM cells to IC50 for human CCRF-CEM cells2014European journal of medicinal chemistry, Aug-18, Volume: 83The synthesis and biological evaluation of new DNA-directed alkylating agents, phenyl N-mustard-4-anilinoquinoline conjugates containing a urea linker.
AID247822Inhibition of tubulin polymerization interacting at the colchicine binding site.2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata.
AID680883TP_TRANSPORTER: efflux in MDR1-expressing BeWo cells2003American journal of physiology. Cell physiology, Sep, Volume: 285, Issue:3
Role of MDR1 and MRP1 in trophoblast cells, elucidated using retroviral gene transfer.
AID135803Number of survivors on 60th day at dose 4 mg/kg/day in 7 mice implanted with P388 leukemia cell line for 1,8,15 acheduled days form Exp-1; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID270360Cytotoxicity against human K562 cells2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells.
AID526953Resistance index, ratio of IC50 for human multidrug-resistant MDA-MB-435/LCCMDR1 cells to IC50 for human MDA-MB-435 cells2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents.
AID596500Cytotoxicity against mouse L929 cells after 5 days by MTT assay2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Marinoquinolines A-F, pyrroloquinolines from Ohtaekwangia kribbensis (Bacteroidetes).
AID540211Fraction unbound 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.
AID721881Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID663890Ratio of IC50 for human vinblastine-resistant CCRF-CEM cells to IC50 for human CCRF-CEM cells2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antitumor evaluation of novel benzo[d]pyrrolo[2,1-b]thiazole derivatives.
AID1183704Resistance index, ratio of IC50 for human CEM/VBL100 cells to IC50 for human CEM cells2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID680078TP_TRANSPORTER: inhibition of Azidopine photoaffinity labelling (Azidopine: 0.4 uM, Vinblastine: 400 uM) in membranes from MDR1-expressing LLC-PK1 cells1999Biological & pharmaceutical bulletin, Dec, Volume: 22, Issue:12
Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs.
AID45282Absorptive transport in Caco-2 cells in comparison to metoprolol2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.
AID603117Ratio of IC50 for human taxol-resistant CCRF-CEM cells to IC50 for human CCRF-CEM cells2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates.
AID618916Anticancer activity against P-gp overexpressing human NCI/ADR-RES cells after 96 hrs by SRB assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents.
AID518933Inhibition of tubulin in rabbit corneal cells by alamar blue assay2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Molecular basis for resistance of acanthamoeba tubulins to all major classes of antitubulin compounds.
AID375832Induction of apoptosis in human T47D cells measured after 48 hrs by cell and caspase based HTS assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2: Structure-activity relationships of the 4-, 5-, 6-, 7- and 8-positions.
AID426737Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes.
AID430804Cytotoxicity against human HepG2 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12.
AID1221956Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID263817Cytotoxicity against human KB cells by clonogenic assay2006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
AID249995Ability to induce cells in G2/M phase2004Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20
Antimitotic activity of 5-hydroxy-7-methoxy-2-phenyl-4-quinolones.
AID152988Cytotoxic activity was evaluated against P388/ADR + reserpine cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID551393Cytotoxicity against human PC3 cells after 72 hrs by Alamar blue assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Novel bifunctional alkylating agents, 5,10-dihydropyrrolo[1,2-b]isoquinoline derivatives, synthesis and biological activity.
AID679471TP_TRANSPORTER: transepithelial transport (basal to apical) in Mdr1b-expressing LLC-PK1 cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs.
AID312973Induction of apoptosis in human SNU398 cells assessed as caspase activation after 24 hrs by HTS assay2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.
AID605772Antiproliferative activity against paclitaxel-resistant CHO-VV 3-2 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID459123Growth inhibition of human HCT116 cells after 48 hrs2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 9-oxo-9H-fluorene ring.
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID137485Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intraperitoneally at a dose of 2 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID132543Percent increase in life span at dose 9 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID132348Percent increase in life span at dose 10 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID777499Growth inhibition of human ZR-75-1 cells after 72 hrs by MTS assay
AID137824Number of survivors of DBA2 mice on 60th day after inoculation with L1210 leukemia cell line intravenously at a dose of 6 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID335774Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.8 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID1183746Cell cycle arrest in human RD cells at 1000 to 2000 nM incubated for 24 hrs followed by compound washout measured after 24 hrs2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID605770Antiproliferative activity against paclitaxel-resistant CHO-TAX 5-6 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID605775Resistant ratio of IC50 for multidrug-resistant human CEM-VLB cells to IC50 for human CEM cells2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID519606Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
New active drugs against liver stages of Plasmodium predicted by molecular topology.
AID729161Cytotoxicity against human MDA-MB-435/LCC6MDR1 cells assessed as growth inhibition after 48 hrs by SRB assay2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1183742Cell cycle arrest in human PC3 cells assessed as rounded cells at 500 nM after 24 hrs by propidium iodide staining-based flow cytometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID426739Cross-resistance, IC50 for human vinblastine-resistant CCRF-CEM cells to IC50 for human CCRF-CEM cells2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes.
AID338222Cytotoxicity against human KB cells1993Journal of natural products, Apr, Volume: 56, Issue:4
Bisamides from Aglaia species: structure analysis and potential to reverse drug resistance with cultured cells.
AID680155TP_TRANSPORTER: binding in membrane vesicle from CEM/VLB100 cells1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
AID335772Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 20 ug/mL1993Journal of natural products, Oct, Volume: 56, Issue:10
Cytotoxic constituents from Hyptis verticillata.
AID777517Growth inhibition of mouse L1210 cells after 72 hrs by phosphatase assay
AID678743TP_TRANSPORTER: inhibition of TBuMA transepithelial transport (basal to apical)(TBuMA: 10 uM, Vinblastine: 2 uM) in Mdr1a-expressing LLC-PK1 cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs.
AID553099Cytotoxicity against human HCT116 cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID249998Ability to induce cells in G0/G1 phase2004Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20
Antimitotic activity of 5-hydroxy-7-methoxy-2-phenyl-4-quinolones.
AID132551Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intraperitoneally at a dose of 3 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID679122TP_TRANSPORTER: transepithelial transport (basal to apical) in Mdr1a-expressing LLC-PK1 cells1998The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1
Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs.
AID312975Growth inhibition of human HCT116 cells after 48 hrs2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.
AID342493Growth inhibition of human M21 cells after 48 hrs by sulforhodamine B assay2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression.
AID288695Growth inhibition of human M21 cells after 48 hrs2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Alkylation potency and protein specificity of aromatic urea derivatives and bioisosteres as potential irreversible antagonists of the colchicine-binding site.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID721879Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID579804Antiproliferative activity against P-gp overexpressing human MES-SA/Dx5-Rx1 cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID721873Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID626620Antiproliferative activity against colchicine and vinblastine-resistant CHO-VV 3-2 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID459113Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs by HTS assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 9-oxo-9H-fluorene ring.
AID588974Substrates of transporters of clinical importance in the absorption and disposition of drugs, MDR12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID642110Induction of mitotic arrest in human HeLa cells assessed as accumulation at G2/M phase at 2 to 20 nM after 24 hrs by flow cytometry analysis relative to control2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID134234Acute iv toxicity against Swiss strain of 40 mice after 4 doses of injection1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID45400Effect on cross resistance of CHO cells resistant to colchicine (CHRC5)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID459124Growth inhibition of human SNU398 cells after 48 hrs2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 9-oxo-9H-fluorene ring.
AID266300Antiproliferative activity against human HCT116 cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity.
AID132705Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia intravenously at a dose of 3 mg/kg per day1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID44202Effect on cross resistance of CCRF-CEM cells resistant to vincristine.1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID627398Antiproliferative activity against human P388D1 after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID319349Resistant ratio, IC50 for multidrug resistant human K562 cells to IC50 for human K562 cells2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID414575Apparent permeability across human Caco-2 cells2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID217192Cytotoxic activity against african green monkey (Cercopithecus aethiops) kidney epithelial cells (VERO)2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Synthesis, spectroscopy, and cytotoxicity of glycosylated acetogenin derivatives as promising molecules for cancer therapy.
AID745771Cytotoxicity against human A2058 cells assessed as growth inhibition after 96 hrs by CellTiter-Glo luminescence assay2013Journal of natural products, May-24, Volume: 76, Issue:5
Antiproliferative Homoisoflavonoids and Bufatrienolides from Urginea depressa.
AID137650Number of survivors of DBA2 mice on 30th day after inoculation with L1210 leukemia cell line intravenously at a dose of 8 mg/kg/day; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
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.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID462936Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID101912Cytotoxic activity was evaluated against MCF-7/ADR+Reserpine cells1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.
AID125973Inhibition of bovine brain microtubule polymerization2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID103735Compound was tested in vitro for growth inhibition of MCF-7 cells derived from human breast tumor.1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Novel antineoplastic agents with efficacy against multidrug resistant tumor cells.
AID1194489Cytotoxicity against human K562 cells assessed as inhibition of cell proliferation after 72 hrs2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives.
AID355920Cytotoxicity against human KB cells2003Journal of natural products, Jun, Volume: 66, Issue:6
Two unusual acetogenins from the roots of Annona salzmanii.
AID132372Percent increase in life span at dose 3 mg/kg/day in 10 mice implanted with P388 leukemia cell line1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID367774Ratio of IC50 for vinblastine-resistant human CCRF-CEM cells to IC50 for human CCRF-CEM cells2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Novel DNA-directed alkylating agents: design, synthesis and potent antitumor effect of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker.
AID134235Acute iv toxicity against mice after a dose of injection1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID270357Activity against human TK1 assessed as thymidine phosphorylation relative to thymidine2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID696926Induction of human MDR1 ATPase activity assessed as inorganic phosphate production in presence of MDR1 inhibitor cyclosporin A2011Journal of natural products, Apr-25, Volume: 74, Issue:4
The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes.
AID291494Growth inhibition of Pgp deficient MCF7 cells expressing MRP12007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
AID736270Cytotoxicity against human H460 cells after 96 hrs by CellTiter-Glo assay2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Mycoleptodiscins A and B, cytotoxic alkaloids from the endophytic fungus Mycoleptodiscus sp. F0194.
AID430794Cytotoxicity against human MCF7 cells expressing P-glycoprotein after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12.
AID681122TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
AID1221957Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID426738Cytotoxicity against human taxol-resistant CCRF-CEM cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes.
AID477295Octanol-water partition coefficient, log P of the compound2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations.
AID777505Growth inhibition of human KPL4 cells after 72 hrs by MTS assay
AID312976Growth inhibition of human SNU398 cells after 48 hrs2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions.
AID579984Cytotoxicity against human HCT15 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID462947Cytotoxicity against human MCF7 cells after 72 hrs by alamar blue assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID291495Growth inhibition of NCI/ADR cells expressing Pgp/MRP12007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
AID607290Antiproliferative activity against human CEM cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1121896Resistance factor, ratio of GI50 for P-gp expressing NCI-ADR-RES cells to GI50 for human OVCAR8 cells
AID143034Antiproliferative activity against the human non small cell lung carcinoma cell line NCI-H4602002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID1200320Antiproliferative activity against human MES-SA/Dx5 cells assessed as reduction in cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Activity of 2-aryl-2-(3-indolyl)acetohydroxamates against drug-resistant cancer cells.
AID605769Antiproliferative activity against human CEM cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID338004Cytotoxicity against human drug-resistant KBV1 cells by SRB assay in absence of vinblastine1994Journal of natural products, Nov, Volume: 57, Issue:11
Indole alkaloids from Peschiera laeta that enhance vinblastine-mediated cytotoxicity with multidrug-resistant cells.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID134231Acute iv toxicity against CD1 strain of 40 mice after 4 doses of injection1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID298669Effect on apoptosis in Jurkat cells assessed as cleavage of PARP at 1 uM2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Discovery and investigation of antiproliferative and apoptosis-inducing properties of new heterocyclic podophyllotoxin analogues accessible by a one-step multicomponent synthesis.
AID553041Cytotoxicity against human MDA231 cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Novel flavaglines displaying improved cytotoxicity.
AID616984Antiproliferative activity against MDR-1 overexpressing human 786-0 cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID721878Cytotoxicity against human HCT116 assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID319345Growth inhibition of doxorubicin resistant human HepG2 cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Methoxylation of 3',4'-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells.
AID336107Resistance index, ratio for IC50 for multidrug-resistant human KBV1 cells to IC50 for drug-resistant human KB-3-1 cells2002Journal of natural products, Sep, Volume: 65, Issue:9
In vitro cytotoxic activity of phenanthroindolizidine alkaloids from Cynanchum vincetoxicum and Tylophora tanakae against drug-sensitive and multidrug-resistant cancer cells.
AID137967Number of survivors on 30th day at dose 11 mg/kg/day in 10 mice implanted with P388 leukemia cell line; 0/101985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID124263In vivo activity against transplanted Panc-03 tumors of mice2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Design, synthesis, and biological evaluation of analogues of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
AID669248Cytotoxicity against human WM164 cells after 72 hrs by XTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
AID721764Cytotoxicity against vinblastine-resistant human HCT116/VM46 cells after 72 hrs by phosphatase assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
A remarkable series of vinblastine analogues displaying enhanced activity and an unprecedented tubulin binding steric tolerance: C20' urea derivatives.
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID605768Antiproliferative activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID46882Inhibition against CRFF-CEM-T-Cell leukemic cell line1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
In vitro metabolic transformations of vinblastine: oxidations catalyzed by human ceruloplasmin.
AID677621Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Identification of selective tubulin inhibitors as potential anti-trypanosomal agents.
AID132546Percent increase in life span of DBA2 mice after inoculation with L1210 leukemia cells intraperitoneally at a dose of 0.33 mg/kg per day for 1-9 scheduled days1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID214009Inhibition of tubulin polymerization using isolated calf brain1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives.
AID602935Cytotoxicity against human taxol-resistant CCRF-CEM cells after 72 hrs by XTT assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates.
AID248428Concentration required for growth inhibition of human HCT116 colon tumor cell line (CCRF-CEM) was determined2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Potent antitumor N-mustard derivatives of 9-anilinoacridine, synthesis and antitumor evaluation.
AID462937Cytotoxicity against taxol-resistant human CCRF-CEM cells after 72 hrs by XTT assay2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID408350Cytotoxicity against human CCRF-CEM cells after 72 hrs by XTT assay2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage.
AID430792Cytotoxicity against human KB cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12.
AID132378Percent increase in life span at dose 4 mg/kg/day in 7 mice implanted with P388 leukemia cell line for 1,8,15 scheduled day from Exp-11985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias.
AID333845Genotoxicity against CHO cells after UV irradiation
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (274)

TimeframeStudies, This Drug (%)All Drugs %
pre-199031 (11.31)18.7374
1990's41 (14.96)18.2507
2000's108 (39.42)29.6817
2010's92 (33.58)24.3611
2020's2 (0.73)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 66.88

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 Index66.88 (24.57)
Research Supply Index5.50 (2.92)
Research Growth Index5.50 (4.65)
Search Engine Demand Index112.12 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (66.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials19 (38.78%)5.53%
Trials0 (0.00%)5.53%
Reviews2 (4.08%)6.00%
Reviews4 (1.65%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other28 (57.14%)84.16%
Other239 (98.35%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (164)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Risk-Adapted Stanford V-C With Radiotherapy for Clinical Stage I and IIA Favorable Hodgkin's Disease: The G5 Study [NCT00026208]Phase 276 participants (Actual)Interventional2001-06-30Completed
Target-specific Therapy With Pazopanib as Add-on to Vinflunine in Patients With Advanced or Metastatic Urothelial Carcinoma of the Bladder After Failure of Platinum-based Treatment [NCT01265940]Phase 1/Phase 25 participants (Actual)Interventional2011-03-31Completed
Phase III Trial of High Dose Interferon Alfa 2-b Versus Cisplatin, Vinblastine, DTIC Plus IL-2 and Interferon in Patients With High Risk Melanoma [NCT00006237]Phase 3432 participants (Actual)Interventional2000-08-31Completed
H-9926-LCH III: Treatment Protocol of the Third International Study for Langerhans Cell Histiocytosis [NCT00488605]Phase 30 participants (Actual)Interventional2023-08-01Withdrawn(stopped due to This is a duplicate record and the sponsor has registered the study.)
A Three-Arm Phase III Study of Concomitant Versus Sequential Chemotherapy and Thoracic Radiotherapy for Patients With Locally Advanced Inoperable Non-small Cell Lung Cancer [NCT01134861]Phase 3610 participants (Actual)Interventional1994-07-31Completed
A Phase I Study of Vinblastine and Sirolimus in Pediatric Patients With Recurrent or Refractory Solid Tumors Including CNS Tumors [NCT01135563]Phase 114 participants (Actual)Interventional2010-04-30Completed
A Randomized, Open-label, Multicenter, Phase III, 2-arm Study Comparing Efficacy and Tolerability of the Intensified Variant 'Dose-dense/Dose-intense ABVD' (ABVD DD-DI) With an Interim PET Response-adapted ABVD Program as Upfront Therapy in Advanced-stage [NCT03159897]Phase 3500 participants (Anticipated)Interventional2017-08-01Active, not recruiting
A Study of Vinblastine and Temsirolimus in Pediatric Patients With Recurrent or Refractory Lymphoma or Solid Tumours Including CNS Tumours [NCT02343718]Phase 17 participants (Actual)Interventional2015-06-24Completed
A Randomised Phase III Trial With a PET Response Adapted Design Comparing ABVD +/- ISRT With A2VD +/- ISRT in Patients With Previously Untreated Stage IA/IIA Hodgkin Lymphoma [NCT04685616]Phase 31,042 participants (Anticipated)Interventional2022-04-14Recruiting
Non-Comparative, Multi-Cohort, Single Arm, Open-Label, Phase 2 Study of Nivolumab (BMS-936558) in Classical Hodgkin Lymphoma (cHL) Subjects [NCT02181738]Phase 2294 participants (Actual)Interventional2014-08-12Completed
A Randomized Phase III Randomized Study to Compare R-CHOP Versus R-mini-CEOP in Elderly Patients (>65 Years) With Diffuse Large B Cell Lymphoma (DLBCL) [NCT01148446]Phase 3226 participants (Actual)Interventional2003-01-31Completed
First Line Chemotherapy for Classical Hodgkin Lymphoma in Russia [NCT04638790]Phase 3300 participants (Anticipated)Interventional2020-02-01Recruiting
LCH-IV, International Collaborative Treatment Protocol for Children and Adolescents With Langerhans Cell Histiocytosis [NCT02205762]Phase 2/Phase 31,400 participants (Anticipated)Interventional2016-11-02Recruiting
Nivolumab and AVD in Early-stage Unfavorable Classical Hodgkin Lymphoma [NCT03004833]Phase 2110 participants (Actual)Interventional2017-02-21Active, not recruiting
Outcome of Cisplatin and Vinblastine Versus Paclitaxel and Carboplatin as Sequential Chemotherapy Followed by Radiotherapy in Locally Advanced Non-small Cell Lung Cancer [NCT03092986]Phase 460 participants (Actual)Interventional2017-01-01Completed
Prospective Controlled Trial in Clinical Stages I-II Supradiaphragmatic Hodgkin's Disease: Evaluation of Treatment Efficacy, (Long Term) Toxicity and Quality of Life in Two Different Prognostic Subgroups [NCT00005584]Phase 31,649 participants (Actual)Interventional1998-10-31Active, not recruiting
A Phase II, Multicenter, Open Label Study of Treatment Intensification With ACVD and Brentuximab-Vedotin in Advanced-stage Hodgkin Lymphoma Patients With a Positive Interim PET Scan After 2 ABVD Cycles [NCT03527628]Phase 2220 participants (Anticipated)Interventional2018-01-01Recruiting
MVAC (Methotrexate, Vinblastine, Adriamycin, and Cisplatin) in Organ-Confined Bladder Cancer Based on p53 Status [NCT00005047]Phase 3521 participants (Actual)Interventional1997-08-31Terminated(stopped due to Accrual was halted on the basis of the Data and Safety Monitoring Board review of a futility analysis.)
HD17 for Intermediate Stages - Treatment Optimization Trial in the First-Line Treatment of Intermediate Stage Hodgkin Lymphoma [NCT01356680]Phase 31,100 participants (Actual)Interventional2012-01-13Completed
A Prospective Randomized Phase III, Trial Comparing Consolidation Therapy With or Without Strontium-89 Following Induction Chemotherapy in Androgen-Independent Prostate Cancer [NCT00024167]Phase 3265 participants (Actual)Interventional2002-04-30Terminated(stopped due to Terminated due to slow accrual)
A Pilot Trial of AVD and Brentuximab Vedotin (SGN-35) in the Treatment of Stage II-IV HIV-Associated Hodgkin Lymphoma [NCT01771107]Phase 1/Phase 241 participants (Actual)Interventional2013-03-07Active, not recruiting
Prospective Randomized Comparison of ABVD Versus BEACOPP Chemotherapy With or Without Radiotherapy for Advanced Stage or Unfavorable Hodgkin's Lymphoma (HL) [NCT01251107]Phase 3331 participants (Actual)Interventional2000-03-31Completed
A Pilot Study of Brentuximab Vedotin Combined With AVD Chemotherapy in Patients With Newly Diagnosed Early Stage, Unfavorable Risk Hodgkin Lymphoma [NCT01868451]118 participants (Actual)Interventional2013-05-31Active, not recruiting
Phase III Randomized Trial of Adjuvant Involved-Field Radiotherapy vs No Adjuvant Therapy Following Remission Induction With MOPP/ABV Hybrid Chemotherapy in Patients With Stage III/IV Hodgkin's Disease [NCT00002462]Phase 3615 participants (Actual)Interventional1989-09-30Active, not recruiting
Phase 2 Study of Pembrolizumab and Chemotherapy in Patients With Newly Diagnosed Classical Hodgkin Lymphoma (KEYNOTE-C11) [NCT05008224]Phase 2146 participants (Actual)Interventional2021-10-07Active, not recruiting
Phase III Study Comparing Rituximab-supplemented ABVD (R-ABVD) With ABVD Followed by Involved-field Radiotherapy (ABVD-RT) in Limited Stage (Stage I-IIA With no Areas of Bulk) Hodgkin's Lymphoma [NCT00992030]Phase 3112 participants (Actual)Interventional2009-09-30Terminated(stopped due to Low recruitment and difficulty in having study data)
A Phase III Trial of Treatment of Advanced-Stage Anaplastic Large Cell Lymphoma (ALCL) With Standard APO (Doxorubicin, Prednisone, Vincristine) Versus Consolidation With a Regimen Including Vinblastine [NCT00059839]Phase 3129 participants (Actual)Interventional2003-11-30Completed
Phase III Randomized, Multi-center Study to Evaluate the Effect of R-mabHDI in Patients With Lymphocytic Predominant Hodgkin's Lymphoma [NCT00816959]Phase 31,200 participants (Anticipated)Interventional2011-07-31Not yet recruiting
A Phase III Randomized Trial of Either M-VAC or Paclitaxel + Carboplatin as Postoperative Adjuvant Therapy in Patients With Muscle-Invasive Transitional Cell Carcinoma of the Bladder at High-Risk for Relapse [NCT00003701]Phase 3490 participants (Anticipated)Interventional1999-04-02Completed
Sequential High Dose MVAC (Methotrexate, Vinblastine, Doxorubicin and Cisplatin), Followed by Gemcitabine Plus Cisplatin in Treating Patients With Locally Advanced or Metastatic Bladder Cancer [NCT00635726]Phase 241 participants (Actual)Interventional2008-02-29Terminated(stopped due to Due to poor accrual)
Genetic Variates of Response to Cisplatin, Vinblastine, and Temozolomide (CVT) in Patients With Metastatic Melanoma [NCT00885534]Phase 27 participants (Actual)Interventional2009-04-30Completed
Randomization of Cytarabine Monotherapy Versus Standard-of-Care Vinblastine/Prednisone for Frontline Treatment of Langerhans Cell Histiocytosis (TXCH LCH0115) [NCT02670707]Phase 3124 participants (Anticipated)Interventional2016-03-07Recruiting
A Randomized Phase 3 Interim Response Adapted Trial Comparing Standard Therapy With Immuno-oncology Therapy for Children and Adults With Newly Diagnosed Stage I and II Classic Hodgkin Lymphoma [NCT05675410]Phase 31,875 participants (Anticipated)Interventional2023-05-11Recruiting
Stanford V Chemotherapy With Low-Dose Tailored-Field Radiation Therapy for Intermediate Risk Pediatric Hodgkin Lymphoma [NCT00352027]Phase 281 participants (Actual)Interventional2006-07-20Completed
Rituximab and Combination Chemotherapy in Treating Patients With Newly Diagnosed Stage II, Stage III, or Stage IV Hodgkin's Lymphoma [NCT00369681]Phase 251 participants (Actual)Interventional2006-05-31Completed
A Phase II Trial of Response-Adapted Therapy of Stage III-IV Hodgkin Lymphoma Using Early Interim FDG-PET Imaging [NCT00822120]Phase 2371 participants (Actual)Interventional2009-07-31Completed
Evaluation of Chemotherapy Influence on Clinical and Biological Markers of Ovarian Reserve. [NCT00712452]19 participants (Actual)Interventional2008-06-30Terminated(stopped due to problems of insuffisant recruitment)
Phase I Trial of AVD Plus Lenalidomide (Revlimid) in Elderly Intermediate or Advanced Stage Hodgkin Lymphoma Patients [NCT01056679]Phase 130 participants (Anticipated)Interventional2010-04-30Completed
A Phase II Open Label, Multicenter, Randomized, Parallel Study Comparing the Efficacy of R-mabHD Alone and a Combination of Adriamycin, Bleomycin, Vinblastine and Dacarbazine (ABVD)in Treating Patients With Hodgkin's Disease. [NCT00797472]Phase 2120 participants (Anticipated)Interventional2011-07-31Not yet recruiting
A Randomized Phase II Study of Rituximab With ABVD Versus Standard ABVD for Patients With Advanced-Stage Classical Hodgkin Lymphoma With Poor Risk Features (IPS Score > 2) [NCT00654732]Phase 258 participants (Actual)Interventional2008-03-19Completed
Multiple Part Clinical Trial of Brentuximab Vedotin in Classical Hodgkin Lymphoma Subjects [NCT03646123]Phase 2255 participants (Actual)Interventional2019-01-28Active, not recruiting
A Pilot Trial of Adriamycin, Pembrolizumab, Vinblastine, and Dacarbazine (APVD) for Patients With Untreated Classical Hodgkin Lymphoma [NCT03331341]Phase 250 participants (Actual)Interventional2019-01-09Active, not recruiting
PD-1 Immune Checkpoint Inhibitors and Immune-Related Adverse Events: a Cohort Study [NCT04115410]4,724 participants (Anticipated)Observational2020-07-01Not yet recruiting
PVAG - Phase I/II Dose Finding Trial in Elderly Patients (> 60 Years) With Advanced Stages Hodgkin's Lymphoma [NCT00147875]Phase 1/Phase 260 participants (Actual)Interventional2004-03-31Completed
An Open-label Study to Assess the Effect of First-line Treatment With Avastin in Combination With Standard Therapy on Progression-free Survival in Patients With Metastatic Renal Cell Cancer. [NCT00520403]Phase 225 participants (Actual)Interventional2007-09-30Completed
A Phase III, Randomized Study of Nivolumab (Opdivo) Plus AVD or Brentuximab Vedotin (Adcetris) Plus AVD in Patients (Age >/= 12 Years) With Newly Diagnosed Advanced Stage Classical Hodgkin Lymphoma [NCT03907488]Phase 3995 participants (Actual)Interventional2019-08-29Active, not recruiting
First International Inter-Group Study for Nodular Lymphocyte-Predominant Hodgkin's Lymphoma in Children and Adolescents [NCT01088750]Phase 4225 participants (Actual)Interventional2009-11-01Completed
A Phase 1 Dose-Escalation Safety Study of Brentuximab Vedotin in Combination With Multi-Agent Chemotherapy as Frontline Therapy in Patients With Hodgkin Lymphoma [NCT01060904]Phase 151 participants (Actual)Interventional2010-01-31Completed
A Phase 2 Study of Vinblastine Sulphate Injection in Children With Recurrent or Refractory Low Grade Glioma [NCT00213278]Phase 250 participants (Actual)Interventional2002-01-31Completed
A Randomized Phase II Study of Co-Expression Extrapolation (COXEN) With Neoadjuvant Chemotherapy for Localized, Muscle-Invasive Bladder Cancer [NCT02177695]Phase 2237 participants (Actual)Interventional2014-08-28Completed
A Phase II Trial of Stanford VI ± Radiation Therapy in Locally Extensive and Advanced Stage Hodgkin's Disease With 3+ Risk Factors: the G6 Study [NCT00225173]Phase 245 participants (Anticipated)Interventional2001-10-31Terminated
A Prospective Phase II Trial of Neoadjuvant Systemic Chemotherapy Followed by Extirpative Surgery for Patients With High Grade Upper Tract Urothelial Carcinoma [NCT02412670]Phase 236 participants (Actual)Interventional2015-08-27Completed
Weekly Vinblastine for Chemotherapy Naive Children With Progressive Low Grade Glioma (PLGGs) [NCT00575796]Phase 250 participants (Anticipated)Interventional2007-10-31Active, not recruiting
Phase II Trial of Response-Adapted Chemotherapy Based on Positron Emission Tomography for Non-Bulky Stage I and II Hodgkin Lymphoma [NCT01132807]Phase 2164 participants (Actual)Interventional2010-05-31Completed
Phase Ib/II Study of the Gamma-Secretase Inhibitor (GSI) RO4929097 in Combination With Cisplatin, Vinblastine, and Temozolomide (CVT) in Patients With Metastatic Melanoma [NCT01196416]Phase 1/Phase 214 participants (Actual)Interventional2010-08-31Completed
Phase 2 Open Label Study of Durvalumab With Neoadjuvant Chemotherapy in Variant Histology Bladder Cancer [NCT03912818]Phase 27 participants (Actual)Interventional2019-04-10Terminated(stopped due to Difficulty with enrollment)
A Phase II Trial of Neoadjuvant Dose-Dense MVAC With Pegfilgrastim Support in Subjects With Muscle-Invasive Urothelial Carcinoma [NCT00808639]Phase 239 participants (Actual)Interventional2008-12-31Completed
Treatment Protocol of the Third International Study For Langerhans Cell Histiocytosis [NCT00276757]376 participants (Anticipated)Interventional2001-04-30Completed
Prophylactic Use of Filgrastim SD/01 In Patients With Hodgkin's Disease Receiving ABVD Chemotherapy [NCT00038558]Phase 325 participants (Actual)Interventional2001-11-30Completed
Phase I Study of Interstitial Colloidal 32P Integrated With External Radiation Therapy and Chemotherapy in the Treatment of Non-Resectable or Medically Inoperable Non-Small Cell Carcinoma of the Lung [NCT00006212]Phase 10 participants Interventional1999-11-30Active, not recruiting
A Phase II, Open-Labeled, Multi-Center, Randomized Controlled Trial of Vinblastine +/- Bevacizumab for the Treatment of Chemotherapy-Naïve Children With Unresectable or Progressive Low Grade Glioma (LGG) [NCT02840409]Phase 2150 participants (Anticipated)Interventional2016-08-31Recruiting
Intensified Methotrexate, Vinblastine, Doxorubicin and Cisplatin +/-Panitumumab as First-line Treatment of Advanced Urothelial Carcinoma in Patients Without Harvey Nor Kirsten Rat Sarcoma Viral Oncogene Homolog Mutations. Phase II Study [NCT02818725]Phase 3133 participants (Actual)Interventional2010-06-30Completed
A Randomized, Open-label, Phase 3 Trial of A+AVD Versus ABVD as Frontline Therapy in Patients With Advanced Classical Hodgkin Lymphoma [NCT01712490]Phase 31,334 participants (Actual)Interventional2012-11-09Active, not recruiting
A Phase II/III Trial of Durvalumab and Chemotherapy for Patients With High Grade Upper Tract Urothelial Cancer Prior to Nephroureterectomy [NCT04628767]Phase 2/Phase 3249 participants (Anticipated)Interventional2021-11-12Recruiting
A Randomized Phase II Study of Prednisone, Vinblastine, Doxorubicin, and Gemcitabine in Patients With Intermediate Stage Hodgkin's Lymphoma [NCT00512980]Phase 20 participants Interventional2008-08-31Terminated(stopped due to lower recruitment rates as expected)
Large Cell Lymphoma, Pilot Study III [NCT00187070]8 participants (Actual)Interventional1997-12-31Completed
Pembrolizumab and aMVAC Chemotherapy as Neoadjuvant Therapy in Non-Urothelial Histology Muscle-Invasive Bladder Cancer: A Pilot Trial [NCT04383743]Phase 217 participants (Anticipated)Interventional2020-11-24Recruiting
PHASE II TRIAL OF THE COMBINATION OF TRANSURETHRAL RESECTION AND NEOADJUVANT CHEMOTHERAPY FOR PATIENTS WITH INVASIVE UROTHELIAL TRACT TUMORS SELECTED BY STAGE AND P53 NUCLEAR EXPRESSION [NCT00002919]Phase 230 participants (Anticipated)Interventional1996-11-30Completed
A Major Randomised Trial to Determine the Value of Cisplatin-Based Chemotherapy For All Patients With Non-Small Cell Lung Cancer [NCT00003240]Phase 31,800 participants (Anticipated)Interventional1995-10-31Active, not recruiting
A Comprehensive Study of Clinically Staged Pediatric Hodgkin's Disease: Chemotherapy for All Patients; Supplementary Low Dose Involved Field Irradiation for Selected Patients (CCG 5942) [NCT00592111]Phase 221 participants (Actual)Interventional1996-03-31Completed
Phase II Clinical Trial Concerning Gene Expression Profiling to Predict the Chemosensitivity of Invasive Bladder Cancer [NCT00516750]Phase 2100 participants (Anticipated)Interventional2007-07-31Terminated(stopped due to Withdrawn due to lack of enrollment.)
Vinblastine/Methotrexate For Severe Progressive Plexiform Neurofibromas: A Phase II Study [NCT00030264]Phase 223 participants (Actual)Interventional2001-02-28Completed
An Open-Label Study of Brentuximab Vedotin + Adriamycin, Vinblastine, and Dacarbazine in Pediatric Patients With Advanced Stage Newly Diagnosed Hodgkin Lymphoma [NCT02979522]Phase 1/Phase 259 participants (Actual)Interventional2017-09-06Completed
A Randomized Phase II Trial of Taxol/VP-16/Estramustine vs. Ketoconazole/Doxorubicin/Vinblastine/Estramustine in Androgen Independent Prostate Cancer [NCT00003084]Phase 275 participants (Actual)Interventional1997-12-31Completed
A Phase II Trial of Sequential SGN-35 Therapy With Adriamycin, Vinblastine, and Dacarbazine (S-AVD) for Older Patients With Untreated Hodgkin Lymphoma [NCT01476410]Phase 248 participants (Actual)Interventional2011-11-30Active, not recruiting
A Randomized Phase III Study of Paclitaxel, Ifosfamide and Cisplatin Versus Vinblastine, Ifosfamide and Cisplatin as Second-Line Therapy for Patients With Relapsed/Resistant Germ Cell Tumors [NCT00072215]Phase 31 participants (Actual)Interventional2004-04-30Terminated(stopped due to poor accrual)
[NCT00265018]Phase 31,370 participants (Actual)Interventional1998-05-31Completed
Hodgkin's Disease Study [NCT00416377]353 participants (Anticipated)InterventionalActive, not recruiting
Phase II Trial of Doxorubicin, Vinblastine, and Gemcitabine (AVG) Chemotherapy for Non-Bulky Stage I and II Hodgkin's Lymphoma [NCT00086801]Phase 2104 participants (Actual)Interventional2004-05-31Completed
A Phase I Study of Vinblastine in Combination With Carboplatin for Children With Newly Diagnosed and Recurrent Low-Grade Gliomas [NCT00352495]Phase 126 participants (Actual)Interventional2006-06-30Completed
Phase I Evaluation of Sodium Stibogluconate in Combination With Interferon α-2b Followed by Cisplatin, Vinblastine and Dacarbazine for Patients With Melanoma or Malignancies Potentially Responsive to SSG and/or Interferons [NCT00498979]Phase 122 participants (Actual)Interventional2007-05-31Completed
A Phase II Study of Rituximab + ABVD for Patients With Hodgkin's Disease [NCT00504504]Phase 285 participants (Actual)Interventional2001-03-31Completed
A Phase II Clinical Trial Using Metronomic Oral Low-dose Cyclophosphamide Alternating With Low-dose Oral Methotrexate With Continuous Celecoxib and Weekly Vinblastine in Children and Adolescents With Relapsed or Progressing Solid Tumours. [NCT01285817]Phase 279 participants (Actual)Interventional2011-01-12Completed
A Phase II Study of a-Interferon With Adriamycin, Bleomycin, Velban, and Dacarbazine (ABVD) for Patients With Hodgkin's Disease [NCT01404936]Phase 235 participants (Actual)Interventional1996-07-31Completed
Vinblastine and Methotrexate in Children With Multivessel Pulmonary Vein Stenosis-A Phase II Study [NCT00215046]Phase 228 participants (Actual)Interventional2000-03-31Completed
Phase I-II Study of Vinblastine in Combination With Nilotinib in Children, Adolescents, and Young Adults With Refractory or Recurrent Low-Grade Glioma [NCT01887522]Phase 2144 participants (Actual)Interventional2016-07-06Terminated(stopped due to the results of the interim analysis are clear with a significant advantage in terms of PFS in favor of the control arm (Vinblastine alone) over the investigational arm (Vinblastine + Nilotinib).)
A PHASE II TRIAL OF EIGHT-WEEK STANFORD V CHEMOTHERAPY PLUS MODIFIED INVOLVED FIELD RADIOTHERAPY IN FAVORABLE, LIMITED STAGE HODGKIN'S DISEASE [NCT00002714]Phase 20 participants Interventional1995-04-30Completed
Randomized Phase III Trial Comparing Immediate Versus Deferred Chemotherapy After Radical Cystectomy in Patients With pT3-pT4, and/or N+M0 Transitional Cell Carcinoma (TCC) of the Bladder [NCT00028756]Phase 3285 participants (Actual)Interventional2001-10-31Completed
Randomized Phase II/III Study Assessing Gemcitabine/Carboplatin And Methotrexate/Carboplatin/Vinblastine In Previously Untreated Patients With Advanced Urothelial Cancer Ineligible For Cisplatin Based Chemotherapy [NCT00014274]Phase 2/Phase 3238 participants (Actual)Interventional2001-01-31Completed
Randomized Trial of Surgical Resection With or Without Pre-Operative Chemotherapy in Patients With Operable Non-Small Cell Lung Cancer (NSCLC) of Any Stage [NCT00003159]Phase 3600 participants (Anticipated)Interventional1997-08-31Completed
Pilot Study for Therapy Optimising for Hodgkin's Lymphoma in Childhood and Adolescence; Optimising Therapy for Boys With Hodgkin's Lymphoma in Intermediate and Advanced Stages. Safety and Efficacy Study for Drug Combination VECOPA [NCT00398554]Phase 216 participants (Actual)Interventional2005-06-30Completed
A Phase II Study VEPEMB In Patients With Hodgkin's Lymphoma Aged ≥ 60 Years; Vinblastine, Cyclophosphamide, Procarbazine, Prednisolone, Etoposide, Mitoxantrone, and Bleomycin in Treating Older Patients With Hodgkin's Lymphoma [NCT00079105]Phase 2175 participants (Actual)Interventional2004-01-31Completed
Positron Emission Tomography Pre- and Post-treatment Assessment For Locally Advanced Non-Small Cell Lung Carcinoma [NCT00083083]Phase 2250 participants (Anticipated)Interventional2005-03-31Active, not recruiting
Protocol for the Treatment of Extracranial Germ Cell Tumours in Children and Adolescents (GC III) [NCT00274950]Phase 3105 participants (Anticipated)Interventional2005-05-31Active, not recruiting
Randomized Feasibility Study Of Active Symptom Control With Or Without Chemotherapy In The Treatment Of Patients With Mesothelioma [NCT00030459]Phase 20 participants Interventional2000-11-30Active, not recruiting
A Phase III Randomized Study of Patients With High Risk, Hormone-Naive Prostate Cancer: Androgen Blockade With 4 Cycles of Immediate Chemotherapy Versus Androgen Blockade With Delayed Chemotherapy [NCT00030654]Phase 321 participants (Actual)Interventional2002-10-31Completed
Protocol For The Treatment Of Children And Adolescents With Hodgkin's Disease [NCT00025064]Phase 2260 participants (Anticipated)Interventional2000-01-31Active, not recruiting
Protocol for a Randomized Phase III Study of the Stanford V Regimen, Compared With ABVD for the Treatment of Advanced Hodgkin's Disease [NCT00041210]Phase 3850 participants (Anticipated)Interventional2001-10-31Active, not recruiting
Pilot Study I for Treatment of Cancer in Children With Ataxia-Telangiectasia [NCT00187057]6 participants (Actual)Interventional2002-09-30Completed
A Phase II Clinical Trial of Neoadjuvant Chemotherapy With M-VAC Plus Avastin in Patients With Locally Advanced Urothelial Cancer [NCT00506155]Phase 260 participants (Actual)Interventional2007-06-30Completed
Durvalumab and Standard Chemotherapy for the Treatment of Lymph Node Positive Bladder Cancer [NCT05137262]Phase 260 participants (Anticipated)Interventional2021-10-13Recruiting
[NCT00264953]Phase 31,395 participants (Actual)Interventional1998-05-31Completed
Hodgkins Disease Study [NCT00417014]358 participants (Anticipated)InterventionalActive, not recruiting
"Prospective Non Randomized Study With Chemotherapy in Patients With Hodgkin's Disease and HIV Infection: Stanford V Regimen For Low Risk Patients, EBVP Regimen For High Risk Patients" [NCT00003262]Phase 230 participants (Anticipated)Interventional1997-05-31Active, not recruiting
A Phase II Multi-Center Open-Label Trial of Six Doses of Pembrolizumab Monotherapy Prior to Limited Chemotherapy as Front-Line Therapy for Patients With Classical Hodgkin Lymphoma, Including Elderly Patients. [NCT06164275]Phase 230 participants (Anticipated)Interventional2023-12-31Not yet recruiting
Randomized Phase II Trial Of Adjuvant Chemotherapy For Urothelial Carcinoma Comparing GC To Dose-Dense MVAC [NCT01639521]Phase 20 participants (Actual)Interventional2013-05-31Withdrawn(stopped due to Lack of funding)
Randomized Phase III Study of Gemcitabine/Cisplatine (GC) Versus High-dose Intensity Methotrexate, Vinblastine, Doxorubicine and Cisplatin (HD-MVAC) in the Perioperative Setting for Patients With Locally Advanced Transitional Cell Cancer of the Bladder [NCT01812369]Phase 3500 participants (Actual)Interventional2013-02-28Active, not recruiting
A Phase II Study of Therapy for Pediatric Relapsed or Refractory Precursor B-Cell Acute Lymphoblastic Leukemia and Lymphoma [NCT01700946]Phase 280 participants (Actual)Interventional2013-04-15Completed
A Phase II Pilot Study of Short Term (12 Week) Combination Chemotherapy (Stanford V) in Unfavorable Hodgkin's Disease [NCT00002715]Phase 250 participants (Anticipated)Interventional1989-04-30Completed
Phase III Trial of Methotrexate, Vinblastine, Doxorubicin and Cisplatin vs Carboplatin and Paclitaxel in Advanced Carcinoma of the Urothelium [NCT00003376]Phase 3330 participants (Anticipated)Interventional1998-12-03Completed
A Phase II Trial of PET-Directed Therapy Using AVD (Doxorubicin, Vinblastine, and Dacarbazine) Plus Brentuximab Vedotin Induction Chemotherapy, With or Without Brentuximab Vedotin Plus Nivolumab, Followed by Nivolumab Consolidation for Patients With Previ [NCT03233347]Phase 282 participants (Anticipated)Interventional2017-10-13Active, not recruiting
A Prospective Multicenter Study on HIV-associated Hodgkin Lymphoma [NCT01468740]Phase 2130 participants (Anticipated)Interventional2004-03-31Recruiting
A Phase I Study of Continuous Intravenous Infusion of PSC 833 and Vinblastine in Patients With Metastatic Renal Cancer [NCT00001570]Phase 146 participants Interventional1997-02-28Completed
INTERNATIONAL RANDOMIZED STUDY FOR THE SALVAGE TREATMENT OF GERM CELL TUMOURS [NCT00002566]Phase 3280 participants (Anticipated)Interventional1994-02-28Completed
A Feasibility Study of Thorough Transurethral Resection (TURB) and Escalated Dose M-VAC Chemotherapy as Primary Treatment of T2-T3a, N0-Nx, M0 Transitional Cell Carcinoma of the Bladder, With the Intention of Bladder Preservation [NCT00003640]Phase 273 participants (Anticipated)Interventional1998-09-30Terminated(stopped due to low accrual)
A Randomized Phase III Trial to Assess Response Adapted Therapy Using FDG-PET Imaging in Patients With Newly Diagnosed, Advanced Hodgkin Lymphoma [NCT00678327]Phase 31,202 participants (Actual)Interventional2008-08-29Active, not recruiting
Risk-Adapted Therapy for Young Children With Embryonal Brain Tumors, Choroid Plexus Carcinoma, High Grade Glioma or Ependymoma [NCT00602667]Phase 2293 participants (Actual)Interventional2007-12-17Active, not recruiting
Brentuximab Vedotin Associated With Chemotherapy in Untreated Patients With Stage I/II Unfavourable Hodgkin Lymphoma. A Randomized Phase II LYSA-FIL-EORTC Intergroup Study [NCT02292979]Phase 2170 participants (Actual)Interventional2015-03-31Completed
Metronomic Therapy in Patients With Metastatic Melanoma: A Phase II Study of Low Dose Vinblastine, Cyclophosphamide, and Dacarbazine [NCT01542255]Phase 27 participants (Actual)Interventional2010-06-30Terminated(stopped due to Low accrual not allowing to support statistical endpoints)
A Prospective Phase II Study of Bendamustine in Patients Aged Over 60 Years With Classical Hodgkin Lymphoma Treated by Prednisone, Vinblastine and Doxorubicin [NCT02414568]Phase 290 participants (Actual)Interventional2015-07-17Completed
A Study of Therapy for Pediatric Relapsed or Refractory Acute Lymphoblastic Leukemia [NCT00186875]Phase 247 participants (Actual)Interventional2003-11-30Completed
Randomized Phase II Study Assessing the Combination of Vinflunine With Gemcitabine and Vinflunine With Carboplatin in Patients Ineligible to Cisplatin With Advanced or Metastatic Transitional Cell Carcinoma of the Urothelium [NCT01599013]Phase 269 participants (Actual)Interventional2011-02-28Completed
A Phase II Trial of Risk Enabled Therapy After Initiating Neoadjuvant Chemotherapy for Bladder Cancer (RETAIN BLADDER) [NCT02710734]Phase 278 participants (Actual)Interventional2016-02-24Active, not recruiting
Treatment Protocol for Relapsed Anaplastic Large Cell Lymphoma of Childhood and Adolescence [NCT00317408]96 participants (Anticipated)Interventional2004-04-30Active, not recruiting
Phase II Study of Filgrastim (G-CSF) Plus ABVD in the Treatment of HIV-Associated Hodgkin's Disease [NCT00000626]Phase 227 participants InterventionalCompleted
Adjuvant Therapy for Melanoma Patients With Regional Lymph Node Metastases With Interferon Alfa-2B vs. Biochemotherapy Using Cisplatin + Vinblastine + DTIC + Interferon Plus IL-2 [NCT00002882]Phase 3140 participants (Actual)Interventional1995-11-30Completed
Pilot Study for the Treatment of Children With Newly Diagnosed Advanced Stage Hodgkin's Disease: Upfront Dose Intensive Chemotherapy [NCT00004010]Phase 299 participants (Actual)Interventional1999-10-31Completed
A Randomized Phase III Trial Comparing Early High Dose Chemotherapy and an Autologous Stem Cell Transplant to Conventional Dose ABVD Chemotherapy for Patients With Advanced Stage Poor Prognosis Hodgkin's Disease as Defined by the International Prognostic [NCT00005090]Phase 311 participants (Actual)Interventional2000-04-30Terminated(stopped due to poor accrual)
A UKLG Randomised Trial of Initial Chemotherapy for Advanced Stage Hodgkins Disease [NCT00003421]Phase 3800 participants (Anticipated)Interventional1998-06-30Completed
Vinblastine and Methotrexate in Children With Desmoid Tumor (Aggressive Fibromatosis) Which is Recurrent or Not Amenable to Surgical Resection or Irradiation - A Pediatric Oncology Group Phase II Study [NCT00003019]Phase 228 participants (Actual)Interventional1997-08-31Completed
PHASE I TRIAL OF HYDROXYUREA FOR SALVAGE OF INCURABLE NON-SMALL CELL LUNG CANCER [NCT00002887]Phase 130 participants (Anticipated)Interventional1995-07-31Active, not recruiting
A Phase II Study Using Low Dose Subcutaneous IL-2, Vinblastine and GM-CSF in the Treatment of Metastatic Renal Cell Carcinoma [NCT00003181]Phase 235 participants (Anticipated)Interventional1997-05-31Active, not recruiting
Randomized Trial of Subtotal Nodal Irradiation Versus Doxorubicin, Vinblastine and Subtotal Nodal Irradiation for Stage I-IIA Hodgkin's Disease [NCT00002495]Phase 3348 participants (Actual)Interventional1992-09-30Completed
A Phase III Study of Radiotherapy or ABVD Plus Radiotherapy Versus ABVD Alone in the Treatment of Early Stage Hodgkin's Disease [NCT00002561]Phase 3405 participants (Actual)Interventional1994-01-25Completed
A Randomized and Controlled Phase II National Protocol in Non NF1 Pediatric and AYA (Adolescent and Young Adults) Patients Bearing a Wild Type BRAF Gene Newly Diagnosed Comparing a Daily Oral MEK Inhibitor (Trametinib) Versus Weekly Vinblastine During 18 [NCT05180825]Phase 2134 participants (Anticipated)Interventional2022-05-05Recruiting
Phase II Trial of Response-Adapted Therapy Based on Positron Emission Tomography (PET) for Bulky Stage I and II Classical Hodgkin Lymphoma (HL) [NCT01390584]Phase 26 participants (Actual)Interventional2013-05-24Terminated(stopped due to slow accrual)
A Randomized Phase III Trial of ABVD Versus Stanford V (+/-) Radiation Therapy in Locally Extensive and Advanced Stage Hodgkin's Disease [NCT00003389]Phase 3854 participants (Actual)Interventional1999-06-17Completed
A LARGE-SCALE TRIAL EVALUATING ADJUVANT CHEMOTHERAPY AFTER CURATIVE RESECTION OF NON-SMALL CELL LUNG CANCER [NCT00002823]Phase 33,300 participants (Anticipated)Interventional1995-02-28Completed
A Randomized Phase III Comparative Study of Paclitaxel With Carboplatin Versus Mitomycin, Ifosfamide, Cisplatin (MIC) Chemotherapy in Inoperable Advanced Stage Non-Small Cell Lung Cancer [NCT00004887]Phase 30 participants Interventional1999-01-31Active, not recruiting
A Randomized Study of MVP 3 Versus 6 Cycles in Advanced Non-Small Cell Lung Cancer [NCT00004209]Phase 30 participants Interventional1998-05-31Active, not recruiting
Protocol H8 for a Prospective Controlled Trial in Clinical Stage I-II Supradiaphragmatic Hodgkin's Disease. Evaluation of Treatment Efficacy and (Long Term) Toxicity in Three Different Prognostic Subgroups [H8 Trial] [NCT00379041]Phase 31,158 participants (Anticipated)Interventional1993-09-01Active, not recruiting
A Randomized Phase III Trial of Concurrent Biochemotherapy With Cisplatin, Vinblastine, Dacarbazine, IL-2 and Interferon A-2B Versus Cisplatin, Vinblastine, Dacarbazine Alone in Patients With Metastatic Malignant Melanoma [NCT00003027]Phase 3482 participants (Anticipated)Interventional1997-11-13Completed
Biochemotherapy With Temozolomide, Velban, Cisplatin, Interleukin-2, Interferon-alpha and Thalidomide for Metastatic Melanoma With Optional Intrathecal Interleukin-2 Treatment [NCT00505635]Phase 25 participants (Actual)Interventional2007-03-31Terminated(stopped due to Slow accrual)
Vinblastine Versus Oral Hydroxiurea in Newly Diagnosed AML With Hyperleukocytosis: a Phase 2 Clinical Study [NCT05062278]Phase 246 participants (Anticipated)Interventional2021-07-26Recruiting
Phase II Trial of Neoadjuvant Dose Dense MVAC in Muscle Invasive Bladder Cancer and High Risk Urothelial Carcinoma of the Upper Urinary Tract [NCT01031420]Phase 254 participants (Actual)Interventional2009-12-07Completed
PAZOPANIB Efficacy and Tolerance in Desmoids Tumors : Phase 2 Clinical Trial [NCT01876082]Phase 272 participants (Actual)Interventional2012-09-18Completed
Metro-PD1: a Phase I/II Trial Evaluating Anti-PD1 (Nivolumab) in Combination With Metronomic Chemotherapy in Children and Teenagers With Refractory / Relapsing Solid Tumors [NCT03585465]Phase 1/Phase 2102 participants (Anticipated)Interventional2019-03-26Recruiting
Pediatric Classical Hodgkin Lymphoma Consortium Study: cHOD17 [NCT03755804]Phase 2250 participants (Anticipated)Interventional2018-12-12Recruiting
PHASE I-II STUDY OF VINBLASTINE IN COMBINATION WITH NILOTINIB IN CHILDREN, ADOLESCENTS, AND YOUNG ADULTS WITH REFRACTORY OR RECURRENT LOW-GRADE GLIOMA [NCT01884922]Phase 135 participants (Actual)Interventional2013-05-29Completed
Very Early PET-response Adapted Targeted Therapy for Advanced Hodgkin Lymphoma: a Single -Arm Phase II Study [NCT03517137]Phase 2150 participants (Actual)Interventional2019-08-01Active, not recruiting
BEACOPP (4 Cycles Escalated + 4 Cycles Baseline) Versus ABVD (8 Cycles) In Stage III & IV Hodgkin's Lymphoma [NCT00049595]Phase 3552 participants (Actual)Interventional2002-08-31Completed
A Phase II Randomized Window of Opportunity Trial Evaluating Clinical and Biological Effects of Intratumoral INT230-6 in Early Stage Breast Cancer: The INVINCIBLE Trial [NCT04781725]Phase 290 participants (Anticipated)Interventional2021-03-25Recruiting
An Open-label, Uncontrolled, Multicenter Phase II Trial of MK-3475 (Pembrolizumab) in Children and Young Adults With Newly Diagnosed Classical Hodgkin Lymphoma With Inadequate (Slow Early) Response to Frontline Chemotherapy (KEYNOTE 667) [NCT03407144]Phase 2340 participants (Anticipated)Interventional2018-04-09Active, not recruiting
A Phase 3 Trial of Androgen Ablation Alone vs. Chemo/Hormonal Therapy as Initial Treatment of Unresectable/Metastatic Adenocarcinoma of the Prostate [NCT00002855]Phase 3306 participants (Actual)Interventional1996-08-31Completed
A Randomized Phase III Study of Chemotherapy and Radiotherapy Versus Radiotherapy Alone as Adjuvant Treatment to Patients With Node Positive Stages IB or IIA Cervix Cancer [NCT00003209]Phase 3700 participants (Anticipated)Interventional1997-12-31Completed
A Phase 3 Study of Selumetinib (NSC# 748727) or Selumetinib in Combination With Vinblastine for Non-NF1, Non-TSC Patients With Recurrent or Progressive Low-Grade Gliomas (LGGs) Lacking BRAFV600E or IDH1 Mutations [NCT04576117]Phase 3300 participants (Anticipated)Interventional2021-02-16Suspended(stopped due to Other - pending eval of pts currently enrolled)
A Phase 2 Front-Line PET/CT-2 Response-Adapted Brentuximab Vedotin and Nivolumab Incorporated and Radiation-Free Management of Early Stage Classical Hodgkin Lymphoma (cHL) [NCT03712202]Phase 2155 participants (Actual)Interventional2018-11-28Active, not recruiting
International Protocol for the Treatment of Childhood Anaplastic Large Cell Lymphoma [NCT00006455]Phase 3885 participants (Actual)Interventional1999-11-26Completed
Fitness-adapted, Pembrolizumab-based Therapy for Untreated Classical Hodgkin Lymphoma Patients 60 Years of Age and Above (cHL 001) [NCT05404945]Phase 244 participants (Anticipated)Interventional2022-07-26Recruiting
Phase II Study of PET-Directed Frontline Therapy With Pembrolizumab and AVD for Patients With Classical Hodgkin Lymphoma [NCT03226249]Phase 230 participants (Actual)Interventional2017-11-09Active, not recruiting
PERSONALIZED MEDICINE GROUP / UCBG UC-0105/1304: SAFIR02_Breast - Evaluation of the Efficacy of High Throughput Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer [NCT02299999]Phase 21,460 participants (Actual)Interventional2014-04-07Active, not recruiting
A Pilot Study of Low-Dose Antiangiogenic Chemotherapy in Combination With Standard Multiagent Chemotherapy for Patients With Newly Diagnosed Metastatic Ewing Sarcoma Family of Tumors [NCT00061893]Phase 238 participants (Actual)Interventional2004-04-30Completed
Phase I/II of Nivolumab and A(B)VD in the Front-line Setting for High Risk Hodgkin Lymphoma [NCT03033914]Phase 1/Phase 281 participants (Anticipated)Interventional2017-01-25Recruiting
Brentuximab Vedotin Plus AVD in Non-bulky Limited Stage Hodgkin Lymphoma [NCT01534078]Phase 234 participants (Actual)Interventional2012-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00003389 (3) [back to overview]5-year Overall Survival
NCT00003389 (3) [back to overview]Incidence of Second Cancers
NCT00003389 (3) [back to overview]Failure-free Survival at 5 Years
NCT00005047 (4) [back to overview]Probability of Overall Survival
NCT00005047 (4) [back to overview]Probability of Overall Survival
NCT00005047 (4) [back to overview]Probability of Recurrence
NCT00005047 (4) [back to overview]Probability of Recurring
NCT00006237 (3) [back to overview]5-year Overall Survival
NCT00006237 (3) [back to overview]5-year Relapse-Free Survival
NCT00006237 (3) [back to overview]Toxicity
NCT00024167 (2) [back to overview]Overall Survival From Randomization
NCT00024167 (2) [back to overview]Overall Survival From Registration
NCT00026208 (7) [back to overview]Early Treatment-related Toxicity
NCT00026208 (7) [back to overview]Frequency of Complete Response
NCT00026208 (7) [back to overview]Overall Survival (OS)
NCT00026208 (7) [back to overview]Progression-free Survival (PFS)
NCT00026208 (7) [back to overview]Second Hodgkin's Disease Progression
NCT00026208 (7) [back to overview]Late Treatment-related Toxicity
NCT00026208 (7) [back to overview]Survival at 5 and 10 Years
NCT00030264 (1) [back to overview]Time to Disease Progression
NCT00059839 (1) [back to overview]Event-free Survival (EFS)
NCT00061893 (2) [back to overview]Occurrence of Severe Toxicity
NCT00061893 (2) [back to overview]Event Free Survival
NCT00186875 (4) [back to overview]Overall Survival (OS)
NCT00186875 (4) [back to overview]Response Rate
NCT00186875 (4) [back to overview]Minimal Residual Disease (MRD) Compared With Historical Data From TOTXV Protocol (NCT00137111)
NCT00186875 (4) [back to overview]Minimal Residual Disease (MRD) Compared With Historical Data From TOTXV Protocol (NCT00137111)
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.4.0: School Functioning
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.4.0: Total Score
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.4.0:Social Functioning
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), Symptom Distress Scale
NCT00352027 (76) [back to overview]Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: (Echocardiogram)
NCT00352027 (76) [back to overview]Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: (Electrocardiogram)
NCT00352027 (76) [back to overview]Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: (Pulmonary Function)
NCT00352027 (76) [back to overview]Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: Thyroid (TSH)
NCT00352027 (76) [back to overview]Local and Distant Failure for Children Treated With Tailored-field Radiation
NCT00352027 (76) [back to overview]Prognostic Factors for Treatment Failure: Gender
NCT00352027 (76) [back to overview]Prognostic Factors for Treatment Failure: Histology
NCT00352027 (76) [back to overview]Prognostic Factors for Treatment Failure: Stage
NCT00352027 (76) [back to overview]Toxicities With Grade >1
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Pain and Hurt
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Perceived Physical Appearance
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Procedural Anxiety
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Total Score
NCT00352027 (76) [back to overview]Prognostic Factors for Treatment Failure: Age
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Treatment Anxiety
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Worry
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.4.0: Emotional Functioning
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQl v.4.0: Physical Functioning
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Communication
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Pain and Hurt
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.4.0: Psychosocial Health
NCT00352027 (76) [back to overview]3-year Event-free Survival (EFS) Probability
NCT00352027 (76) [back to overview]3-year Event-Free Survival Probability
NCT00352027 (76) [back to overview]3-year Local Failure-free Survival Probability
NCT00352027 (76) [back to overview]3-year Overall Survival (OS) Probability
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Cognitive Problems
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Cognitive Problems
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Nausea
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Pain and Hurt
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Perceived Physical Appearance
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Procedural Anxiety
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Total Score
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Treatment Anxiety
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Worry
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Emotional Functioning
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Physical Functioning
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Psychosocial Health
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: School Functioning
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Social Functioning
NCT00352027 (76) [back to overview]Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Total Score
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Communication
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Nausea
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Pain and Hurt
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Perceived Physical Appearance
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Procedural Anxiety
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Total Score
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Treatment Anxiety
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Worry
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Emotional Functioning
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Physical Functioning
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Psychosocial Health
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: School Functioning
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Social Functioning
NCT00352027 (76) [back to overview]Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Total Score
NCT00352027 (76) [back to overview]Disease Failure Rate Within Radiation Fields
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Cognitive Problems
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Communication
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Nausea
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Perceived Physical Appearance
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Procedural Anxiety
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Total Score
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Treatment Anxiety
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Worry
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Emotional Functioning
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Physical Functioning
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Psychosocial Health
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.4.0: School Functioning
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Social Functioning
NCT00352027 (76) [back to overview]Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Total Score
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Cognitive Problems
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Communication
NCT00352027 (76) [back to overview]Patient Quality of Life (QoL), PedsQL v.3.0: Nausea
NCT00369681 (3) [back to overview]Effect of Rituximab on EBV(+) Tumors
NCT00369681 (3) [back to overview]Event-free Survival
NCT00369681 (3) [back to overview]Relationship Between Marker Detection and Clinical Outcome
NCT00504504 (1) [back to overview]5-year Failure-free Survival Rate for Participants With Hodgkin's Disease Given Rituximab With ABVD
NCT00505635 (1) [back to overview]Time to Progression (TTP)
NCT00506155 (2) [back to overview]Percentage of Participants With Response Defined as the Absence of Residual Muscle Invasive Cancer in Resected Specimen
NCT00506155 (2) [back to overview]5-year Overall Survival (OS)
NCT00520403 (4) [back to overview]Overall Survival (OS)
NCT00520403 (4) [back to overview]Percentage of Participants With Disease Progression or Death
NCT00520403 (4) [back to overview]PFS - Time to Event
NCT00520403 (4) [back to overview]Percentage of Participants With Objective Response (OR)
NCT00602667 (62) [back to overview]Concentration of Cerebrospinal Fluid Neurotransmitters
NCT00602667 (62) [back to overview]Number and Type of Genetic Polymorphisms
NCT00602667 (62) [back to overview]Number of Participants With Chromosomal Abnormalities
NCT00602667 (62) [back to overview]Number of Successful Collections for Frozen and Fixed Tumor Samples
NCT00602667 (62) [back to overview]Numbers of Patients With Gene Alterations
NCT00602667 (62) [back to overview]Numbers of Patients With Molecular Abnormalities by Tumor Type
NCT00602667 (62) [back to overview]Pharmacogenetic Variation on Central Nervous System Transmitters
NCT00602667 (62) [back to overview]Percent Probability of Event-free Survival (EFS) for Medulloblastoma Patients
NCT00602667 (62) [back to overview]4-OH Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]4-OH Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]4-OH Cyclophosphamide AUC0-24h in Induction Chemotherapy
NCT00602667 (62) [back to overview]4-OH Cyclophosphamide AUC0-24h in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]CEPM AUC0-24h in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]CEPM AUC0-24h in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]CEPM AUC0-24h in Induction Chemotherapy
NCT00602667 (62) [back to overview]CEPM AUC0-24h in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]Cyclophosphamide Apparent Oral Clearance in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]Cyclophosphamide AUC0-24h in Induction Chemotherapy
NCT00602667 (62) [back to overview]Cyclophosphamide AUC0-24h in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]Cyclophosphamide Clearance in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]Cyclophosphamide Clearance in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]Cyclophosphamide Clearance in Induction Chemotherapy
NCT00602667 (62) [back to overview]Erlotinib Apparent Oral Clearance
NCT00602667 (62) [back to overview]Erlotinib Apparent Volume of Central Compartment
NCT00602667 (62) [back to overview]Erlotinib AUC0-24h
NCT00602667 (62) [back to overview]Event-free Survival (EFS) Compared to Historical Controls
NCT00602667 (62) [back to overview]Feasibility and Toxicity of Administering Consolidation Therapy Including Cyclophosphamide and Pharmacokinetically Targeted Topotecan to Patients With Metastatic Disease Based on the Percentage of Courses Delayed for More Than 7 Days Due to Toxicity
NCT00602667 (62) [back to overview]Feasibility and Toxicity of Administering Oral Maintenance Therapy in Children <3 Years of Age as Measured by the Percentage of Total Scheduled Maintenance Doses Received
NCT00602667 (62) [back to overview]Feasibility and Toxicity of Administering Vinblastine With Induction Chemotherapy for Patients With Metastatic Disease as Measured by the Percentage of Courses Delayed for More Than 7 Days Due to Toxicity
NCT00602667 (62) [back to overview]Methotrexate AUC0-66h in Induction Cycle 1
NCT00602667 (62) [back to overview]Methotrexate AUC0-66h in Induction Cycle 2
NCT00602667 (62) [back to overview]Methotrexate AUC0-66h in Induction Cycle 3
NCT00602667 (62) [back to overview]Methotrexate AUC0-66h in Induction Cycle 4
NCT00602667 (62) [back to overview]Methotrexate Clearance in Induction Cycle 1
NCT00602667 (62) [back to overview]Methotrexate Clearance in Induction Cycle 2
NCT00602667 (62) [back to overview]Methotrexate Clearance in Induction Cycle 3
NCT00602667 (62) [back to overview]Methotrexate Clearance in Induction Cycle 4
NCT00602667 (62) [back to overview]Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 1
NCT00602667 (62) [back to overview]Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 2
NCT00602667 (62) [back to overview]Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 3
NCT00602667 (62) [back to overview]Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 4
NCT00602667 (62) [back to overview]Methotrexate Volume of Central Compartment in Induction Cycle 1
NCT00602667 (62) [back to overview]Methotrexate Volume of Central Compartment in Induction Cycle 2
NCT00602667 (62) [back to overview]Methotrexate Volume of Central Compartment in Induction Cycle 3
NCT00602667 (62) [back to overview]Methotrexate Volume of Central Compartment in Induction Cycle 4
NCT00602667 (62) [back to overview]OSI-420 AUC0-24h
NCT00602667 (62) [back to overview]Overall Survival (OS) Compared to Historical Controls
NCT00602667 (62) [back to overview]Participants With Empirical Dosage Achieving Target System Exposure of Intravenous Topotecan
NCT00602667 (62) [back to overview]Participants With PK-guided Dosage Adjustment Achieving Target System Exposure of Intravenous Topotecan
NCT00602667 (62) [back to overview]Percent of Patients With Sustained Objective Responses Rate After Consolidation
NCT00602667 (62) [back to overview]Percent of PET Scans With Loss of Signal Intensity
NCT00602667 (62) [back to overview]Percent Probability of Progression-free Survival (PFS) for Medulloblastoma Patients
NCT00602667 (62) [back to overview]Percent Probability of Progression-free Survival (PFS) for Medulloblastoma Patients by DNA Methylation Subgroup
NCT00602667 (62) [back to overview]Percentage of Patients With Objective Responses Rate to Induction Chemotherapy
NCT00602667 (62) [back to overview]Rate of Distant Disease Progression
NCT00602667 (62) [back to overview]Rate of Local Disease Progression
NCT00602667 (62) [back to overview]Topotecan Apparent Oral Clearance in Maintenance Chemotherapy
NCT00602667 (62) [back to overview]Topotecan AUC0-24h in Consolidation Chemotherapy
NCT00602667 (62) [back to overview]Topotecan AUC0-24h in Maintenance Chemotherapy
NCT00602667 (62) [back to overview]Topotecan Clearance in Consolidation Chemotherapy
NCT00654732 (1) [back to overview]Event-free Survival (EFS) Rate
NCT00808639 (3) [back to overview]Number of Patients Experiencing Surgery-related Toxicity
NCT00808639 (3) [back to overview]Number of Patients Achieving Pathologic Response
NCT00808639 (3) [back to overview]Number of Patients Experiencing Febrile Neutropenia
NCT00822120 (8) [back to overview]Percentage of HIV-positive Patients With 2-year Progression-free Survival (PFS) Treated With Initial 2 Cycles of Adriamycin, Bleomycin, Vnblastine, and Dacarbazine (ABVD) Followed by Response-adapted Therapy Based on Interim FDG-PET Imaging.
NCT00822120 (8) [back to overview]Percentage of HIV-positive Patients With 5-year Overall Survival (OS) Treated With 2 Initial Cycles of ABVD Followed by Response-Adapted Therapy Based on Interim FDG-PET Imaging.
NCT00822120 (8) [back to overview]Number of HIV-negative Patients With Grade 3 Through Grade 5 Adverse Events That Are Related to Study Drug
NCT00822120 (8) [back to overview]Number of HIV-positive Patients With Grade 3 Through Grade 5 Adverse Events That Are Related to Study Drug
NCT00822120 (8) [back to overview]Percentage of HIV-negative Patients Who Are PET-positive After 2 Cycles of ABVD With 2-year PFS
NCT00822120 (8) [back to overview]Complete and Partial Response Rates for HIV-negative Patients Treated With Response- Adapted Therapy Based on FDG-PET Imaging After 2 Cycles of ABVD
NCT00822120 (8) [back to overview]Percentage of HIV-negative Patients With 2-year Overall Survival (OS) Treated With 2 Initial Cycles of ABVD Followed by Response-Adapted Therapy Based on Interim FDG-PET Imaging
NCT00822120 (8) [back to overview]Percentage of HIV-negative Patients With 2-year Progression-free Survival (PFS) Treated With 2 Initial Cycles of Adriamycin, Bleomycin, Vnblastine, and Dacarbazine (ABVD) Followed by Response-adapted Therapy Based on Interim FDG-PET Imaging.
NCT00885534 (1) [back to overview]Overall Response to CVT Chemotherapy.
NCT01031420 (2) [back to overview]Toxicity Profile of Dose Dense MVAC Given in the Neoadjuvant Setting.
NCT01031420 (2) [back to overview]Percentage of Participants With Complete Response at Cystectomy or Ureterectomy Following Preoperative Dose Dense MVAC
NCT01132807 (3) [back to overview]Complete Response Rate
NCT01132807 (3) [back to overview]Progression-Free Survival (PFS) at 36-Months for Patients Who Received 4 Cycles of ABVD
NCT01132807 (3) [back to overview]36 Month Progression Free Survival Rate of Patients Receiving 4 Cycles of ABVD Versus Patients Receiving 2 Cycles of ABVD and 2 Cycles of BEACOPP and Radiation.
NCT01196416 (9) [back to overview]Cycle 1 AUC/Pharmacokinetics of Gamma-secretase Inhibitor RO4929097 in Combination With Temozolomide (Phase IB)
NCT01196416 (9) [back to overview]Maximum-tolerated Dose for Cisplatin, Vinblastine and TMZ
NCT01196416 (9) [back to overview]Progression-free Survival (Phase II)
NCT01196416 (9) [back to overview]Cycle 1 C Max/Pharmacokinetics of Gamma-secretase Inhibitor RO4929097 in Combination With Temozolomide (Phase IB)
NCT01196416 (9) [back to overview]Overall Survival (Phase II)
NCT01196416 (9) [back to overview]Number of Participants With Presence or Absence of Markers of Notch Signalling Pathway Inhibition in Patient Tumors (Phase Ib)
NCT01196416 (9) [back to overview]Participants Evaluated for Toxicity
NCT01196416 (9) [back to overview]Maximum Tolerated Dose for RO4929097
NCT01196416 (9) [back to overview]Cycle 1 Mean Day 2 Trough/Pharmacokinetics of Gamma-secretase Inhibitor RO4929097 in Combination With Temozolomide (Phase IB)
NCT01390584 (5) [back to overview]Complete Response (CR) Rate After Induction Treatment
NCT01390584 (5) [back to overview]Proportion of Patients Who Are PET Negative After Induction Treatment
NCT01390584 (5) [back to overview]Progression-free Survival Rate
NCT01390584 (5) [back to overview]Progression-free Survival at 36 Months Among Patients Who Are PET Positive After Induction Treatment
NCT01390584 (5) [back to overview]Overall Survival
NCT01404936 (1) [back to overview]Participants' Response
NCT01534078 (4) [back to overview]Grade III or IV Adverse Events
NCT01534078 (4) [back to overview]Overall Response Rate
NCT01534078 (4) [back to overview]Overall Response Rate After One Cycle of Brentuximab
NCT01534078 (4) [back to overview]Complete Response Rate
NCT01542255 (1) [back to overview]Progression Free Survival
NCT01700946 (4) [back to overview]Median CD20 Expression Levels
NCT01700946 (4) [back to overview]3-year Overall Survival Rate of Patients With Relapsed ALL
NCT01700946 (4) [back to overview]3-year Event-free Survival Rates in Patients With Relapsed ALL
NCT01700946 (4) [back to overview]Mean of CD20 Expression Levels
NCT01712490 (19) [back to overview]Disease-free Survival (DFS) Per IRF
NCT01712490 (19) [back to overview]Duration of Complete Remission (DOCR) Per IRF
NCT01712490 (19) [back to overview]Duration of Response (DOR) Per IRF
NCT01712490 (19) [back to overview]Event-free Survival (EFS) Per IRF
NCT01712490 (19) [back to overview]Modified Progression-free Survival (mPFS) Per Independent Review Facility (IRF)
NCT01712490 (19) [back to overview]Number of Participants With Abnormal Clinical Laboratory Values
NCT01712490 (19) [back to overview]Overall Response Rate (ORR) Per IRF
NCT01712490 (19) [back to overview]Overall Survival (OS)
NCT01712490 (19) [back to overview]Positron Emission Tomography (PET) Negativity Rate Per IRF at Cycle 2
NCT01712490 (19) [back to overview]A+AVD: AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Brentuximab Vedotin ADC and TAb
NCT01712490 (19) [back to overview]A+AVD: Cmax: Maximum Observed Plasma Concentration for Brentuximab Vedotin Monomethyl Auristatin E (MMAE)
NCT01712490 (19) [back to overview]A+AVD: Cmax: Maximum Observed Serum Concentration for Brentuximab Vedotin Antibody-drug Conjugate (ADC) and Total Antibody (TAb)
NCT01712490 (19) [back to overview]A+AVD: Number of Participants With Antitherapeutic Antibody (ATA) and Neutralizing Antitherapeutic Antibody (nATA) Positive for Brentuximab Vedotin
NCT01712490 (19) [back to overview]Change From Baseline in Patient-Reported Outcome (PRO) Scores by mPFS Based on European Organization for Research and Treatment of Cancer (EORTC) Quality of Life Questionnaire-C30 (EORTC QLQ-C30) at EOT
NCT01712490 (19) [back to overview]Number of Participants Who Experience at Least One Treatment Emergent Adverse Event (TEAE) and Serious Adverse Event (SAE)
NCT01712490 (19) [back to overview]Percentage of Participants Not in CR Per IRF Who Received Subsequent Radiation After Completion of Frontline Therapy
NCT01712490 (19) [back to overview]A+AVD: AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Brentuximab Vedotin MMAE
NCT01712490 (19) [back to overview]Complete Remission (CR) Per IRF Rate at the End of Frontline Therapy
NCT01712490 (19) [back to overview]Complete Remission (CR) Rate at the End of Randomized Regimen Per IRF
NCT01771107 (12) [back to overview]2-year Progression-free Survival (PFS)
NCT01771107 (12) [back to overview]CD8 Counts
NCT01771107 (12) [back to overview]Complete Response Rate
NCT01771107 (12) [back to overview]Characterization of Histologic Subtypes in HIV-HL in the HAART Era
NCT01771107 (12) [back to overview]Frequency of Adverse Events
NCT01771107 (12) [back to overview]2-year Overall Survival
NCT01771107 (12) [back to overview]CD4 Counts
NCT01771107 (12) [back to overview]Event-free Survival
NCT01771107 (12) [back to overview]Incidence of Neurotoxicity
NCT01771107 (12) [back to overview]Maximal Tolerated Dose of Brentuximab Vedotin (Phase I)
NCT01771107 (12) [back to overview]Partial Response Rate
NCT01771107 (12) [back to overview]Viral Load
NCT01876082 (4) [back to overview]Progression-free Survival
NCT01876082 (4) [back to overview]Percentage of Patients Remaining Alive With Best Overall Response as Per RECIST v1.1.
NCT01876082 (4) [back to overview]Overall Survival
NCT01876082 (4) [back to overview]Percentage of Patients Remaining Alive and Progression-free at 6 Months as Per RECIST 1.1 After the Day of Randomisation (6-month Non-progression Rate).
NCT02177695 (7) [back to overview]Assessment of Whether the Treatment-specific COXEN Score is Prognostic of pT0 Rate
NCT02177695 (7) [back to overview]Correlation Between GC-and ddMVAC-COXEN Score
NCT02177695 (7) [back to overview]Number of Participants With Gr 3 Through 5 Adverse Events That Are Related to Study Drugs
NCT02177695 (7) [back to overview]Predictability of the CO-eXpression ExtrapolatioN (COXEN) Score to Direct Which of the Two Regimens the Patient Should Receive: Gemcitabine+Cisplatin (GC) Versus Dose-dense Methotrexate, Vinblastin, Doxorubicin, and Cisplatin (DDMVAC)
NCT02177695 (7) [back to overview]Assessment of Whether the Treatment-specific COXEN Score is Prognostic of ≤ pT1 Rate
NCT02177695 (7) [back to overview]Pathologic T0 Rate Evaluation: Gemcitabine+Cisplatin (GC) Versus Dose-dense Methotrexate, Vinblastin, Doxorubicin, and Cisplatin (DDMVAC)
NCT02177695 (7) [back to overview]Assessment of COXEN Score as a Predictive Factor Distinguishing Between GC and ddMVAC
NCT02181738 (22) [back to overview]Number of Participants With Laboratory Abnormalities in Specific Thyroid Tests in Cohort D Monotherapy Phase
NCT02181738 (22) [back to overview]Number of Participants With Select AEs in Cohort D
NCT02181738 (22) [back to overview]Treatment Discontinuation Rate in Cohort D
NCT02181738 (22) [back to overview]Number of Participants With Serious Adverse Events (SAEs) in Cohort D
NCT02181738 (22) [back to overview]Complete Response (CR) Rate at Planned End of Therapy Based on IRRC Assessments in Cohort D
NCT02181738 (22) [back to overview]Duration of Complete Remission (CR) Based on IRRC Assessments for Cohorts A, B, and C
NCT02181738 (22) [back to overview]Duration of Objective Response (DOR) Based on Investigator Assessments in Cohorts A, B, and C
NCT02181738 (22) [back to overview]Duration of Objective Response Based on IRRC Assessments in Cohorts A, B, and C
NCT02181738 (22) [back to overview]Duration of PR Based on IRRC Assessments in Cohorts A, B, and C
NCT02181738 (22) [back to overview]Number of Participants With Laboratory Abnormalities in Specific Liver Tests in Cohort D Combination Therapy Phase
NCT02181738 (22) [back to overview]Objective Response Rate (ORR) Based on IRRC Assessments in Cohorts A, B, and C
NCT02181738 (22) [back to overview]Complete Remission (CR) Rate Based on IRRC Assessments in Cohorts A, B, and C
NCT02181738 (22) [back to overview]Objective Response Rate (ORR) Based on IRRC Assessments in Cohorts A, B, and C Extended Collection
NCT02181738 (22) [back to overview]Objective Response Rates (ORR) Based on Investigator Assessments for Cohorts A, B, and C
NCT02181738 (22) [back to overview]Partial Remission (PR) Rate Based on IRRC Assessments in Cohorts A, B, and C
NCT02181738 (22) [back to overview]Number of Participants Laboratory Abnormalities in Specific Thyroid Tests in Cohort D Combination Therapy Phase
NCT02181738 (22) [back to overview]Number of Participants Who Died in Cohort D
NCT02181738 (22) [back to overview]Number of Participants Who Experienced at Least One Treatment Related Grade 3-5 AE in Cohort D
NCT02181738 (22) [back to overview]Number of Participants With Adverse Events (AEs) in Cohort D
NCT02181738 (22) [back to overview]Number of Participants With AEs Leading to Discontinuation in Cohort D
NCT02181738 (22) [back to overview]Number of Participants With AEs Leading to Dose Delay in Cohort D
NCT02181738 (22) [back to overview]Number of Participants With Laboratory Abnormalities in Specific Liver Tests in Cohort D Monotherapy Phase
NCT02412670 (7) [back to overview]Cumulative Incidence of Cancer-specific Death at 24 Months
NCT02412670 (7) [back to overview]Complete Pathologic Response Rate
NCT02412670 (7) [back to overview]Proportion of Patients With Renal Insufficiency at Completion of Chemotherapy
NCT02412670 (7) [back to overview]Recurrence-free Survival
NCT02412670 (7) [back to overview]Proportion of Patients With Renal Insufficiency at Completion of Surgery
NCT02412670 (7) [back to overview]Event-free Survival
NCT02412670 (7) [back to overview]Bladder Cancer-free Survival
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in Haemophilus Influenzae B Antibody, IgG at EOT
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Achieving CR Per IRF Assessment Per IWG Criteria in ATA Positive and ATA Negative Participants
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Experienced SAEs From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy
NCT02979522 (57) [back to overview]Phase 2: Median Tmax of Brentuximab Vedotin and TAb in Serum
NCT02979522 (57) [back to overview]Phase 2: Mean Serum Cmax of Brentuximab Vedotin and TAb
NCT02979522 (57) [back to overview]Phase 2: Mean Serum AUC0-15d of Brentuximab Vedotin and TAb
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in Peripheral Blood CD34+A at EOT
NCT02979522 (57) [back to overview]Phase 2: Time to Onset and Resolution for All Peripheral Neuropathy Events
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants With Low and High ATA Titer Values
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Were ATA Positive, Persistently Positive, or Transiently Positive, and nATA Positive
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Achieving CR Per IRF Assessment Per IWG Criteria in ATA Positive and ATA Negative Participants
NCT02979522 (57) [back to overview]Phase 2: Number of ATA Positive and ATA Negative Participants With AEs and SAEs
NCT02979522 (57) [back to overview]Phase 2: Median Tmax of MMAE in Plasma
NCT02979522 (57) [back to overview]Phase 2: Mean Plasma Cmax of MMAE
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Who Achieved a CR Per IRF Assessment Per IWG Criteria at EOT Visit
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Who Achieved a PR Per IRF Assessment Per IWG Criteria at EOT Visit
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Who Achieved an ORR Per IRF Assessment Per IWG Criteria at EOT Visit
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Who Experienced Adverse Events (AEs) From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Who Experienced Serious Adverse Events (SAEs) From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Whose Disease Was PET Negative After 2 Cycles of Protocol Therapy Per IRF Assessment
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Whose Disease Was PET Positive After 6 Cycles of Protocol Therapy Per IRF Assessment
NCT02979522 (57) [back to overview]Phase 1: Recommended Dose of Brentuximab Vedotin in Combination With Doxorubicin, Vinblastine, and Dacarbazine in a Pediatric Population
NCT02979522 (57) [back to overview]Phase 2: Duration of Response (DOR)
NCT02979522 (57) [back to overview]Phase 2: Event-free Survival (EFS)
NCT02979522 (57) [back to overview]Phase 2: Overall Survival (OS)
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Receiving Irradiation for HL Following Study Treatment
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Achieved a Complete Remission (CR) Per Independent Review Facility (IRF) Assessment Per International Working Group (IWG) Criteria at End of Treatment (EOT) Visit
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Achieved a Partial Remission (PR) Per IRF Assessment Per IWG Criteria at EOT Visit
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Achieved an Overall Response Rate (ORR) Per IRF Assessment Per IWG Criteria at EOT Visit
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Experienced AEs From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Experienced Peripheral Neuropathy, Regardless of Seriousness, From the First Dose of Protocol Therapy
NCT02979522 (57) [back to overview]Phase 2: Mean Plasma AUC0-15 of MMAE
NCT02979522 (57) [back to overview]Phase 2: Mean Cmax of Brentuximab Vedotin in ATA Positive and ATA Negative Participants
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Who Were Able to Complete 6 Cycles of Protocol Therapy at the Recommended Dose
NCT02979522 (57) [back to overview]Phase 2: Percentage of Participants Whose Disease Was Positron Emission Tomography (PET) Negative After 2 Cycles of Protocol Therapy Per IRF Assessment
NCT02979522 (57) [back to overview]Phase 2: Progression-free Survival (PFS)
NCT02979522 (57) [back to overview]Phase 1: Mean Area Under the Plasma Concentration-Time Curve From Day 0 to Day 15 (AUC0-15) of MMAE
NCT02979522 (57) [back to overview]Phase 1: Mean Area Under the Serum Concentration-Time Curve From Day 0 to Day 15 (AUC0-15) of Brentuximab Vedotin and TAb
NCT02979522 (57) [back to overview]Phase 1: Mean AUC 0-15d of Brentuximab Vedotin in ATA Positive and ATA Negative Participants
NCT02979522 (57) [back to overview]Phase 1: Mean Cmax of Brentuximab Vedotin in ATA Positive and ATA Negative Participants
NCT02979522 (57) [back to overview]Phase 1: Mean Maximum Observed Plasma Concentration (Cmax) of Monomethyl Auristatin E (MMAE)
NCT02979522 (57) [back to overview]Phase 1: Mean Maximum Observed Serum Concentration (Cmax) of Brentuximab Vedotin Total Conjugated and Therapeutic Antibody (TAb)
NCT02979522 (57) [back to overview]Phase 1: Median Time to Reach Cmax (Tmax) of Brentuximab Vedotin and TAb in Serum
NCT02979522 (57) [back to overview]Phase 1: Median Time to Reach Cmax (Tmax) of MMAE in Plasma
NCT02979522 (57) [back to overview]Phase 1: Number of ATA Positive and ATA Negative Participants With AEs and SAEs
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants Who Were Antitherapeutic Antibody (ATA) Positive, Persistently Positive or Transiently Positive, and Neutralizing Antitherapeutic Antibody (nATA) Positive
NCT02979522 (57) [back to overview]Phase 1: Percentage of Participants With Low and High ATA Titer Values
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline Immunoglobulin G Levels at End of Treatment (EOT)
NCT02979522 (57) [back to overview]Phase 2: Mean AUC 0-15 of Brentuximab Vedotin in ATA Positive and ATA Negative Participants
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline Total Immunoglobulin at EOT
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline Poliovirus Antibodies Ratio at EOT
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in Total Lymphocyte Count at EOT
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in the Percentage of CD8+ (CD8+CD45RA-CD197- and CD8+CD45RA-CD197+) Subset of Cells at EOT
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in the Percentage of CD4+ (CD4+CD45RA-CD197- and CD4+CD45RA+CD197+) Subset of Cells at EOT
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in Tetanus at EOT
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in Immunoglobulin M at the End of Treatment (EOT)
NCT02979522 (57) [back to overview]Phase 2: Immune Reconstitution-Change From Baseline in Immunoglobulin A at EOT
NCT03226249 (3) [back to overview]Complete Response (CR) With Pembrolizumab Treatment Alone
NCT03226249 (3) [back to overview]Overall Survival at Treatment Completion
NCT03226249 (3) [back to overview]Progression Free Survival (PFS) at Treatment Completion
NCT03646123 (16) [back to overview]Actual Dose Intensity: Brentuximab Vedotin (Part A)
NCT03646123 (16) [back to overview]Complete Response (CR) Rate (Parts B and C)
NCT03646123 (16) [back to overview]Complete Response Rate (Part A)
NCT03646123 (16) [back to overview]Subsequent Anticancer Therapy Utilization Rate (Part A)
NCT03646123 (16) [back to overview]Relative Dose Intensity (Part A)
NCT03646123 (16) [back to overview]Rate of Dose Reduction and Delays: Vinblastine (Part A)
NCT03646123 (16) [back to overview]Rate of Dose Reduction and Delays: Doxorubicin (Part A)
NCT03646123 (16) [back to overview]Rate of Dose Reduction and Delays: Dacarbazine (Part A)
NCT03646123 (16) [back to overview]Rate of Dose Reduction and Delays: Brentuximab Vedotin (Part A)
NCT03646123 (16) [back to overview]Incidence of Laboratory Abnormalities (Parts B and C)
NCT03646123 (16) [back to overview]Incidence of Adverse Events (Parts B and C)
NCT03646123 (16) [back to overview]Febrile Neutropenia (FN) Rate (Part A)
NCT03646123 (16) [back to overview]Actual Dose Intensity: Doxorubicin, Vinblastine, Dacarbazine (Part A)
NCT03646123 (16) [back to overview]Primary Refractory Disease Rate (Part A)
NCT03646123 (16) [back to overview]Physician-reported Progression Free Survival (PFS) (Part A)
NCT03646123 (16) [back to overview]Overall Response Rate (ORR) at EOT (Parts B and C)
NCT03912818 (2) [back to overview]Incidence of Grade 3-5 Adverse Events
NCT03912818 (2) [back to overview]Proportion of Subjects Who Initiate Study Treatment and Achieve Tumor Stage of pT2 N0 M0 or Better (e.g., pT0, pT1 N0) at Cystectomy

5-year Overall Survival

Overall survival is defined as the time from randomization to death or last known alive. The 5-year survival rate is the probability a patient survives 5 years. (NCT00003389)
Timeframe: Assessed every 2 months if patient is < 1 year from study entry, every 3 months for the second year, every 4 months for the third year, every 6 months for years 4 and 5, and yearly for 5 years

InterventionProportion of patients (Number)
Arm A (ABVD)0.88
Arm B (Stanford V)0.88

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Incidence of Second Cancers

Number of patients who developed second primary cancers (NCT00003389)
Timeframe: Assessed every 2 months if patient is < 1 year from study entry, every 3 months for the second year, every 4 months for the third year, every 6 months for years 4 and 5, and yearly for 5 years

Interventionparticipants (Number)
Arm A (ABVD)15
Arm B (Stanford V)19

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Failure-free Survival at 5 Years

"Failure-free survival is defined as the time from randomization to the earlier of progression/relapse or death. The 5-year failure-free survival is the probability a patient is failure-free and survives 5 years.~Progression is defined as an increase in size of 25% of the sum of the products of the pretreatment measurements or appearance of new lesions. Significant enlargement of the liver or spleen is evidence of progression. A significant increase in size is defined as > 2.0 cm in distance between costal margin and the inferior margin of either organ.~Relapse is defined as the re-appearance of any clinical evidence of Hodgkin's disease in a patient who has had a complete response. Relapse for partial responders is defined as progressive disease relative to disease status during the partial remission." (NCT00003389)
Timeframe: Assessed every 2 months if patient is < 1 year from study entry, every 3 months for the second year, every 4 months for the third year, every 6 months for years 4 and 5

InterventionProportion of patients (Number)
Arm A (ABVD)0.74
Arm B (Stanford V)0.71

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Probability of Overall Survival

p53 positive patients randomized to MVAC (arm I) compared to p53 positive patients randomized to observation (arm II). Survival is calculated from registration to death due to any cause. Probabilities of survival were based on the Kaplan-Meier product-limit method. (NCT00005047)
Timeframe: 5 years

Interventionprobability (Median)
Arm I: M-VAC x 30.87
Arm II: Observation0.84

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Probability of Overall Survival

Patients with tumors demonstrating alteration in p53 compared to patients with no p53 alterations. Probabilities of survival were based on the Kaplan-Meier product-limit method. (NCT00005047)
Timeframe: 5 years

Interventionprobability (Median)
p53 Positive Patients0.82
p53 Negative Patients0.84

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Probability of Recurrence

"Patients with tumors demonstrating alteration in p53 compared to patients with no p53 alterations.~Probabilities of recurring were based on cumulative incidence curves. Recurrence is defined as first radiological appearance of bladder cancer, per local standard of care." (NCT00005047)
Timeframe: 5 years

Interventionprobability (Median)
p53 Positive Patients0.83
p53 Negative Patients0.77

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Probability of Recurring

"p53 positive patients randomized to MVAC (arm I) compared to p53 positive patients randomized to observation (arm II). Time from registration to the first observation of disease recurrence, censoring patients who died of unrelated causes. Probabilities of recurring were based on cumulative incidence curves.~Recurrence is defined as first radiological appearance of bladder cancer, per local standard of care." (NCT00005047)
Timeframe: 5 years

Interventionprobability (Median)
Arm I: M-VAC x 30.85
Arm II: Observation0.84

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5-year Overall Survival

Overall survival was measured from the date of registration to study until death from any cause with observations censored at the date of last contact for patients last known to be alive. (NCT00006237)
Timeframe: Every three months for a year, every six months for years 2-5, annual for years 5-10

InterventionPercent of population (Number)
Interferon56
Biochemotherapy56

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5-year Relapse-Free Survival

Measured from date of registration to date of first observation of progressive disease or death due to any cause. (NCT00006237)
Timeframe: Every three months for the first year, every 6 months for years 2-5, annually for years 6-10

InterventionPercentage of population (Number)
Interferon47
Biochemotherapy38

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Toxicity

Number of patients with Grade 3-5 adverse events that are related to study drug by given type of adverse event (NCT00006237)
Timeframe: While on treatment, patients on the HDIFN arm were assessed weekly for the 1st month, then every 2 weeks for the 2nd month, then every 3 months therafter; patients on the biochemo arm were assessed daily for the 1st 5 days, then weekly thereafter.

,
InterventionParticipants (Number)
Abdominal pain/crampingAcidosisAcute vascular leak syndromeAlkaline phosphatase increaseAllergic reactionAnal incontinenceAnemiaAnorexiaAnxiety/agitationApneaArrhythmia, NOSArthralgiaBilirubin increaseBone painCPK increaseCardiovascular-otherCatheter related infectionCerebrovascular ischemiaColitisConfusionConstipation/bowel obstructionCranial neuropathyCreatinine increaseDehydrationDelusionsDepressionDiarrhea without colostomyDizziness/light headednessDizziness/vertigo, NOSDouble visionDyspneaEryth/rash/eruption/desq, NOSEsophagitis/dysphagiaEye-otherFatigue/malaise/lethargyFebrile neutropeniaFever without neutropeniaFever, NOSHallucinationsHeadacheHemorrhage w/ 3-4 thrombocytHyperglycemiaHyperkalemiaHypermagnesemiaHypertensionHypertriglyceridemiaHypocalcemiaHypokalemiaHypomagnesemiaHyponatremiaHypophosphatemiaHypotensionHypoxiaInfection w/o 3-4 neutropeniaInfection with 3-4 neutropeniaInfection, unk ANCInsomniaLeukopeniaLipase increaseLocal injection site reactionLymphopeniaMood/consciousness change, NOSMuscle weakness (not neuro)MyalgiaNauseaNeutropenia/granulocytopeniaPRBC transfusionPancreatitisPersonality/behavioral changePetechiae/purpuraPlatelet transfusionPruritusRash/desquamationRenal failureReportable adverse event, NOSRespiratory infect w/ neutropRigors/chillsSGOT (AST) increaseSGPT (ALT) increaseSeizuresSensory neuropathyStomatitis/pharyngitisSurgery-wound infectionSyncopeThrombocytopeniaThrombosis/embolismTyphlitisVertigoVomitingWeakness (motor neuropathy)Weight loss
Biochemotherapy1113018950031410202340471461112320229511513111018756416139213820211451613101531011217822100501103720
Interferon10001001412400010102010101422001101381101902010101000000011121100071025001001401021832000321101913

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Overall Survival From Randomization

Overall survival (OS) was computed using the number of months from the date of randomization to the date of death. Participants still alive were censored at the last follow-up date. Kaplan-Meier methodology was used to evaluate OS. (NCT00024167)
Timeframe: Followed every 4 weeks from randomization until death, up to 7 years.

Interventionmonths (Median)
Induction Treatment + Strontium-8924.2
Induction Treatment + No Strontium-8922.8

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Overall Survival From Registration

Overall survival (OS) was computed using the number of months from the date of registration to the date of death. Participants still alive were censored at the last follow-up date. Kaplan-Meier methodology was used to evaluate OS. (NCT00024167)
Timeframe: Followed every 4 weeks from registration until death, up to 7 years.

Interventionmonths (Median)
Induction Treatment + Strontium-8927.9
Induction Treatment + No Strontium-8926.6

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Frequency of Complete Response

"The frequency of complete response (CR) is reported as the number (proportion) of subjects in complete response, as assessed during weeks 4 to 5 of chemotherapy. Per protocol, CR is defined as complete regression of all palpable and radiographic demonstrable disease by computed tomography (CT) scan or positron emission tomography-CT (PET-CT)." (NCT00026208)
Timeframe: 5 weeks

InterventionParticipants (Count of Participants)
Stanford V-C + Low-dose Radiotherapy31

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Overall Survival (OS)

Overall survival was assessed at up to 16 years from date of diagnosis, and reported as the median years of survival with standard deviation. (NCT00026208)
Timeframe: 16 years

Interventionyears (Median)
Stanford V-C + Low-dose Radiotherapy10.4
Stanford V-C Only13.2

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Progression-free Survival (PFS)

Progression-free survival was assessed for 3 years from the completion of treatment. Progression-free survival was considered to mean the proportion of patients (percentage) still alive without disease recurrence or progression. (NCT00026208)
Timeframe: up to 3 years

Interventionpercentage of participants (Number)
Stanford V-C + Low-dose Radiotherapy89.7
Stanford V-C Only50

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Second Hodgkin's Disease Progression

Second Hodgkin's disease progression is reported as the number of participants experiencing 2 instances of progression of the underlying Hodgkin's disease, assessed at up to 16 years from date of diagnosis. (NCT00026208)
Timeframe: 16 years

InterventionParticipants (Count of Participants)
Stanford V-C + Low-dose Radiotherapy3
Stanford V-C Only1

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Survival at 5 and 10 Years

Survival at 5 and 10 years is expressed at the percentage of subjects known to remain alive at those timepoints. (NCT00026208)
Timeframe: 5 and 10 years

,
InterventionParticipants (Count of Participants)
5 years10 years
Stanford V-C + Low-dose Radiotherapy6741
Stanford V-C Only33

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Time to Disease Progression

"Disease progression was assessed both radiographically and clinically.~Tumor assessments to assess for radiographic disease progression were assessed by magnetic resonance imaging (MRI) measurement whenever possible or computed tomography (CT) scan and/or tumor measurement during physical examination of palpable lesions. Clinical assessments for clinical progression of disease were assessed by treating physician or designee.~Progressive disease as measured by the appearance of new lesions; an increased size of index tumor(s) by >/= 25% of the sum of the products of baseline measurements; and/or by increase in symptoms." (NCT00030264)
Timeframe: 6 months

InterventionMonths (Mean)
TotalRadiographic ProgressionClinical Progression
Methotrexate & Vinblastine25.829.225.8

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Event-free Survival (EFS)

Percentage of EFS patients. This is measured as the time from study entry until disease progression, disease recurrence, occurrence of a second malignant neoplasm, or death from any cause. To measure Event Free Survival, repeated one-sided logrank tests will be performed The upper critical values are based on the one-sided alpha-spending functions of t2 (alpha=0.05) and the lower critical values are based on testing the alternative hypothesis at 0.005 level. (NCT00059839)
Timeframe: From first enrollment up to 3 years.

Interventionpercentage of participants (Number)
Standard (APO) With Vincristine (Arm I)74
Consolidation (Includes Vinblastine) (Arm II)79

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Occurrence of Severe Toxicity

An incidence of severe toxicity is defined to be the occurrence of grade 3 or higher infection or grade 3 or higher sensory neuropathy during cycles 1-2 of protocol therapy. If 12 or more patients experience grade 3 or higher infection or five or more patients experience grade 3 or higher sensory neuropathy during cycles 1-2 of protocol therapy, the regimen will be flagged as being associated with an excessive rate of severe toxicity. (NCT00061893)
Timeframe: The first two cycles (6 weeks) of protocol chemotherapy

Interventionparticipants (Number)
Grade 3 or Higher InfectionGrade 3 or Higher Sensory Neuropathy
Combination Chemotherapy11

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Event Free Survival

(NCT00061893)
Timeframe: 24 months after start of protocol therapy

Interventionpercentage of participants (Number)
Combination Chemotherapy35

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Overall Survival (OS)

OS is measured from the start of on-study to the date of death or to the last date of follow-up. Measurement is determined by Kaplan-Meyer estimate. The probability of survival at 5 years after diagnosis is given. (NCT00186875)
Timeframe: 2 years after last patient completes therapy (approximately 4 years after enrollment)

Interventionprobability (Mean)
Standard Risk0.654
High Risk0.357

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Response Rate

"The response rate is defined as the proportion of participants who attain morphological complete remission after the re-induction Block C, inclusive of all patients who begin re-induction. Morphological complete remission was defined as <5% blasts in bone marrow by morphology." (NCT00186875)
Timeframe: End of re-induction Block C (approximately 1 month after the start of therapy)

,
Interventionproportion of participants (Number)
Complete remissionFailure to reach complete remission
High Risk0.7860.214
Standard Risk0.8460.154

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Minimal Residual Disease (MRD) Compared With Historical Data From TOTXV Protocol (NCT00137111)

The prevalence of MRD in children undergoing treatment for relapsed ALL and to compare the results to those obtained in children with newly diagnosed ALL. MRD is considered as positive (i.e., prevalent) if its level is >=0.01%. The prevalence of MRD after Block C is defined as the proportion of MRD positives. (NCT00186875)
Timeframe: End of Block Block C therapy (Day 46)

,,
InterventionParticipants (Count of Participants)
Negative <0.01%Positive ≥0.01%
High Risk18
Standard Risk119
TOTXV Participants390102

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Minimal Residual Disease (MRD) Compared With Historical Data From TOTXV Protocol (NCT00137111)

The prevalence of MRD in children undergoing treatment for relapsed ALL and to compare the results to those obtained in children with newly diagnosed ALL. MRD is considered as positive (i.e., prevalent) if its level is >=0.01%. The prevalence of MRD after Block B is defined as the proportion of MRD positives. (NCT00186875)
Timeframe: End of Block B therapy (Day 19)

,,
InterventionParticipants (Count of Participants)
Negative <0.01%Positive ≥0.01%
High Risk210
Standard Risk1111
TOTXV Participants191297

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Patient Quality of Life (QoL), PedsQL v.4.0: School Functioning

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy73.1
Week 869.5
Week 1272.6
After Radiation78.4
Off-therapy81.3

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Patient Quality of Life (QoL), PedsQL v.4.0: Total Score

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy80.9
Week 874.4
Week 1275.3
After Radiation83.1
Off-therapy84.5

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Patient Quality of Life (QoL), PedsQL v.4.0:Social Functioning

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy90.9
Week 888.6
Week 1288.0
After Radiation90.1
Off-therapy91.1

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Patient Quality of Life (QoL), Symptom Distress Scale

"The patient's degree of discomfort from specific treatment-related symptoms across multiple time points.~Instrument interpretation: SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy17.3
Week 819.6
Week 1218.1
After Radiation15.1
Off-therapy14.3

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Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: (Echocardiogram)

Echocardiograms will be carried out on the patient at 1, 2, 5, and 10 years after therapy. Outcomes will be categorized. (NCT00352027)
Timeframe: 1, 2, 5, and 10 years post therapy

,,,
InterventionParticipants (Count of Participants)
NormalAbnormal
Year 1 Off Therapy680
Year 10 Off Therapy151
Year 2 Off Therapy571
Year 5 Off Therapy362

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Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: (Electrocardiogram)

Electrocardiograms (EKGs) will be conducted on the patient at 1, 2, 5, and 10 years after therapy. Results will be categorized as either normal or abnormal, determined by the test outcome. (NCT00352027)
Timeframe: 1, 2, 5, and 10 years post therapy

,,,
InterventionParticipants (Count of Participants)
NormalAbnormal
Year 1 Off Therapy515
Year 10 Off Therapy106
Year 2 Off Therapy448
Year 5 Off Therapy244

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Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: (Pulmonary Function)

Patient pulmonary function will undergo assessment at 1, 2, 5, and 10 years after therapy. Results will be categorized as either normal or abnormal, depending on the test results. (NCT00352027)
Timeframe: 1, 2, 5, and 10 years post therapy

,,,
InterventionParticipants (Count of Participants)
NormalAbnormal
Year 1 Off Therapy4620
Year 10 Off Therapy91
Year 2 Off Therapy4120
Year 5 Off Therapy2511

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Describe Toxicities, Particularly the Frequency and Severity of Late Effects of Therapy: Thyroid (TSH)

For patients that received cervical radiation, TSH laboratory testing will be conducted at 1, 2, 5 and 10 years. TSH results will be categorized as Normal, Hypothyroid, Hyperthyroid, or Thyroid Nodule, depending on the test's findings. (NCT00352027)
Timeframe: 1, 2, 5, and 10 years post therapy

,,,
InterventionParticipants (Count of Participants)
NormalHypothyroidHyperthyroidThyroid Nodule
Year 1 Off Therapy60820
Year 10 Off Therapy20300
Year 2 Off Therapy541110
Year 5 Off Therapy37810

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Local and Distant Failure for Children Treated With Tailored-field Radiation

The cumulative incidence of local and distant failure will be estimated. Effect of competing risks will be taken into account. Local failure is defined as in-field, and distant failure is defined as out-of-field. (NCT00352027)
Timeframe: from first enrollment date up to 3 years follow-up

Interventionprobability that the event occurs (Number)
Cumulative incidence of distant failure at 3 yearsCumulative incidence of local failure at 3 years
Stanford V Chemotherapy0.03750.1127

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Prognostic Factors for Treatment Failure: Gender

Event-free survival (EFS) was calculated for the 80 eligible patients. EFS was defined as the interval between on study to relapse, second malignant tumor, or last contact (all alive) whichever came first. For those who had multiple relapses, the first one was counted. Given only 11 events, we examined individually age, gender, histology and stage for its association with EFS using Cox model. P values from Score test were computed for the statistical significance. (NCT00352027)
Timeframe: 3 years follow-up

Interventionevents (Number)
MaleFemale
Stanford V Chemotherapy56

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Prognostic Factors for Treatment Failure: Histology

Event-free survival (EFS) was calculated for the 80 eligible patients. EFS was defined as the interval between on study to relapse, second malignant tumor, or last contact (all alive) whichever came first. For those who had multiple relapses, the first one was counted. Given only 11 events, we examined individually age, gender, histology and stage for its association with EFS using Cox model. P values from Score test were computed for the statistical significance. (NCT00352027)
Timeframe: 3 years follow-up

Interventionevents (Number)
Classical, Nodular SclerosingOther
Stanford V Chemotherapy101

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Prognostic Factors for Treatment Failure: Stage

Ann Arbor staging classification was used to stage all patients. Stage was examined (I/II versus III) for the association with event-free survival (EFS), defined as the interval between date on study and of relapse/disease progression, second malignancy, death, or last contact, whichever came first. Given only 11 events, the investigators used univariate Cox model with Score test to compute the p value for the statistical significance. Stage NCT00352027)
Timeframe: 5.5 (years) median follow-up with minimum 0.3 to maximum 9.4 years follow-up

Interventionevents (Number)
Stage Stage ≥III
Stanford V Chemotherapy83

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Toxicities With Grade >1

Comparison of the toxicities of intermediate risk patients treated with Stanford V chemotherapy low dose tailored-field radiation (current HOD05 protocol) to those patients on HOD99 (NCT00145600). Grading of toxicities for HOD05 and HOD99 used the NCI Common Terminology Criteria for Adverse Events (CTCAE) version 3.0. (NCT00352027)
Timeframe: 3 years

,,,,,,,
Interventionadverse events (Number)
Alanine transaminase (ALT)Aspartate transaminase (AST)Allergic reaction/hypersensitivityConstipationFebrile neutropeniaFever (in the absence of neutropenia)GlucoseGGT (gamma-Glutamyltranspeptidase)HemoglobinHypoxiaIleus, GI (functional obstruction of bowel)Infection with Grade 3 or 4 neutrophilsInfection - OtherInfection with normal ANC or Grade 1-2 neutrophilsInfection with unknown ANCInsomniaLeukocytes (total WBC)LymphopeniaMucositis/stomatitis (functional/symptomatic)NauseaNeuropathy: motorNeuropathy: sensoryNeutrophils/granulocytes (ANC/AGC)PainPhosphatePlateletsPotassiumSodiumSyndromes - OtherThrombosis/embolism (vascular access-related)Thrombosis/thrombus/embolismVomiting
HOD05 - Grade 200000000000000000000000000000000
HOD05 - Grade 3114072012611213014122010124510211202
HOD05 - Grade 40000100060000000157000032000000010
HOD05 - Grade 500000000000000000000000000000000
HOD99 - Grade 200000000000000000000000000000001
HOD99 - Grade 3000150002002011019012119103000004
HOD99 - Grade 4000020100000000050000030100000000
HOD99 - Grade 500000000000000000000000000000000

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Patient Quality of Life (QoL), PedsQL v.3.0: Pain and Hurt

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 863.9
Week 1271.5
After Radiation79.9
Off-therapy88.0

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Patient Quality of Life (QoL), PedsQL v.3.0: Perceived Physical Appearance

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 877.6
Week 1281.3
After Radiation81.4
Off-therapy84.7

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Patient Quality of Life (QoL), PedsQL v.3.0: Procedural Anxiety

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 871.8
Week 1270.9
After Radiation68.1
Off-therapy80.1

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Patient Quality of Life (QoL), PedsQL v.3.0: Total Score

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 874.1
Week 1274.2
After Radiation81.7
Off-therapy83.5

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Prognostic Factors for Treatment Failure: Age

Age was examined for the association with event-free survival (EFS) which was defined as the interval between date on study and date of relapse/disease progression, second malignant tumor, death, or last contact, whichever came first. Given only 11 events, the investigators used univariate Cox model with Score test to compute the p value for the statistical significance. (NCT00352027)
Timeframe: 5.5 (years) median follow-up with minimum 0.3 to maximum 9.4 years follow-up

Interventionevents (Number)
Stanford V Chemotherapy11

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Patient Quality of Life (QoL), PedsQL v.3.0: Treatment Anxiety

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 889.2
Week 1282
After Radiation89.4
Off-therapy87.3

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Patient Quality of Life (QoL), PedsQL v.3.0: Worry

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 871.2
Week 1272.2
After Radiation74.5
Off-therapy76.0

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Patient Quality of Life (QoL), PedsQL v.4.0: Emotional Functioning

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy72.6
Week 875.3
Week 1275.7
After Radiation84.5
Off-therapy81.6

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Patient Quality of Life (QoL), PedsQl v.4.0: Physical Functioning

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy83.2
Week 868.4
Week 1269.1
After Radiation80.8
Off-therapy85.2

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Communication

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.35

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Pain and Hurt

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 861.2
Week 1261.8
After Radiation73.1
Off-therapy82.7

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Patient Quality of Life (QoL), PedsQL v.4.0: Psychosocial Health

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy79.3
Week 877.6
Week 1278.6
After Radiation84.3
Off-therapy84.3

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3-year Event-free Survival (EFS) Probability

Comparison of thee-year EFS probability along with the whole EFS distributions of intermediate risk patients treated with Stanford V chemotherapy low dose tailored-field radiation to those patients on HOD99. (NCT00352027)
Timeframe: 3 years

Interventionprobability (Number)
HOD05 Participants0.887
HOD99 Participants0.844

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3-year Event-Free Survival Probability

The survival probability for the time interval from treatment start to the time of the first failure (disease recurrence, second malignancy or death) within a 3-year time frame. (NCT00352027)
Timeframe: 3 years

Interventionprobability (Number)
Stanford V Chemotherapy0.887

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3-year Local Failure-free Survival Probability

Comparison of the 3-year local failure-free survival probability along with the whole local failure-free survival distributions of intermediate risk patients treated with Stanford V chemotherapy low dose tailored-field radiation to those patients on HOD99. (NCT00352027)
Timeframe: 3 years

Interventionprobability (Number)
HOD05 Participants0.887
HOD99 Participants0.932

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3-year Overall Survival (OS) Probability

Comparison of the 3-year OS probability along with the whole OS distributions of intermediate risk patients treated with Stanford V chemotherapy low dose tailored-field radiation to those patients on HOD99. (NCT00352027)
Timeframe: 3-years

Interventionprobability (Number)
HOD05 Participants1.00
HOD99 Participants0.978

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Cognitive Problems

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.46

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Cognitive Problems

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-1.0
Parent and Patient Scores at Week 120.14
Parent and Patient Scores at After Radiation-8.0
Parent and Patient Scores at Off-therapy-4.0

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Nausea

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-2.31

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Pain and Hurt

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-2.52

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Perceived Physical Appearance

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.20

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Procedural Anxiety

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-0.87

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Total Score

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.41

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Treatment Anxiety

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-0.96

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.3.0: Worry

"Relationship between quality of life and symptom distress across multiple time points [completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.3.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.06

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Emotional Functioning

"Relationship between quality of life and symptom distress instruments aggregated across multiple time points [At diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.56

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Physical Functioning

"Relationship between quality of life and symptom distress instruments aggregated across multiple time points [At diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.9

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Psychosocial Health

"Relationship between quality of life and symptom distress instruments aggregated across multiple time points [At diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-0.92

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: School Functioning

"Relationship between quality of life and symptom distress instruments aggregated across multiple time points [At diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.21

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Social Functioning

"Relationship between quality of life and symptom distress instruments aggregated across multiple time points [At diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-0.79

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Association Between Patient-Reported QoL and Symptom Distress, PedsQL v.4.0: Total Score

"Relationship between quality of life and symptom distress instruments aggregated across multiple time points [At diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy]. Generalized estimating equations (GEE) were used to examine the association between symptoms distress and QoL scores.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. SDS, higher scores indicate higher overall symptom distress with a range of 10-50." (NCT00352027)
Timeframe: 6 months after the completion of therapy

Interventionbeta coefficient (Number)
QoL Participants-1.46

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Communication

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-0.3
Parent and Patient Scores at Week 12-3.6
Parent and Patient Scores at After Radiation-7.4
Parent and Patient Scores at Off-therapy-6.3

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Nausea

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-1.2
Parent and Patient Scores at Week 12-3.4
Parent and Patient Scores at After Radiation-3.0
Parent and Patient Scores at Off-therapy-1.1

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Pain and Hurt

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-2.0
Parent and Patient Scores at Week 12-9.5
Parent and Patient Scores at After Radiation-5.6
Parent and Patient Scores at Off-therapy-5.4

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Perceived Physical Appearance

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-2.5
Parent and Patient Scores at Week 12-9.5
Parent and Patient Scores at After Radiation-5.9
Parent and Patient Scores at Off-therapy-9.3

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Procedural Anxiety

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-0.2
Parent and Patient Scores at Week 12-9.3
Parent and Patient Scores at After Radiation-2.2
Parent and Patient Scores at Off-therapy-8.7

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Total Score

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-1.5
Parent and Patient Scores at Week 12-5.2
Parent and Patient Scores at After Radiation-4.5
Parent and Patient Scores at Off-therapy-5

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Treatment Anxiety

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-6.1
Parent and Patient Scores at Week 12-8.8
Parent and Patient Scores at After Radiation-7.9
Parent and Patient Scores at Off-therapy-6.6

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.3.0: Worry

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Week 8-0.7
Parent and Patient Scores at Week 12-3.9
Parent and Patient Scores at After Radiation-2.7
Parent and Patient Scores at Off-therapy-0.5

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Emotional Functioning

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Pre-therapy-4.9
Parent and Patient Scores at Week 8-9.4
Parent and Patient Scores at Week 12-8.0
Parent and Patient Scores at After Radiation-10.8
Parent and Patient Scores at Off-therapy-1.7

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Physical Functioning

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Pre-therapy-2.9
Parent and Patient Scores at Week 8-2.3
Parent and Patient Scores at Week 12-1.9
Parent and Patient Scores at After Radiation-5.4
Parent and Patient Scores at Off-therapy-2

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Psychosocial Health

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Pre-therapy-2.8
Parent and Patient Scores at Week 8-6.4
Parent and Patient Scores at Week 12-6.3
Parent and Patient Scores at After Radiation-5.6
Parent and Patient Scores at Off-therapy-3.3

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: School Functioning

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Pre-therapy1.3
Parent and Patient Scores at Week 8-5.3
Parent and Patient Scores at Week 12-4.1
Parent and Patient Scores at After Radiation-3.4
Parent and Patient Scores at Off-therapy-4.3

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Social Functioning

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Pre-therapy-5.3
Parent and Patient Scores at Week 8-5.7
Parent and Patient Scores at Week 12-7.4
Parent and Patient Scores at After Radiation-5.0
Parent and Patient Scores at Off-therapy-3.3

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Correlation of Agreement Between Patient QoL and Parent Proxy QoL at Multiple Time Points, PedsQL v.4.0: Total Score

"Assess and compare the patient reported and parent proxy quality of life across multiple time points. Reported mean differences were calculated as parent score minus patient score.~Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. Reported mean differences were calculated as: parent score - patient score." (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Parent and Patient Scores at Pre-therapy-2.9
Parent and Patient Scores at Week 8-4.8
Parent and Patient Scores at Week 12-4.8
Parent and Patient Scores at After Radiation-5
Parent and Patient Scores at Off-therapy-2.9

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Disease Failure Rate Within Radiation Fields

Defined as disease that recurs in the initially involved nodal region within the field of irradiation. The disease failure rate within the radiation fields will be estimated with a 95% confidence interval using appropriate methods (e.g., estimate cumulative incidence in the presence of competing risks). (NCT00352027)
Timeframe: 3 years

Interventionproportion of participants (Number)
Stanford V Chemotherapy0.1125

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Cognitive Problems

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 877.6
Week 1279.5
After Radiation78.6
Off-therapy79.9

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Communication

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 879.2
Week 1280.4
After Radiation80.3
Off-therapy84.3

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Nausea

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 861.2
Week 1257.4
After Radiation72.2
Off-therapy83.2

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Perceived Physical Appearance

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 874.9
Week 1272.2
After Radiation73.7
Off-therapy76.3

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Procedural Anxiety

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 870.0
Week 1260.0
After Radiation63.1
Off-therapy73.8

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Total Score

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 871.7
Week 1269.3
After Radiation74.5
Off-therapy80.0

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Treatment Anxiety

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 881.9
Week 1272.6
After Radiation78.5
Off-therapy81.8

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Parent Proxy Quality of Life (QoL), PedsQL v.3.0: Worry

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100. (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 870
Week 1269.2
After Radiation71.9
Off-therapy78.7

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Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Emotional Functioning

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy67.7
Week 865.4
Week 1268.1
After Radiation73.0
Off-therapy82.0

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Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Physical Functioning

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy79.8
Week 865.3
Week 1267.3
After Radiation73.6
Off-therapy84.6

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Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Psychosocial Health

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy76.2
Week 871.0
Week 1274.1
After Radiation79.0
Off-therapy88.0

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Parent Proxy Quality of Life (QoL), PedsQL v.4.0: School Functioning

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy74.4
Week 862.8
Week 1270.8
After Radiation75.6
Off-therapy78.9

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Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Social Functioning

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy86.1
Week 883.0
Week 1280.7
After Radiation85.1
Off-therapy89.1

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Parent Proxy Quality of Life (QoL), PedsQL v.4.0: Total Score

Parent's assessment of child's functioning over multiple time points. Instrument interpretation: PedsQL v.4.0, higher scores indicate better HRQOL with a range of 0-100. (NCT00352027)
Timeframe: At Diagnosis (T1), completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Pre-therapy77.6
Week 869.1
Week 1272.3
After Radiation77.8
Off-therapy83.5

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Patient Quality of Life (QoL), PedsQL v.3.0: Cognitive Problems

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 879.1
Week 1278.2
After Radiation87.0
Off-therapy82.0

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Patient Quality of Life (QoL), PedsQL v.3.0: Communication

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 880.7
Week 1283.0
After Radiation87.2
Off-therapy89.0

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Patient Quality of Life (QoL), PedsQL v.3.0: Nausea

"Patient QOL will be measured at multiple time points to assess the patient's functioning.~Instrument interpretation: PedsQL v.3.0, higher scores indicate lower problems with a range of 0-100." (NCT00352027)
Timeframe: At completion of 2 cycles of chemotherapy (T2), completion of 4 cycles of chemotherapy (T3), completion of radiation (T4), and 3-6 months (T5) after the completion of therapy

Interventionunits on a scale (Mean)
Week 862.7
Week 1260.1
After Radiation76.7
Off-therapy81.6

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Effect of Rituximab on EBV(+) Tumors

Number of relapses among participants who had tumors positive for Epstein-Barr virus (EBV). (NCT00369681)
Timeframe: Up to 56 months

Interventionrelapses (Number)
R-ABVD0

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Event-free Survival

Percentage of participants who did not experience death, relapse, or progression (worsening) of their lymphoma. (NCT00369681)
Timeframe: 3 years

Interventionpercentage of participants (Number)
R-ABVD83

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Relationship Between Marker Detection and Clinical Outcome

Number of relapses for participants who did and did not have re-emergence of clonal CD27(+) ALDH(+) B cells after completing study intervention. (NCT00369681)
Timeframe: 3 years

Interventionrelapses (Number)
No re-emergence of cloneRe-emergence of clone
R-ABVD02

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5-year Failure-free Survival Rate for Participants With Hodgkin's Disease Given Rituximab With ABVD

Five year Event Free Survival (EFS) is proportion of surviving participants who remain event free out of total participants at 5 years after receiving Rituximab + ABVD (RABVD). Event-free Survival (EFS) analyzed every 6 months. (NCT00504504)
Timeframe: Baseline to 5 Years or until disease progression

Interventionpercentage of participants (Number)
Rituximab + ABVD Chemotherapy83

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Time to Progression (TTP)

TTP defined as the time from date of first dose of study medication to first documentation of objective tumor progression in days. Response evaluation by Response Evaluation Criteria in Solid Tumors (RECIST) done following 2 cycles and 3 cycles. Progression is defined, using RECIST, as a measurable increase in the smallest dimension of any target or non-target lesion, or the appearance of new lesions, since baseline. (NCT00505635)
Timeframe: Following two 21 day cycles until disease progression

Interventiondays (Geometric Mean)
Biochemotherapy With Temozolomide93.2

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Percentage of Participants With Response Defined as the Absence of Residual Muscle Invasive Cancer in Resected Specimen

"Number of participants out of total with a response defined as downstaging to <= pT1N0 in the resected specimen. A binary variable was defined for downstaging (pathologic stage below initial clinical stage and below pT1N1N0M0); staging using American Joint Committee on Cancer (AJCC) TNM system of TNM; T describes size tumor & cancer spread into nearby tissue; N describes spread to nearby lymph nodes; & M describes metastasis (spread to other parts of body). Numbers after T (such as T1, T2, T3, and T4) describe tumor size and/or amount of spread into nearby structures, higher the T number, the larger the tumor and/or more it has grown into nearby tissues. Responses of lesser magnitude scored as treatment failure. Response Evaluation Criteria In Solid Tumors (RECIST) criteria do not apply for this cohort of neoadjuvant participants since this study does not require measurable disease by traditional assessment." (NCT00506155)
Timeframe: Following 20 weeks of chemotherapy

InterventionPercentage of Participants (Number)
pT0N0pT1N0
Neoadjuvant Chemotherapy With M-VAC + Avastin3853

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5-year Overall Survival (OS)

The overall survival rate stated as a five-year survival rate, which is the percentage of participants in study who are alive five years after the start of treatment. (NCT00506155)
Timeframe: 5 years

InterventionPercentage of Participants (Number)
Neoadjuvant Chemotherapy With M-VAC + Avastin63

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Overall Survival (OS)

OS was defined as the duration from treatment start to death from any cause. Overall survival was censored at the last contact for surviving participants and missing data points. (NCT00520403)
Timeframe: Baseline, Day 1 of every cycle to disease progression or death (up to Week 102)

Interventionweeks (Median)
Bevacizumab + IFN/VinblastineNA

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Percentage of Participants With Disease Progression or Death

Disease progression was evaluated according to the Response Evaluation Criteria In Solid Tumors (RECIST) using computed tomography (CT) scans (preferred method), magnetic resonance imaging (MRI) scans, X-ray, bone scans, or clinical examination. (NCT00520403)
Timeframe: Days 0, 91, 182, 273, 365, 456, and 547

Interventionpercentage of participants (Number)
Bevacizumab + IFN/Vinblastine66.9

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PFS - Time to Event

PFS was defined as the time in days from the date of treatment start to the date of first documented disease progression or death. Disease progression was evaluated according to RECIST using CT scans (preferred method), MRI scans, X-ray, bone scans, or clinical examination. Median PFS was estimated using the Kaplan-Meier method (NCT00520403)
Timeframe: Days 0, 91, 182, 273, 365, 456, and 547

Interventiondays (Median)
Bevacizumab + IFN/Vinblastine274

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Percentage of Participants With Objective Response (OR)

Percentage of participants with OR based on assessment of confirmed complete remission (CR) or confirmed partial remission (PR) according to RECIST. (NCT00520403)
Timeframe: Baseline and Cycles 3, 6, 9, 13, and 17

Interventionpercentage of participants (Number)
Week 9 (n=14)Week 18 (n=16)Week 27 (n=16)Week 39 (n=16)Week 51 (n=16)
Bevacizumab + IFN/Vinblastine21.431.337.531.331.3

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Concentration of Cerebrospinal Fluid Neurotransmitters

Concentrations of various neurotransmitters in cerebrospinal fluid were measured at 5 timepoints. The median concentration of each neurotransmitter at each time point was calculated and provided with a full range. (NCT00602667)
Timeframe: Baseline, at the completion of therapy, and every 12 months up to 36 months after off therapy date

Interventionng/ml (Median)
Dopamine concentration at baselineDopamine concentration at completion of treatmentDopamine concentration at 12 months off treatmentDopamine concentration at 24 months off treatmentDopamine concentration at 36 months off treatment3,4-dihydroxyphenylacetic acid concentration at baseline3,4-dihydroxyphenylacetic acid concentration at completion of treatment3,4-dihydroxyphenylacetic acid concentration at 12 months off treatment3,4-dihydroxyphenylacetic acid concentration at 24 months off treatment3,4-dihydroxyphenylacetic acid concentration at 36 months off treatmentHydroxytryptamine concentration at baselineHydroxytryptamine concentration at completion of treatmentHydroxytryptamine concentration at 12 months off treatmentHydroxytryptamine concentration at 24 months off treatmentHydroxytryptamine concentration at 36 months off treatmentHydroxyindoleacetic acid concentration at baselineHydroxyindoleacetic acid concentration at completion of treatmentHydroxyindoleacetic acid concentration at 12 months off treatmentHydroxyindoleacetic acid concentration at 24 months off treatmentHydroxyindoleacetic acid concentration at 36 months off treatmentHomovanillic acid concentration at baselineHomovanillic acid concentration at completion of treatmentHomovanillic acid concentration at 12 months off treatmentHomovanillic acid concentration at 24 months off treatmentHomovanillic acid concentration at 36 months off treatment
Patients With Neurotransmitter Studies3.163.706.434.464.052.561.621.041.521.002.382.012.002.441.6252.0352.7235.7233.9831.5682.44114.1368.2888.2779.78

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Number and Type of Genetic Polymorphisms

Types of genetic polymorphisms of neurotransmitters were examined. We studied 3 genetic polymorphisms; these were types of genetic polymorphisms involved in dopamine metabolism. They were as follows: rs6323, rs4680, and rs6280. (NCT00602667)
Timeframe: At study enrollment (Day 0)

InterventionParticipants (Count of Participants)
rs6323rs4680rs6280
Number of Patients With Neurotransmitter Studies171717

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Number of Participants With Chromosomal Abnormalities

Amplifications and deletions (gains and losses) for chromosomes of interest are shown in the table of measured values. (NCT00602667)
Timeframe: Based on samples obtained at the time of initial surgery or repeat surgery prior to treatment

,,
InterventionParticipants (Count of Participants)
chr2p gain/amplificationchr2p loss/deletionchr2q gain/amplificationchr2q loss/deletionchr6p gain/amplificationchr6p loss/deletionchr6q gain/amplificationchr6q loss/deletionchr8p gain/amplificationchr8p loss/deletionchr8q gain/amplificationchr8q loss/deletionchr9p gain/amplificationchr9p loss/deletionchr9q gain/amplificationchr9q loss/deletionchr10p gain/amplificationchr10p loss/deletionchr10q gain/amplificationchr10q loss/deletionchr20p gain/amplificationchr20p loss/deletionchr20q gain/amplificationchr20q loss/deletion
High-Risk Group606032320807331507090505
Intermediate-Risk Group121230302635601505070403
Low-Risk Group505010101010442600030201

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Number of Successful Collections for Frozen and Fixed Tumor Samples

Successful collections will be defined as the number of patients who have frozen/fixed tumor samples available. (NCT00602667)
Timeframe: Based on samples obtained at the time of initial surgery or repeat surgery prior to treatment

,,
InterventionParticipants (Count of Participants)
Number with frozen tumor tissueNumber with fixed tumor tissue
High-Risk Group3271
Intermediate-Risk Group73153
Low-Risk Group2754

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Numbers of Patients With Gene Alterations

Gene alterations, which include single nucleotide variants (SNPs), amplifications, deletions, translocations, indels, and germline alterations are shown for specific genes of interest in the results table. (NCT00602667)
Timeframe: Based on samples obtained at the time of initial surgery or repeat surgery prior to treatment

,,
InterventionParticipants (Count of Participants)
PTCH1 alterationSUFU alterationKMT2D alterationSMO alterationBCOR alterationPTEN alterationBRCA2 alterationGLI2 alterationSMARCA4 alterationTP53 alterationMYCN alteration
High-Risk Group31310000001
Intermediate-Risk Group41100000101
Low-Risk Group76521100200

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Numbers of Patients With Molecular Abnormalities by Tumor Type

Alterations included single nucleotide variants (SNPs), amplifications, deletions, translocations, indels, and germline alterations. Cytogenetic information shows gains and losses as specified in the table of measured values. (NCT00602667)
Timeframe: Based on samples obtained at the time of initial surgery or repeat surgery prior to treatment

,,,,,,
InterventionParticipants (Count of Participants)
PTCH1 alterationSUFU alterationKMT2D alterationSMO alterationBCOR alterationPTEN alterationBRCA2 alterationGLI2 alterationSMARCA4 alterationTP53 alterationMYCN amplificationchr2p gain/amplificationchr2p loss/deletionchr2q gain/amplificationchr2q loss/deletionchr6p gain/amplificationchr6p loss/deletionchr6q gain/amplificationchr6q loss/deletionchr8p gain/amplificationchr8p loss/deletionchr8q gain/amplificationchr8q loss/deletionchr9p gain/amplificationchr9p loss/deletionchr9q gain/amplificationchr9q loss/deletionchr10p gain/amplificationchr10p loss/deletionchr10q gain/amplificationchr10q loss/deletionchr20p gain/amplificationchr20p loss/deletionchr20q gain/amplificationchr20q loss/deletion
High-risk Group 3 Patients00000000001101032320706030307080404
High-risk Group 4 Patients00000000000000000000101000000000000
High-risk SHH Patients31310000000404000000000301200010101
Intermediate-risk Group 3 Patients00000000100010120201221100005050303
Intermediate-risk Group 4 Patients00000000000010110100404101000000000
Intermediate-risk SHH Patients41100000001000000000000400500020100
Low-risk SHH Patients76521100200505010101010442600030201

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Pharmacogenetic Variation on Central Nervous System Transmitters

Frequencies of genetic polymorphisms were reported. (NCT00602667)
Timeframe: At study enrollment (Day 0)

InterventionParticipants (Count of Participants)
Genetic Polymorphisms for monoamine oxidase A (MAOA) rs632372067969Genetic Polymorphisms for catecholamine-O-methyltransferase (COMT) rs468072067969Genetic Polymorphisms for dopamine receptor D (DRD3) rs628072067969
AGCCTCTTGGAATG
Patients With Neurotransmitter Studies2
Patients With Neurotransmitter Studies13
Patients With Neurotransmitter Studies7
Patients With Neurotransmitter Studies5
Patients With Neurotransmitter Studies0
Patients With Neurotransmitter Studies6
Patients With Neurotransmitter Studies4

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Percent Probability of Event-free Survival (EFS) for Medulloblastoma Patients

Defined as the time interval from date on treatment until the date of first progression, second malignancy or death due to any cause; or date of last contact for patients who have not experienced an event. All eligible medulloblastoma patients who received any methotrexate are included in this analysis. (NCT00602667)
Timeframe: From date on treatment to date of first progression, relapse, second malignancy or death from any cause or to date of last contact, estimated at 1 year after

InterventionPercent Probability (Number)
Low-Risk Group73.9
Intermediate-Risk Group46.9
High-Risk Group30.8

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4-OH Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 1

4-OH cyclophosphamide plasma concentration-time data are collected in consolidation cycle 1. Individual estimates of 4-OH cyclophosphamide AUC0-24h (area under concentration curve from time 0 to 24 hours post- dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group96.8
Intermediate-Risk Group48.7
High-Risk Group39.8

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4-OH Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 2

4-OH cyclophosphamide plasma concentration-time data are collected in consolidation cycle 2. Individual estimates of 4-OH cyclophosphamide AUC0-24h (area under concentration curve from time 0 to 24 hours post- dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group95.9
Intermediate-Risk Group49.5
High-Risk Group43.5

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4-OH Cyclophosphamide AUC0-24h in Induction Chemotherapy

4-OH cyclophosphamide plasma concentration-time data are collected on day 9 in one cycle of induction chemotherapy. Individual estimates of 4-OH cyclophosphamide AUC0-24h (area under concentration curve from time 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group116.4
Intermediate-Risk Group111.3
High-Risk Group109.1

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4-OH Cyclophosphamide AUC0-24h in Maintenance Chemotherapy Cycle A1

4-OH cyclophosphamide plasma concentration-time data are collected on day 1 of maintenance cycle A1. Individual estimates of 4-OH cyclophosphamide AUC0-24h (area under concentration curve from time 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 0.5, 1.75, 3, 6, and 24 hours post-dose

Interventionµmol·h/L (Median)
Low-Risk Group1.98
Intermediate-Risk Group1.96
High-Risk Group1.82

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CEPM AUC0-24h in Consolidation Chemotherapy Cycle 1

Carboxyethylphosphoramide mustard (CEPM) plasma concentration-time data are collected in consolidation cycle 1. Individual estimates of CEPM AUC0-24h (area under concentration curve from time 0 to 24 hours post- dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group128.9
Intermediate-Risk Group62.2
High-Risk Group51.8

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CEPM AUC0-24h in Consolidation Chemotherapy Cycle 2

Carboxyethylphosphoramide mustard (CEPM) plasma concentration-time data are collected in consolidation cycle 2. Individual estimates of CEPM AUC0-24h (area under concentration curve from time 0 to 24 hours post- dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group132.7
Intermediate-Risk Group46.8
High-Risk Group44.0

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CEPM AUC0-24h in Induction Chemotherapy

Carboxyethylphosphoramide mustard (CEPM) plasma concentration-time data are collected on day 9 in one induction cycle. Individual estimates of CEPM AUC0-24h (area under concentration curve from time 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group140.2
Intermediate-Risk Group137.8
High-Risk Group135.3

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CEPM AUC0-24h in Maintenance Chemotherapy Cycle A1

Carboxyethylphosphoramide mustard (CEPM) plasma concentration-time data are collected on day 1 of maintenance cycle A1. Individual estimates of CEPM AUC0-24h (area under concentration curve from time 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 0.5, 1.75, 3, 6, and 24 hours post-dose

Interventionµmol·h/L (Median)
Low-Risk Group1.59
Intermediate-Risk Group1.65
High-Risk Group1.41

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Cyclophosphamide Apparent Oral Clearance in Maintenance Chemotherapy Cycle A1

Cyclophosphamide plasma concentration-time data are collected on day 1 of maintenance cycle A1. Individual estimates of cyclophosphamide apparent oral clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 0.5, 1.75, 3 and 6 hours post-dose

InterventionL/h/m^2 (Median)
Low-Risk Group2.95
Intermediate-Risk Group2.83
High-Risk Group2.74

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Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 1

Cyclophosphamide plasma concentration-time data are collected in consolidation cycle 1. Individual estimates of cyclophosphamide AUC0-24h (area under concentration curve from time 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group1968
Intermediate-Risk Group1504
High-Risk Group868

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Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 2

Cyclophosphamide plasma concentration-time data are collected in consolidation cycle 2. Individual estimates of cyclophosphamide AUC0-24h (area under concentration curve from time 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group1966
Intermediate-Risk Group799
High-Risk Group899

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Cyclophosphamide AUC0-24h in Induction Chemotherapy

Cyclophosphamide plasma concentration-time data are collected on day 9 in one cycle of induction chemotherapy. Individual estimates of cyclophosphamide AUC0-24h (area under concentration curve from time 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

Interventionµmol·h/L (Median)
Low-Risk Group2070
Intermediate-Risk Group2150
High-Risk Group2105

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Cyclophosphamide AUC0-24h in Maintenance Chemotherapy Cycle A1

Cyclophosphamide plasma concentration-time data are collected on day 1 of maintenance cycle A1. Individual estimates of cyclophosphamide AUC0-24h are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 0.5, 1.75, 3, 6, and 24 hours post-dose

Interventionµmol·h/L (Median)
Low-Risk Group39.9
Intermediate-Risk Group38.7
High-Risk Group42.2

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Cyclophosphamide Clearance in Consolidation Chemotherapy Cycle 1

Cyclophosphamide plasma concentration-time data are collected in consolidation cycle 1. Individual estimates of cyclophosphamide clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

InterventionL/h/m^2 (Median)
Low-Risk Group2.39
Intermediate-Risk Group2.08
High-Risk Group2.43

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Cyclophosphamide Clearance in Consolidation Chemotherapy Cycle 2

Cyclophosphamide plasma concentration-time data are collected in consolidation cycle 2. Individual estimates of cyclophosphamide clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

InterventionL/h/m^2 (Median)
Low-Risk Group2.48
Intermediate-Risk Group2.55
High-Risk Group2.37

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Cyclophosphamide Clearance in Induction Chemotherapy

Cyclophosphamide plasma concentration-time data are collected on day 9 in one cycle of induction chemotherapy. Individual estimates of cyclophosphamide clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, end of infusion, 3, 6, and 24 hours from end of cyclophosphamide infusion

InterventionL/h/m^2 (Median)
Low-Risk Group2.40
Intermediate-Risk Group2.23
High-Risk Group2.25

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Erlotinib Apparent Oral Clearance

Erlotinib plasma concentration-time data are collected on day 1 of maintenance cycle B2. Individual estimates of erlotinib apparent oral clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 1, 2, 4, 8, and 24 hours post-dose

InterventionL/h/m^2 (Median)
Low-Risk Group6.53
Intermediate-Risk Group7.79
High-Risk Group8.40

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Erlotinib Apparent Volume of Central Compartment

Erlotinib plasma concentration-time data are collected on day 1 of maintenance cycle B2. Individual estimates of erlotinib apparent volume of central compartment are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 1, 2, 4, 8, and 24 hours post-dose

InterventionL/m^2 (Median)
Low-Risk Group72.9
Intermediate-Risk Group61.7
High-Risk Group104.8

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Erlotinib AUC0-24h

Erlotinib plasma concentration-time data are collected on day 1 of maintenance cycle B2. Individual estimates of erlotinib AUC0-24h (area under concentration curve from 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 1, 2, 4, 8, and 24 hours post-dose

Interventionµmol·h/L (Median)
Low-Risk Group31.0
Intermediate-Risk Group23.5
High-Risk Group22.0

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Event-free Survival (EFS) Compared to Historical Controls

EFS was measured from the date of initial treatment to the earliest date of disease progression, second malignancy or death for patients who fail; and to the date of last contact for patients who remain at risk for failure. 1-year EFS estimates are reported by risk group. EFS was compared to St. Jude historical cohorts by risk group using hazard ratios with 95% confidence intervals. (NCT00602667)
Timeframe: From date on treatment until date of first event (progression, second malignancy or death) or until date of last contact, assessed up to 10 years

InterventionPercent probability (Number)
SJYC07 Low-risk Medulloblastoma Patients73.9
SJYC07 Intermediate-risk Medulloblastoma Patients46.9
SJYC07 High-risk Medulloblastoma Patients30.8

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Feasibility and Toxicity of Administering Consolidation Therapy Including Cyclophosphamide and Pharmacokinetically Targeted Topotecan to Patients With Metastatic Disease Based on the Percentage of Courses Delayed for More Than 7 Days Due to Toxicity

For the subset of patients with metastatic disease (high-risk group patients), during consolidation, we will calculate the number and proportion of courses during which subsequent chemotherapy administration was delayed for more than 7 days due to toxicity. Patients were to received 2 courses of consolidation chemotherapy and then maintenance therapy. (NCT00602667)
Timeframe: At completion of consolidation therapy (up to 6 months after on-study date)

InterventionPercentage of courses delayed (Number)
High-Risk Group2.6

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Feasibility and Toxicity of Administering Oral Maintenance Therapy in Children <3 Years of Age as Measured by the Percentage of Total Scheduled Maintenance Doses Received

These data are based on patient diaries. For children <3 years of age, we will calculate the percentage of total scheduled doses each patient received per course for each of the oral maintenance courses and report the overall average number percentage of doses received per course across patients. If patients received all planned doses, their percentage would be 100%. If the average percentage was less than 75%, then feasibility would be in question. (NCT00602667)
Timeframe: From start of oral maintenance therapy (approximately 6 months after on-study date) to completion of oral maintenance therapy (up to 1 year after on-study date)

InterventionPercentage of scheduled doses received (Mean)
Low-Risk Group96
Intermediate-Risk Group91
High-Risk Group98

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Feasibility and Toxicity of Administering Vinblastine With Induction Chemotherapy for Patients With Metastatic Disease as Measured by the Percentage of Courses Delayed for More Than 7 Days Due to Toxicity

For the subset of patients with metastatic disease (high-risk group patients), during induction, the proportion percentage of courses during which subsequent chemotherapy administration was delayed for more than 7 days due to toxicity will be calculated. Patients were to receive 4 courses of induction and then consolidation chemotherapy. (NCT00602667)
Timeframe: From on-study date up to 4 months after on-study date

InterventionPercentage of courses delayed (Number)
High-Risk Group3.8

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Methotrexate AUC0-66h in Induction Cycle 1

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 1. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate AUC0-66h (area under concentration curve from time 0 to 66 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

Interventionµmol·h/L (Median)
Low-Risk Group1797
Intermediate-Risk Group1813
High-Risk Group1821

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Methotrexate AUC0-66h in Induction Cycle 2

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 2. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate AUC0-66h (area under concentration curve from time 0 to 66 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

Interventionµmol·h/L (Median)
Low-Risk Group1900
Intermediate-Risk Group1902
High-Risk Group1879

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Methotrexate AUC0-66h in Induction Cycle 3

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 3. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate AUC0-66h (area under concentration curve from time 0 to 66 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

Interventionµmol·h/L (Median)
Low-Risk Group1872
Intermediate-Risk Group1879
High-Risk Group1831

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Methotrexate AUC0-66h in Induction Cycle 4

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 4. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate AUC0-66h (area under concentration curve from time 0 to 66 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

Interventionµmol·h/L (Median)
Low-Risk Group1804
Intermediate-Risk Group1841
High-Risk Group1886

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Methotrexate Clearance in Induction Cycle 1

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 1. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of Methotrexate (MTX)

InterventionL/h/m^2 (Median)
Low-Risk Group5.69
Intermediate-Risk Group6.06
High-Risk Group5.65

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Methotrexate Clearance in Induction Cycle 2

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 2. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

InterventionL/h/m^2 (Median)
Low-Risk Group5.47
Intermediate-Risk Group5.70
High-Risk Group5.70

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Methotrexate Clearance in Induction Cycle 3

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 3. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

InterventionL/h/m^2 (Median)
Low-Risk Group5.68
Intermediate-Risk Group5.78
High-Risk Group5.81

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Methotrexate Clearance in Induction Cycle 4

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 4. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

InterventionL/h/m^2 (Median)
Low-Risk Group5.75
Intermediate-Risk Group5.89
High-Risk Group5.79

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Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 1

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 1. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate concentration at 42 hours post-dose are obtained using post hoc analysis. (NCT00602667)
Timeframe: 42 hours from start of MTX

Interventionµmol/L (Median)
Low-Risk Group0.49
Intermediate-Risk Group0.57
High-Risk Group0.61

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Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 2

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 2. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate concentration at 42 hours post-dose are obtained using post hoc analysis. (NCT00602667)
Timeframe: 42 hours from start of MTX

Interventionµmol/L (Median)
Low-Risk Group0.75
Intermediate-Risk Group0.72
High-Risk Group0.69

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Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 3

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 3. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate concentration at 42 hours post-dose are obtained using post hoc analysis. (NCT00602667)
Timeframe: 42 hours from start of MTX

Interventionµmol/L (Median)
Low-Risk Group0.65
Intermediate-Risk Group0.70
High-Risk Group0.58

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Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 4

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 4. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate concentration at 42 hours post-dose are obtained using post hoc analysis. (NCT00602667)
Timeframe: 42 hours from start of MTX

Interventionµmol/L (Median)
Low-Risk Group0.64
Intermediate-Risk Group0.64
High-Risk Group0.55

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Methotrexate Volume of Central Compartment in Induction Cycle 1

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 1. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate volume of central compartment are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

InterventionL/m^2 (Median)
Low-Risk Group11.63
Intermediate-Risk Group13.70
High-Risk Group13.25

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Methotrexate Volume of Central Compartment in Induction Cycle 2

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 2. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate volume of central compartment are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

InterventionL/m^2 (Median)
Low-Risk Group13.77
Intermediate-Risk Group13.73
High-Risk Group13.62

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Methotrexate Volume of Central Compartment in Induction Cycle 3

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 3. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate volume of central compartment are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

InterventionL/m^2 (Median)
Low-Risk Group12.70
Intermediate-Risk Group13.55
High-Risk Group13.87

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Methotrexate Volume of Central Compartment in Induction Cycle 4

Methotrexate plasma concentration-time data are collected after the start of methotrexate infusion in induction cycle 4. Population parameters and inter-subject variability are estimated. Individual estimates of methotrexate volume of central compartment are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion and 6, 23, 42, 66 hours from start of MTX

InterventionL/m^2 (Median)
Low-Risk Group12.64
Intermediate-Risk Group13.31
High-Risk Group13.68

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OSI-420 AUC0-24h

Erlotinib metabolite OSI-420 plasma concentration-time data are collected on day 1 of maintenance cycle B2. Individual estimates of OSI-420 AUC0-24h (area under concentration curve from 0 to 24 hours post-dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 1, 2, 4, 8, and 24 hours post-dose

Interventionµmol·h/L (Median)
Low-Risk Group2.17
Intermediate-Risk Group1.81
High-Risk Group1.62

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Overall Survival (OS) Compared to Historical Controls

OS was measured from the date of initial treatment to date of death or to date of last contact for survivors. 1-year OS estimates were reported by risk group. OS was compared to St. Jude historical cohorts by risk group using hazard ratios with 95% confidence intervals. (NCT00602667)
Timeframe: 1 year after treatment initiation of last patient

InterventionPercent probability (Number)
SJYC07 Low-risk Medulloblastoma Patients100
SJYC07 Intermediate-risk Medulloblastoma Patients84.4
SJYC07 High-risk Medulloblastoma Patients61.5

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Participants With Empirical Dosage Achieving Target System Exposure of Intravenous Topotecan

Number of participants who successfully achieve target systemic exposure of intravenous topotecan after an empiric dosage during consolidation phase of therapy are reported. (NCT00602667)
Timeframe: Pre-infusion, 5 min., 1, and 3 hours from end of infusion

Interventionparticipants (Number)
Intermediate-Risk Group0
High-Risk Group8

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Participants With PK-guided Dosage Adjustment Achieving Target System Exposure of Intravenous Topotecan

Number of participants who successfully achieve target systemic exposure of intravenous topotecan after a pharmacokinetic-guided dosage adjustment during consolidation phase of therapy are reported. (NCT00602667)
Timeframe: Pre-infusion, 5 min., 1, and 3 hours from end of infusion

Interventionparticipants (Number)
Intermediate-Risk Group1
High-Risk Group20

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Percent of Patients With Sustained Objective Responses Rate After Consolidation

For patients enrolled on the high-risk arm with measurable residual disease after induction treated with consolidation therapy, we will estimate the objective response (complete response (CR)/partial response (PR)) rate after consolidation therapy with a 95% confidence interval. Objective responses must be sustained for at least eight weeks. All patients who receive at least 1 dose of cyclophosphamide or topotecan during consolidation are evaluable for response. (NCT00602667)
Timeframe: 8 weeks after completion of consolidation therapy (up to 8 months after on-study date)

Interventionpercentage of participants (Number)
High-Risk Group13.2

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Percent of PET Scans With Loss of Signal Intensity

Measures will be analyzed for intermediate risk participants who receive proton beam therapy (PBT) and who consent. This objective aims to assess the feasibility of using post-proton beam therapy (PBT) positron emission tomography (PET) as an in-vivo dosimetric and distal edge verification system in this patient population. To quantify the decay in signal, 134 scans from 53 patients were analyzed by recording the mean activation value (MAV), the average recorded PET signal from activation, within the target volume. With each patient being given the same dose, the percent standard deviation in the MAV can serve as a quantitative representation of signal loss due to radioactive decay. (NCT00602667)
Timeframe: Up to 3 times during RT consolidation

Interventionmean activation value (MAV) (Mean)
Intermediate Risk Group60

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Percent Probability of Progression-free Survival (PFS) for Medulloblastoma Patients

Progression was defined as 25% increase in the size of any measurable lesion; the appearance of a new lesion; or the conversion of negative cerebrospinal fluid (CSF) cytology to positive. Defined as the time interval from date on treatment until the date of first progression, medulloblastoma-related death or date of last contact for patients who have not experienced an event. All eligible medulloblastoma patients who received any methotrexate are included in this analysis. (NCT00602667)
Timeframe: From date on treatment until date of first progression or relapse or disease related death or date of last contact, estimated at 1 year after treatment

InterventionPercent Probability (Number)
Low-Risk Group73.9
Intermediate-Risk Group46.9
High-Risk Group30.8

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Percent Probability of Progression-free Survival (PFS) for Medulloblastoma Patients by DNA Methylation Subgroup

Defined as the time interval from date on treatment until the date of first progression, medulloblastoma-related death or date of last contact for patients who have not experienced an event. Eligible medulloblastoma patients who received any methotrexate and had molecularly confirmed medulloblastoma are included in this analysis. Five patients were excluded as 3 had no archival tissue available and 2 were found to not be medulloblastoma by methylation profile. (NCT00602667)
Timeframe: From date on treatment to date of first progression or relapse or disease related death or date of last contact, estimated at 1 year after treatment

InterventionPercent Probability (Number)
Low-risk SHH Patients73.9
Intermediate-risk SHH Patients50.0
High-risk SHH Patients54.5
Intermediate-risk Group 3 Patients30.8
High-risk Group 3 Patients9.1
Intermediate-risk Group 4 Patients62.5
High-risk Group 4 Patients50.0

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Percentage of Patients With Objective Responses Rate to Induction Chemotherapy

For patients treated in the intermediate and high risk strata with residual or metastatic disease we will estimate the stratum-specific objective response rate (complete response (CR) or partial response [ PR]). All patients who receive at least 1 -dose of methotrexate are evaluable for response. Objective responses must be sustained for at least eight weeks. (NCT00602667)
Timeframe: From on-study date to 2 months after completion of induction chemotherapy (up to 4 months after on-study date)

InterventionPercentage of patients (Number)
Intermediate-Risk Group58.3
High-Risk Group21.1

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Rate of Distant Disease Progression

Distant failure was defined as the interval from end of RT to date of distant failure (or combined local + distant failure). Competing events were local failure or second malignancy. Patients without an event were censored at date of last contact. The 1-year cumulative incidence was estimated and reported with a 95% confidence interval. (NCT00602667)
Timeframe: 1 year after completion of radiation therapy for last patient

Interventionpercentage of participants (Number)
Intermediate-risk Patients Who Received Focal Radiation25.6

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Rate of Local Disease Progression

Local failure was defined as the interval from end of RT to date of local failure (or combined local + distant failure). Competing events were distant failure or second malignancy. Patients without an event were censored at date of last contact. The 1-year cumulative incidence was estimated and reported with a 95% confidence interval. (NCT00602667)
Timeframe: 1 year after completion of radiation therapy for last patient

InterventionPercentage of participants (Number)
Intermediate-risk Patients Who Received Focal Radiation13.2

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Topotecan Apparent Oral Clearance in Maintenance Chemotherapy

Topotecan plasma concentration-time data are collected on day 1 of maintenance cycle A1 after a single oral dose. Individual estimates of topotecan apparent oral clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 0.25, 1.5 and 6 hours post-dose

InterventionL/h (Median)
Low-Risk Group41.4
Intermediate-Risk Group41.0
High-Risk Group44.6

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Topotecan AUC0-24h in Consolidation Chemotherapy

Topotecan plasma concentration-time data are collected on day 1 of consolidation cycle 1 after a single IV dose. Individual estimates of topotecan AUC0-24h (area under concentration curve from time 0 to 24 hours post- dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, 5 min., 1, 3, and 24 hours from end of infusion

Interventionµg·h/L (Median)
Intermediate-Risk Group117
High-Risk Group116

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Topotecan AUC0-24h in Maintenance Chemotherapy

Topotecan plasma concentration-time data are collected on day 1 of maintenance cycle A1 after a single oral dose. Individual estimates of topotecan AUC0-24h (area under concentration curve from time 0 to 24 hours post- dose) are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-dose, 0.25, 1.5, 6, and 24 hours post-dose

Interventionµg·h/L (Median)
Low-Risk Group10.90
Intermediate-Risk Group11.60
High-Risk Group10.33

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Topotecan Clearance in Consolidation Chemotherapy

Topotecan plasma concentration-time data are collected on day 1 of consolidation cycle 1 after a single IV dose. Individual estimates of topotecan clearance are obtained using post hoc analysis. (NCT00602667)
Timeframe: Pre-infusion, 5 min., 1, and 3 hours from end of infusion

InterventionL/h/m^2 (Median)
Intermediate-Risk Group30.3
High-Risk Group26.40

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Event-free Survival (EFS) Rate

EFS will be estimated using the Kaplan-Meier method. The log-rank test will be performed to test the difference in time-to-event distributions between patient groups. Cox proportional hazards model will be utilized to include multiple covariates in the time-to-event analysis. Logistic regression will be utilized to assess the effect of patient prognostic factors on the response rate. (NCT00654732)
Timeframe: From the start of study treatment up to 3 years

InterventionParticipants (Count of Participants)
RABVD17
ABVD20

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Number of Patients Achieving Pathologic Response

Pathological response is defined as down-staging to NCT00808639)
Timeframe: After completion of 4 cycles of chemotherapy with pegfilgrastim support (cycle length 2 weeks)

Interventionpercentage of pathologic responders (Number)
Dose Dense MVAC49

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Number of Patients Experiencing Febrile Neutropenia

Febrile neutropenia defined per CTCAEv3 as Grade 3 or higher and treatment attribution possibly, probably or definitely-related. (NCT00808639)
Timeframe: After completion of 4 cycles of chemotherapy with pegfilgrastim support (cycle length 2 weeks)

Interventionparticipants (Number)
Dose Dense MVAC0

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Percentage of HIV-positive Patients With 2-year Progression-free Survival (PFS) Treated With Initial 2 Cycles of Adriamycin, Bleomycin, Vnblastine, and Dacarbazine (ABVD) Followed by Response-adapted Therapy Based on Interim FDG-PET Imaging.

Disease progression is defined using the 2007 revised Cheson et al. criteria that is at least 50% increase in sum of the product of the diameters (SPD) of target measurable nodal lesions over the smallest sum observed, or >= 50% increase in greatest transverse diameter (GTD) of any nodal > 1 cm in shortest axis, or >= 50% increase in the SPD of other target measurable lesions over the smallest sum observed, any new bone marrow involvement, any new lesion, lymph node with long axis is >1.5 cm or if both long and short axes are > 1 cm, PET positive if patients with no pretreatment PET scan or when PET scan was positive before therapy. progression-free survival is measured from date of registration to date of first observation of progressive disease, or death due to any cause. Patients last known to be alive and progression-free are censored at date of last contact. (NCT00822120)
Timeframe: 2 years

Interventionpercentage of patients (Number)
HIV-positive: 2 Cycles of ABVD Followed by PET-directed Therap83

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Percentage of HIV-positive Patients With 5-year Overall Survival (OS) Treated With 2 Initial Cycles of ABVD Followed by Response-Adapted Therapy Based on Interim FDG-PET Imaging.

Measured from date of registration to date of death due to any cause. Patients last known to be alive and are censored at date of last contact. (NCT00822120)
Timeframe: 5 years

Interventionpercentage of participants (Number)
HIV-positive: 2 Cycles of ABVD Followed by PET-directed Therap89

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Percentage of HIV-negative Patients Who Are PET-positive After 2 Cycles of ABVD With 2-year PFS

Disease progression is defined using the 2007 revised Cheson et al. criteria that is at least 50% increase in sum of the product of the diameters (SPD) of target measurable nodal lesions over the smallest sum observed, or >= 50% increase in greatest transverse diameter (GTD) of any nodal > 1 cm in shortest axis, or >= 50% increase in the SPD of other target measurable lesions over the smallest sum observed, any new bone marrow involvement, any new lesion, lymph node with long axis is > 1.5 cm or if both long and short axes are > 1 cm, PET positive if patients with no pretreatment PET scan or when PET scan was positive before therapy. Progression-free survival is measured from date of registration to date of first observation of progressive disease, or death due to any cause. Patients last known to be alive and progression-free are censored at date of last contact. (NCT00822120)
Timeframe: 2 years

Interventionpercentage of participants (Number)
HIV-negative: 2 Cycles of ABVD Followed by Escalated BEACOPP64

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Complete and Partial Response Rates for HIV-negative Patients Treated With Response- Adapted Therapy Based on FDG-PET Imaging After 2 Cycles of ABVD

Complete Response (CR) is a complete disappearance of all disease with the exception of the following. If no PET scan or when the PET scan was positive before therapy, a post-treatment residual mass of any size is permitted if it is PET negative. If the PET scan was negative before therapy, all nodal masses at baseline must have regressed. No new lesions. Previously enlarged organs must have regressed and not be palpable. Bone marrow (BM) must be negative if positive at baseline. Normalization of markers. Partial Response (PR) is a 50% decrease in the sum of products of greatest diameters (SPD) for up to 6 identified dominant lesions, including spleenic and hepatic nodules from baseline. No new lesions and no increase in the size of liver, spleen or other nodes. If PET scan or when the PET scan was positive before therapy, PET should be positive in at least one previously involved site. (NCT00822120)
Timeframe: 7 months after registration

Interventionpercentage of patients (Number)
PET-negative: Continued ABVD After 2 Cycles of ABVD100
PET-positive: BEACOPP Escalated After 2 Cycles of ABVD93

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Percentage of HIV-negative Patients With 2-year Overall Survival (OS) Treated With 2 Initial Cycles of ABVD Followed by Response-Adapted Therapy Based on Interim FDG-PET Imaging

Measured from date of registration to date of death due to any cause. Patients last known to be alive and are censored at date of last contact. (NCT00822120)
Timeframe: 2 years

Interventionpercentage of participants (Number)
HIV-negative:2 Cycles of ABVD Followed by PET-directed Therapy98

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Percentage of HIV-negative Patients With 2-year Progression-free Survival (PFS) Treated With 2 Initial Cycles of Adriamycin, Bleomycin, Vnblastine, and Dacarbazine (ABVD) Followed by Response-adapted Therapy Based on Interim FDG-PET Imaging.

Disease progression is defined using the 2007 revised Cheson et al. criteria that is at least 50% increase in sum of the product of the diameters (SPD) of target measurable nodal lesions over the smallest sum observed, or >= 50% increase in greatest transverse diameter (GTD) of any nodal > 1 cm in shortest axis, or >= 50% increase in the SPD of other target measurable lesions over the smallest sum observed, any new bone marrow involvement, any new lesion, lymph node with long axis is > 1.5 cm or if both long and short axes are > 1 cm, PET positive if patients with no pretreatment PET scan or when PET scan was positive before therapy. Progression-free survival is measured from date of registration to date of first observation of progressive disease, or death due to any cause. Patients last known to be alive and progression-free are censored at date of last contact. (NCT00822120)
Timeframe: 2 years

Interventionpercentage of participants (Number)
HIV-negative: 2 Cycles of ABVD Followed by PET-directed Therap79

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Overall Response to CVT Chemotherapy.

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and 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 (NCT00885534)
Timeframe: 2 years

Interventionparticipants (Number)
Partial ResponseStable Disease
Cisplatin, Vinblastine, Temozolomide15

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Toxicity Profile of Dose Dense MVAC Given in the Neoadjuvant Setting.

Defined by number of patients who complete all three cycles of treatment without dose reduction (NCT01031420)
Timeframe: Ongoing throughout treatment at each MD visit every 14 days.

Interventionparticipants (Number)
All three cycles of chemotherapy were completedDiscontinued chemotherapy
Dose Dense MVAC373

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Percentage of Participants With Complete Response at Cystectomy or Ureterectomy Following Preoperative Dose Dense MVAC

complete response rate (pT0), as defined by pathologic staging at cystectomy or ureterectomy, following neoadjuvant DD-MVAC chemotherapy. (NCT01031420)
Timeframe: Following completion of the 3rd/final cycle of chemotherapy (about week 9) by CT imaging and at time of surgery for pathologic response.

Interventionpercentage of total participants (Number)
Dose Dense MVAC38

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Complete Response Rate

A Complete Response (CR) was defined as having the following conditions: 1. A complete disappearance of all detectable clinical evidence of disease and disease-related symptoms if present before therapy. 2. In patients with a PET scan that was positive before therapy, a post-treatment residual mass of any size is permitted as long as it is PET-negative. A Complete Response rate was defined as the number of patients who achieved a CR divided by the number of patients that were eligible for analysis in each group. The CR rate was calculated for patients that completed 4 cycles of ABVD and for patients that completed 2 cycles of ABVD and 2 cycles of BEACOPP and IFRT. (NCT01132807)
Timeframe: Up to 5 years

Interventionproportion of participants (Number)
Treatment (ABVD: 4 Cycles).97
Escalated BEACOPP and Involved Field Radiation Therapy.85

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Progression-Free Survival (PFS) at 36-Months for Patients Who Received 4 Cycles of ABVD

The primary objective of this trial is to estimate the 3 year PFS in patients who received 4 cycles of ABVD. PFS for each patient is measured as the time from registration on trial to the first incident of death or progression. The PFS at 36 months is calculated as the number of patients who have a progression-free survival time greater than 36 months divided by the total number of patients that started treatment. For this endpoint, all patients that received 4 cycles of doxorubicin, bleomycin, vinblastine, and dacarbazine (ABVD) are included. (NCT01132807)
Timeframe: 36 Months

Interventionproportion of patients (Number)
Treatment (ABVD: 4 Cycles).91

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36 Month Progression Free Survival Rate of Patients Receiving 4 Cycles of ABVD Versus Patients Receiving 2 Cycles of ABVD and 2 Cycles of BEACOPP and Radiation.

All patients received an initial 2-28 day cycles of doxorubicin, bleomycin, vinblastine, and dacarbazine (ABVD) on Days 1 and 15. After the first 2 cycles of ABVD, PET/CT was performed and submitted for central review (cycle 2, days 23-25) and determined whether patients would receive 2 cycles of escalated BEACOPP and involved-field RT (IFRT) or an additional 2 cycles of ABVD. PFS for each patient is measured as the time from registration on trial to the first incident of death or progression. The PFS rate at 36 months is calculated as the number of patients who have a progression-free survival time greater than 36 months divided by the total number of patients that started treatment. For this endpoint, we compare the PFS rate between patients who received 4 cycles of ABVD and patients who received 2 cycles of ABVD and 2 cycles of IFRT. (NCT01132807)
Timeframe: at 36 months

Interventionproportion of participants (Number)
Treatment (ABVD:4 Cycles).91
Escalated BEACOPP and Involved Field Radiation Therapy.67

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Cycle 1 AUC/Pharmacokinetics of Gamma-secretase Inhibitor RO4929097 in Combination With Temozolomide (Phase IB)

(NCT01196416)
Timeframe: Days 4 and 5

Interventionhr·ng/mL (Mean)
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)5410

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Maximum-tolerated Dose for Cisplatin, Vinblastine and TMZ

"based on the incidence of dose-limiting toxicity as assessed the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0 (Phase IB)~Data is not yet available, as it's currently being analyzed." (NCT01196416)
Timeframe: 21 days

Interventionmg/m2 (Number)
CisplatinVinblastineTemozolomide
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)201.2150

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Progression-free Survival (Phase II)

Progression-free survival curves will be generated using Kaplan-Meier methodology. (NCT01196416)
Timeframe: Time from start of treatment to time of progression or death, whichever occurs first, assessed up to 2 years

Interventionmonths (Median)
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)2.7

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Cycle 1 C Max/Pharmacokinetics of Gamma-secretase Inhibitor RO4929097 in Combination With Temozolomide (Phase IB)

(NCT01196416)
Timeframe: At Cycle 1

Interventionng/mL (Mean)
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)301

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Overall Survival (Phase II)

Overall response rate (complete [CR] or partial response [PR]) according to RECIST version 1.1 (NCT01196416)
Timeframe: Up to 2 years

Interventionparticipants (Number)
Partial ResponseStable DiseaseProgression of Disease
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)356

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Number of Participants With Presence or Absence of Markers of Notch Signalling Pathway Inhibition in Patient Tumors (Phase Ib)

The association of response or clinical benefit with the presence or absence of markers of pathway inhibition in patient tumors will be tested using Fisher's exact test. (NCT01196416)
Timeframe: 2 weeks

InterventionParticipants (Count of Participants)
Insufficient tissue to asses any changeSig decrease in post-treatment cleaved Notch
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)14

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Participants Evaluated for Toxicity

Number of patients with AE's as assessed by NCI CTCAE v. 4.0 Please see Adverse Events section for specifics. (NCT01196416)
Timeframe: Up to 30 days post-treatment

InterventionParticipants (Count of Participants)
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)14

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Maximum Tolerated Dose for RO4929097

based on the incidence of dose-limiting toxicity as assessed the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0 (Phase IB) (NCT01196416)
Timeframe: 21 days

Interventionmg/day (Number)
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)15

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Cycle 1 Mean Day 2 Trough/Pharmacokinetics of Gamma-secretase Inhibitor RO4929097 in Combination With Temozolomide (Phase IB)

(NCT01196416)
Timeframe: At Day 2 of Cycle 1

Interventionng/mL (Mean)
Treatment (RO4929097, Cisplatin, Vinblastine, Temozolomide)129

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Complete Response (CR) Rate After Induction Treatment

Complete response (CR) is defined as complete disappearance of all detectable clinical evidence of disease and disease-related symptoms if present prior to therapy. (NCT01390584)
Timeframe: Assessed at end of Cycle 2

Interventionproportion of participants (Number)
Step 1: Induction Tx1.0

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Proportion of Patients Who Are PET Negative After Induction Treatment

(NCT01390584)
Timeframe: Assessed at end of Cycle 2

Interventionproportion of participants (Number)
Step 1: Induction Tx0.8

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Progression-free Survival Rate

Progression-free survival is defined as the time from study entry to lymphoma progression or death from any cause. Proportion of patients who are progression-free and alive at 36 months will be reported. Progression is defined as appearance of any new lesions more than 1.5 cm in any axis, at least a 50% increase from nadir in sum of the product of the diameters (SPD) of any previously involved nodes or extranodal masses or the size of other lesions, or at least 50% increase in the longest diameter of any single previously identified node or extranodal mass more than 1 cm in its short axis. (NCT01390584)
Timeframe: Assessed at 36 months

Interventionproportion of participants (Number)
ABVD + INRTNA
ABVD + BEACOPP + INRTNA

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Progression-free Survival at 36 Months Among Patients Who Are PET Positive After Induction Treatment

Progression-free survival is defined as the time from study entry to lymphoma progression or death from any cause. Proportion of patients who are progression-free and alive at 36 months will be reported. Progression is defined as appearance of any new lesions more than 1.5 cm in any axis, at least a 50% increase from nadir in sum of the product of the diameters (SPD) of any previously involved nodes or extranodal masses or the size of other lesions, or at least 50% increase in the longest diameter of any single previously identified node or extranodal mass more than 1 cm in its short axis. (NCT01390584)
Timeframe: Assessed at 36 months

Interventionproportion of participants (Number)
ABVD + BEACOPP + INRTNA

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Overall Survival

Overall survival is defined as the time from study entry to death or date last known alive. (NCT01390584)
Timeframe: Assessed at 36 months

Interventionmonths (Median)
ABVD + INRTNA
ABVD + BEACOPP + INRTNA

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Participants' Response

Complete Response (CR): Disappearance of all clinical evidence of active tumors for a minimum of 8 weeks. Partial Response (PR): 50% or greater decrease in sum of products all measured lesions persisting for at least 4 weeks. No Change: Steady state or change of +/- 25% of tumor size and no progression for minimum of 8 weeks with no appearance of new lesions. Progressive Disease: > 25 % increase in size of any measurable lesion or appearance of significant new lesions. (NCT01404936)
Timeframe: After 6 courses (3 months)

Interventionparticipants (Number)
Complete ResponseUncomfirmed Complete ResponsePartial ResponseProgressive Disease
Interferon-2A + Chemotherapy23231

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Grade III or IV Adverse Events

A summary of the grade 3 or 4 adverse events experienced by participants as determined by Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. The data is shown as the number of participants that experienced at least one grade 3 or 4 adverse event for each of the specified toxicities. (NCT01534078)
Timeframe: 2 years

Interventionparticipants (Number)
Peripheral sensory neuropathyNeutrophil count decreasedFatigueNauseaAnemiaWhite blood cell decreasedAbdominal painDiarrheaFebrile neutropeniaVomitingMucositis oralWeight lossDehydrationHypertensionInfections and infestations - Other, specifyBlood and lymphatic system disorders - Other, spec
Treatment Arm821312621121121111

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Overall Response Rate

"The number of participants achieving a Partial Response (PR) or Complete Response (CR) at the end of therapy as measured via PET/CT response. Response is evaluated using the Revised International Working Group Criteria.~CR: Disappearance of all evidence of disease~PR: Regression of measurable disease and no new sites" (NCT01534078)
Timeframe: End of Therapy (median duration of four months)

InterventionParticipants (Count of Participants)
Complete ResponsePartial Response
Treatment Arm310

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Overall Response Rate After One Cycle of Brentuximab

"The number of participants achieving a Partial Response (PR) or Complete Response (CR) after one cycle of Brentuximab monotherapy as measured via PET/CT response. Response is evaluated using the Revised International Working Group Criteria.~CR: Disappearance of all evidence of disease~PR: Regression of measurable disease and no new sites" (NCT01534078)
Timeframe: 28 days

InterventionParticipants (Count of Participants)
Treatment Arm18

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Complete Response Rate

Complete response rate at the end of therapy as measured by Positron emission tomography-computed tomography (PET/CT). Response is evaluated using Revised International Working Group Criteria. Complete response is defined as disappearance of all evidence of disease. (NCT01534078)
Timeframe: End of Therapy (median duration of four months)

InterventionParticipants (Count of Participants)
Treatment Arm31

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Progression Free Survival

Tumor evaluation will be performed every 8 weeks from day 1 of cycle 1 (+/- 1 week) while on therapy assessed by RECIST 1.0 criteria. (NCT01542255)
Timeframe: From date of registration until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 100 months

Interventionweeks (Median)
Single Arm3

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Median CD20 Expression Levels

To estimate median levels of CD20 expression at baseline, during treatment with dexamethasone-containing chemotherapy and following rituximab treatment in Block I of remission induction therapy for relapsed precursor B-cell ALL. (NCT01700946)
Timeframe: Baseline and at the end of Block I (approximately 5 weeks after the on-study date)

,,
Interventionpercentage of CD20 Antigen (Median)
At BaselineAt Block 1
All Patients Enrolled on the Study22.015.58
HIGH RISK23.1319.58
STANDARD RISK16.4011.83

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3-year Overall Survival Rate of Patients With Relapsed ALL

Estimate the 3-year survival rate of participants with first relapse or primary refractory precursor B-cell ALL treated with risk-directed therapy. (NCT01700946)
Timeframe: 3 years of follow-up since the on-study date

Interventionpercentage of participants (Number)
STANDARD RISK94.4
HIGH RISK55.5
All Patients Enrolled on the Study72.63

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3-year Event-free Survival Rates in Patients With Relapsed ALL

Estimate the 3-year event-free survival rate of participants with first relapse or primary refractory precursor B-cell ALL treated with risk-directed therapy. (NCT01700946)
Timeframe: 3 years of follow-up since the on-study date

Interventionpercentage of participants (Number)
STANDARD RISK83.3
HIGH RISK55.7
All Patients Enrolled on the Study67.83

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Mean of CD20 Expression Levels

To estimate mean levels of CD20 expression at baseline, during treatment with dexamethasone-containing chemotherapy and following rituximab treatment in Block I of remission induction therapy for relapsed precursor B-cell ALL. (NCT01700946)
Timeframe: Baseline and at the end of Block I (approximately 5 weeks after the on-study date)

,,
Interventionpercentage of CD20 Antigen (Mean)
At BaselineAt Block I
All Patients Enrolled on the Study36.2319.43
HIGH RISK39.8220.10
STANDARD RISK31.1018.54

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Disease-free Survival (DFS) Per IRF

DFS per IRF was defined as the time from CR to disease progression as determined by an IRF or to death from lymphoma or acute toxicity from treatment. CR was defined as disappearance of all evidence of disease. (NCT01712490)
Timeframe: From CR until PD or death (approximately up to 4 years)

Interventionmonths (Median)
A+AVDNA
ABVDNA

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Duration of Complete Remission (DOCR) Per IRF

DOCR per IRF in participants with CR was the time between first documentation of CR and PD as determined by an IRF. PD was defined as any new lesion or increase by >=50% of previously involved sites from nadir. CR was defined as disappearance of all evidence of disease. (NCT01712490)
Timeframe: From first documentation of CR until PD (approximately 4 years)

Interventionmonths (Median)
A+AVDNA
ABVDNA

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Duration of Response (DOR) Per IRF

DOR per IRF in participants with response was the time between first documentation of response (PR or CR) and PD as determined by an IRF. PD was defined as any new lesion or increase by >=50% of previously involved sites from nadir. CR was defined as disappearance of all evidence of disease. PR was defined as regression of measurable disease and no new sites. (NCT01712490)
Timeframe: From first documented response until PD (approximately 4 years)

Interventionmonths (Median)
A+AVDNA
ABVDNA

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Event-free Survival (EFS) Per IRF

EFS was defined as the time from randomization until any cause of treatment failure: PD, premature discontinuation of randomized treatment for any reason, or death due to any cause, whichever occurs first. PD was defined as any new lesion or increase by >=50% of previously involved sites from nadir per IRF. (NCT01712490)
Timeframe: Baseline until PD or discontinuation of treatment or death, whichever occurs first (approximately up to 4 years)

Interventionmonths (Median)
A+AVDNA
ABVDNA

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Modified Progression-free Survival (mPFS) Per Independent Review Facility (IRF)

mPFS was defined as the time from the date of randomization to the date of the first of documentation of progressive disease (PD), death due to any cause, or for participants who were confirmed non complete responders per IRF, receipt of subsequent anticancer therapy for Hodgkin lymphoma (HL) after completion of frontline therapy. PD was defined as any new lesion or increase by greater than or equal to (>=) 50 percent (%) of previously involved sites from nadir. Frontline therapy is the part of standard set of treatments. (NCT01712490)
Timeframe: Baseline until PD or death or receipt of any subsequent anticancer therapy for HL after completion of frontline therapy (approximately up to 4 years)

Interventionmonths (Median)
A+AVDNA
ABVDNA

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Number of Participants With Abnormal Clinical Laboratory Values

(NCT01712490)
Timeframe: Baseline up to 30 days after last dose of study drug (approximately 1 year)

Interventionparticipants (Number)
A+AVD662
ABVD658

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Overall Response Rate (ORR) Per IRF

ORR per IRF was defined as the percentage of participants who achieved CR or partial remission (PR) at the end of treatment with randomized regimen (ABVD or A+AVD) as determined by an IRF. CR was defined as disappearance of all evidence of disease. PR was defined as regression of measurable disease and no new sites. (NCT01712490)
Timeframe: Baseline up to end of randomized regimen (approximately 1 year)

Interventionpercentage of participants (Number)
A+AVD86
ABVD83

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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 documented death at the time of analysis were censored at the date last known to be alive. (NCT01712490)
Timeframe: Baseline until death (approximately up to 4 years)

Interventionmonths (Median)
A+AVDNA
ABVDNA

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Positron Emission Tomography (PET) Negativity Rate Per IRF at Cycle 2

PET negativity rate at Cycle 2 was defined as the percentage of participants with negative Cycle 2 PET results defined as Deauville score less than or equal to (<=) 3 at Cycle 2. The Deauville score according to IRF assessment of response was used to evaluate the results of PET scans. (NCT01712490)
Timeframe: Cycle 2 Day 25

Interventionpercentage of participants (Number)
A+AVD89
ABVD86

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A+AVD: AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Brentuximab Vedotin ADC and TAb

(NCT01712490)
Timeframe: Cycle 1 Day 1: pre-dose and at multiple timepoints (up to 48 hours) post-dose

Interventionday*microgram per milliliter (day*ug/mL) (Mean)
Cycle 1 Day 1: ADCCycle 1 Day 1: TAb
A+AVD47.493.0

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A+AVD: Cmax: Maximum Observed Plasma Concentration for Brentuximab Vedotin Monomethyl Auristatin E (MMAE)

(NCT01712490)
Timeframe: Cycle 1 Day 1 and Cycle 3 Day 1: pre-dose and at multiple timepoints (up to 48 hours) post-dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Cycle 1 Day 1Cycle 3 Day 1
A+AVD3.201.36

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A+AVD: Cmax: Maximum Observed Serum Concentration for Brentuximab Vedotin Antibody-drug Conjugate (ADC) and Total Antibody (TAb)

(NCT01712490)
Timeframe: Cycle 1 Day 1 and Cycle 3 Day 1: pre-dose and at multiple timepoints (up to 48 hours) post-dose

Interventionmicrogram per milliliter (microgm/mL) (Geometric Mean)
Cycle 1 Day 1: ADCCycle 3 Day 1: ADCCycle 1 Day 1: TAbCycle 3 Day 1: TAb
A+AVD22.923.622.626.4

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A+AVD: Number of Participants With Antitherapeutic Antibody (ATA) and Neutralizing Antitherapeutic Antibody (nATA) Positive for Brentuximab Vedotin

The nATA positive was defined as positive ATA with neutralizing activity at any postbaseline visit. (NCT01712490)
Timeframe: Baseline up to end of treatment (approximately 1 year)

Interventionparticipants (Number)
ATA positivenATA positive
A+AVD10912

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Change From Baseline in Patient-Reported Outcome (PRO) Scores by mPFS Based on European Organization for Research and Treatment of Cancer (EORTC) Quality of Life Questionnaire-C30 (EORTC QLQ-C30) at EOT

EORTC QLQ-C30 included 30 items across 5 functional scales (physical, role, cognitive, emotional, and social), 9 symptom scales (fatigue, nausea and vomiting, pain, dyspnea, insomnia, appetite loss, constipation, diarrhea, and financial difficulties) and global health status/QOL scale. It has 28 questions (4-point scale where 1=not at all [best] to 4=Very Much [worst]) and 2 questions (7-point scale where 1=very poor [worst] to 7= excellent [best]). Raw scores were converted into scale scores from 0 to 100. For functional scales and global health status/QOL scale, higher scores show better QOL; for symptom scales, lower scores show better QOL. mPFS was time from date of randomization to date of first of documentation of PD, death due to any cause, or for participants who were confirmed non complete responders per IRF, receipt of subsequent anticancer therapy for HL after completion of frontline therapy. PD is any new lesion or increase by >=50% of previously involved sites from nadir. (NCT01712490)
Timeframe: Baseline up to end of treatment (approximately 1 year)

,
Interventionunits on scale (Mean)
Baseline: With mPFS eventWithout mPFS eventChange at end of treatment: with mPFS eventChange at end of treatment: without mPFS event
A+AVD78.1579.852.683.35
ABVD76.6879.918.586.08

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Number of Participants Who Experience at Least One Treatment Emergent Adverse Event (TEAE) and Serious Adverse Event (SAE)

(NCT01712490)
Timeframe: Baseline up to 30 days after last dose of study drug (approximately 1 year)

,
Interventionparticipants (Number)
TEAESAE
A+AVD653284
ABVD646178

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Percentage of Participants Not in CR Per IRF Who Received Subsequent Radiation After Completion of Frontline Therapy

CR was defined as disappearance of all evidence of disease as determined by an IRF. (NCT01712490)
Timeframe: Baseline up to end of frontline therapy (approximately 4 years)

Interventionpercentage of participants (Number)
A+AVD8
ABVD13

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A+AVD: AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Brentuximab Vedotin MMAE

(NCT01712490)
Timeframe: Cycle 1 Day 1: pre-dose and at multiple timepoints (up to 48 hours) post-dose

Interventionday*nanogram per milliliter (day*ng/mL) (Mean)
A+AVD25.3

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Complete Remission (CR) Per IRF Rate at the End of Frontline Therapy

CR rate at the end of frontline therapy per IRF was defined as the percentage of participants who achieved CR at the end of frontline therapy that is after completion of either randomized regimen or alternate frontline therapy as determined by an IRF. CR was defined as disappearance of all evidence of disease. (NCT01712490)
Timeframe: Baseline up to end of frontline therapy (approximately 4 years)

Interventionpercentage of participants (Number)
A+AVD73
ABVD71

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Complete Remission (CR) Rate at the End of Randomized Regimen Per IRF

CR rate at the end of randomized regimen per investigator was defined as the percentage of participants who achieved CR at the end of treatment with randomized regimen (ABVD or A+AVD) as determined by IRF. CR was defined as disappearance of all evidence of disease. (NCT01712490)
Timeframe: Baseline up to end of randomized regimen (approximately 1 year)

Interventionpercentage of participants (Number)
A+AVD73
ABVD70

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2-year Progression-free Survival (PFS)

2-year PFS is determined based on the Kaplan-Meier estimates and corresponding 95% confidence intervals based on standard errors using Greenwood's formula. (NCT01771107)
Timeframe: 2 years

Interventionproportion of participants (Number)
Phase I - Brentuximab 1.2 mg/kg1.0
Phase II - Brentuximab 1.2 mg/kg0.84

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CD8 Counts

Absolute CD8 counts at cycle 5 (NCT01771107)
Timeframe: 5 months

Interventioncells/µL (Median)
Phase I - Brentuximab 1.2 mg/kg719.5
Phase II - Brentuximab 1.2 mg/kg666.5

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Complete Response Rate

Number of participants who experienced a complete response per RECIST v1.0 criteria (NCT01771107)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Phase I - Brentuximab 1.2 mg/kg6
Phase II - Brentuximab 1.2 mg/kg32

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Characterization of Histologic Subtypes in HIV-HL in the HAART Era

Participants with mixed cellularity histologic subtype (NCT01771107)
Timeframe: Baseline

InterventionParticipants (Count of Participants)
Phase I - Brentuximab 1.2 mg/kg2
Phase II - Brentuximab 1.2 mg/kg13

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Frequency of Adverse Events

Number of Participants who had one or more adverse events (NCT01771107)
Timeframe: Up to 5 years

InterventionParticipants (Count of Participants)
Phase I - Brentuximab 1.2 mg/kg6
Phase II - Brentuximab 1.2 mg/kg35

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2-year Overall Survival

Proportion of study participants who are alive at 2 years estimated using the Kaplan-Meier survival function (NCT01771107)
Timeframe: 2 years

Interventionproportion of participants (Number)
Phase I - Brentuximab 1.2 mg/kg1.0
Phase II - Brentuximab 1.2 mg/kg0.91

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CD4 Counts

CD4 counts (absolute) at visit 4 (cycle 5) (NCT01771107)
Timeframe: 5 months

Interventioncells/µL (Median)
Phase I - Brentuximab 1.2 mg/kg378
Phase II - Brentuximab 1.2 mg/kg401

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Event-free Survival

Proportion of participants who are alive and progression-free at 2 years (NCT01771107)
Timeframe: 2 years

Interventionproportion of participants (Number)
Phase I - Brentuximab 1.2 mg/kg1.0
Phase II Brentuximab 1.2 mg/kg0.84

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Incidence of Neurotoxicity

Number of participants who experience neurotoxicity at cycle 5 (visit 4) (NCT01771107)
Timeframe: 5 months

InterventionParticipants (Count of Participants)
Phase I - Brentuximab 1.2 mg/kg4
Phase II - Brentuximab 1.2 mg/kg23

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Maximal Tolerated Dose of Brentuximab Vedotin (Phase I)

Defined as the dose level at which =< 1 of 6 subjects experience dose limiting toxicity. (NCT01771107)
Timeframe: 28 days

Interventionmg/kg (Number)
Treatment (Brentuximab and Combination Chemotherapy)1.2

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Partial Response Rate

Number of participants who achieved a partial response per RECIST v1.0 criteria (NCT01771107)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Phase I - Brentuximab 1.2 mg/kg1
Phase II - Brentuximab 1.2 mg/kg4

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Viral Load

HIV viral load (detectable) (NCT01771107)
Timeframe: 5 months

InterventionParticipants (Count of Participants)
Phase I - Brentuximab 1.2 mg/kg1
Phase II - Brentuximab 1.2 mg/kg7

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Progression-free Survival

"Progression-free survival (PFS) defined as the time from randomization to the first documented progression (as per RECIST v1.1) or death (due to any cause), whichever occurs first. Patients alive and progression free were censored at the date of last follow-up, death, or last patient contact. Progression is assessed as per RECIST v1.1. Progression-free survival is estimated as a function of time using Kaplan-Meier method.~1- and 2-year PFS rates were reported." (NCT01876082)
Timeframe: Randomization to disease progression, or death due to any cause, whichever occurs first; until 2 years after the last patient randomized.

,
Interventionpercentage of participants (Number)
PFS rate at 1 yearPFS rate at 2 years
PAZOPANIB84.865.2
Vinblastine and Methotrexate68.668.6

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Percentage of Patients Remaining Alive With Best Overall Response as Per RECIST v1.1.

"Best overall response is defined as the best response across all time points (RECIST v1.1). The best overall response is determined once all the data for the participant is known.~Each patient has been assigned one of the following categories (RECIST 1.1): complete response (disappearance of all target lesions); partial response (>=30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum diameters); progression (20% increase in the sum of diameters of target lesions (taking as reference the smallest sum on study) and stable disease (nor CR, PR or progression)." (NCT01876082)
Timeframe: 1 year

,
Interventionpercentage of participants (Number)
Complete responsePartial responseStable diseaseProgressionInevaluable for response
PAZOPANIB041.354.44.40
Vinblastine and Methotrexate030.045.020.05.0

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Overall Survival

Overall survival (OS) defined as the time from randomization to death (due to any cause). Patients alive were censored at the date of last follow-up or last patient contact. Overall survival was estimated as a function of time using Kaplan-Meier method.1- and 2-Year OS rates were reported. (NCT01876082)
Timeframe: Randomization to disease progression, or death due to any cause, whichever occurs first; until 2 years after the last patient randomized.

,
InterventionPercentage of participants (Number)
OS rate at 1 yearOS rate at 2 years
PAZOPANIB100.097.8
Vinblastine and Methotrexate100.0100.0

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Percentage of Patients Remaining Alive and Progression-free at 6 Months as Per RECIST 1.1 After the Day of Randomisation (6-month Non-progression Rate).

"Percentage of patients remaining alive and progression-free at 6 months as per RECIST 1.1 after the day of randomisation.~Progression is defined using New Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1), as a 20% increase in the sum of diameters of target lesions (taking as reference the smallest sum on study), or a unequivocal progression of existing non-target lesions, or the appearance of one or more new lesions." (NCT01876082)
Timeframe: 6 months

Interventionpercentage of participants (Number)
PAZOPANIB84.8
Vinblastine and Methotrexate45.0

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Assessment of Whether the Treatment-specific COXEN Score is Prognostic of pT0 Rate

"The proportion of participants achieving pT0 in both favorable and unfavorable treatment specific-COXEN score categories.~Unit of measure is the number of participants in each category that achieved pT0~_____________________________________________________________________________________________________________________~The relationship of dose-dense methotrexate, vinblastin, doxorubicin, and cisplatin (DDMVAC)- and gemcitabine+cisplatin (GC)- specific CO-eXpression ExtrapolatioN (COXEN) scores~This will be done in two ways:~By assessing whether the treatment-specific COXEN score is prognostic of pT0 rate or ≤ pT1 in this patient population and to assess in a preliminary fashion whether the COXEN score is a predictive factor distinguishing between these two chemotherapy regimens. .~By evaluating the correlation between the GC- and the DDMVAC-COXEN score." (NCT02177695)
Timeframe: Up to 5 years post registration

,
InterventionParticipants (Count of Participants)
Favorable treatment-COXEN scoreUnfavorable treatment-COXEN score
Dose Dense MVAC1017
Gemcitabine & Cisplatin820

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Correlation Between GC-and ddMVAC-COXEN Score

"The Pearson and Spearman correlation coefficients for GC-and ddMVAC-COXEN score were calculated and are reported below.~___________________________________________________________________________________________________________________ The relationship of dose-dense methotrexate, vinblastin, doxorubicin, and cisplatin (DDMVAC)- and gemcitabine+cisplatin (GC)- specific CO-eXpression ExtrapolatioN (COXEN) scores~This will be done in two ways:~By assessing whether the treatment-specific COXEN score is prognostic of pT0 rate or ≤ pT1 in this patient population and to assess in a preliminary fashion whether the COXEN score is a predictive factor distinguishing between these two chemotherapy regimens. .~By evaluating the correlation between the GC- and the DDMVAC-COXEN score." (NCT02177695)
Timeframe: up to 5 years post-registration

Interventioncorrelation coefficient (Number)
Pearson correlation coefficientSpearman correlation coefficient
All Participants0.3850.386

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Predictability of the CO-eXpression ExtrapolatioN (COXEN) Score to Direct Which of the Two Regimens the Patient Should Receive: Gemcitabine+Cisplatin (GC) Versus Dose-dense Methotrexate, Vinblastin, Doxorubicin, and Cisplatin (DDMVAC)

In addition to stratification factors and dichotomous COXEN GEM score, an indicator for treatment arm and the interaction of treatment arm with COXEN GEM score was also included in a logistic regression model. A significant interaction would suggest that the respective COXEN GEM score was able to differentiate whether a patient was more likely to respond to one chemotherapy regimen over another. *note that this is the same objective at Primary Outcome #3 above - this was erroneously listed twice in the protocol. (NCT02177695)
Timeframe: Up to 5 years post registration

Interventionp-value (Number)
Pvalue of interaction term (GCscore*treatment arm) in model predicting pT0Pvalue of interaction term (GCscore*treatment arm) in model predicting <=pT1Pvalue of interaction term (MVACscore*treatment arm) in model predicting pT0Pvalue of interaction term (MVACscore*treatment arm) in model predicting <=pT1
All Participants0.880.430.660.85

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Assessment of Whether the Treatment-specific COXEN Score is Prognostic of ≤ pT1 Rate

"The proportion of participants achieving <=pT1 in both favorable and unfavorable treatment specific-COXEN score categories.~Unit of measure is the number of participants in each category that achieved <= pT1~____________________________________________________________________________________________________________________ The relationship of dose-dense methotrexate, vinblastin, doxorubicin, and cisplatin (DDMVAC)- and gemcitabine+cisplatin (GC)- specific CO-eXpression ExtrapolatioN (COXEN) scores~This will be done in two ways:~By assessing whether the treatment-specific COXEN score is prognostic of pT0 rate or ≤ pT1 in this patient population and to assess in a preliminary fashion whether the COXEN score is a predictive factor distinguishing between these two chemotherapy regimens. .~By evaluating the correlation between the GC- and the DDMVAC-COXEN score." (NCT02177695)
Timeframe: up to 5 years post-registration

,
InterventionParticipants (Count of Participants)
Favorable treatment-COXEN scoreUnfavorable treatment-COXEN score
Dose Dense MVAC1631
Gemcitabine & Cisplatin1030

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Pathologic T0 Rate Evaluation: Gemcitabine+Cisplatin (GC) Versus Dose-dense Methotrexate, Vinblastin, Doxorubicin, and Cisplatin (DDMVAC)

Pathologic complete response rate at the time of cystectomy following GC or DDMVAC treatment (NCT02177695)
Timeframe: Up to 5 years post-registration

Interventionpercentage of participants (Number)
Gemcitabine & Cisplatin28
Dose Dense MVAC30

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Assessment of COXEN Score as a Predictive Factor Distinguishing Between GC and ddMVAC

"To assess in a hypothesis generating fashion, the ability of COXEN to select for an individual chemotherapy regimen (GC vs DDMVAC)~P-values are reported as a measure of whether COXEN can select between GC/DDMVAC and to determine the significance of interactions between treatment specific COXEN scores and treatment arms in models predicting either pT0 or <= pT1. Interactions with p-values > 0.05 are interpreted as not significant.~________ The relationship of dose-dense methotrexate, vinblastin, doxorubicin, and cisplatin (DDMVAC)- and gemcitabine+cisplatin (GC)- specific CO-eXpression ExtrapolatioN (COXEN) scores~This will be done in two ways:~By assessing whether the treatment-specific COXEN score is prognostic of pT0 rate or ≤ pT1 in this patient population and to assess in a preliminary fashion whether the COXEN score is a predictive factor distinguishing between these two chemotherapy regimens. .~By evaluating the correlation between the GC- and the DDMVAC-COXEN score." (NCT02177695)
Timeframe: up to 5 years post-registration

Interventionp-value (Number)
P-value of interaction term (GCscore*treatment arm) in model predicting pT0P-value of interaction term (GCscore*treatment arm) in logistic regression model predicting <=pT1P-value of interaction term (MVACscore*treatment arm) in logistic regression model predicting pT0P-value of interaction term (MVACscore*treatment arm) in logistic regression model predicting <=pT1
All Participants0.880.430.660.85

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Number of Participants With Laboratory Abnormalities in Specific Thyroid Tests in Cohort D Monotherapy Phase

The number of participants with laboratory abnormalities in specific thyroid tests based on SI conventional units. TSH = Thyroid Stimulating Hormone LLN = Lower Limit of Normal ULN = Upper Limit of Normal (NCT02181738)
Timeframe: From first dose of monotherapy to 30 days after last dose of monotherapy phase (up to approximately 3 months)

InterventionParticipants (Count of Participants)
TSH > ULNTSH > ULN WITH TSH <= ULN AT BASELINETSH >ULN WITH ATLEAST ONE FT3/FT4 TEST VALUE TSH >ULN WITH ALL OTHER FT3/FT4 TEST VALUES >= LLNTSH > ULN WITH FT3/FT4 TEST MISSINGTSH < LLNTSH = LLN AT BASELINETSH ULNTSH TSH < LLN WITH FT3/FT4 TEST MISSING
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)1100155104

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Number of Participants With Select AEs in Cohort D

An Adverse Event (AE) is defined as any new untoward medical occurrence or worsening of a preexisting medical condition in a clinical investigation participant administered study drug and that does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (such as an abnormal laboratory finding), symptom, or disease temporally associated with the use of study drug, whether or not considered related to the study drug. Toxicities were graded using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. Select AEs have been categorized into seven areas: pulmonary toxicity, gastrointestinal toxicity, hepatotoxicity, endocrinopathy, skin toxicity, neurological toxicity and renal toxicity. Select AEs, in particular pneumonitis, are considered clinically meaningful as they require greater vigilance and for early recognition and prompt intervention. (NCT02181738)
Timeframe: From first dose of the considered therapy phase to 30 days after last dose of study therapy phase (or up to first dose of combination if any when considering the monotherapy period) (an average of 8 months and a maximum of 11 months)

InterventionParticipants (Count of Participants)
Gastrointestinal MonotherapyGastrointestinal Combination TherapyHepatic MonotherapyHepatic Combination TherapyPulmonary MonotherapyPulmonary Combination TherapyRenal MonotherapyRenal Combination TherapySkin MonotherapySkin Combination TherapyHypersensitivity/Infusion Reactions MonotherapyHypersensitivity/Infusion Reactions Combination
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)613230310179164

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Treatment Discontinuation Rate in Cohort D

"Treatment discontinuation rate (TDR) is the number of treated participants who received <4 doses of monotherapy or <12 doses of their assigned combination regimen. A participant is considered as having received an AVD/NAVD dose as soon as they received at least one drug of AVD/NAVD for the considered dose. Participants must have received at least one dose of Nivolumab during the combination therapy phase to be included in participants treated with NAVD. If a participant subsequently met Criteria to Resume Nivolumab Dosing, the combination of nivolumab and AVD could be used. Participants who underwent treatment beyond progression during the Monotherapy phase could use the combination of nivolumab and AVD if all 4 doses of nivolumab monotherapy are completed.~Discontinuation can be due to any reason including, but not limited to, drug-related toxicity, diseases progression, or death." (NCT02181738)
Timeframe: From first dose up until the date of treatment discontinuation (up to approximately 100 months).

InterventionParticipants (Count of Participants)
MonotherapyCombination Therapy (receiving AVD or NAVD)Combination Therapy (NAVD receivers only)Overall Therapy
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)2556

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Number of Participants With Serious Adverse Events (SAEs) in Cohort D

A Serious Adverse Event (SAE) is any untoward medical occurrence that at any dose results in death, is life-threatening (defined as an event in which the participant was at risk of death at the time of the event; it does not refer to an event which hypothetically might have caused death if it were more severe), requires inpatient hospitalization or causes prolongation of existing hospitalization. Toxicities were graded using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. (NCT02181738)
Timeframe: From first dose of the considered therapy phase to 30 days after last dose of study therapy phase (or up to first dose of combination if any when considering the monotherapy period) (an average of 8 months and a maximum of 11 months)

InterventionParticipants (Count of Participants)
MonotherapyCombination Therapy (receiving AVD or NAVD)
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)210

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Complete Response (CR) Rate at Planned End of Therapy Based on IRRC Assessments in Cohort D

"CR rate is the percent of participants who show CR (disappearance of all evidence of disease) according to the 2007 IWG criteria at the planned end of study therapy radiographic tumor assessment.~Confidence interval based on the Klopper and Pearson method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months)

InterventionPercent of Participants (Number)
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)66.7

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Duration of Complete Remission (CR) Based on IRRC Assessments for Cohorts A, B, and C

"The duration of CR was only evaluated in participants with BOR of CR and was defined as the time from first documentation of CR (the date of first negative FDG-PET scan or the date of first documentation of no disease involvement in the bone marrow (if required), whichever occurred later) to the date of initial objectively documented progression (Any new lesion or increase by >=50% of previously involved sites from nadir) as determined using the 2007 IWG criteria or death due to any cause, whichever occurred first. Censoring was applied as per DOR definition.~Computed using Kaplan-Meier method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months)

InterventionMonths (Median)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin43.47
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant30.32
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant26.41

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Duration of Objective Response (DOR) Based on Investigator Assessments in Cohorts A, B, and C

"DOR is the time from first response (complete remission (CR) or partial remission (PR)) to the date of initial objectively documented progression as determined using the 2007 IWG criteria or death due to any cause, whichever occurred first. For participants who neither progressed nor died, the DOR was censored on the date of their last tumor assessment. Participants who started subsequent therapy without a prior reported progression were censored at the last tumor assessments prior to initiation of the subsequent anticancer therapy.~CR is the percent of participants with a best overall response (BOR) of CR (disappearance of all evidence of disease) according to the 2007 IWG criteria, based on IRRC assessment.~PR is the percent of participants with a best overall response (BOR) of PR (regression of measurable disease and no new sites) according to the 2007 IWG criteria, based on IRRC assessment.~Computed using Kaplan-Meier method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months)

InterventionMonths (Median)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin39.10
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant25.26
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant28.85

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Duration of Objective Response Based on IRRC Assessments in Cohorts A, B, and C

"DOR is the time from first response (complete remission (CR) or partial remission (PR)) to the date of initial objectively documented progression as determined using the 2007 IWG criteria or death due to any cause, whichever occurred first. For participants who neither progressed nor died, the DOR was censored on the date of their last tumor assessment. Participants who started subsequent therapy without a prior reported progression were censored at the last tumor assessments prior to initiation of the subsequent anticancer therapy.~CR is the percent of participants with a best overall response (BOR) of CR (disappearance of all evidence of disease) according to the 2007 IWG criteria, based on IRRC assessment.~PR is the percent of participants with a best overall response (BOR) of PR (regression of measurable disease and no new sites) according to the 2007 IWG criteria, based on IRRC assessment.~Computed using Kaplan-Meier method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months).

InterventionMonths (Median)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin26.18
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant16.59
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant18.17

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Duration of PR Based on IRRC Assessments in Cohorts A, B, and C

"The duration of PR was only evaluated in participants with BOR of PR and was defined as the time from first documentation of PR (regression of measurable disease and no new sites) to the date of initial objectively documented progression (any new lesion or increase by >=50% of previously involved sites from nadir) as determined using the 2007 IWG criteria or death due to any cause, whichever occurred first. Censoring was applied as per DOR definition.~Computed using Kaplan-Meier method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months)

InterventionMonths (Median)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin12.78
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant10.58
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant14.65

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Number of Participants With Laboratory Abnormalities in Specific Liver Tests in Cohort D Combination Therapy Phase

The number of participants with laboratory abnormalities in specific liver tests based on SI conventional units. ALT = Alanine Aminotransferase, AST = Aspartate Aminotransferase, ULN = Upper Limit of Normal. (NCT02181738)
Timeframe: From first dose of the combination therapy to 30 days after last dose of combination therapy (an average of 8 months and a maximum of 11 months)

InterventionParticipants (Count of Participants)
ALT OR AST > 3XULNALT OR AST> 5XULNALT OR AST> 10XULNALT OR AST > 20XULNTOTAL BILIRUBIN > 2XULNALT/AST ELEV>3XULN;TOTAL BILIRUBIN>2XULN IN 1 DAYALT/AST ELEV>3XULN;TOTAL BILIRUBIN>2XULN IN 30 DAYS
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)4110000

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Objective Response Rate (ORR) Based on IRRC Assessments in Cohorts A, B, and C

"ORR is the percent of participants achieving either a complete remission (CR) or partial remission (PR) according to the 2007 IWG criteria. Analyses of efficacy endpoints were performed separately for each cohort, according to IWG 2007. For cohort A and B, if the bone marrow was involved by lymphoma before treatment, the infiltrate must have cleared on repeat bone marrow biopsy. For cohort C, no evidence of FDG-avid disease in bone marrow was required in all participants in lieu of bone marrow aspirate/ biopsy.~CR is the percent of participants with a best overall response (BOR) of CR (disappearance of all evidence of disease) according to the 2007 IWG criteria, based on IRRC assessment.~PR is the percent of participants with a best overall response (BOR) of PR (regression of measurable disease and no new sites) according to the 2007 IWG criteria, based on IRRC assessment.~Confidence interval based on Clopper-Pearson method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, whichever occurred first (up to approximately 28 months)

InterventionPercentage of Particpants (Number)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin65.1
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant67.5
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant73.0

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Complete Remission (CR) Rate Based on IRRC Assessments in Cohorts A, B, and C

"The CR rate was defined as the percent of participants with a BOR of CR (disappearance of all evidence of disease) according to the 2007 IWG criteria, based on IRRC assessment.~Confidence interval based on Clopper-Pearson method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months)

InterventionPercentage of Participants (Number)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin31.7
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant13.8
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant21

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Objective Response Rate (ORR) Based on IRRC Assessments in Cohorts A, B, and C Extended Collection

Represents an updated version of the primary endpoint to include additional data collection that occurred after the primary completion date. (Assessments were made until 30 Nov 2022). Clinical benefit of nivolumab, as measured by ORR per IRRC assessment, and defined as percent of participants achieving either complete remission (CR) or partial remission (PR) according to the 2007 IWG criteria. For cohort A and B, if the bone marrow was involved by lymphoma before treatment, the infiltrate must have cleared on repeat bone marrow biopsy. For cohort C, no evidence of FDG-avid disease in bone marrow was required in all patients in lieu of bone marrow aspirate/ biopsy. CR is the percent of participants with a best overall response (BOR) of CR (disappearance of all evidence of disease) according to the 2007 IWG criteria. PR is the percent of participants with a best overall response (BOR) of PR (regression of measurable disease and no new sites) according to the 2007 IWG criteria. (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, whichever occurred first (up to approximately 100 months)

InterventionPercentage of Participants (Number)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin65.1
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant71.3
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant75.0

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Objective Response Rates (ORR) Based on Investigator Assessments for Cohorts A, B, and C

"ORR is the percent of participants achieving either a complete remission (CR) or partial remission (PR) according to the 2007 IWG criteria. Analyses of efficacy endpoints were performed separately for each cohort, according to IWG 2007. For cohort A and B, if the bone marrow was involved by lymphoma before treatment, the infiltrate must have cleared on repeat bone marrow biopsy. For cohort C, no evidence of FDG-avid disease in bone marrow was required in all participants in lieu of bone marrow aspirate/ biopsy.~CR is the percent of participants with a best overall response (BOR) of CR (disappearance of all evidence of disease) according to the 2007 IWG criteria, based on IRRC assessment.~PR is the percent of participants with a best overall response (BOR) of PR (regression of measurable disease and no new sites) according to the 2007 IWG criteria, based on IRRC assessment.~Confidence interval based on Clopper-Pearson method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months)

InterventionPercentage of Participants (Number)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin69.8
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant73.8
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant70.0

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Partial Remission (PR) Rate Based on IRRC Assessments in Cohorts A, B, and C

"The PR rate was defined as the percent of participants with a BOR of PR (regression of measurable disease and no new sites) according to the 2007 IWG criteria, based on IRRC assessment.~Confidence interval based on Clopper-Pearson method." (NCT02181738)
Timeframe: From first dose to the date of initial objectively documented progression or the date of subsequent therapy, or death whichever occurred first (up to approximately 100 months)

InterventionPercentage of Participants (Number)
Cohort A: Post-Transplant, Never Taken Brentuximab Vedotin33.3
Cohort B: Post Transplant, Brentuximab Vedotin Taken Post-Autologous Stem Cell Transplant57.5
Cohort C: Post Transplant, Brentuximab Vedotin Taken Pre-and/or Post-Autologous Stem Cell Transplant54.0

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Number of Participants Laboratory Abnormalities in Specific Thyroid Tests in Cohort D Combination Therapy Phase

The number of participants with laboratory abnormalities in specific thyroid tests based on SI conventional units. TSH = Thyroid Stimulating Hormone LLN = Lower Limit of Normal ULN = Upper Limit of Normal (NCT02181738)
Timeframe: From first dose of the combination therapy to 30 days after last dose of combination therapy (an average of 8 months and a maximum of 11 months)

InterventionParticipants (Count of Participants)
TSH > ULNTSH > ULN WITH TSH <= ULN AT BASELINETSH >ULN WITH ATLEAST ONE FT3/FT4 TEST VALUE TSH >ULN WITH ALL OTHER FT3/FT4 TEST VALUES >= LLNTSH > ULN WITH FT3/FT4 TEST MISSINGTSH < LLNTSH = LLN AT BASELINETSH ULNTSH TSH < LLN WITH FT3/FT4 TEST MISSING
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)12831855104

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Number of Participants Who Died in Cohort D

Number of participants who died in Cohort D within 100 days after last dose of study therapy. (NCT02181738)
Timeframe: From first dose of the considered therapy phase to 100 days after last dose of study therapy phase (or up to first dose of combination if any when considering the monotherapy period) (an average of 10 months up to a maximum of 13 months)

InterventionParticipants (Count of Participants)
MonotherapyCombination Therapy (receiving AVD or NAVD)
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)01

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Number of Participants With Adverse Events (AEs) in Cohort D

An Adverse Event (AE) is defined as any new untoward medical occurrence or worsening of a preexisting medical condition in a clinical investigation participant administered study drug and that does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (such as an abnormal laboratory finding), symptom, or disease temporally associated with the use of study drug, whether or not considered related to the study drug. Toxicities were graded using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. (NCT02181738)
Timeframe: From first dose of the considered therapy phase to 30 days after last dose of study therapy phase (or up to first dose of combination if any when considering the monotherapy period) (an average of 8 months and a maximum of 11 months)

InterventionParticipants (Count of Participants)
MonotherapyCombination Therapy (receiving AVD or NAVD)
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)4849

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Number of Participants With AEs Leading to Discontinuation in Cohort D

An Adverse Event (AE) is defined as any new untoward medical occurrence or worsening of a preexisting medical condition in a clinical investigation participant administered study drug and that does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (such as an abnormal laboratory finding), symptom, or disease temporally associated with the use of study drug, whether or not considered related to the study drug. Toxicities were graded using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. (NCT02181738)
Timeframe: From first dose of the considered therapy phase to 30 days after last dose of study therapy phase (or up to first dose of combination if any when considering the monotherapy period) (an average of 8 months and a maximum of 11 months)

InterventionParticipants (Count of Participants)
MonotherapyCombination Therapy (receiving AVD or NAVD)
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)13

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Number of Participants With AEs Leading to Dose Delay in Cohort D

An Adverse Event (AE) is defined as any new untoward medical occurrence or worsening of a preexisting medical condition in a clinical investigation participant administered study drug and that does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (such as an abnormal laboratory finding), symptom, or disease temporally associated with the use of study drug, whether or not considered related to the study drug. Toxicities were graded using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. (NCT02181738)
Timeframe: From first dose of the considered therapy phase to 30 days after last dose of study therapy phase (or up to first dose of combination if any when considering the monotherapy period) (an average of 8 months and a maximum of 11 months)

InterventionParticipants (Count of Participants)
MonotherapyCombination Therapy (receiving AVD or NAVD)
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)329

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Number of Participants With Laboratory Abnormalities in Specific Liver Tests in Cohort D Monotherapy Phase

The number of participants with laboratory abnormalities in specific liver tests based on SI conventional units. ALT = Alanine Aminotransferase, AST = Aspartate Aminotransferase, ULN = Upper Limit of Normal. (NCT02181738)
Timeframe: From first dose of monotherapy to 30 days after last dose of monotherapy phase (up to approximately 3 months)

InterventionParticipants (Count of Participants)
ALT OR AST > 3XULNALT OR AST> 5XULNALT OR AST> 10XULNALT OR AST > 20XULNTOTAL BILIRUBIN > 2XULNALT/AST ELEV>3XULN;TOTAL BILIRUBIN>2XULN IN 1 DAYALT/AST ELEV>3XULN;TOTAL BILIRUBIN>2XULN IN 30 DAYS
Cohort D: Newly Diagnosed, Previously Untreated Advanced Stage cHL (Stage IIB, III and IV)2100000

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Cumulative Incidence of Cancer-specific Death at 24 Months

Cancer-specific survival was defined as the time from registration to death due to cancer; deaths due to other causes are counted as competing events. Cancer-specific survival was analyzed using Gray's method and cumulative incidence of cancer-specific death at 24 months is reported. (NCT02412670)
Timeframe: Assessed every 3 months for 2 years

Interventionproportion of patients died of cancer (Number)
Arm A (Methotrexate, Vinblastine, Doxorubicin, Cisplatin)0.09
Arm B (Gemcitabine, Carboplatin)0.20

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Complete Pathologic Response Rate

Complete pathologic response is defined as pT0pN0 (no evidence of disease) as assessed by pathologic evaluation of nephrectomy/ureterectomy and any identifiable regional lymph nodes. (NCT02412670)
Timeframe: Assessed at nephroureterectomy or regional lymph node dissection (21-60 days from completion of chemotherapy; chemotherapy was administered for a total of 4 cycles; cycle length is 14 days and 21 days for arms A and B, respectively)

Interventionproportion of participants (Number)
Arm A (Methotrexate, Vinblastine, Doxorubicin, Cisplatin)0.103
Arm B (Gemcitabine, Carboplatin)0.167

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Proportion of Patients With Renal Insufficiency at Completion of Chemotherapy

Renal insufficiency is defined as CrCl < 60 ml/min. (NCT02412670)
Timeframe: Assessed at completion of chemotherapy; at 8 weeks for Arm A and 12 weeks for Arm B

Interventionproportion of participants (Number)
Arm A (Methotrexate, Vinblastine, Doxorubicin, Cisplatin)0.2
Arm B (Gemcitabine, Carboplatin)0.833

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Recurrence-free Survival

Recurrence-free survival is defined as the time from the date of surgery to disease recurrence or death from any cause. Patients alive without documented recurrence will be censored at the date of last disease assessment. (NCT02412670)
Timeframe: Assessed every 3 months for 2 years; and every 6 months for 3-5 years

Interventionmonths (Median)
Arm A (Methotrexate, Vinblastine, Doxorubicin, Cisplatin)NA
Arm B (Gemcitabine, Carboplatin)8.5

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Proportion of Patients With Renal Insufficiency at Completion of Surgery

Renal insufficiency is defined as CrCl < 60 ml/min. (NCT02412670)
Timeframe: Assessed at completion of surgery (21-60 days from completion of chemotherapy; chemotherapy was administered for a total of 4 cycles; cycle length is 14 days and 21 days for arms A and B, respectively)

Interventionproportion of participants (Number)
Arm A (Methotrexate, Vinblastine, Doxorubicin, Cisplatin)0.69
Arm B (Gemcitabine, Carboplatin)0.833

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Event-free Survival

Event-free survival is defined as the time from registration to the earliest occurrence of recurrence of any type, disease progression, new invasive primary cancer, or death from any cause. Disease progression will be assessed using RECIST 1.1. Disease progression is defined as appearance of one or more new lesions, unequivocal progression of existing non-target lesions, or at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study. In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. (NCT02412670)
Timeframe: Assessed every 3 months for 2 years, and every 6 months for 3-5 years

Interventionmonths (Median)
Arm A (Methotrexate, Vinblastine, Doxorubicin, Cisplatin)NA
Arm B (Gemcitabine, Carboplatin)10.2

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Bladder Cancer-free Survival

Bladder cancer-free survival was defined as the time from the date of surgery to the earlier of a return of bladder cancer or death from any cause. Patients alive without documented bladder cancer were censored at the date of last disease assessment. (NCT02412670)
Timeframe: Assessed every 3 months for 2 years, and every 6 months for 3-5 years

Interventionmonths (Median)
Arm A (Methotrexate, Vinblastine, Doxorubicin, Cisplatin)NA
Arm B (Gemcitabine, Carboplatin)NA

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Phase 2: Immune Reconstitution-Change From Baseline in Haemophilus Influenzae B Antibody, IgG at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Interventionµg/mL (Mean)
BaselineChange from Baseline at EOT
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD9.50-6.03
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD10.39-7.00

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Phase 1: Percentage of Participants Achieving CR Per IRF Assessment Per IWG Criteria in ATA Positive and ATA Negative Participants

CR was defined as the disappearance of all evidence of disease as assessed by IRF as per IWG Criteria. The data is reported per ATA status as categories. This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Up to 24 months

Interventionpercentage of participants (Number)
ATA Negative who Achieved CRTransiently ATA Positive who Achieved CR
Phase 1: Brentuximab Vedotin 48 mg/m^2 + AVD86100

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Phase 2: Percentage of Participants Who Experienced SAEs From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: From first dose in Cycle 1 Day 1 until 30 days after the last dose of study drug in Cycle 6 Day 15 (up to Cycle 7 Day 15) (Cycle length=28 days)

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD45
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD41

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Phase 2: Median Tmax of Brentuximab Vedotin and TAb in Serum

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionhour (Median)
Tmax of Brentuximab Vedotin at Cycle 1 Day 1Tmax of Brentuximab Vedotin at Cycle 1 Day 15Tmax of Brentuximab Vedotin at Cycle 3 Day 1Tmax of Brentuximab Vedotin at Cycle 3 Day 15Tmax of TAb at Cycle 1 Day 1Tmax of TAb at Cycle 1 Day 15Tmax of TAb at Cycle 3 Day 1Tmax of TAb at Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.001.001.001.001.001.001.001.00
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.031.001.001.001.011.001.001.00

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Phase 2: Mean Serum Cmax of Brentuximab Vedotin and TAb

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionµg/mL (Mean)
Cmax of Brentuximab Vedotin at Cycle 1 Day 1Cmax of Brentuximab Vedotin at Cycle 1 Day 15Cmax of Brentuximab Vedotin at Cycle 3 Day 1Cmax of Brentuximab Vedotin at Cycle 3 Day 15Cmax of TAb Vedotin at Cycle 1 Day 1Cmax of TAb Vedotin at Cycle 1 Day 15Cmax of TAb Vedotin at Cycle 3 Day 1Cmax of TAb Vedotin at Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD23.024.927.325.822.426.429.531.4
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD23.125.327.425.422.126.529.532.2

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Phase 2: Mean Serum AUC0-15d of Brentuximab Vedotin and TAb

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionday*µg/mL (Mean)
AUC0-15d of Brentuximab Vedotin at Cycle 1 Day 1AUC0-15d of Brentuximab Vedotin at Cycle 1 Day 15AUC0-15d of Brentuximab Vedotin at Cycle 3 Day 1AUC0-15d of Brentuximab Vedotin at Cycle 3 Day 15AUC0-15d of TAb at Cycle 1 Day 1AUC0-15d of TAb at Cycle 1 Day 15AUC0-15d of TAb at Cycle 3 Day 1AUC0-15d of TAb at Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD48.854.063.961.477.698.1120125
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD49.754.962.660.677.297.3119124

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Phase 2: Immune Reconstitution-Change From Baseline in Peripheral Blood CD34+A at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
InterventionµL (Mean)
BaselineChange from Baseline at EOT
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD3.917-1.456
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD4.182-1.512

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Phase 2: Time to Onset and Resolution for All Peripheral Neuropathy Events

Time to onset of first event was defined as time from first dose of study drug to onset of first treatment-emergent PN event. Time to resolution was calculated as the time from onset date to the date of resolution PN (SMQ) event. Participants with multiple resolved events were counted once at the longest time to resolution. Resolution was defined as an event outcome of resolved or resolved with sequelae. This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

,
Interventionweeks (Median)
Time to OnsetTime to Resolution
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD5.931.57
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD5.931.57

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Phase 2: Percentage of Participants With Low and High ATA Titer Values

High ATA titer was defined as participants who have at least one postbaseline ATA titer >25. Low ATA titer was defined as participants whose postbaseline ATA titer are all <=25. This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 6 months

,
Interventionpercentage of participants (Number)
ATA Titer LowATA Titer High
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD70
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD60

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Phase 2: Percentage of Participants Who Were ATA Positive, Persistently Positive, or Transiently Positive, and nATA Positive

ATA positive was defined as participants who have a positive ATA in any postbaseline sample. Transiently ATA positive was defined as participants who have positive ATA in 1 or 2 postbaseline samples. Persistently ATA positive was defined as participants who have positive ATA in more than 2 postbaseline timepoints. Transiently ATA positive was defined as participants who have positive ATA in 1 or 2 postbaseline samples. nATA positive was defined as participants who have at least one positive nATA in any postbaseline ATA positive sample. Here, percentage of participants who were transiently or persistently ATA positive are considered as ATA positive. This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: From first dose until 30 days after the last dose of study drug (up to 7 months)

,
Interventionpercentage of participants (Number)
Transiently ATA PositivePersistently ATA PositivenATA Positive
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD703
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD604

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Phase 2: Percentage of Participants Achieving CR Per IRF Assessment Per IWG Criteria in ATA Positive and ATA Negative Participants

CR is defined as the disappearance of all evidence of disease as assessed by IRF as per IWG Criteria. This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

,
Interventionpercentage of participants (Number)
ATA NegativeTransiently ATA Positive
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD7675
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD7567

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Phase 2: Number of ATA Positive and ATA Negative Participants With AEs and SAEs

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

,
InterventionParticipants (Count of Participants)
ATA Negative: AEsATA Positive: AEsATA Negative: SAEsATA Positive: SAEs
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD554213
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD483212

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Phase 2: Median Tmax of MMAE in Plasma

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionhour (Median)
Cycle 1 Day 1Cycle 1 Day 15Cycle 3 Day 1Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD44.442.945.346.0
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD44.142.944.945.4

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Phase 2: Mean Plasma Cmax of MMAE

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionng/mL (Mean)
Cycle 1 Day 1Cycle 1 Day 15Cycle 3 Day 1Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD5.492.811.691.61
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD5.492.951.751.74

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Phase 1: Percentage of Participants Who Achieved a CR Per IRF Assessment Per IWG Criteria at EOT Visit

CR was defined as the disappearance of all evidence of disease as assessed by IRF as per IWG Criteria. The confidence interval was based on exact binomial distribution (Clopper-Pearson method). This outcome measure was planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: At EOT visit 30 days after the last dose of study drug (at Month 7)

Interventionpercentage of participants (Number)
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD88

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Phase 1: Percentage of Participants Who Achieved a PR Per IRF Assessment Per IWG Criteria at EOT Visit

PR was defined as regression of measurable disease and no new diseases as per IWG Criteria based on IRF. The confidence interval was based on exact binomial distribution (Clopper-Pearson method). This outcome measure was planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: At EOT visit 30 days after the last dose of study drug (at Month 7)

Interventionpercentage of participants (Number)
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD13

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Phase 1: Percentage of Participants Who Achieved an ORR Per IRF Assessment Per IWG Criteria at EOT Visit

Overall response rate was defined as the percentage of participants with CR or PR as assessed by an IRF using IWG Revised Response Criteria. CR was defined as the disappearance of all evidence of disease and PR was defined as regression of measurable disease and no new sites. The confidence interval was based on exact binomial distribution (Clopper-Pearson method). This outcome measure was planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: At EOT visit 30 days after the last dose of study drug (at Month 7)

Interventionpercentage of participants (Number)
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD100

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Phase 1: Percentage of Participants Who Experienced Adverse Events (AEs) From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy

AE means any untoward medical occurrence in a participant administered a pharmaceutical product; the untoward medical occurrence does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal (investigational) product whether or not it is related to the medicinal product. This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: From first dose in Cycle 1 Day 1 until 30 days after the last dose of study drug in Cycle 6 Day 15 (up to Cycle 7 Day 15) (Cycle length=28 days)

Interventionpercentage of participants (Number)
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD100

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Phase 1: Percentage of Participants Who Experienced Serious Adverse Events (SAEs) From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy

AE means any untoward medical occurrence in a participant administered a pharmaceutical product; the untoward medical occurrence does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal (investigational) product whether or not it is related to the medicinal product. SAE is defined as 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, Is a medically important event. (NCT02979522)
Timeframe: From first dose in Cycle 1 Day 1 until 30 days after the last dose of study drug in Cycle 6 Day 15 (up to Cycle 7 Day 15) (Cycle length=28 days)

Interventionpercentage of participants (Number)
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD13

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Phase 1: Percentage of Participants Whose Disease Was PET Negative After 2 Cycles of Protocol Therapy Per IRF Assessment

The Deauville score according to IRF assessment of response was used to evaluate the results of PET scans. PET negative after Cycle 2 was defined as an IRF Deauville score of (1 or 2 or 3). This outcome measure was planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: From first dose of study drug up to Cycle 2 (Each Cycle length=28 days)

Interventionpercentage of participants (Number)
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD88

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Phase 1: Percentage of Participants Whose Disease Was PET Positive After 6 Cycles of Protocol Therapy Per IRF Assessment

The Deauville score according to IRF assessment of response was used to evaluate the results of PET scans. PET positive after Cycle 6 defined as an IRF Deauville score of (4 or 5). This outcome measure was planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: From first dose of study drug up to Cycle 6 (Each Cycle length=28 days)

Interventionpercentage of participants (Number)
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD13

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Phase 2: Duration of Response (DOR)

DOR per IRF in participants with a response (CR or PR per IRF) was defined as the time from start of the first objective tumor response (CR or PR per IRF) to the first subsequent PD or death due to any cause, whichever occurred first. For patients who did not have an objective PD, did not die and are either still on a study follow-up at the time of the analysis, or were removed from the study prior to documentation of PD, DOR has been censored on the date of last adequate disease assessment. This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

Interventionmonths (Median)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA

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Phase 2: Event-free Survival (EFS)

EFS:Time from first dose until any treatment failure:PD per IRF including progression events during follow-up period,failing to complete 6 cycles of treatment due to any reason or death due to any cause,whichever occurred first.EFS per IRF were censored on last adequate disease assessment date per IRF if none of above events occur during study.Participants with antitumor treatment,other than SCT/radiotherapy as part of frontline treatment were censored at last adequate disease assessment before initiation of such alternative treatment.If a participant experienced disease progression per IRF/died after initiation of antitumor treatment,other than SCT/radiotherapy,such participant was censored,and not be considered having EFS.This outcome measure was planned to be assessed for all patients treated at recommended dose in Phase 2.As prespecified in SAP,data for Phase 2 was summarized and reported in two arms:Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

Interventionmonths (Median)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA

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Phase 2: Overall Survival (OS)

Overall survival was defined as time from first dose until death. In the absence of confirmation of death, survival time was censored at the last date the participant was known to be alive, including study closure. This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

Interventionmonths (Median)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA

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Phase 2: Percentage of Participants Receiving Irradiation for HL Following Study Treatment

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD25
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD24

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Phase 2: Percentage of Participants Who Achieved a Complete Remission (CR) Per Independent Review Facility (IRF) Assessment Per International Working Group (IWG) Criteria at End of Treatment (EOT) Visit

CR was defined as the disappearance of all evidence of disease as assessed by IRF as per IWG Criteria. The confidence interval was based on exact binomial distribution (Clopper-Pearson method). This outcome measure was planned to be assessed for all participants treated at the recommended dose in Phase 2. As prespecified in the statistical analysis plan (SAP) , data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: At end of treatment (EOT) visit 30 days after the last dose of study drug (at Month 7)

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD75
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD76

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Phase 2: Percentage of Participants Who Achieved a Partial Remission (PR) Per IRF Assessment Per IWG Criteria at EOT Visit

PR was defined as regression of measurable disease and no new sites as assessed by IRF as per IWG criteria. Percentage of participants in the response-evaluable population who achieved a partial response based on the IRF assessment at the EOT visit based on the IWG criteria are reported. The confidence interval was based on exact binomial distribution (Clopper-Pearson method). This outcome measure was planned to be assessed for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: At EOT visit 30 days after the last dose of study drug (at Month 7)

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD12
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD12

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Phase 2: Percentage of Participants Who Achieved an Overall Response Rate (ORR) Per IRF Assessment Per IWG Criteria at EOT Visit

Overall response rate was defined as the percentage of participants with CR or PR as assessed by IRF using IWG criteria. CR was defined as the disappearance of all evidence of disease and PR was defined as regression of measurable disease and no new diseases. The confidence interval was based on exact binomial distribution (Clopper-Pearson method). This outcome measure was planned to be assessed for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: At EOT visit 30 days after the last dose of study drug (at Month 7)

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD86
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD88

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Phase 2: Percentage of Participants Who Experienced AEs From the First Dose of Protocol Therapy Through 30 Days After Administration of the Last Dose of Protocol Therapy

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: From first dose in Cycle 1 Day 1 until 30 days after the last dose of study drug in Cycle 6 Day 15 (up to Cycle 7 Day 15) (Cycle length=28 days)

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD100
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD100

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Phase 2: Percentage of Participants Who Experienced Peripheral Neuropathy, Regardless of Seriousness, From the First Dose of Protocol Therapy

Peripheral Neuropathy (PN) was defined by the peripheral neuropathy standardized MedDRA query (SMQ) broad search. This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD20
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD19

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Phase 2: Mean Plasma AUC0-15 of MMAE

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionday*ng/mL (Mean)
Cycle 1 Day 1Cycle 1 Day 15Cycle 3 Day 1Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD31.017.911.111.3
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD31.218.411.512.3

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Phase 2: Mean Cmax of Brentuximab Vedotin in ATA Positive and ATA Negative Participants

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Cycle 1-3: Days 1 and 15 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionµg/mL (Mean)
ATA Positive: Cycle 1 Day 1ATA Positive: Cycle 1 Day 15ATA Positive: Cycle 3 Day 1ATA Positive: Cycle 3 Day 15ATA Negative: Cycle 1 Day 1ATA Negative: Cycle 1 Day 15ATA Negative: Cycle 3 Day 1ATA Negative: Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD26.722.722.424.222.725.227.626.0
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD27.823.322.025.622.825.427.725.4

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Phase 2: Percentage of Participants Whose Disease Was Positron Emission Tomography (PET) Negative After 2 Cycles of Protocol Therapy Per IRF Assessment

The Deauville score according to IRF assessment of response was used to evaluate the results of PET scans. PET negative after Cycle 2 was defined as an IRF Deauville score of (1 or 2 or 3). This outcome measure was planned to be assessed for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: From first dose of study drug up to Cycle 2 Day 25 (Each Cycle length=28 days)

Interventionpercentage of participants (Number)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD90
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD90

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Phase 2: Progression-free Survival (PFS)

PFS per IRF:time from first dose until disease progression per IRF/death due to any cause,whichever occurred first.Participants with no objective progressive disease (PD),did not die,were still on study follow-up at time of analysis were removed from study prior to documentation of PD,PFS was censored on date of last adequate disease assessment before initiation of any non-protocol,alternative therapy.Participants who were on antitumor treatment,other than SCT/radiotherapy,censoring was at last adequate disease assessment before initiation of such alternative treatment.If participant experienced disease progression per IRF/died after initiation of antitumor treatment,other than SCT/radiotherapy,such participant was censored and not considered having PFS.Outcome measure was planned to be assessed for all participant treated at recommended dose in Phase 2.As per SAP,Phase 2 data was summarized and reported in two arms:Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Up to 24 months

Interventionmonths (Median)
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVDNA

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Phase 1: Mean Area Under the Plasma Concentration-Time Curve From Day 0 to Day 15 (AUC0-15) of MMAE

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionday* nanogram per milliliter (day*ng/mL) (Mean)
Cycle 1 Day 1Cycle 1 Day 15Cycle 3 Day 1Cycle 3 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD29.813.18.887.17

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Phase 1: Mean Area Under the Serum Concentration-Time Curve From Day 0 to Day 15 (AUC0-15) of Brentuximab Vedotin and TAb

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionday*microgram per milliliter(day*mcg/mL) (Mean)
AUC0-15d of Brentuximab Vedotin at Cycle 1 Day 1AUC0-15d of Brentuximab Vedotin at Cycle 1 Day 15AUC0-15d of Brentuximab Vedotin at Cycle 3 Day 1AUC0-15d of Brentuximab Vedotin at Cycle 3 Day 15AUC0-15d of TAb at Cycle 1 Day 1AUC0-15d of TAb at Cycle 1 Day 15AUC0-15d of TAb at Cycle 3 Day 1AUC0-15d of TAb at Cycle 3 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD42.348.872.764.880.6103127128

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Phase 1: Mean AUC 0-15d of Brentuximab Vedotin in ATA Positive and ATA Negative Participants

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Cycle 1 and 3: Days 1 and 15 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionday*µg/mL (Mean)
ATA Positive: Cycle 1 Day 1ATA Positive: Cycle 1 Day 15ATA Positive: Cycle 3 Day 1ATA Positive: Cycle 3 Day 15ATA Negative: Cycle 1 Day 1ATA Negative: Cycle 1 Day 15ATA Negative: Cycle 3 Day 1ATA Negative: Cycle 3 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 + AVD42.450.056.663.042.248.675.465.1

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Phase 1: Mean Cmax of Brentuximab Vedotin in ATA Positive and ATA Negative Participants

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Cycle 1 and 3: Days 1 and 15 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionµg/mL (Mean)
ATA Positive: Cycle 1 Day 1ATA Positive: Cycle 1 Day 15ATA Positive: Cycle 3 Day 1ATA Positive: Cycle 3 Day 15ATA Negative: Cycle 1 Day 1ATA Negative: Cycle 1 Day 15ATA Negative: Cycle 3 Day 1ATA Negative: Cycle 3 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 + AVD23.321.123.121.622.523.527.228.3

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Phase 1: Mean Maximum Observed Plasma Concentration (Cmax) of Monomethyl Auristatin E (MMAE)

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionnanogram per milliliter (ng/ml) (Mean)
Cycle 1 Day 1Cycle 1 Day 15Cycle 3 Day 1Cycle 3 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD5.512.081.381.19

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Phase 1: Mean Maximum Observed Serum Concentration (Cmax) of Brentuximab Vedotin Total Conjugated and Therapeutic Antibody (TAb)

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionmicrogram per milliliter(mcg/mL) (Mean)
Conjugate Brentuximab Vedotin at Cycle 1 Day 1Conjugate Brentuximab Vedotin at Cycle 1 Day 15Conjugate Brentuximab Vedotin at Cycle 3 Day 1Conjugate Brentuximab Vedotin at Cycle 3 Day 15TAb at Cycle 1 Day 1TAb at Cycle 1 Day 15TAb at Cycle 3 Day 1TAb at Cycle 3 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD22.623.126.727.324.925.529.628.1

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Phase 1: Median Time to Reach Cmax (Tmax) of Brentuximab Vedotin and TAb in Serum

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Cycle 1-6: Days 1 and 15 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionhour (Median)
Tmax of Brentuximab Vedotin at Cycle 1 Day 1Tmax of Brentuximab Vedotin at Cycle 1 Day 15Tmax of Brentuximab Vedotin at Cycle 3 Day 1Tmax of Brentuximab Vedotin at Cycle 3 Day 15Tmax of TAb at Cycle 1 Day 1Tmax of TAb at Cycle 1 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD1.000.9151.000.8301.000.915

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Phase 1: Median Time to Reach Cmax (Tmax) of MMAE in Plasma

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Days 1 and 15 of Cycles 1 and 3 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

Interventionhour (Median)
Cycle 1 Day 1Cycle 1 Day 15Cycle 3 Day 1Cycle 3 Day 15
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD44.943.148.048.2

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Phase 1: Number of ATA Positive and ATA Negative Participants With AEs and SAEs

This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Up to 24 months

InterventionParticipants (Count of Participants)
ATA Negative: AEsATA Positive: AEsATA Negative: SAEsATA Positive: SAEs
Phase 1: Brentuximab Vedotin 48 mg/m^2 + AVD7101

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Phase 1: Percentage of Participants Who Were Antitherapeutic Antibody (ATA) Positive, Persistently Positive or Transiently Positive, and Neutralizing Antitherapeutic Antibody (nATA) Positive

ATA positive was defined as participants who have a positive ATA in any postbaseline sample. Transiently ATA positive was defined as participants who have positive ATA in 1 or 2 postbaseline samples. Persistently ATA positive was defined as participants who have positive ATA in more than 2 postbaseline timepoints. Transiently ATA positive was defined as participants who have positive ATA in 1 or 2 postbaseline samples. nATA positive was defined as participants who have at least one positive nATA in any postbaseline ATA positive sample. Here, percentage of participants who were transiently or persistently ATA positive are considered as ATA positive. This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Up to 7 months

Interventionpercentage of participants (Number)
Transiently ATA PositivePersistently ATA PositivenATA Positive
Phase 1: Brentuximab Vedotin 48 mg/m^2 +AVD1300

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Phase 1: Percentage of Participants With Low and High ATA Titer Values

High ATA titer was defined as participants who have at least one postbaseline ATA titer less than (>) 25. Low ATA titer was defined as participants whose postbaseline ATA titer are all less than or equal to (<=) 25. This outcome measure is planned to be assessed only for participants treated in Phase 1 arm. (NCT02979522)
Timeframe: Up to 6 months

Interventionpercentage of participants (Number)
ATA Titer lowATA Titer High
Phase 1: Brentuximab Vedotin 48 mg/m^2 + AVD130

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Phase 2: Immune Reconstitution-Change From Baseline Immunoglobulin G Levels at End of Treatment (EOT)

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline and End of Treatment (Month 7)

,
Interventiong/L (Mean)
BaselineChange from Baseline at EOT
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD16.217-4.675
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD16.518-4.822

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Phase 2: Mean AUC 0-15 of Brentuximab Vedotin in ATA Positive and ATA Negative Participants

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Cycle 1-3: Days 1 and 15 pre-infusion and up to 30 minutes after the end of infusion (Cycle length=28 days)

,
Interventionday*µg/mL (Mean)
ATA Positive: Cycle 1 Day 1ATA Positive: Cycle 1 Day 15ATA Positive: Cycle 3 Day 1ATA Positive: Cycle 3 Day 15ATA Negative: Cycle 1 Day 1ATA Negative: Cycle 1 Day 15ATA Negative: Cycle 3 Day 1ATA Negative: Cycle 3 Day 15
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD49.346.754.659.148.854.864.461.7
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD51.645.653.757.249.655.863.060.9

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Phase 2: Immune Reconstitution-Change From Baseline Total Immunoglobulin at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Interventionmg/dl (Mean)
BaselineChange from Baseline at EOT
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD2045.1-556.3
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD2086.6-582.3

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Phase 2: Immune Reconstitution-Change From Baseline Poliovirus Antibodies Ratio at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Interventionratio (Mean)
Baseline: Type IEOT: Type IBaseline: Type IIIEOT: Type III
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD0.023730.008450.034320.01013
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD0.024470.009130.036410.01141

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Phase 2: Immune Reconstitution-Change From Baseline in Total Lymphocyte Count at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Intervention10^9 lymphocytes/L (Mean)
BaselineChange from Baseline at EOT
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.74080.5965
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.80220.6736

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Phase 2: Immune Reconstitution-Change From Baseline in the Percentage of CD8+ (CD8+CD45RA-CD197- and CD8+CD45RA-CD197+) Subset of Cells at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Interventionpercentage of CD8+ subset cells (Mean)
Baseline: CD8+CD45RA-CD197-Change from Baseline at EOT: CD8+CD45RA-CD197-Baseline: CD8+CD45RA-CD197+Change from Baseline at EOT: CD8+CD45RA-CD197+Baseline: CD8+CD45RA+CD197-Change from Baseline at EOT: CD8+CD45RA+CD197-Baseline: CD8+CD45RA+CD197+Change from Baseline at EOT: CD8+CD45RA+CD197+
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD40.6-11.02.32.125.8-6.530.815.4
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD39.9-11.52.41.625.9-6.031.315.7

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Phase 2: Immune Reconstitution-Change From Baseline in the Percentage of CD4+ (CD4+CD45RA-CD197- and CD4+CD45RA+CD197+) Subset of Cells at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Interventionpercentage of CD4+ subset cells (Mean)
Baseline: CD4+CD45RA-CD197-Change from Baseline at EOT: CD4+CD45RA-CD197-Baseline: CD4+CD45RA-CD197+Change from Baseline at EOT: CD4+CD45RA-CD197+Baseline: CD4+CD45RA+CD197-Change from Baseline at EOT: CD4+CD45RA+CD197-Baseline: CD4+CD45RA+CD197+Change from Baseline at EOT: CD4+CD45RA+CD197+
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD29.0-5.122.312.63.1-0.746.3-6.8
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD28.0-5.023.713.02.9-0.746.2-7.2

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Phase 2: Immune Reconstitution-Change From Baseline in Tetanus at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Intervention(IU)/mL (Mean)
BaselineChange from Baseline at EOT
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.935-0.914
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.636-0.648

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Phase 2: Immune Reconstitution-Change From Baseline in Immunoglobulin M at the End of Treatment (EOT)

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Interventiong/L (Mean)
BaselineChange at EOT (Month 7)
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.261-0.375
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD1.275-0.345

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Phase 2: Immune Reconstitution-Change From Baseline in Immunoglobulin A at EOT

This outcome measure was planned to be assessed only for all participants treated at the recommended dose in Phase 2. As prespecified in SAP, data for Phase 2 was summarized and reported in two arms: Phase 2 and Phase 1 + Phase 2. (NCT02979522)
Timeframe: Baseline, EOT [Month 7]

,
Interventiong/L (Mean)
BaselineChange from Baseline at EOT
Phase 1 + Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD2.671-0.125
Phase 2: Brentuximab Vedotin 48 mg/m^2 + AVD2.708-0.195

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Complete Response (CR) With Pembrolizumab Treatment Alone

"To assess the primary objective of response rate following PET #2 performed after 3 doses of pembrolizumab. PET response will be assessed using the Lugano Criteria (2014) which recommends the 5 point Deauville score for assessing response. The Deauville five-point scale is an internationally-recommended scale for routine clinical reporting and clinical trials using FDG PET-CT in the initial staging and assessment of treatment response in Hodgkin lymphoma (HL). Patients with a Deauville score of 1-3 will be considered a complete response.~Deauville criteria is defined as follows:~No residual uptake~Slight uptake, but below blood pool (mediastinum)~Uptake above mediastinum, but below or equal to uptake in the liver~Uptake slightly to moderately higher than liver~Markedly increased uptake or any new lesions~Patients will be evaluable for response assessment if they have received at least one dose of pembrolizumab." (NCT03226249)
Timeframe: After 3 cycles of pembrolizumab (1 cycle = 21 days)

Interventionpercentage of participants (Number)
Treatment: Pembrolizumab and AVD Chemotherapy Guided by PET-CT37

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Overall Survival at Treatment Completion

Overall survival will be defined as the number of patients that are alive at the time of treatment completion (3 cycles of pembrolizumab and 2-6 cycles of AVD) (NCT03226249)
Timeframe: At completion of treatment with 3 cycles of pembrolizumab (21 day cycles) and up to 6 cycles of AVD (28 days cycles)

InterventionParticipants (Count of Participants)
Treatment: Pembrolizumab and AVD Chemotherapy Guided by PET-CT30

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Progression Free Survival (PFS) at Treatment Completion

"PFS is defined as the number of patients that are progression/relapse free at the time of treatment completion (3 cycles of pembrolizumab and up to 6 cycles of AVD).~Progressive or relapse disease is defined as of the following:~Appearance of any new lesion more than 1.5 cm in any axis during treatment, even if other lesions are decreasing in size.~At least a 50% increased from nadir in the sum of the product of the diameter (SPD) of any previously involved nodes, or in a single involved node, or the size of other lesions (e.g., splenic or hepatic nodules). To be considered progressive disease, a lymph node with a diameter of the short axis of less than 1.0 cm must increase by at least 50% and to a size of more than 1.5 x 1.5 cm or more than 1.5 cm in the long axis.~At least a 50% increase in the longest diameter of any single previously identified node more than 1.0 cm in its short axis.~Lymphoma confirmed by repeat biopsy." (NCT03226249)
Timeframe: At completion of treatment with 3 cycles of pembrolizumab (21 day cycles) and up to 6 cycles of AVD (28 days cycles)

InterventionParticipants (Count of Participants)
Treatment: Pembrolizumab and AVD Chemotherapy Guided by PET-CT30

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Actual Dose Intensity: Brentuximab Vedotin (Part A)

(NCT03646123)
Timeframe: 6.5 months

Interventionmg/kg/week (Mean)
Part A0.5

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Complete Response (CR) Rate (Parts B and C)

CR rate at EOT is defined as the percentage of subjects with CR at EOT, according to the Lugano Classification Revised Staging System for malignant lymphoma (Cheson 2014) with the incorporation of LYRIC (Cheson 2016), in subjects with previously untreated cHL. (NCT03646123)
Timeframe: 7.8 months

Interventionpercentage of participants (Number)
Part B88
Part C90

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Complete Response Rate (Part A)

The complete response rate is defined as the percentage of participants with CR at EOT according to the Lugano Classification Revised Staging System for nodal non-Hodgkin and Hodgkin lymphomas (Cheson 2014). (NCT03646123)
Timeframe: 7.2 months

Interventionpercentage of participants (Number)
Part A80

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Subsequent Anticancer Therapy Utilization Rate (Part A)

Number of participants with subsequent anticancer therapy (NCT03646123)
Timeframe: 33.8 months

InterventionParticipants (Count of Participants)
Participants with any subsequent therapyConsolidative radiotherapy: RadiotherapyConsolidative radiotherapy: Proton radiationImmunotherapy: NivolumabMaintenance: NivolumabMaintenance radiotherapy: Radiation therapySystemic therapy for progressive disease: Bendamustine monotherapySystemic therapy for relapsed disease: Nivolumab
Part A63111111

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Relative Dose Intensity (Part A)

(NCT03646123)
Timeframe: 6.5 months

Interventionpercentage of intended dose (Mean)
Brentuximab vedotinDoxorubicinVinblastineDacarbazine
Part A91.094.289.094.0

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Rate of Dose Reduction and Delays: Vinblastine (Part A)

(NCT03646123)
Timeframe: 6.5 months

InterventionParticipants (Count of Participants)
Participants with any dose modificationParticipants with any dose delayParticipants with any dose delay due to AEParticipants with any dose delay due to other reasonParticipants with any dose reduction due to AE
Part A2722151412

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Rate of Dose Reduction and Delays: Doxorubicin (Part A)

(NCT03646123)
Timeframe: 6.5 months

InterventionParticipants (Count of Participants)
Participants with any dose modificationParticipants with any dose delayParticipants with any dose delay due to AEParticipants with any dose delay due to other reasonParticipants with any dose reduction due to AE
Part A252315157

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Rate of Dose Reduction and Delays: Dacarbazine (Part A)

(NCT03646123)
Timeframe: 6.5 months

InterventionParticipants (Count of Participants)
Participants with any dose modificationParticipants with any dose delayParticipants with any dose delay due to AEParticipants with any dose delay due to other reasonParticipants with any dose reduction due to AE
Part A252215146

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Rate of Dose Reduction and Delays: Brentuximab Vedotin (Part A)

(NCT03646123)
Timeframe: 6.5 months

InterventionParticipants (Count of Participants)
Participants with any dose modificationParticipants with any dose delayParticipants with any dose delay due to AEParticipants with any dose delay due to other reasonParticipants with any dose reduction due to AE
Part A2922151414

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Incidence of Laboratory Abnormalities (Parts B and C)

Laboratory values were graded according to the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE version 4.03). (NCT03646123)
Timeframe: 8.9 months

,
InterventionParticipants (Count of Participants)
Hemoglobin high, Grade 1Hemoglobin high, Grade 2Hemoglobin high, Grade 3Hemoglobin high, Grade 4Hemoglobin low, Grade 1Hemoglobin low, Grade 2Hemoglobin low, Grade 3Hemoglobin low, Grade 4Leukocytes high, Grade 1Leukocytes high, Grade 2Leukocytes high, Grade 3Leukocytes high, Grade 4Leukocytes low, Grade 1Leukocytes low, Grade 2Leukocytes low, Grade 3Leukocytes low, Grade 4Lymphocytes high, Grade 1Lymphocytes high, Grade 2Lymphocytes high, Grade 3Lymphocytes high, Grade 4Lymphocytes low, Grade 1Lymphocytes low, Grade 2Lymphocytes low, Grade 3Lymphocytes low, Grade 4Neutrophils low, Grade 1Neutrophils low, Grade 2Neutrophils low, Grade 3Neutrophils low, Grade 4Neutrophils low, value missingPlatelets low, Grade 1Platelets low, Grade 2Platelets low, Grade 3Platelets low, Grade 4Alanine aminotransferase high, Grade 1Alanine aminotransferase high, Grade 2Alanine aminotransferase high, Grade 3Alanine aminotransferase high, Grade 4Albumin low, Grade 1Albumin low, Grade 2Albumin low, Grade 3Albumin low, Grade 4Alkaline phosphatase high, Grade 1Alkaline phosphatase high, Grade 2Alkaline phosphatase high, Grade 3Alkaline phosphatase high, Grade 4Amylase high, Grade 1Amylase high, Grade 2Amylase high, Grade 3Amylase high, Grade 4Aspartate aminotransferase high, Grade 1Aspartate aminotransferase high, Grade 2Aspartate aminotransferase high, Grade 3Aspartate aminotransferase high, Grade 4Calcium corrected for albumin high, Grade 1Calcium corrected for albumin high, Grade 2Calcium corrected for albumin high, Grade 3Calcium corrected for albumin high, Grade 4Calcium corrected for albumin low, Grade 1Calcium corrected for albumin low, Grade 2Calcium corrected for albumin low, Grade 3Calcium corrected for albumin low, Grade 4Ionized calcium high, Grade 1Ionized calcium high, Grade 2Ionized calcium high, Grade 3Ionized calcium high, Grade 4Ionized calcium low, Grade 1Ionized calcium low, Grade 2Ionized calcium low, Grade 3Ionized calcium low, Grade 4Creatinine high, Grade 1Creatinine high, Grade 2Creatinine high, Grade 3Creatinine high, Grade 4Estimated glomerular filtration rate low, Grade 1Estimated glomerular filtration rate low, Grade 2Estimated glomerular filtration rate low, Grade 3Estimated glomerular filtration rate low, Grade 4Estimated glomerular filtration rate low, value missingGlucose high, Grade 1Glucose high, Grade 2Glucose high, Grade 3Glucose high, Grade 4Glucose low, Grade 1Glucose low, Grade 2Glucose low, Grade 3Glucose low, Grade 4Lipase high, Grade 1Lipase high, Grade 2Lipase high, Grade 3Lipase high, Grade 4Phosphate low, Grade 1Phosphate low, Grade 2Phosphate low, Grade 3Phosphate low, Grade 4Potassium high, Grade 1Potassium high, Grade 2Potassium high, Grade 3Potassium high, Grade 4Potassium low, Grade 1Potassium low, Grade 2Potassium low, Grade 3Potassium low, Grade 4Sodium high, Grade 1Sodium high, Grade 2Sodium high, Grade 3Sodium high, Grade 4Sodium low, Grade 1Sodium low, Grade 2Sodium low, Grade 3Sodium low, Grade 4Total bilirubin high, Grade 1Total bilirubin high, Grade 2Total bilirubin high, Grade 3Total bilirubin high, Grade 4Urate high, Grade 1Urate high, Grade 2Urate high, Grade 3Urate high, Grade 4
Part B000037101000001912000100111971414422610026340113003020032002712012000700000000000475101400045511121009150172030009021200011020120000100
Part C4000966100000412420030031279012381130221007116100226005110015660757101800051000000000012511008110026911130180001366331440610019000301025020800000281

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Incidence of Adverse Events (Parts B and C)

(NCT03646123)
Timeframe: 8.9 months

,
InterventionParticipants (Count of Participants)
Any treatment-emergent adverse event (TEAE)Treatment-related TEAEGrade 3 or higher TEAEGrade 3 or higher treatment-related TEAEAny treatment-emergent serious adverse event (SAE)Treatment-related treatment-emergent SAEParticipants who discontinued treatment due to TEAEParticipants who discontinued treatment due to treatment-related TEAETEAE leading to death
Part B57562919158440
Part C15314967522919440

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Febrile Neutropenia (FN) Rate (Part A)

The FN rate is defined as the number of participants who experience treatment-emergent FN. (NCT03646123)
Timeframe: 7.5 months

InterventionParticipants (Count of Participants)
Any treatment-emergent FNTreatment-related treatment-emergent FNGrade 3 or higher treatment-emergent FNGrade 3 or higher treatment-related treatment-emergent FN
Part A5555

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Actual Dose Intensity: Doxorubicin, Vinblastine, Dacarbazine (Part A)

(NCT03646123)
Timeframe: 6.5 months

Interventionmg/m2/week (Mean)
DoxorubicinVinblastineDacarbazine
Part A11.82.7176.3

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Primary Refractory Disease Rate (Part A)

The primary refractory disease rate is defined as the percentage of participants with less than complete response or relapse within 3 months of EOT, according to the Lugano Classification Revised Staging System for nodal non-Hodgkin and Hodgkin lymphomas (NCT03646123)
Timeframe: 10.2 months

Interventionpercentage of participants (Number)
Part A10

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Physician-reported Progression Free Survival (PFS) (Part A)

The physician-reported PFS rate at 2 years is estimated based on Kaplan-Meier methodology. (NCT03646123)
Timeframe: 24 months

Interventionpercentage of participants (Number)
Part A89.23

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Overall Response Rate (ORR) at EOT (Parts B and C)

ORR is defined as the proportion of participants with CR or partial response (PR) at EOT according to the Lugano Classification Revised Staging System for malignant lymphoma (Cheson 2014) with the incorporation of LYRIC (Cheson 2016) in subjects with previously untreated cHL. (NCT03646123)
Timeframe: 7.8 months

Interventionpercentage of participants (Number)
Part B93
Part C95

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Incidence of Grade 3-5 Adverse Events

Graded per National Cancer Institute Common Terminology Criteria for Adverse Events version 5.0. The safety and tolerability of durvalumab in combination with chemotherapy in subjects with variant histology bladder cancer who initiate study treatment will be assessed as the number, by treatment cohort, of grade 3, 4, or 5 adverse events, considered probably or definitely related by the investigator. (NCT03912818)
Timeframe: At 120 days

,
Interventionevents (Number)
Grade 3Grade 4Grade 5
Cohort I (Durvalumab, DD MVAC)100
Cohort III (Durvalumab, Carbo-gem)200

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Proportion of Subjects Who Initiate Study Treatment and Achieve Tumor Stage of pT2 N0 M0 or Better (e.g., pT0, pT1 N0) at Cystectomy

"Achievement of tumor staging will be determined by pathologist at cystectomy and reported by treatment cohort. Assessed per National Comprehensive Cancer Network bladder cancer guidelines.~T0 N0 M0 = No evidence of primary tumor~T1 N0 M0 = Tumor staging by pathological assessment detected in lamina propria (T0), with no tumor positive nodes (N0).~T2 N0 M0 = Tumor staging by pathological assessment detected in muscularis propria (pT2), with no tumor positive nodes (N0) or tumor metastases (M0) observed." (NCT03912818)
Timeframe: At 20 weeks

InterventionParticipants (Count of Participants)
Cohort I (Durvalumab, DD MVAC)1
Cohort III (Durvalumab, Carbo-gem)1

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