Page last updated: 2024-10-15

allopurinol

Description

Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID135401907
CHEMBL ID1467
CHEBI ID40279
SCHEMBL ID4627
SCHEMBL ID1128219
MeSH IDM0000745

Synonyms (314)

Synonym
MLS001148183
AB00173448-03
AB00173448-04
4h-pyrazolo[3,4-d]pyrimidin-4-one, 1,2-dihydro-
smr000059083
MLS000069453 ,
4h-pyrazolo[3,4-d]pyrimidin-4-one, 1,5-dihydro-
KBIO1_000685
DIVK1C_000685
NCIOPEN2_001825
ketanrift
remid
1,5-dihydro-4h-pyrazolo(3,4-d)pyrimidin-4-one
ledopur
4h-pyrazolo(3,4-d)pyrimidin-4-one
4'-hydroxypyrazolol(3,4-d)pyrimidine
4-hydroxy-1h-pyrazolo(3,4-d)pyrimidine
4h-pyrazolo[3,4-d]pyrimidin-4-one, 1,7-dihydro-
adenock
dabroson
monarch
aloral
suspendol
takanarumin
gichtex
allopurinolum [inn-latin]
allozym
1,5-dihydro-4h-pyrazolo(3,4-d)pyrimidine-4-one
apurin
cosuric
allural
apulonga
4-hydroxypyrazolo(3,4-d)pyrimidine
dabrosin
cellidrin
urtias
hexanuret
4h-pyrazolo(3,4-d)pyrimidin-4-one, 1,5-dihydro-
lysuron
nektrohan
4-hydroxypyrazolopyrimidine
aluline
urtias 100
caplenal
dura al
allo-puren
miniplanor
4-hydroxypyrazolyl(3,4-d)pyrimidine
hamarin
riball
epuric
1h-pyrazolo(3,4-d)pyrimidin-4-ol
alopurinol [inn-spanish]
EU-0100102
allopurinol, xanthine oxidase inhibitor
1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-one
1,5-dihydropyrazolo[3,4-d]pyrimidin-4-one
ailurial
SPECTRUM_000026
xanthine oxidase
PRESTWICK_511
NCGC00015094-01
lopac-a-8003
BSPBIO_001798
IDI1_000685
LOPAC0_000102
b. w. 56-158
bloxanth
4-hydroxypyrazolo[3,4-d]pyrimidine
urosin
wln: t56 bmn gn inj fq
ketobun-a
4-hydroxy-1h-pyrazolo[3,4-d]pyrimidine
bw 56158
anzief
urolit
4h-pyrazolo[3, 1,5-dihydro-
315-30-0
allopurinol
apurol
uripurinol
bleminol
allopurinol(i)
geapur
nsc101655
xanturat
4-hydroxy-3,4-pyrazolopyrimidine
4-hydroxypyrazolyl[3,4-d]pyrimidine
allopur
foligan
milurit
alositol
4-hpp
bw 56-158
ailural
zyloprim
progout
anoprolin
4'-hydroxypyrazolol[3,4-d]pyrimidine
1h-pyrazolo[3,4-d]pyrimidin-4-ol
gotax
uriprim
urbol
atisuril
zyloric
epidropal
lopurin
embarin
uricemil
nsc-101655
inchi=1/c5h4n4o/c10-5-3-1-8-9-4(3)6-2-7-5/h1-2h,(h2,6,7,8,9,10
NCGC00091134-01
bw-56-158
aloprim
BIM-0061756.0001
nsc 1390
einecs 206-250-9
hsdb 3004
ccris 626
nsc 101655
nsc-1390
9002-17-9
1,4-d]pyrimidin-4-one
nsc1390
CHEBI:40279 ,
al-100
alopurinol
allopurinolum
DB00437
zyloprim (tn)
D00224
allopurinol (jp17/usp/inn)
NCGC00094580-01
NCGC00094580-02
KBIO2_002954
KBIOSS_000386
KBIO2_005522
KBIO3_001298
KBIOGR_000550
KBIO2_000386
SPECTRUM3_000289
SPECTRUM2_000098
NINDS_000685
SPBIO_000056
SPECTRUM4_000135
SPECTRUM1500108
SPECTRUM5_000768
allopurinol (4-hydroxypyrazolo[3,4-d]pyrimidine)
NCGC00091134-02
NCGC00091134-03
NCGC00015094-03
AC-019
A 8003 ,
HMS2091G15
A0907
NCGC00015094-06
CHEMBL1467
AKOS000269759
AKOS000267490
HMS502C07
FT-0661492
HMS1920A15
1h,4h,7h-pyrazolo[3,4-d]pyrimidin-4-one
NCGC00015094-02
1h-pyrazolo[3,4-d]pyrimidin-4-ol;1h-pyrazolo[3,4-d]pyrimidin-4(5h)-one
AB-323/25048497
NCGC00188948-01
NCGC00094580-04
HMS3260E06
HMS3259K13
tox21_200922
NCGC00258476-01
pharmakon1600-01500108
nsc755858
nsc-755858
dtxsid4022573 ,
tox21_110082
dtxcid502573
cas-315-30-0
uritas
sigapurol
CCG-204197
1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-one
HMS2234M09
4-hydroxypyrazol[3,4-d]pyrimidine
CCG-38916
NCGC00015094-05
NCGC00015094-04
NCGC00015094-07
1h-pyrazolo[3,4-d]pyrimidin-4(5h)-one
1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-one synonym: allopurinol
916980-04-6
FT-0685730
ath008
63cz7gjn5i ,
unii-63cz7gjn5i
allopurinol [usan:usp:inn:ban:jan]
180749-09-1
2h-pyrazolo[3,4-d]pyrimidin-4-ol
180749-08-0
FT-0602537
NCGC00094580-05
LP00102
S1630
F3329-0375
SC2251
SC1118
73334-58-4
1h-pyrazolo[3,4-d]pyrimidin-4(7h)-one
bw-56158
gtpl6795
1h,2h,4h-pyrazolo[3,4-d]pyrimidin-4-one
HMS3371I11
allopurinol [ep monograph]
allopurinol [mi]
allopurinol [mart.]
allopurinolum [who-ip]
allopurinol [orange book]
allopurinol [usan]
allopurinol [who-ip]
allopurinol [hsdb]
allopurinol [jan]
allopurinol [usp monograph]
184856-42-6
allopurinol [ep impurity]
allopurinol [who-dd]
allopurinol [inn]
duzallo component allopurinol
allopurinol [usp-rs]
CCG-221406
HY-B0219
1,5-dihydropyrazolo[3,4-d]-pyrimidin-4-one
NC00492
SCHEMBL4627
tox21_110082_1
AB01274719-01
NCGC00260787-01
tox21_500102
J-504736
SCHEMBL1128219
4-hydroxy-pyrazolo[3,4-d]pyrimidin
AKOS024255717
TS-00028
1h,4h,5h-pyrazolo[3,4-d]pyrimidin-4-one
1h-pyrazolo[3,4-d]pyrimidin-4-ol (9ci)
cid_2094
bdbm35440
hexanurat
W-106892
STR05189
bdbm50016784
4h-pyrazolo[3,4-d]pyrimidin-4-one, 1,7-dihydro- (9ci)
180749-06-8
180749-07-9
184789-03-5
allopurinol, british pharmacopoeia (bp) reference standard
1h-pyrazolo[3,4-d]pyrimidin-4(2h)-one
AB00173448_05
OPERA_ID_1680
AB01274719_02
zyloric-300
aluline 300
xanthomax-300
xanthomax-100
bdbm50140241
hamarin 100
aluline 100
hamarin 300
uricto
mfcd00599413
us9138393, allopurinol
us9144538, allopurinol
bdbm181133
VU0611037-1
F2173-0394
allopurinol, european pharmacopoeia (ep) reference standard
SR-05000001983-2
sr-05000001983
allopurinol, united states pharmacopeia (usp) reference standard
HMS3651O13
SR-05000001983-1
allopurinol, pharmaceutical secondary standard; certified reference material
sr-01000075595
SR-01000075595-1
SBI-0050090.P004
HMS3714L22
SW199406-4
FT-0764079
Q412486
F18007
allopurinol (zyloprim)
4h-pyrazolo[3,4-d]pyrimidin-4-one, 2,5-dihydro- (9ci)
4h-pyrazolo[3,4-d]pyrimidin-4-one, 2,7-dihydro- (9ci)
BCP26973
AMY18272
SB10164
SDCCGSBI-0050090.P005
NCGC00015094-08
CCG-266128
NCGC00015094-22
2h-pyrazolo[3,4-d]pyrimidin-4-ol (9ci)
EN300-34144
zurinol
1h-pyrazolo(3,4-d)pyrimdin-4-ol
allopurinol (mart.)
allopurinol (usp-rs)
allopurinol (usp monograph)
allopurinolo
m04aa01
4'-hpp
allopurinol (ep monograph)
1,5-dihydro-4h-pyrazolo(3,4-d)pryimidin-4-one
allopurinol (ep impurity)
Z104486670

Research Excerpts

Overview

Allopurinol is a xanthine-oxidase inhibitor and can potentially reduce the formation of these superoxides that lead to brain damage in HIE. It is widely used for the treatment of hyperuricemia and gout.

ExcerptReference
"Allopurinol is a potent inhibitor of the enzyme xanthine oxidase used primarily in the treatment of hyperuricemia and gout. "( Allopurinol attenuates postoperative pain and modulates the purinergic system in patients undergoing abdominal hysterectomy: a randomized controlled trial.
Andrade, CF; de Oliveira, ED; Fagundes, AC; Hansel, G; Lara, DR; Martinelli, ES; Pedrini, RO; Schmidt, AP; Schmidt, SRG; Souza, DO; Valdameri, A, 2021
)
"Allopurinol is a xanthine-oxidase inhibitor and can potentially reduce the formation of these superoxides that lead to brain damage in HIE."( Allopurinol: Old Drug, New Indication in Neonates?
Annink, KV; Bel, FV; Benders, MJNL; Derks, JB; Franz, AR; Rudiger, M, 2017
)
"Allopurinol acts as a xanthine oxidase inhibitor that reduces the amount of free radicals after reactive oxygen species generation."( Effect of High-Dose Allopurinol Pretreatment on Cardiac Biomarkers of Patients Undergoing Elective Percutaneous Coronary Intervention: A Randomized Clinical Trial.
Alemzadeh-Ansari, MJ; Hosseini, SK; Jalali, A; Mohammadi, M; Pourhosseini, H; Talasaz, AH; Tokaldani, ML,
)
"Allopurinol is an inhibitor of xanthine oxidase. "( Allopurinol reverses liver damage induced by chronic carbon tetrachloride treatment by decreasing oxidative stress, TGF-β production and NF-κB nuclear translocation.
Aldaba-Muruato, LR; Moreno, MG; Muriel, P; Shibayama, M; Tsutsumi, V, 2013
)
"Allopurinol is a xanthine oxidase inhibitor and antioxidant free radical scavenger which facilitates the protection of ischemic organs in part via this mechanism of action. "( Allopurinol in renal ischemia.
Aliena-Valero, A; Carabén-Redaño, A; Cejalvo, D; Flores-Bellver, M; Lloris Carsí, JM; Martínez-Gil, N; Prieto-Moure, B; Toledo, AH; Toledo-Pereyra, LH, 2014
)
"Allopurinol is a purine hypoxanthine-based structural analog and a well-known inhibitor of xanthine oxidase."( Effects of allopurinol on exercise-induced muscle damage: new therapeutic approaches?
Fiuza-Luces, C; Garatachea, N; Lippi, G; Lucia, A; Pareja-Galeano, H; Perez-Quilis, C; Sanchis-Gomar, F; Santos-Lozano, A, 2015
)
"Allopurinol is a commonly used medication to treat hyperuricemia and its complications."( Pallidifloside D from Smilax riparia enhanced allopurinol effects in hyperuricemia mice.
Anderson, S; He, Y; Hou, PY; Mi, C; Wang, SQ; Wu, XH; Yu, F; Zhang, J; Zhang, YW, 2015
)
"Allopurinol is a xanthine oxidase enzyme inhibitor that is widely used for the treatment of hyperuricemia and gout. "( Antidepressant-like effects of the xanthine oxidase enzyme inhibitor allopurinol in rats. A comparison with fluoxetine.
Aksu, H; Birincioğlu, M; Dost, T; Gürbüz Özgür, B, 2015
)
"Allopurinol is an inhibitor of xanthine oxidase (XO) and thus can serve as an antioxidant that reduces oxidative stress."( Allopurinol Protects against Ischemia/Reperfusion-Induced Injury in Rat Urinary Bladders.
Chun, KS; Kim, GH; Kim, SI; Lim, JS; Na, YG; Shin, JH; Song, KH, 2015
)
"Allopurinol is a commonly used medication to treat hyperuricemia and its complications. "( Hypouricemic effect of allopurinol are improved by Pallidifloside D based on the uric acid metabolism enzymes PRPS, HGPRT and PRPPAT.
Anderson, S; He, Y; Hou, PY; Li, HG; Wang, SQ; Wu, XH; Zhang, J; Zhang, X; Zhang, YW, 2016
)
"Allopurinol is a potent inhibitor of the enzyme xanthine oxidase, used primarily in the treatment of hyperuricemia and gout. "( Anti-nociceptive properties of the xanthine oxidase inhibitor allopurinol in mice: role of A1 adenosine receptors.
Antunes, C; Böhmer, AE; Elisabetsky, E; Lara, DR; Porciúncula, LO; Schallenberger, C; Schmidt, AP; Souza, DO, 2009
)
"Allopurinol is an old and extensively used compound and seems to be well tolerated with no obvious central nervous system toxic effects at high doses."( Anti-nociceptive properties of the xanthine oxidase inhibitor allopurinol in mice: role of A1 adenosine receptors.
Antunes, C; Böhmer, AE; Elisabetsky, E; Lara, DR; Porciúncula, LO; Schallenberger, C; Schmidt, AP; Souza, DO, 2009
)
"Allopurinol seems to be a useful, inexpensive, well tolerated, and safe anti-ischaemic drug for patients with angina."( Effect of high-dose allopurinol on exercise in patients with chronic stable angina: a randomised, placebo controlled crossover trial.
Ang, DS; Lang, CC; Noman, A; Ogston, S; Struthers, AD, 2010
)
"Allopurinol is a prodrug converted to oxypurinol by xanthine oxidase, a process followed by an efficient enzyme inhibition. "( A new method for the quantification of superoxide dismutase mimics with an allopurinol-xanthine oxidase-lucigenin enhanced system.
Bordeianu, G; Nechifor, M; Serban, DN; Stanescu, R; Stoica, BA, 2011
)
"Allopurinol is an inhibitor of xanthine oxidase (XO), and XO is an enzyme that generates great amounts of reactive oxygen species. "( Secondary biliary cirrhosis in the rat is prevented by decreasing NF-κB nuclear translocation and TGF-β expression using allopurinol, an inhibitor of xanthine oxidase.
Aldaba-Muruato, LR; Hernández-Mercado, E; Moreno, MG; Muriel, P; Shibayama, M, 2012
)
"Allopurinol is a xanthine oxidase inhibitor that prevents the generation of free radicals and may play a role in the protection of the cells during cerebral ischemia."( Effect of allopurinol in focal cerebral ischemia in rats: an experimental study.
Berkman, MZ; Işik, N; Kalelioğlu, M; Pamir, MN; Sav, A, 2005
)
"Allopurinol is a specific inhibitor of xanthine oxidase activity."( A quantitative histochemical study of xanthine oxidase activity in rat liver using the cerium capture method in the presence of polyvinyl alcohol.
Bosch, KS; Frederiks, WM; Van den Munckhof, RJ; Van Noorden, CJ, 1994
)
"Allopurinol is a xanthine oxidase inhibitor widely used to control plasma uric acid levels. "( Allopurinol hypersensitivity syndrome: hypersensitivity to oxypurinol but not allopurinol.
Hamanaka, H; Mizutani, H; Nouchi, N; Shimizu, M; Shimizu, Y, 1998
)
"Allopurinol is a scavenger of the highly reactive hydroxyl radical (k2 approx. "( Allopurinol and oxypurinol are hydroxyl radical scavengers.
Grootveld, M; Gutteridge, JM; Halliwell, B; Moorhouse, PC; Quinlan, JG, 1987
)
"Allopurinol, which is an inhibitor of xanthine oxidase, inhibited blastogenic responses of human lymphocytes to PHA, PWM, and bacterial LPS."( Purine metabolic enzymes in lymphocytes. IV. Effects of enzyme inhibitors and enzyme substrates on the blastogenic responses of human lymphocytes.
Akuzawa, Y; Kurashige, S; Mitsuhashi, S, 1985
)
"Allopurinol is a potent inhibitor of the enzyme xanthine oxidase used in the treatment of hyperuricemia and gout. "( Effects of allopurinol on pain and anxiety in fibromyalgia patients: a pilot study.
Fagundes, AC; Schmidt, AP; Souza, DO,
)
"Allopurinol is an agent of first choice for urate lowering therapy."( What's new on the front-line of gout pharmacotherapy?
Blake, KEG; Saag, JL; Saag, KG, 2022
)
"Allopurinol is a urate-lowering therapy used to treat patients with gout. "( Allopurinol versus usual care in UK patients with ischaemic heart disease (ALL-HEART): a multicentre, prospective, randomised, open-label, blinded-endpoint trial.
Avery, AJ; Barr, RJ; Begg, AG; Duce, SL; Dumbleton, JS; Ford, I; Greenlaw, N; Hawkey, CJ; MacDonald, TM; Mackenzie, IS; Pigazzani, F; Ritchie, LD; Rogers, A; Rooke, ED; Struthers, AD; Taggar, JS; Townend, JN; Walker, A; Wei, L, 2022
)
"Allopurinol is a xanthine oxidase inhibitor that inhibits uric acid and reactive oxygen species (ROS) production."( Allopurinol inhibits excess glucose-induced trophoblast IL-1β and ROS production.
Abrahams, VM; Han, CS; Mulla, MJ; Negi, M, 2020
)
"Allopurinol is an orally administered inhibitor of xanthine oxidase used primarily in the treatment of hyperuricemia associated with gout. "( Physicochemical Stability of Compounded Allopurinol Suspensions in PCCA Base, SuspendIt.
Bostanian, LA; Graves, RA; Le, G; Mandal, TK; Morris, TC; Pramar, YV,
)
"Allopurinol is a potent inhibitor of the enzyme xanthine oxidase used in the treatment of hyperuricemia and gout. "( Allopurinol for fibromyalgia pain in adults: A randomized controlled trial.
Andrade, CF; Botelho, LM; de Oliveira, ED; Dos Santos, LMM; Fagundes, AC; Ferrari, SG; Lara, DR; Schmidt, AP; Schmidt, SRG; Souza, DO, 2022
)
"Allopurinol is a drug indicated for the treatment and prevention of gout. "( Allopurinol for the Treatment of Refractory Aggression: A Case Series.
Baugh, TB; Carr, CN; Straley, CM, 2017
)
"Allopurinol seems to be a good neuroprotector in several animal studies, but it has never been tested in combination with hypothermia."( Neuroprotection with hypothermia and allopurinol in an animal model of hypoxic-ischemic injury: Is it a gender question?
Alcántara-Horillo, S; Balada Caballé, R; Camprubí Camprubí, M; Durán Fernández-Feijóo, C; Lopez Ramos, MG; Lopez-Abad, M; Rodríguez-Fanjul, J, 2017
)
"Allopurinol is a xanthine oxidase inhibitor commonly used in the treatment of gout. "( Allopurinol augmentation in acute mania: A meta-analysis of placebo-controlled trials.
Chen, AT; Malmstrom, T; Nasrallah, HA, 2018
)
"Allopurinol is an effective urate-lowering therapy, but it has severe side effects."( A retrospective investigation of HLA-B*5801 in hyperuricemia patients in a Han population of China.
Cheng, H; Liu, J; Liu, W; Yan, D; Zhang, Y; Zuo, X, 2018
)
"Allopurinol is a xanthine oxidase inhibitor used in the treatment of patients with gout. "( [De-sensitization to allopurinol in a patient with tophi gout].
Hernández-Montoya, G; López-Rocha, EG; Rodríguez-Mireles, KA; Rodríguez-Pesina, AH,
)
"Allopurinol is a cornerstone therapy for patients with gout; however, non-adherence to allopurinol is prevalent in Singapore and limits its effectiveness."( Cost-effectiveness of an adherence-enhancing intervention for gout based on real-world data.
Lim, AYN; Lin, LW; Teng, GG; Wee, HL; Yoong, JS; Zethraeus, N, 2019
)
"Allopurinol is a first line agent in treating gout, but it also carries the risk of severe side effects. "( Allopurinol-Induced Stevens-Johnson Syndrome.
Gupta, SS; Kupfer, Y; Patti, R; Sabharwal, N, 2019
)
"Allopurinol is an FDA -Approved xanthine oxidase inhibitor, which is effective in the treatment of gout, hyperuricemia and uremic kidney stones in patients with an increased level of uric acid excretion. "( Allopurinol and Loss of Consciousness in a 78-old Year Man Suffering from Gout.
AkbariRad, M; Arian, M; Firoozi, A; Jami, M; Moghaddam, AB, 2020
)
"Allopurinol is a xanthine oxidase inhibitor that reduces the production of oxygen radicals as superoxide, which contributes to secondary energy failure and apoptosis in neurons and glial cells after reperfusion of hypoxic brain tissue and may further improve outcome if administered in addition to therapeutic hypothermia."( Effect of allopurinol in addition to hypothermia treatment in neonates for hypoxic-ischemic brain injury on neurocognitive outcome (ALBINO): study protocol of a blinded randomized placebo-controlled parallel group multicenter trial for superiority (phase
Allegaert, K; Annink, KV; Bassler, D; Benders, MJNL; Cattarossi, L; Franz, AR; Guimarães, H; Jacobs, Y; Klebermaß-Schrehof, K; Maiwald, CA; Mazela, J; Metsäranta, M; Metsvaht, T; Naulaers, G; Rüdiger, M; Stiris, T; van Bel, F; Vanhatalo, S; Vento, M, 2019
)
"Allopurinol is a potent xanthine oxidase inhibitor that is used in hyperuricemic patients to prevent gout. "( Effect of allopurinol on blood pressure: a systematic review and meta-analysis.
Agarwal, V; Hans, N; Messerli, FH, 2013
)
"Allopurinol is a popular and widely-prescribed anti-hyperuricemic agent that has been implicated in drug interactions with substrates of several cytochrome P450 (CYP) enzymes. "( Effects of repeated allopurinol administration on rat cytochrome P450 activity.
Hu, LF; Llu, YJ; Pan, XF; Shi, DW; Xu, RA; Xu, ZS; Ye, XL; Zhang, CH; Zhang, XH, 2013
)
"Allopurinol is a purine analogue that inhibits xanthine oxidase. "( Allopurinol Use during Pregnancy - Outcome of 31 Prospectively Ascertained Cases and a Phenotype Possibly Indicative for Teratogenicity.
Hoeltzenbein, M; Panse, M; Schaefer, C; Stieler, K; Wacker, E, 2013
)
"Allopurinol is a main cause of severe cutaneous adverse reactions (SCAR). "( Allopurinol hypersensitivity is primarily mediated by dose-dependent oxypurinol-specific T cell response.
Fontana, S; Largiadèr, CR; Mattsson, J; Pichler, WJ; Schnyder, K; Yerly, D; Yun, J, 2013
)
"Allopurinol is a frequently prescribed drug. "( Allopurinol use in pregnancy in three women with inflammatory bowel disease: safety and outcomes: a case series.
Andrews, JM; Bampton, PA; Doogue, MP; Fazal, MW; Leong, RW, 2013
)
"Allopurinol is a known inhibitor of xanthine oxidase, a source of free radicals during exercise."( GC-MS analysis of blood for the metabonomic investigation of the effects of physical exercise and allopurinol administration on rats.
Chatziioannou, AC; Kouretas, D; Mougios, V; Pechlivanis, A; Theodoridis, GA; Veskoukis, AS, 2014
)
"Allopurinol is a drug used primarily to treat hyperuricemia. "( In a double-blind, randomized and placebo-controlled trial, adjuvant allopurinol improved symptoms of mania in in-patients suffering from bipolar disorder.
Bajoghli, H; Brand, S; Ghaleiha, A; Haghighi, M; Holsboer-Trachsler, E; Jahangard, L; Soroush, S, 2014
)
"Allopurinol is a safe option, slightly better than other ULDs."( Safety of allopurinol compared with other urate-lowering drugs in patients with gout: a systematic review and meta-analysis.
Carmona, L; Castrejon, I; Loza, E; Pérez-Ruiz, F; Rosario, MP; Toledano, E, 2015
)
"Allopurinol is a commonly used medication to treat hyperuricemia and its complications."( Anti-hyperuricemia effects of allopurinol are improved by Smilax riparia, a traditional Chinese herbal medicine.
Anderson, S; He, Y; Mi, C; Wang, CZ; Wang, SQ; Wu, XH; Yuan, CS; Zhang, J; Zhang, YW, 2015
)
"Allopurinol is a urate-lowering agent that is commonly used to prevent chemotherapy-related hyperuricemia. "( Allopurinol hypersensitivity syndrome in patients with hematological malignancies: characteristics and clinical outcomes.
Ju, JH; Kim, WU; Kwok, SK; Lee, B; Min, HK; Park, SH; Park, YM, 2015
)
"Allopurinol is an efficacious urate-lowering therapy (ULT), but is associated with rare serious adverse drug reactions of Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), with higher risk among HLA-B*5801 carriers. "( Cost-effectiveness analysis of genotyping for HLA-B*5801 and an enhanced safety program in gout patients starting allopurinol in Singapore.
Dong, D; Finkelstein, E; Sung, C; Tan-Koi, WC; Teng, GG, 2015
)
"Allopurinol is an effective urate-lowering drug."( Effect of Allopurinol on Cardiovascular Outcomes in Hyperuricemic Patients: A Cohort Study.
Hallas, J; Larsen, KS; Lindegaard, HM; Pottegård, A, 2016
)
"Allopurinol is a potent xanthine oxidase inhibitor used in hyperuricemic patients."( Benefits of Allopurinol Treatment on Blood Pressure and Renal Function in Patients with Early Stage of Chronic Kidney Disease.
Burata, A; Ruangkanchanasetr, P; Satirapoj, B; Supasyndh, O; Wirajit, O, 2015
)
"Allopurinol is a frequent cause of severe cutaneous adverse reactions (SCARs), such as drug reaction with eosinophilia and systemic symptoms (DRESS), Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). "( In vitro test to confirm diagnosis of allopurinol-induced severe cutaneous adverse reactions.
Chakkavittumrong, P; Chanprapaph, K; Chularojanamontri, L; Disphanurat, W; Klaewsongkram, J; Rerknimitr, P; Rerkpattanapipat, T; Srinoulprasert, Y; Srisuttiyakorn, C; Sukasem, C; Suthumchai, N; Thantiworasit, P; Tovanabutra, N; Tuchinda, P, 2016
)
"Allopurinol is a xanthine oxidase inhibitor used to prevent gout that also has several positive effects on the cardiovascular system."( Multicentre, prospective, randomised, open-label, blinded end point trial of the efficacy of allopurinol therapy in improving cardiovascular outcomes in patients with ischaemic heart disease: protocol of the ALL-HEART study.
Avery, A; Begg, A; Ford, I; Hawkey, C; MacDonald, TM; Mackenzie, IS; Struthers, AD; Taggar, J; Walker, A; Wei, L, 2016
)
"Allopurinol is a well-known antioxidant that protects tissue against ischemia and reperfusion injury, blocking purine catabolism, and possibly reducing TNF-α and other cytokines. "( Allopurinol Protective Effect of Renal Ischemia by Downregulating TNF-α, IL-1β, and IL-6 Response.
Belda-Antolí, M; Cejalvo-Lapeña, D; Lloris-Carsí, JM; Prieto-Moure, B; Toledo-Pereyra, LH, 2017
)
"Allopurinol is an inhibitor of xanthine oxidoreductase (XOR) and inhibits the generation of uric acid (UA) as the final product of purine catabolism, as well as the resulting generation of superoxide (O2(-)), in humans. "( Allopurinol, an inhibitor of uric acid synthesis--can it be used for the treatment of metabolic syndrome and related disorders?
Nozaki, S; Onuma, M; Suzuki, I; Yamauchi, T, 2009
)
"Allopurinol (ALLO) is a xanthine oxidase inhibitor that also scavenges free radicals."( Effects of allopurinol on cardiac function and oxidant stress in chronic intermittent hypoxia.
Chen, L; Scharf, SM; Williams, AL, 2010
)
"Allopurinol is an effective urate lowering drug, which is usually well-tolerated with no adverse effects in most cases, but about 2% of the treated patients develop a skin rash, and patients may experience severe allopurinol-induced hypersensitivity syndrome."( [Allopurinol-induced hypersensitivity syndrome].
Bata-Csörgő, Z; Gyulai, R; Kemény, L; Kinyó, A; Lakatos, A; Varga, A; Varga, E, 2012
)
"Allopurinol is a drug that has been used for decades to lower serum urate levels in patients with gout or chronic renal failure and in cancer patients undergoing chemotherapy at risk of tumor lysis syndrome. "( Pharmacogenetics of allopurinol--making an old drug safer.
Cheung, BM; Lam, MP; Yeung, CK, 2013
)
"Allopurinol is an inhibitor of the enzyme xanthine oxidase, with previously suggested anti-aggressive effects."( Allopurinol for the treatment of aggressive behaviour in patients with dementia.
Cruz, MR; Lara, DR; Moriguchi, EH; Souza, DO; Xavier, F, 2003
)
"allopurinol is a safe and effective dose in Red-tailed Hawks (Buteo jamaicensis) to reduce plasma uric acid concentrations, experimental studies were performed using the physiologically occurring postprandial hyperuricaemia."( Further studies on the use of allopurinol to reduce plasma uric acid concentrations in the Red-tailed Hawk (Buteo jamaicensis) hyperuricaemic model.
Lumeij, JT; Poffers, J; Redig, PT; Timmermans-Sprang, EP, 2002
)
"Allopurinol is a free radical scavenger, suppresses the production of TNF-alpha and downregulates the expression of ICAM-1 and P2X(7) receptors on monocyte/macrophages."( Cetirizine and allopurinol as novel weapons against cellular autoimmune disorders.
Namazi, MR, 2004
)
"Allopurinol is a hypoxanthine analogue used to treat Leishmania infections that also displays activity against the related parasite Trypanosoma brucei. "( Trypanosoma brucei: expression of multiple purine transporters prevents the development of allopurinol resistance.
Al-Salabi, MI; Candlish, D; Coutts, SE; de Koning, HP; Natto, MJ; Wallace, LJ, 2005
)
"Allopurinol is a very efficacy and fairly safety drug for the treatment of uric acid overproduction in patients with complete and partial HPRT deficiency."( Efficacy and safety of allopurinol in patients with the Lesch-Nyhan syndrome and partial hypoxanthine- phosphoribosyltransferase deficiency: a follow-up study of 18 Spanish patients.
Prior, C; Puig, JG; Torres, RJ, 2006
)
"Allopurinol is a drug that is widely used to treat hyperuricemia, but it is often prescribed inappropriately."( Inappropriate prescription of allopurinol in a teaching hospital.
Athisakul, S; Louthrenoo, W; Wangkaew, S, 2007
)
"Allopurinol is a uric acid lowering drug used in the treatment of gout and the prevention of tumor lysis syndrome. "( A simple method for quantification of allopurinol and oxipurinol in human serum by high-performance liquid chromatography with UV-detection.
Brouwers, JR; Jansen, TL; Movig, KL; Nijdam, LC; Reinders, MK; van de Laar, MA; van Roon, EN, 2007
)
"Allopurinol is a moderately active hypouricemic drug."( Optimizing therapy with allopurinol: factors limiting hypouricemic efficacy.
Chung, Y; Day, RO; Graham, GG; Stocker, SL, 2008
)
"Allopurinol is a widely-prescribed urate-lowering agent. "( Allopurinol hypersensitivity syndrome: a preventable severe cutaneous adverse reaction?
Ariyasinghe, JT; Lee, HY; Thirumoorthy, T, 2008
)
"Allopurinol is a drug of wide clinical use and good tolerance. "( [Syndrome of allopurinol hypersensitivity. Report of a new case and review of the Spanish literature].
Andrada, E; Berbegal, J; Lluch, V; López-Benito, I; Morera, J; Navarro, V, 1994
)
"Allopurinol test is a useful tool for the preliminary investigation of urea cycle function, avoiding the possible hyperammonemia caused by other test, and permitting extensive familial studies without hospitalization. "( [Diagnosis of ornithine carbamoyl transferase deficiency and heterozygote detection with allopurinol loading test].
Fábrega, C; Fernández Alvarez, E; Mas, A; Pineda, M; Vilaseca, MA, 1993
)
"Allopurinol is a potent xanthine oxidase inhibitor that has been administered to animals to protect tissues from oxidant injury. "( Allopurinol inhibition of neutrophilic alveolar response during hyperoxia.
Bryan, CL; Emanuel, B; Jenkinson, SG; Lewis, RE; Owens, SL, 1993
)
"Allopurinol riboside is an experimental agent for the treatment of leishmaniasis and American trypanosomiasis. "( Effects of probenecid on the pharmacokinetics of allopurinol riboside.
Shapiro, TA; Were, JB, 1993
)
"Allopurinol promises to be a useful alternative to steroids in the treatment of uveitis."( Effects of systemically applied allopurinol and prednisolone on experimental autoimmune uveitis.
Augustin, AJ; Grus, FH; Loeffler, KU; Lutz, J; Sekundo, W, 1999
)
"Allopurinol is a xanthine oxidase inhibitor."( Aldehyde oxidase-catalysed oxidation of methotrexate in the liver of guinea-pig, rabbit and man.
Beedham, C; Brown, JE; Clarke, SE; Jordan, CG; Laljee, H; Rashidi, MR, 1999
)
"Allopurinol is known to be a causative agent of aplastic anemia, but there have been few reports of acute PRCA induced by allopurinol."( Acute pure red cell aplasia associated with allopurinol therapy.
Akiyama, Y; Hamahata, K; Kubota, M; Lin, YW; Okazaki, S; Usami, I; Watanabe, K; Yoshibayashi, M, 1999
)
"Allopurinol is a scavenger of oxygen-derived free radicals, which it is suggested play a role in the development of UC and pouchitis."( Allopurinol as prophylaxis against pouchitis following ileal pouch-anal anastomosis for ulcerative colitis. A randomized placebo-controlled double-blind study.
Andersson, M; Bark, T; Gullberg, K; Hallgren, T; Jiborn, H; Joelsson, M; Magnusson, I; Ojerskog, B; Oresland, T; Raab, Y; Sjödahl, R, 2001
)
"Allopurinol is a drug which could be valuable in the treatment of stone patients. "( The effect of allopurinol on urinary oxalate excretion in stone formers.
Mathieson, A; Paterson, PJ; Scott, R; Smith, M, 1978
)
"Allopurinol was shown to be an effective inhibitor of this reaction in the laboratory experiments, but not in patients."( Protective influence of pretreatment with allopurinol on myocardial function in patients undergoing coronary artery surgery.
Bochenek, A; Gryzbek, H; Mistarz, K; Religa, Z; Spyt, TJ; Zembala, M, 1990
)
"Allopurinol is a widely used drug in the management of hyperuricaemia. "( Clinical pharmacokinetics of allopurinol.
Murrell, GA; Rapeport, WG,
)

Effects

Allopurinol has a synergistic effect when used with intra-lesional sodium Stibogluconate and effectively reduces the treatment duration required for complete cure of cutaneous Leishmaniasis. Gout/allopur inol intake has a high prevalence in elderly patients acutely admitted to hospital and are associated with renal and cardiovascular diseases.

Allopurinol has been used for the treatment of gout and conditions associated with hyperuricemia for several decades. The drug has been successfully used in granulomatous diseases like sarcoidosis or reactions to polymethylmethacrylate spheres.

ExcerptReference
"Allopurinol has an antioxidant property that might partially reverse endothelial dysfunction in patients with certain comorbidities. "( Allopurinol and endothelial function: A systematic review with meta-analysis of randomized controlled trials.
Alem, MM, 2018
)
"Oral Allopurinol has a synergistic effect when used with intra-lesional sodium Stibogluconate and effectively reduces the treatment duration required for complete cure of cutaneous Leishmaniasis. "( Synergistic Effect Of Oral Allopurinol And Intralesional Sodium Stibogluconate In The Treatment Of Cutaneous Leishmaniasis.
Adeeb, H; Mohammad, A; Rashid, HU; Rehman, N; Ullah, I; Zeb, M,
)
"As allopurinol has a more polar character than benzaldehyde azine, it was easy to wash out from the SPE phase."( Hydrazine determination in allopurinol using derivatization and SPE for sample preparation.
Kormány, R; Tamás, K; Wachter-Kiss, E, 2018
)
"Gout/allopurinol intake has a high prevalence in elderly patients acutely admitted to hospital and are associated with renal and cardiovascular diseases, an increased rate of adverse events and a high degree of drug consumption. "( Gout, allopurinol intake and clinical outcomes in the hospitalized multimorbid elderly.
Conca, A; Corrao, S; Djade, CD; Franchi, C; Mannucci, PM; Marcucci, M; Marengoni, A; Nobili, A; Pasina, L; Salerno, F; Tettamanti, M, 2014
)
"Allopurinol has a remarkable effect in the treatment of ACS and can improve the oxidative stress and inflammatory reaction indicators of patients. "( Clinical Study on efficacy of allopurinol in patients with acute coronary syndrome and its functional mechanism.
Du, H; Huang, Y; Shen, J; Xu, Z; Zhang, C; Zhang, D; Zhang, K; Zhang, X,
)
"Allopurinol has a significant, positive effect on nonbacterial prostatitis. "( Ameliorative effect of allopurinol on nonbacterial prostatitis: a parallel double-blind controlled study.
Ekblom, M; Persson, BE; Ronquist, G, 1996
)
"Allopurinol has been used for the treatment of gout and conditions associated with hyperuricemia for several decades. "( Anti-gout agent allopurinol exerts cytotoxicity to human hormone-refractory prostate cancer cells in combination with tumor necrosis factor-related apoptosis-inducing ligand.
Goda, AE; Horinaka, M; Miki, T; Mizutani, Y; Sakai, T; Shiraishi, T; Wakada, M; Yano, K; Yasuda, T; Yoshida, T, 2008
)
"Allopurinol has been successfully used in granulomatous diseases such as sarcoidosis or reactions to polymethylmethacrylate spheres; therefore, we decided to evaluate the possible efficacy of this drug in three patients with long-lasting, therapy-resistant DGA."( Treatment of disseminated granuloma annulare with allopurinol: case report.
Ghilardi, A; Grazzini, M; Mazzatenta, C,
)
"Allopurinol has been widely used for treatment of hyperuricemia, however, it may be associated with various adverse effects. "( An allopurinol-controlled, randomized, double-dummy, double-blind, parallel between-group, comparative study of febuxostat (TMX-67), a non-purine-selective inhibitor of xanthine oxidase, in patients with hyperuricemia including those with gout in Japan: p
Fujimori, S; Hada, T; Hosoya, T; Kamatani, N; Kohri, K; Matsuzawa, Y; Nakamura, T; Ueda, T; Yamamoto, T; Yamanaka, H, 2011
)
": Allopurinol has been widely used for treatment of hyperuricemia, however, it may be associated with various adverse effects. "( Placebo-controlled, double-blind study of the non-purine-selective xanthine oxidase inhibitor Febuxostat (TMX-67) in patients with hyperuricemia including those with gout in Japan: phase 3 clinical study.
Fujimori, S; Hada, T; Hisashi, Y; Hosoya, T; Kamatani, N; Kenjiro, K; Kohri, K; Matsuzawa, Y; Nakamura, T; Naoyuki, K; Shin, F; Takanori, U; Tatsuo, H; Tetsuya, Y; Toshikazu, H; Toshitaka, N; Ueda, T; Yamamoto, T; Yamanaka, H; Yuji, M, 2011
)
"Allopurinol has been widely used for treatment of hyperuricemia, however, it may be associated with various adverse effects. "( A repeated oral administration study of febuxostat (TMX-67), a non-purine-selective inhibitor of xanthine oxidase, in patients with impaired renal function in Japan: pharmacokinetic and pharmacodynamic study.
Hosoya, T; Iwao, O; Ohno, I; Tatsuo, H, 2011
)
"Allopurinol has been widely used for the treatment of hyperuricemia, however, it may be associated with various adverse effects. "( Placebo-controlled double-blind dose-response study of the non-purine-selective xanthine oxidase inhibitor febuxostat (TMX-67) in patients with hyperuricemia (including gout patients) in japan: late phase 2 clinical study.
Fujimori, S; Hada, T; Hisashi, Y; Hosoya, T; Kamatani, N; Kenjiro, K; Kohri, K; Matsuzawa, Y; Nakamura, T; Naoyuki, K; Shin, F; Takanori, U; Tatsuo, H; Tetsuya, Y; Toshikazu, H; Toshitaka, N; Ueda, T; Yamamoto, T; Yamanaka, H; Yuji, M, 2011
)
"Allopurinol has been widely used for the treatment of hyperuricemia, however, it may be associated with various adverse effects. "( An allopurinol-controlled, multicenter, randomized, open-label, parallel between-group, comparative study of febuxostat (TMX-67), a non-purine-selective inhibitor of xanthine oxidase, in patients with hyperuricemia including those with gout in Japan: phas
Fujimori, S; Hada, T; Hisashi, Y; Hosoya, T; Kamatani, N; Kenjiro, K; Kohri, K; Matsuzawa, Y; Nakamura, T; Naoyuki, K; Shin, F; Takanori, U; Tatsuo, H; Tetsuya, Y; Toshikazu, H; Toshitaka, N; Ueda, T; Yamamoto, T; Yamanaka, H; Yuji, M, 2011
)
"Allopurinol has been the archetypal XO inhibitor for over 40 years."( The role of urate and xanthine oxidase inhibitors in cardiovascular disease.
George, J; Struthers, AD, 2008
)
"Allopurinol has been widely used to reduce the severity of the reperfusion injury. "( Prevention of deleterious effects of reperfusion injury using one-week high-dose allopurinol.
Aşlar, AK; Kale, IT; Köksoy, C; Kuzu, A; Tanik, A; Terzi, C, 2001
)
"Allopurinol has been reported to improve cell survival in a variety of conditions, including the ischemia-reperfusion injury occurring in skin flaps. "( Effect of allopurinol on the survival of experimental pig flaps.
Kerrigan, CL; MacKay, A; Picard-Ami, LA, 1992
)
"Allopurinol has been employed as a "specific" inhibitor of xanthine oxidase in studies of hypoxic/reoxygenation injury. "( On the specificity of allopurinol and oxypurinol as inhibitors of xanthine oxidase. A pulse radiolysis determination of rate constants for reaction of allopurinol and oxypurinol with hydroxyl radicals.
Butler, J; Halliwell, B; Hoey, BM, 1988
)
"Allopurinol has been shown to provide significant protection against ischemia/reperfusion-induced microvascular and parenchymal cell injury. "( Allopurinol does not enhance antioxidant properties of extracellular fluid.
Granger, DN; Grisham, MB; Parks, DA; Zimmerman, BJ, 1988
)
"Allopurinol has been universally successful in lowering the serum uric acid concentration and uric acid excretion to normal levels, while not significantly affecting the clearance of urate or other aspects of renal function."( The treatment of gout and disorders of uric acid metabolism with allopurinol.
Houpt, JB; Ogryzlo, MA; Urowitz, MB; Weber, HM, 1966
)
"Oral allopurinol has been proven to be effective for the management of granulomatous reactions to tattoos."( Granulomatous tattoo reaction treated with topical allopurinol.
Chaves-Álvarez, A; Moreno-Casas, G; Pereira-González, A; Rodríguez-Nevado, I; Rubio-Fernández, A, 2023
)
"Allopurinol has been utilized successfully in adult and pediatric patients with inflammatory bowel disease who have experienced 6MMP related gastrointestinal toxicity."( Allopurinol to Prevent Mercaptopurine Adverse Effects in Children and Young Adults With Acute Lymphoblastic Leukemia.
Bostrom, B; Kamojjala, R, 2021
)
"The allopurinol loading test has been traditionally used to differentiate between HX types I and II."( Modern diagnostic approach to hereditary xanthinuria.
Bartl, J; Dolezel, Z; Fairbanks, L; Hurba, O; Marinaki, A; Mraz, M; Stiburkova, B, 2015
)
"Allopurinol has shown significant efficacy for preventing formation of calcium stones in hyperuricosuric patients."( Prevention of renal stone disease recurrence. A systematic review of contemporary pharmaceutical options.
Duvdevani, M; Gofrit, ON; Pode, D; Sfoungaristos, S; Yutkin, V, 2015
)
"Allopurinol, which has been used in clinical practice for almost 50 years, is the drug of first choice for long-term control of gout."( [The role of uric acid and allopurinol therapy in cardiovascular disease].
Linhart, A; Rob, D, 2015
)
"Allopurinol has been shown in coronary arterial disease to prolong exercise before angina occurs, likely by prevention of oxygen wastage in tissues and reduction of harmful oxidative stress."( A Randomized Controlled Trial of Allopurinol in Patients With Peripheral Arterial Disease.
Robertson, AJ; Struthers, AD, 2016
)
"Allopurinol has been presented as a safe and effective adjunct to thiopurine therapy in inflammatory bowel disease (IBD). "( Combination of thiopurines and allopurinol: adverse events and clinical benefit in IBD.
Govani, SM; Higgins, PD, 2010
)
"Allopurinol has been a standard hypouricemic agent for more than 40 years, but febuxostat, which is also a xanthine oxidase inhibitor, is now available. "( Febuxostat efficacy in allopurinol-resistant tophaceous gout.
Reid, G; Uh, M, 2011
)
"Allopurinol has been reported as a common cause of severe cutaneous adverse reactions (SCARs). "( Association between HLA-B*58:01 allele and severe cutaneous adverse reactions with allopurinol in Han Chinese in Hong Kong.
Chan, JC; Chang, MM; Cheng, SH; Chiu, ML; Hu, M; Li, L; Ng, MH; Tomlinson, B; Yeung, CK, 2012
)
"Allopurinol mouthwash has been used to prevent stomatitis induced by cancer chemotherapy."( Development of patient-friendly preparations: preparation of a new allopurinol mouthwash containing polyethylene(oxide) and carrageenan.
Hanawa, T; Kawata, K; Masuda, N; Mohri, K; Nakajima, S; Suzuki, M, 2004
)
"Allopurinol has been shown to improve endothelial function in chronic heart failure. "( High-dose allopurinol improves endothelial function by profoundly reducing vascular oxidative stress and not by lowering uric acid.
Belch, JJ; Carr, E; Davies, J; George, J; Struthers, A, 2006
)
"Allopurinol has been reported to ameliorate the side effects in patients following shock wave lithotripsy (SWL); however, the mechanism has not been studied. "( Allopurinol blocks shock-wave-induced rises in cytosolic calcium levels in MDCK cells.
Chen, WC; Huang, JK; Jan, CR; Lee, YH; Ou, HC; Tseng, CJ, 1997
)
"Allopurinol has been used in the management of hyperuricemic states for several years. "( Observations and effects of educational consults on allopurinol prescribing.
Bayliff, CD; Bellamy, N; Devlin, JW, 1992
)
"Allopurinol (ALLO) has been shown to reduce the extent of myocardial necrosis in various systems."( Modulation of catecholamine cardiomyopathy by allopurinol.
Chen, V; Downing, SE; Jiang, JP, 1991
)
"Allopurinol and caffeine have been used to measure metabolite formation followed by renal elimination of both parent substance and metabolite."( Liver function assessment by drug metabolism.
Barstow, L; Small, RE, 1990
)
"Allopurinol has been shown to have a protective effect on ischaemic tissue by the indirect prevention of excessive purine loss. "( An assessment of the possible protective effect of allopurinol in acute stroke.
Aspey, BS; Harrison, MJ; Iansek, R; Packham, D, 1986
)
"Allopurinol has been shown to ameliorate the myelotoxicity of 5-fluorouracil (5-FU) given as an infusion. "( Failure of allopurinol to provide clinically significant protection against the hematologic toxicity of a bolus 5-FU schedule.
Ahmann, FR; Garewal, H, 1986
)
"Allopurinol toxicity has been associated with the use of this drug in patients with renal insufficiency, a situation where the half-life of oxipurinol, the major metabolite of allopurinol, is prolonged. "( Evaluation of a thiazide-allopurinol drug interaction.
Hande, KR, 1986
)
"Allopurinol has been shown to decrease the gastro-intestinal and bone marrow toxicity of 5-fluorouracil. "( Allopurinol mouthwashes and 5-fluorouracil induced oral toxicity.
Clark, PI; Slevin, ML, 1985
)

Actions

Allopurinol inhibited the increase in fetal plasma uric acid and suppressed the fetal femoral vasoconstrictor, glycaemic and lactate acidaemic responses during hypoxia. The effect on brain damage was inconclusive in these preclinical trials.

ExcerptReference
"Allopurinol seemed to inhibit the formation of superoxide and to scavenge free radicals directly, but the effect on brain damage was inconclusive in these preclinical trials."( Allopurinol: Old Drug, New Indication in Neonates?
Annink, KV; Bel, FV; Benders, MJNL; Derks, JB; Franz, AR; Rudiger, M, 2017
)
"Allopurinol inhibited the increase in fetal plasma uric acid and suppressed the fetal femoral vasoconstrictor, glycaemic and lactate acidaemic responses during hypoxia (all P < 0.05), effects that were restored to control levels with fetal NO blockade."( Xanthine oxidase and the fetal cardiovascular defence to hypoxia in late gestation ovine pregnancy.
Allison, BJ; Brain, KL; Derks, JB; Giussani, DA; Hansell, JA; Herrera, EA; Kaandorp, JJ; Kane, AD; Niu, Y, 2014
)
"Allopurinol does not inhibit atrophy of skeletal muscle caused by prolonged unloading. "( Allopurinol mitigates muscle contractile dysfunction caused by hindlimb unloading in mice.
Arbogast, S; Matuszczak, Y; Reid, MB, 2004
)
"Allopurinol did not cause further increase in adenosine wash-out in rabbit hearts."( Reperfusion arrhythmias and purine wash-out in isolated rat and rabbit heart. Effect of allopurinol, dimethylthiourea and calcium reduction.
Beresewicz, A; Karwatowska-Prokopczuk, E; Kopacz, M, 1993
)
"Allopurinol reduced the increase of xanthine, uric acid, MDA in the muscle and CPK in blood effluent from gracilis muscle after reperfusion. "( The effect of allopurinol on interstitial purine metabolism and tissue damage in skeletal muscle I-R injury.
Akiyama, Y; Asami, A; Kitajima, M; Orii, M; Shirasugi, N; Yamazaki, M, 1996
)
"Allopurinol did not inhibit superoxide production induced by opsonized zymosan, phorbol myristic acetate, or formylmethionylleucylphenylalanine."( Effect of allopurinol on neutrophil superoxide production, chemotaxis, or degranulation.
Bose, SK; Grisham, MB; Jones, HP; McCord, JM; Schott, A; Shannon, VA, 1985
)
"Allopurinol is known to cause severe cutaneous adverse drug reactions (SCAR) in Malaysia. "( Incidence of allopurinol-induced severe cutaneous adverse drug reaction in Malaysia.
Fong, SL; Hariraj, V; Lai, PSM; Lee, SC; Lim, JR; Lim, KS; Ng, WL; Ramli, A; Wo, WK, 2022
)
"Allopurinol may cause Meige syndrome-like blepharospasm, the mechanism of which may be related to the inhibition of dopamine activity by affecting adenosine level in the brain."( Report: A case report of Meige syndrome-like blepharospasm caused by ingestion of allopurinol.
LaiMin, L, 2020
)
"Allopurinol is known to inhibit thiopurine methyl-transferase which reduces red cell 6MMP and increases 6TGN."( Allopurinol to Prevent Mercaptopurine Adverse Effects in Children and Young Adults With Acute Lymphoblastic Leukemia.
Bostrom, B; Kamojjala, R, 2021
)
"Allopurinol can cause HLA class I-associated life-threatening severe skin reactions. "( Allopurinol hepatotoxicity is associated with human leukocyte antigen Class I alleles.
Barnhart, H; Fontana, RJ; Hoofnagle, J; Kleiner, D; Li, YJ; Phillips, E; Saeed, N, 2021
)
"Allopurinol is a main cause of severe cutaneous adverse reactions (SCAR). "( Allopurinol hypersensitivity is primarily mediated by dose-dependent oxypurinol-specific T cell response.
Fontana, S; Largiadèr, CR; Mattsson, J; Pichler, WJ; Schnyder, K; Yerly, D; Yun, J, 2013
)
"Allopurinol can enhance the potency of thiopurine treatment."( Allopurinol enhanced thiopurine treatment for inflammatory bowel disease: safety considerations and guidelines for use.
McCabe, RP; Min, MX; Weinberg, DI, 2014
)
"Allopurinol is a frequent cause of severe cutaneous adverse reactions (SCARs), such as drug reaction with eosinophilia and systemic symptoms (DRESS), Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). "( In vitro test to confirm diagnosis of allopurinol-induced severe cutaneous adverse reactions.
Chakkavittumrong, P; Chanprapaph, K; Chularojanamontri, L; Disphanurat, W; Klaewsongkram, J; Rerknimitr, P; Rerkpattanapipat, T; Srinoulprasert, Y; Srisuttiyakorn, C; Sukasem, C; Suthumchai, N; Thantiworasit, P; Tovanabutra, N; Tuchinda, P, 2016
)
"Allopurinol is used to lower serum uric acid (sUA) levels in gout patients. "( Relationship between physician specialty and allopurinol prescribing patterns: a study of patients with gout in managed care settings.
Becker, LK; Dabbous, O; Hariri, A; Krishnan, E; Pandya, BJ; Riedel, AA; Swindle, JP, 2011
)
"Allopurinol does not produce additional antihypertensive effects in patients with treated arterial hypertension. "( Effect of allopurinol on blood pressure and aortic compliance in hypertensive patients.
Kostka-Jeziorny, K; Tykarski, A; Uruski, P, 2011
)
"Allopurinol intake caused increase in resting xanthine and hypoxanthine plasma concentrations, however it did not affect the slow component of oxygen uptake during exercise."( Allopurinol intake does not modify the slow component of V(.)O(2) kinetics and oxidative stress induced by severe intensity exercise.
Chlubek, D; Jakubowska, K; Laskowski, R; Olek, RA; Olszewska, M; Safranow, K, 2012
)
"Allopurinol promotes the salvage of purines, possibly increasing endogenous adenosine levels. "( Allopurinol augmentation in the outpatient treatment of bipolar mania: a pilot study.
Berg, A; Bresee, C; Fan, A; Glassman, LH; Rapaport, MH, 2012
)
"Allopurinol can inhibit biomarkers of oxidative activation in colon adenomatous polyps and normal adjacent tissue."( A randomized, placebo-controlled, preoperative trial of allopurinol in subjects with colorectal adenoma.
Argusti, A; Bandelloni, R; Benelli, R; Boccardo, S; Branchi, D; Coccia, G; Crosta, C; De Roberto, G; DeCensi, A; Gatteschi, B; Meroni, E; Michetti, P; Minetti, E; Mori, M; Munizzi, F; Puntoni, M; Salvi, S; Sonzogni, A; Turbino, L; Zanardi, S, 2013
)
"Allopurinol did not produce a significant degree of protection against 5-FU-induced myelosuppression or mucositis on either dose schedule."( Effect of allopurinol on the toxicity of high-dose 5-fluorouracil administered by intermittent bolus injection.
Howell, SB; Pfeifle, CE; Wung, WE, 1983
)
"Allopurinol reduced the increase in right hemisphere water content and markedly reduced atrophy."( Allopurinol administered after inducing hypoxia-ischemia reduces brain injury in 7-day-old rats.
Heitjan, DF; Palmer, C; Roberts, RL; Towfighi, J, 1993
)
"Allopurinol inhibits the increase in portal vein pressure induced by AGEPC, increased [K+]o or phenylephrine; the inhibitory effect increases with increasing concentrations of the agents."( Stimulation of uric acid release from the perfused rat liver by platelet activating factor or potassium.
Hill, CE; Olson, MS, 1987
)

Treatment

Allopurinol and allomaron-treated patients were examined biochemically by 17 parameters of the blood and urine. In allopur inol treated ischemic and reperfused groups, the levels of Na+K+ATPase activity were high compared to the untreated group.

ExcerptReference
"Allopurinol treatment significantly reduced hepatic steatosis, epididymal fat, serum UA, HOMA-IR, hepatic enzyme levels, and cholesterol in the OLETF-HFrD-Allo group."( Allopurinol ameliorates high fructose diet induced hepatic steatosis in diabetic rats through modulation of lipid metabolism, inflammation, and ER stress pathway.
Ahn, KJ; Cho, IJ; Chung, HY; Hwang, YC; Jeong, IK; Jeong, SW; Lee, SH; Lim, SJ; Moon, JY; Oh, DH; Yoo, J, 2021
)
"Allopurinol treatment reduced XO activity to 5% of the basal levels (P < 0.05), with skeletal muscle uric acid levels being almost undetectable."( Xanthine oxidase inhibition attenuates skeletal muscle signaling following acute exercise but does not impair mitochondrial adaptations to endurance training.
Hiam, DS; McConell, GK; Nicolas, MA; Wadley, GD, 2013
)
"Allopurinol treatment was well tolerated and improved the 3-month functional status of patients with acute ischemic stroke who had high levels of SUA without considering the decreasing effect of allopurinol on SUA."( Allopurinol as a preventive contrivance after acute ischemic stroke in patients with a high level of serum uric acid: a randomized, controlled trial.
Hatami, A; Houshmandzad, S; Mahmoodpoor, A; Namdar, S; Pashapour, A; Rikhtegar, R; Sadeghihokmabadi, E; Sharifipour, E; Taheraghdam, AA; Tazik, M, 2014
)
"Allopurinol treatment in the I/R injury was generated significantly ameliorating all I/R-induced changes."( Allopurinol Protects against Ischemia/Reperfusion-Induced Injury in Rat Urinary Bladders.
Chun, KS; Kim, GH; Kim, SI; Lim, JS; Na, YG; Shin, JH; Song, KH, 2015
)
"Allopurinol treatment is well tolerated and attenuates the rise in intercellular adhesion molecule-1 levels seen after stroke. "( Allopurinol use yields potentially beneficial effects on inflammatory indices in those with recent ischemic stroke: a randomized, double-blind, placebo-controlled trial.
Dawson, J; Harrow, C; Lees, KR; Muir, SW; Sattar, N; Walters, MR; Weir, CJ, 2008
)
"Allopurinol treatment significantly lowered uric acid levels, reduced albuminuria, and ameliorated tubulointerstitial injury, but it did not prevent mesangial expansion."( Effect of lowering uric acid on renal disease in the type 2 diabetic db/db mice.
Heinig, M; Johnson, RJ; Kosugi, T; Nakagawa, T; Nakayama, T; Roncal, C; Sanchez-Lozada, LG; Yuzawa, Y; Zhang, L, 2009
)
"Allopurinol pretreatment suppressed O(2)(-) generation in the brain-perfused blood in the jugular vein, and oxidative stress, early inflammation, and endothelial injury in the acute phase of forebrain ischemia/reperfusion."( Xanthine oxidase is one of the major sources of superoxide anion radicals in blood after reperfusion in rats with forebrain ischemia/reperfusion.
Aki, HS; Aoki, T; Fujita, M; Kasaoka, S; Kawamura, Y; Kobayashi, C; Kutsuna, S; Maekawa, T; Maruyama, I; Ono, T; Tsuruta, R; Wakatsuki, J; Yuasa, M, 2009
)
"Allopurinol treatment did not impact the course of DOCA-salt hypertension regardless of the timing of administration."( Allopurinol does not decrease blood pressure or prevent the development of hypertension in the deoxycorticosterone acetate-salt rat model.
Burnett, R; Davis, RP; Fink, GD; Linder, AE; Szasz, T; Watts, SW, 2010
)
"Allopurinol-treated hearts had significantly decreased nerve growth factor expression, which was substantially increased after coadministration of 3-morpholinosydnonimine."( Differential effects of NADPH oxidase and xanthine oxidase inhibition on sympathetic reinnervation in postinfarct rat hearts.
Chen, CC; Hsu, YJ; Lee, TM, 2011
)
"Allopurinol treatment prevented the rise in mitochondrial ROS levels and the decrease in ATP production."( Xanthine oxidase contributes to mitochondrial ROS generation in an experimental model of cocaine-induced diastolic dysfunction.
Monteil, C; Mulder, P; Thuillez, C; Vendeville, C; Ventura-Clapier, R; Vergeade, A, 2012
)
"Allopurinol treatment therefore represents a potential novel strategy to prevent LV remodeling and dysfunction after MI."( Allopurinol attenuates left ventricular remodeling and dysfunction after experimental myocardial infarction: a new action for an old drug?
Drexler, H; Engberding, N; Fuchs, M; Heineke, A; Hilfiker-Kleiner, D; Hornig, B; Landmesser, U; Müller, M; Schaefer, A; Spiekermann, S; Wiencke, A, 2004
)
"Allopurinol treatment also alleviated ventricular dilation and preserved shortening fraction in the transgenic animals."( Chronic xanthine oxidase inhibition prevents myofibrillar protein oxidation and preserves cardiac function in a transgenic mouse model of cardiomyopathy.
Duncan, JG; Murphy, AM; Ravi, R; Stull, LB, 2005
)
"Allopurinol (10 microM) treatment suppressed xanthine oxidase activity induced by hypoxia-reoxygenation injury and the production of reactive oxygen species."( Allopurinol modulates reactive oxygen species generation and Ca2+ overload in ischemia-reperfused heart and hypoxia-reoxygenated cardiomyocytes.
Bae, SM; Chang, W; Chung, JH; Chung, NS; Hwang, KC; Jang, Y; Kang, SM; Kim, HG; Kim, TW; Lee, H; Lee, S; Lim, S; Song, H; Sung, JM; Yoon, DH, 2006
)
"Allopurinol treatment gave approximately 50% protection for both components."( Treatment with the xanthine oxidase inhibitor, allopurinol, improves nerve and vascular function in diabetic rats.
Cameron, NE; Cotter, MA; Inkster, ME, 2007
)
"Allopurinol treatment reduced the incidence of ventricular tachycardia during ischemia from 88% to 50% (P less than 0.05) and the number of premature ventricular complexes from 471 +/- 120 to 116 +/- 46 (P less than 0.02), but the treatment had no effect upon the incidence or duration of ventricular fibrillation or upon mortality."( Ischemia and reperfusion-induced arrhythmias in the rat. Effects of xanthine oxidase inhibition with allopurinol.
Coltart, DJ; Hearse, DJ; Manning, AS, 1984
)
"The allopurinol-treated group exhibited a mild, generalized hyperemia at 5 minutes (ischemic zone: 1.44 versus 1.10 mL/min/g, which returned to control levels at 10 and 30 minutes."( Allopurinol improves myocardial reperfusion injury in a xanthine oxidase-free model.
Chitwood, WR; Hopson, SB; Lust, RM; Morrison, RF; Otaki, M; Sun, YS; Zeri, RS, 1995
)
"Allopurinol treatment resulted in a 350% increase in xanthine, a 630% increase in hypoxanthine, and a 70% reduction in uric acid concentrations."( Allopurinol plus standard resuscitation preserves hepatic blood flow and function following hemorrhagic shock.
Flynn, WJ; Hoover, EL, 1994
)
"Allopurinol treatment had no effect (P > 0.05) on the numbers of macrophages or lymphocytes recoverable by lung lavage."( Xanthine oxidase promotes neutrophil sequestration but not injury in hyperoxic lungs.
Beehler, CJ; Hanley, ME; Moores, HK; Repine, JE; Shanley, PF; Stevens, EE; Terada, LS, 1994
)
"Allopurinol pretreatment significantly reduced the use of inotropic support after the operation (5 of 25 patients versus 13 of 25 patients, p < 0.01) and increased the rate of peripheral warming (11.4 +/- 0.85 hours versus 14.4 +/- 1 hours, p < 0.02)."( Allopurinol pretreatment improves postoperative recovery and reduces lipid peroxidation in patients undergoing coronary artery bypass grafting.
Clutton, SM; Coghlan, JG; Daly, R; Flitter, WD; Ilsley, CD; Panda, R; Slater, TF; Wright, G, 1994
)
"The allopurinol-treated I/R tissue exhibited reduced staining."( Subcellular distribution of xanthine oxidase during cardiac ischemia and reperfusion: an immunocytochemical study.
Ashraf, M; Samra, ZQ, 1993
)
"Allopurinol treatment enhanced wound strength over sham controls and BSO groups at 9 days after wounding (P < 0.05)."( Delayed repair: the role of glutathione in a rat incisional wound model.
Adamson, B; Fisher, J; Gilmont, R; Klugston, P; Lindblad, W; Perry, L; Rees, R; Schwarz, D, 1996
)
"Allopurinol treatment attenuated the frequence of BT in PH and decreased BT in CBDL rats significantly (p < 0.05)."( Allopurinol reduces bacterial translocation, intestinal mucosal lipid peroxidation, and neutrophil-derived myeloperoxidase activity in chronic portal hypertensive and common bile duct-ligated growing rats.
Feierl, G; Höllwarth, ME; Pesendorfer, P; Ratschek, M; Schimpl, G; Steinwender, G, 1996
)
"Allopurinol treatment: All therapy (scavenger) groups (4,5) were significantly different from the respective control group; following exposition to the radical generating system for 60 min, allopurinol showed significantly higher values when given at 1000 micromol as compared to 500 micromol."( Effects of allopurinol on free-radical-induced reduction of the proliferation of retinal pigment epithelial cells.
Augustin, AJ; Grus, FH; Hunt, S,
)
"Allopurinol-treated LoMg++ and NlMg++ patients had no significant change in urinary xanthine excretion, but did have 40%+/-7% and 33%+/-5% decreases, respectively, in creatinine clearance 48 hours after contrast medium exposure."( Oxygen free radicals and contrast nephropathy.
Deitrick, CL; Katholi, CR; Katholi, RE; McCann, WP; Taylor, GJ; Womack, KA; Woods, WT, 1998
)
"Allopurinol treatment markedly reduced the serum amylase elevation (12.631+/-2.257 units/liter at 24 hr) and prevented the increase in tissue MDA concentration (0.55+/-0.09 nM/mg protein at 48 hr)."( Involvement of oxygen-derived free radicals in L-arginine-induced acute pancreatitis.
Czakó, L; Hai, DQ; Hegyi, P; Lonovics, J; Matkovics, B; Takács, T; Tiszlavicz, L; Varga, IS, 1998
)
"Allopurinol pretreatment substantially inhibited intestinal neutrophil sequestration induced by high dose (but not low dose) PAF."( The role of xanthine oxidase in platelet activating factor induced intestinal injury in the rat.
Bulkley, GB; Hsueh, W; Huang, W; Qu, XW; Rozenfeld, RA, 1999
)
"Allopurinol treatment resulted in increased hypoxanthine and decreased uric acid contents in the liver compared with the saline treated group, immediately and 3 h after the exercise."( Role of xanthine oxidase in delayed lipid peroxidation in rat liver induced by acute exhausting exercise.
Hori, S; Ishigaki, T; Kasugai, A; Kaya, M; Koyama, K; Seino, T; Tsujita, J, 1999
)
"Allopurinol pretreatment prevented the generation of reactive oxygen metabolites in the pancreas and reduced their formation in the kidney."( Oxidative stress in distant organs and the effects of allopurinol during experimental acute pancreatitis.
Czakó, L; Hai, DQ; Hegyi, P; Lonovics, J; Matkovics, B; Takács, T; Tiszlavicz, L; Varga, IS, 2000
)
"Allopurinol treatment preserved the concentration of AMP in ischemic liver but inhibited the accumulation of xanthine in reperfused liver."( Protective effect of allopurinol on hepatic energy metabolism in ischemic and reperfused rat liver.
Jeon, BR; Lee, SM; Yeom, DH, 2001
)
"Allopurinol pretreatment abolished the increase in plasma uric acid which occurs in untreated dogs during hemorrhagic hypotension and resulted in a much lesser increase in plasma allantoin."( Effect of a xanthine oxidase inhibitor on adenine nucleotide degradation in hemorrhagic shock.
Cunningham, SK; Keaveny, TV, 1978
)
"Allopurinol pretreatment (20 mg/kg body wt/day for 3 days) improved the postischemic recovery of cardiac function; thus, aortic flow (a representative index) recovered to 68.8 +/- 4.2% compared with 53.2 +/- 2.3% in untreated controls (p less than 0.05)."( Allopurinol-enhanced myocardial protection does not involve xanthine oxidase inhibition or purine salvage.
Chambers, DJ; Harvey, DM; Hearse, DJ; Humphrey, SM; Takahashi, A,
)
"Allopurinol treatment significantly reduced (p less than 0.05 and p less than 0.02, respectively) the increase in water content and limb weight (ratios = 0.54 and 1.01, respectively)."( Allopurinol--a free radical scavenger--reduces reperfusion injury in skeletal muscle.
Oredsson, S; Plate, G; Qvarfordt, P, 1991
)
"Allopurinol-treated animals were able to induce lung glutathione concentrations and glutathione-related and antioxidant enzyme activities compared with the normoxic control (FIO2-PRN) group."( Allopurinol-induced effects in premature baboons with respiratory distress syndrome.
Coalson, JJ; DeLemos, RA; Gerstmann, DR; Jenkinson, SG; King, RJ; Lawrence, RA; Null, DM; Roberts, RJ, 1991
)
"Allopurinol treatment caused a specific, dose-dependent inhibition of the conversion of the caffeine metabolite 1-methylxanthine (1X) to 1-methyluric acid (1U)."( Effect of allopurinol on caffeine disposition in man.
Campbell, ME; Grant, DM; Kalow, W; Tang, BK, 1986
)
"Allopurinol plus standard treatment reduced LDH, ferritin, CRP, procalcitonin, and ET-1 serum level significantly (P < 0.05) compared with Covid-19 patients on standard treatment."( The Prospective Effect of Allopurinol on the Oxidative Stress Index and Endothelial Dysfunction in Covid-19.
Al-Gareeb, AI; Al-Kuraishy, HM; Al-Niemi, MS; Alexiou, A; Aljowaie, RM; Almutairi, SM; Batiha, GE, 2022
)
"The allopurinol-treated group exerted non-significant differences compared with the induction group in both visional and histopathological changes."( Pharmaceutical Characterization and
Al-Notazy, MR; Al-Saedi, HF; Khaled Younis Albahadly, W; Ramadhan, MA, 2022
)
"Allopurinol treatment prevented hepatic and systemic alterations."( Allopurinol Prevents the Lipogenic Response Induced by an Acute Oral Fructose Challenge in Short-Term Fructose Fed Rats.
Andrés-Hernando, A; García-Arroyo, FE; Gonzaga, G; Johnson, RJ; Juárez-Rojas, JG; Lanaspa, MA; Monroy-Sánchez, F; Muñoz-Jiménez, I; Sánchez-Lozada, LG; Zazueta, C, 2019
)
"Allopurinol treatment was associated with the lowest LVMI in the patients with normal serum creatinine (median LVMI; 70.5 g/m"( Effect of Long-Term Allopurinol Therapy on Left Ventricular Mass Index in Patients with Ischemic Heart Disease; A Cross-Sectional Study.
Al-Ghamdi, BS; Aldosari, SR; Alem, MM; Alkahmous, AA; Fagir, NM; Obad, AS, 2019
)
"Allopurinol treatment significantly reduced MAGE (4.16 vs 4.65 mmol/L, P < .001), SDBG (0.99 vs 1.36 mmol/L, P < .001) and HOMA-IR (2.26 vs 3.01, P < .001) in gout patients."( Blood glucose fluctuations detected by continuous glucose monitoring system in gout patients with normal glucose tolerance and the effect of urate-lowering therapy.
Chen, Y; Dong, B; Lv, W; Mu, Z; Wang, F; Wang, J; Wang, W; Wang, Y; Wang, Z; Zhao, Y, 2020
)
"Allopurinol treatment resulted in a decrease in SUA, a decrease in systolic and diastolic BP, a decrease in hsCRP, and an increase in eGFR compared with the baseline values (p < 0.05 for all)."( Effect of allopurinol on the glomerular filtration rate of children with chronic kidney disease.
Assadi, F; Ghane Sharbaf, F, 2018
)
"Allopurinol treatment was interrupted after seven months because of the healing of all lesions and lack of compliance by the owner."( Treatment and long-term follow-up of a cat with leishmaniosis.
Abbate, JM; Arfuso, F; Brianti, E; Celi, N; Gaglio, G; Giannetto, S; Gramiccia, M; Iatta, R; Napoli, E; Otranto, D, 2019
)
"Allopurinol treatment was stopped and steroid treatment was started."( Allopurinol-induced DRESS syndrome mimicking biliary obstruction.
Byun, J; Choi, HG; Han, CJ; Moon, CH; Park, SC; Yang, KY; Yoon, JH, 2014
)
"Allopurinol-treated subjects showed a reduction in serum uric acid in association with improvement in fasting blood glucose, fasting insulin, and HOMA-IR index, as well as a reduction in serum high-sensitivity C-reactive protein. "( Lowering Uric Acid With Allopurinol Improves Insulin Resistance and Systemic Inflammation in Asymptomatic Hyperuricemia.
Afsar, B; ALanaspa, M; Bakan, A; Elcioglu, OC; Erek, A; Johnson, RJ; Kanbay, M; Kostek, O; Mutlu, HH; Odabas, AR; Ozkok, A; Semerci, A; Sharma, S; Smits, G; Takir, M; Telci, O, 2015
)
"Allopurinol treatment is associated with a decreased cardiovascular risk among hyperuricemic patients."( Effect of Allopurinol on Cardiovascular Outcomes in Hyperuricemic Patients: A Cohort Study.
Hallas, J; Larsen, KS; Lindegaard, HM; Pottegård, A, 2016
)
"Allopurinol treatment, based on screening by HLA-B*58:01 genotyping, could be more cost-effective than that not based on screening."( HLA Allele Frequencies in 5802 Koreans: Varied Allele Types Associated with SJS/TEN According to Culprit Drugs.
Kim, DH; Kim, J; Kim, YJ; Lee, JH; Park, HJ; Park, JW; Park, KH, 2016
)
"The allopurinol-treated group had a 0.10 mg/dL lower final creatinine level (95% confidence interval, 0.003-0.20 mg/dL; P = 0.04) than did the control subjects, adjusted for initial creatinine and age."( The Effect of Allopurinol on Renal Function.
Blumenthal, D; Gerber, D; Krishnamurthy, A; Lazaro, D; Patel, S; Stefanov, DG, 2017
)
"Allopurinol treatment did not reduce HOMA or fasting plasma triglyceride levels, but lowered low-density lipoprotein cholesterol relative to control (P<0.02) and also prevented the increase in newly diagnosed metabolic syndrome (0-2%, P=0.009)."( Excessive fructose intake induces the features of metabolic syndrome in healthy adult men: role of uric acid in the hypertensive response.
Johnson, RJ; Lillo, JL; Nakagawa, T; Perez-Pozo, SE; Sánchez-Lozada, LG; Schold, J, 2010
)
"Allopurinol treatment slowed down renal disease progression independently of age, gender, diabetes, C-reactive protein, albuminuria, and renin-angiotensin system blockers use."( Effect of allopurinol in chronic kidney disease progression and cardiovascular risk.
Ampuero, J; Arroyo, D; de Vinuesa, SG; Goicoechea, M; Luño, J; Rincón, A; Ruiz-Caro, C; Verdalles, U, 2010
)
"Allopurinol treatment resulted in a decrease in serum uric acid, a decrease in systolic BP, an increase in FMD, and an increase in eGFR compared with baseline."( A randomized study of allopurinol on endothelial function and estimated glomular filtration rate in asymptomatic hyperuricemic subjects with normal renal function.
Azak, A; Covic, A; Duranay, M; Huddam, B; Johnson, RJ; Kadioglu, GK; Kanbay, M; Kirbas, I; Solak, Y, 2011
)
"Allopurinol treatment was given to all patients at a median dose of 9 mg/kg/day."( Adenine phosphoribosyltransferase deficiency in children.
Bensman, A; Bollée, G; Ceballos-Picot, I; Daudon, M; Harambat, J, 2012
)
"Allopurinol-treated individuals who abstained from caffeine (n = 4) had a greater decrease in YMRS scores (-15.3 ± 1.8) than subjects using caffeine (n = 5) (-9.6 ± 3.4, p = 0.219), with an effect size of -0.86."( Allopurinol augmentation in the outpatient treatment of bipolar mania: a pilot study.
Berg, A; Bresee, C; Fan, A; Glassman, LH; Rapaport, MH, 2012
)
"Allopurinol or uricase treatment did not reduce ventilator-induced inflammation, IκB-α degradation, or up-regulation of NLRP3, Toll-like receptor 2, and Toll-like receptor 4 gene expression in mice."( Pre-treatment with allopurinol or uricase attenuates barrier dysfunction but not inflammation during murine ventilator-induced lung injury.
Aslami, H; Hegeman, MA; Jongsma, G; Juffermans, NP; Kuipers, MT; Roelofs, JJ; Schultz, MJ; Tuip-de Boer, AM; van der Poll, T; Vlaar, AP; Wieland, CW, 2012
)
"Allopurinol treatment was not as effective as 2-iminobiotin treatment after HI."( Pharmacological interventions in the newborn piglet in the first 24 h after hypoxia-ischemia. A hemodynamic and electrophysiological perspective.
Braun, K; Groenendaal, F; Ioroi, T; Nicolay, K; Peeters-Scholte, C; Post, I; van Bel, F; van den Tweel, E; Veldhuis, W, 2002
)
"The allopurinol treatment was adjusted according to clinical and laboratory data."( [Xanthinuria with xanthine lithiasis in a patient with Lesch-Nyhan syndrome under allopurinol therapy].
Muche, J; Rebentisch, G; Stolz, S, 2004
)
"Allopurinol-treated rabbits had a Johnsen score of > 7.6 and those given other antioxidants had scores of < 7.6 at 3 months."( Allopurinol provides long-term protection for experimentally induced testicular torsion in a rabbit model.
Abraham, M; Al-Awadi, F; Anim, JT; Fatinikun, T; Kehinde, EO; Mojiminiyi, OA; Omu, AE; Prasad, A; Shihab-Eldeen, A, 2005
)
"Allopurinol-treated animals exhibited further increased serum alanine aminotransferase(ALT) levels and liver myeloperoxidase(MPO) activities, but further decreased liver adenosine triphosphate(ATP) stores after I/R compared to saline-treated counterparts (830.5+/-108.3 U/L, 56.5+/-11.0 U/mg protein and 1.93+/-0.47 mumol/g vs. "( Nitrite-derived nitric oxide by xanthine oxidoreductase protects the liver against ischemia-reperfusion injury.
Chen, DD; Liu, F; Lu, P; Tian, Y; Wang, CY; Wu, YH; Yao, Z; Zhang, JH, 2005
)
"Allopurinol treatment started postnatally was too late to reduce the early reperfusion induced free radical surge. "( Early postnatal allopurinol does not improve short term outcome after severe birth asphyxia.
Benders, MJ; Bos, AF; Groenendaal, F; Rademaker, CM; Rijken, M; Torrance, HL; van Bel, F, 2006
)
"Allopurinol treatment was associated with a mean 74% reduction in urinary uric acid-to-creatinine ratio."( Efficacy and safety of allopurinol in patients with hypoxanthine-guanine phosphoribosyltransferase deficiency.
Prior, C; Puig, JG; Torres, RJ, 2007
)
"3 Allopurinol pretreatment did increase the volume of distribution of tryptophan."( Metabolism of an oral tryptophan load. II: Effect of pretreatment with the putative tryptophan pyrrolase inhibitors nicotinamide or allopurinol.
Aronson, JK; Curzon, G; Green, AR; Woods, HF, 1980
)
"Allopurinol pretreatment also led to a 300% increase in plasma AUC in monkeys after oral 6-MP (from a mean of 121 microM/min to a mean of 391 microM/min) and a 500% increase in AUC in man (from a mean of 142 microM/min to a mean of 716 microM/min)."( Inhibition of first-pass metabolism in cancer chemotherapy: interaction of 6-mercaptopurine and allopurinol.
Chabner, BA; Collins, JM; O'Neill, D; Poplack, DG; Zimm, S, 1983
)
"The allopurinol only treatment group demonstrated no noticeable histological or functional changes considered to be indicative of nephrotoxicity."( Allopurinol fails to protect against gentamicin-induced renal damage in normotensive and spontaneously hypertensive rats.
Davis, WG; Smyth, BJ, 1994
)
"Allopurinol and allomaron-treated patients were examined biochemically by 17 parameters of the blood and urine."( [The correction of hyperuricemia in patients with different forms of nephrolithiasis using allopurinol and Allomaron].
Darenkov, AF; Ianenko, EK; Konstantinova, OV,
)
"In allopurinol treated ischemic and reperfused groups, the levels of Na+K+ATPase activity were high compared to the untreated group."( The effect of allopurinol on Na+K+ATPase related lipid peroxidation in ischemic and reperfused rabbit kidney.
Aricioğlu, A; Aydin, S; Durmus, O; Turkozkan, N, 1994
)
"Allopurinol-treatment showed no benefit to the kinetics of PCr/(Pi + PCr) and ATP/(Pi + PCr)."( [Modification of ischemia and reperfusion damage of skeletal muscles with allopurinol: in vivo 31P MR spectroscopy of the posterior limb of the rat].
Erhard, P; Gürke, L; Heberer, M; Landmann, J; Marx, A; Sutter, PM, 1993
)
"Allopurinol treatment resulted in a decrease in the neutrophilic alveolar response in oxygen-exposed animals (5.3 +/- 4 x 10(3)/mm3, P < 0.001)."( Allopurinol inhibition of neutrophilic alveolar response during hyperoxia.
Bryan, CL; Emanuel, B; Jenkinson, SG; Lewis, RE; Owens, SL, 1993
)
"Oral allopurinol pretreatment supplemented by an intravenous dose, or oral allopurinol in combination with a superoxide radical scavenger, resulted in a significant amelioration of postischemic histologic changes."( Reperfusion mucosal damage after complete intestinal ischemia in the dog: the effects of antioxidant and phospholipase A2 inhibitor therapy.
Boros, M; Karácsony, G; Kaszaki, J; Nagy, S, 1993
)
"In allopurinol-treated DMD patients, mean total adenylate level was only three times less than in controls (versus 14 times less in untreated DMD patients)."( Purine and carnitine metabolism in muscle of patients with Duchenne muscular dystrophy.
Camiña, F; Castro-Gago, M; Novo-Rodriguez, MI; Rodriguez-Segade, S, 1995
)
"Allopurinol treatment lowered the urate concentration in EPS and relieved the subjective discomfort."( Allopurinol treatment results in elevated prostate-specific antigen levels in prostatic fluid and serum of patients with non-bacterial prostatitis.
Persson, BE; Ronquist, G, 1996
)
"Allopurinol treatment in rats with pouches reduced histology score (4.0 +/- 1.7) and MPO (3.9 +/- 1.6), p < 0.001, compared with rats with pouches that had no treatment."( A rat model of ileal pouch-rectal anastomosis.
Hummel, B; Lacey, S; Lichtman, SN; Sartor, RB; Wang, J, 1998
)
"Allopurinol treatment markedly reduced the serum amylase elevation (12.631 +/- 2.257 U x L(-1) at 24 h), prevented the increase in tissue MDA concentration (0.55 +/- 0.09 nM x mg(-1) protein at 48 h) and significantly ameliorated the pancreatic edema, necrosis and inflammation at 48 h after Arg administration."( The pathogenesis of L-arginine-induced acute necrotizing pancreatitis: inflammatory mediators and endogenous cholecystokinin.
Czakó, L; Hai, DQ; Hegyi, P; Lonovics, J; Mándi, Y; Matkovics, B; Takács, T; Tiszlavicz, L; Varga, IS,
)
"Allopurinol pretreatment prevented the effects of ischemia/reperfusion on anastomotic healing of the left colon."( Effect of ischemia/reperfusion as a systemic phenomenon on anastomotic healing in the left colon.
Aşlar, AK; Kale, IT; Köksoy, C; Kuzu, MA; Tanik, A; Terzi, C, 2000
)
"Allopurinol pretreatment (40 mg kg(-1) iv) maintained higher ATP levels during the ischaemia and inhibited the MDA formation during the reperfusion and decreased the MDA/ATP ratio at both periods."( An alternative parameter for monitoring the therapeutic benefits of allopurinol simultaneously in renal ischaemia-reperfusion injury: MDA/ATP Ratio.
Bor, MV; Cayçi, B; Durmus, O; Türközkan, N, 2000
)
"Allopurinol (0.1 mM) treated hearts had greater levels of ATP (12.3 +/- 0.8 vs."( Allopurinol enhances adenine nucleotide levels and improves myocardial function in isolated hypoxic rat heart.
El-Migdadi, F; Farah, H; Khatib, SY, 2001
)
"IR allopurinol-treated hearts, both unpaced and paced (groups 5 and 6) had normal, similar myocardial performance, while their circulating XO was as low as in group 2 (allopurinol-treated controls)."( External pacing does not potentiate allopurinol protection of the heart from liver ischemia-reperfusion -- a study in an isolated perfused liver-heart rat model.
Dembo, G; Hochhauser, E; Rudick, V; Vidne, BA; Weinbroum, AA,
)
"4. Allopurinol pretreatment (25 mg kg-1, p.o."( Impaired endothelium-dependent relaxation of dog coronary arteries after myocardial ischaemia and reperfusion: prevention by amlodipine, propranolol and allopurinol.
Dalipram, RA; Dusting, GJ; Sobey, CG; Woodman, OL, 1992
)
"Allopurinol pretreatment prevented ischemia-reperfusion-mediated deficits in cardiac contraction and relaxation.(ABSTRACT TRUNCATED AT 250 WORDS)"( Cardiac contractile injury after intestinal ischemia-reperfusion.
Horton, JW; White, DJ, 1991
)
"Allopurinol pretreatment significantly reduced the uric acid plasma level."( Oleic acid-induced injuries in the guinea-pig. Effects of allopurinol on cell dynamics, erythrocyte-catalase and uric acid plasma levels.
Hultkvist-Bengtsson, U; Mårtensson, L, 1991
)
"Allopurinol (2 mM) treatment of hearts made ischaemic for 15 min significantly improved contractile recovery to 89 +/- 7%."( Behaviour of energy metabolites and effect of allopurinol in the "stunned" isovolumic rat heart.
Armiger, LC; Headrick, JP; Willis, RJ, 1990
)
"Allopurinol-treated hearts averaged only 18% less infarction and did not achieve significance."( Oxypurinol limits myocardial infarct size in closed chest dogs without pretreatment.
Cohen, MV; Downey, JM; Matsuki, T; Shirato, C, 1990
)
"Allopurinol treatment did not alter the responses to ischemia per se, yet it largely prevented the further increment in adherence and extravasation associated with reperfusion."( Leukocyte adherence to venular endothelium during ischemia-reperfusion.
Benoit, JN; Granger, DN; Grisham, MB; Suzuki, M, 1989
)
"Allopurinol treatment, however, prevented the rise in total peripheral resistance seen after burn injury."( Effect of allopurinol or superoxide dismutase plus catalase on cardiovascular function after burn injury in the anaesthetized rat.
Chapman, BJ; Speakman, EA, 1989
)
"Allopurinol treatment had no significant effect on myocardial levels of calcium."( Myocardial levels of calcium, glycogen and triglycerides in ethanol-fed turkey poults treated with allopurinol.
Czarnecki, CM; McVey, AS; Olivero, DK; Pessin, MF, 1987
)
"Allopurinol pretreatment had no effect on PX plasma clearance but decreased 1-MU excretion and increased 1-MX excretion, with the combined excretion of these metabolites remaining constant."( Paraxanthine metabolism in humans: determination of metabolic partial clearances and effects of allopurinol and cimetidine.
Birkett, DJ; Kjellen, G; Lelo, A; Miners, JO, 1989
)
"Allopurinol treatment caused 17.9 +/- 3.3% less of the risk zone to be tetrazolium negative after 24 hours of ischemia than that seen in untreated animals."( Protection afforded by allopurinol in the first 24 hours of coronary occlusion is diminished after 48 hours.
Downey, JM; Kingma, J; Miura, T; Yellon, DM, 1988
)
"In allopurinol-pretreated and oxonate-loaded rats, isoproterenol also decreased renal uric acid excretion and showed a less potent hyperuricemic effect than that observed in the animals not pretreated with allopurinol."( Effect of isoproterenol on renal uric acid excretion in rats.
Shimada, H; Sugino, H, 1987
)
"Allopurinol-treated hearts were also significantly improved, especially when the drug was given in the reperfusion phase."( Allopurinol in prevention of reperfusion injury of hypoxically stored rat hearts.
Bergsland, J; Feldman, MJ; Lajos, P; LoBalsamo, L; Mookerjee, B,
)
"Allopurinol-treated animals have reduced levels of four pterins (xanthopterin, isoxanthopterin, biopterin and sepiapterin) as compared with the wild type."( Pigment cell differentiation: the relationship between pterin content, allopurinol treatment, and the melanoid gene in axolotls.
Frost, SK; Thorsteinsdottir, S, 1986
)
"Allopurinol pretreatment inhibited xanthine and uric acid formation and significantly improved key indicators of postischemic left ventricular function."( Purine efflux after cardiac ischemia: relevance to allopurinol cardioprotection.
Grum, CM; Ketai, LH; Myers, CL; Shlafer, M, 1987
)
"Allopurinol treatment in calcium stone disease appears less effective than treatment with thiazides, magnesium hydroxide or orthophosphate."( Allopurinol treatment of renal calcium stone disease.
Backman, U; Danielson, BG; Fellström, B; Holmgren, K; Johansson, G; Lindsjö, M; Ljunghall, S; Wikström, B, 1985
)
"Treatment with allopurinol to ISO induced rats prevented the elevated activities of AST, ALT, and ALP enzymes, and the levels of lipid peroxidation products and increased reduced glutathione concentration."( Xanthine Oxidase Inhibitor, Allopurinol, Prevented Oxidative Stress, Fibrosis, and Myocardial Damage in Isoproterenol Induced Aged Rats.
Alam, MA; Potol, MA; Sagor, MA; Tabassum, N, 2015
)
"Treatment with allopurinol and oxypurinol (0.1-1 µM) reduced XO activity by up to 30%."( Allopurinol and oxypurinol promote osteoblast differentiation and increase bone formation.
Arnett, TR; George, J; Orriss, IR; Witham, MD, 2016
)
"Treatment with allopurinol did not affect the EPR function."( NADPH oxidase-derived reactive oxygen species in skeletal muscle modulates the exercise pressor reflex.
Pan, YX; Wang, HJ; Wang, W; Wang, WZ; Zucker, IH, 2009
)
"Pretreatment with allopurinol, a xanthine oxidase inhibitor, also potentiates the VSMC ASIC-like activity."( ASIC-like currents in freshly isolated cerebral artery smooth muscle cells are inhibited by endogenous oxidase activity.
Chung, WS; Drummond, HA; Farley, JM, 2011
)
"Treatment with allopurinol or benzbromarone limited renal disease, with reduced interstitial fibrosis, cell proliferation, macrophage infiltration, osteopontin expression and arteriolar hyalinosis, in association with restoration of VEGF expression."( Use of uric acid-lowering agents limits experimental cyclosporine nephropathy.
Johnson, RJ; Mazali, FC; Mazzali, M, 2012
)
"Pretreatment with allopurinol (50 mg/kg) significantly protected against ACN-induced rise in XO activity, depletion of GSH, and elevated production of (O(2)(.-))."( Acrylonitrile-induced gastric toxicity in rats: the role of xanthine oxidase.
Al-Abbasi, FA, 2012
)
"Treatment with allopurinol prevented activation of superoxide dismutase."( Generation of free oxygen radicals in the pathogenesis of experimental acute reflux pancreatitis.
Milyakova, MN; Sarbaeva, NN; Shabanov, VV, 2002
)
"Treatment with allopurinol for 2 mo suppressed xanthine oxidase activity and myofibrillar protein oxidation."( Chronic xanthine oxidase inhibition prevents myofibrillar protein oxidation and preserves cardiac function in a transgenic mouse model of cardiomyopathy.
Duncan, JG; Murphy, AM; Ravi, R; Stull, LB, 2005
)
"Treatment with allopurinol from 6 to 12 weeks attenuated LV dysfunction and dilation as well as myocardial fibrosis and the upregulation of a fetal-type cardiac gene."( Xanthine oxidase inhibition improves left ventricular dysfunction in dilated cardiomyopathic hamsters.
Fukata, A; Hashimoto, K; Hayashi, K; Iwase, M; Kimata, H; Koike, Y; Matsushita, A; Nagata, K; Noda, A; Obata, K; Yokota, M, 2008
)
"Treatment with allopurinol and oxypurinol, which inhibited cellular xanthine oxidase, failed to prevent glucose oxidase injury."( Reactive oxygen metabolite-induced toxicity to cultured bovine endothelial cells: status of cellular iron in mediating injury.
Harada, T; Hiraishi, H; Ivey, KJ; Pedram, A; Razandi, M; Sugimoto, T; Terano, A, 1994
)
"Pretreatment with allopurinol or ibuprofen reduced both the incidence and the magnitude of translocation at 6 hr in rats and mice (P < 0.05)."( Role of xanthine oxidase and prostaglandins in inflammatory-induced bacterial translocation.
Deitch, EA; Mainous, MR; Xu, D, 1993
)
"Pretreatment with allopurinol inhibited hepatic xanthine oxidase activity, neutrophil accumulation, and pericentral hepatocyte necrosis in shock/resuscitation in rats."( Zonal heterogeneity of hepatic injury following shock/resuscitation: relationship of xanthine oxidase activity to localization of neutrophil accumulation and central lobular necrosis.
Bulkley, GB; Chan, CK; Clemens, MG; Mayumi, T, 1996
)
"Pretreatment with allopurinol (Allo, 5 mg/kg, i.v.), a XO inhibitor, partially prevented the potentiating effect of cigarette smoke exposure on ulcer formation and also significantly improved the gastric blood flow."( Mechanistic study of adverse actions of cigarette smoke exposure on acetic acid-induced gastric ulceration in rats.
Cho, CH; Chow, JY; Ma, L, 1998
)
"Pretreatment with allopurinol (50 mg/kg/day for 2 days) significantly inhibited enhanced plasma xanthine oxidase activity and hepatocyte glutathione oxidation, however, it did not prevent hepatocellular Ca2+ dysregulation."( Oxyradical-mediated hepatocellular Ca2+ alterations during hemorrhagic shock and resuscitation.
Pizanis, A; Rose, S; Silomon, M, 1999
)
"Treatment with allopurinol and a tungsten-supplemented, molybdenum-free diet significantly attenuated serum liver enzymes, hepatic XO activity, and improved hepatic GSH levels, whereas vitamins C and E had a positive effect only on hepatic GSH levels."( The impact of hepatic xanthine oxidase and xanthine dehydrogenase activities on liver function in chronic cholestasis.
Höllwarth, ME; Kuesz, AM; Pesendorfer, P; Ratschek, M; Schimpl, G, 2000
)
"Pretreatment with allopurinol before ischaemia prevented changes in SOD and CAT activities and attenuated brain oedema during 24 h of ischaemia."( Time-dependent changes in superoxide dismutase, catalase, xanthine dehydrogenase and oxidase activities in focal cerebral ischaemia.
Atmaca, M; Deniz, B; Sermet, A; Taşdemir, N, 2000
)
"Treatment with allopurinol decreases oxidative stress in type 1 diabetic patients: hemoglobin glycation, glutathione oxidation, and the increase in lipid peroxidation are prevented."( Xanthine oxidase is involved in free radical production in type 1 diabetes: protection by allopurinol.
Asensi, M; Desco, MC; Márquez, R; Martínez-Valls, J; Pallardó, FV; Sastre, J; Vento, M; Viña, J, 2002
)
"Pre-treatment with allopurinol, a xanthine oxidase inhibitor, decreased the intracellular EB fluorescence by 54% in HPAEC incubated with 100 microM Lx."( Leukotoxin-activated human pulmonary artery endothelial cell produces nitric oxide and superoxide anion.
Ameshima, S; Demura, Y; Ishizaki, T; Matsukawa, S; Miyamori, I; Okamura, S, 2002
)
"Pretreatment with allopurinol resulted in a significantly lesser release of the lysosomal enzymes, acid phosphatase and beta-glucuronidase, following reinfusion."( Effect of a xanthine oxidase inhibitor on adenine nucleotide degradation in hemorrhagic shock.
Cunningham, SK; Keaveny, TV, 1978
)
"Pretreatment with allopurinol for 2 h caused dose-dependent inhibition of the decreased secretion of insulin by the cells induced by STZ (2 mM, for 1 h), 500 microM allopurinol causing complete inhibition of this effect of STZ."( Allopurinol protects pancreatic beta cells from the cytotoxic effect of streptozotocin: in vitro study.
Kawada, J; Nishida, M; Nukatsuka, M; Yoshimura, Y, 1990
)
"Pretreatment with allopurinol in amounts that effectively inhibited xanthine metabolism also significantly decreased ethanol-induced lipid peroxidation, suggesting participation of free radicals produced by xanthine oxidase in the peroxidative process."( Role of xanthine oxidase in ethanol-induced lipid peroxidation in rats.
Alderman, J; Inatomi, N; Kato, S; Kawase, T; Lieber, CS, 1990
)
"Pretreatment with allopurinol had no influence on the elimination of MTX or the production of 7-OH-MTX during a 3-h infusion of MTX."( No influence of enzyme inhibitors on the hydroxylation of methotrexate in rats.
Brasch, H; Iven, H; Yu, D, 1989
)
"Pretreatment with allopurinol or administration of superoxide dismutase prevented the influx of neutrophils and retarded the drop in reduced glutathione levels."( Xanthine oxidase and neutrophil infiltration in intestinal ischemia.
Granger, DN; Grisham, MB; Hernandez, LA, 1986
)
"Treatment with allopurinol, superoxide dismutase, and dimethyl sulfoxide reduced 51Cr-red cell loss to 15%, 25%, and 21% of control (untreated) animals, respectively."( Role of oxygen radicals in ischemia-induced lesions in the cat stomach.
Granger, DN; Parks, DA; Perry, MA; Pickard, W; Wadhwa, S, 1986
)
"Pretreatment with allopurinol prevented edema formation, markedly attenuated weight gain, and the release of amylase caused by the FFA infusion."( Temporal efficacy of allopurinol during the induction of pancreatitis in the ex vivo perfused canine pancreas.
Bulkley, GB; Cameron, JL; Sarr, MG, 1987
)
"Co-treatment with allopurinol for 21 days improved these functional alterations, whereas late allopurinol treatment failed to affect them."( Allopurinol treatment reduced vascular remodeling and improved vascular functions in monocrotaline-induced pulmonary hypertensive rats.
Gokcen, T; Inci, EE; Inci, K; Serdar, U; Sevgen, O, 2022
)
"Treatment with allopurinol has been suggested to reduce the incidence of contrast-induced acute kidney injury (CI-AKI). "( Effects of allopurinol pretreatment on the risk of contrast-induced acute kidney injury in patients undergoing percutaneous coronary intervention: A meta-analysis of randomized controlled trials
.
Jia, S; Lin, Z; Xin, W; Zhang, T, 2020
)
"Pretreatment with allopurinol reduces the incidence of CI-AKI in patients undergoing contrast exposure in PCI. "( Effects of allopurinol pretreatment on the risk of contrast-induced acute kidney injury in patients undergoing percutaneous coronary intervention: A meta-analysis of randomized controlled trials
.
Jia, S; Lin, Z; Xin, W; Zhang, T, 2020
)
"The treatment with allopurinol was ineffective in more than half of participants."( Prevalence of Hyperuricemia and the Use of Allopurinol in Older Poles-Results from a Population-Based PolSenior Study.
Broczek, K; Chudek, J; Grodzicki, T; Mossakowska, M; Owczarek, AJ; Wierucki, Ł; Winder, M, 2021
)
"Treatment with Allopurinol (10 mg/kg, BID) orally led to rapid improvement of ocular signs, general condition and blood cell count with complete remission of lid and corneal lesions within 2 months of treatment."( Ocular signs, diagnosis and long-term treatment with allopurinol in a cat with leishmaniasis.
, 2014
)
"Pretreatment with allopurinol significantly improved renal functional and histological grade scores following I/R injury (p<0.05). "( Allopurinol preconditioning attenuates renal ischemia/reperfusion injury by inhibiting HMGB1 expression in a rat model.
Chen, ZB; Li, D; Ma, XX; Qiu, T; Wang, ZS; Zhang, L; Zhou, JQ, 2016
)
"Pretreatment with allopurinol had a protective effect on kidney ischemia/reperfusion injury, which might be related to the inhibition of HMGB1 expression."( Allopurinol preconditioning attenuates renal ischemia/reperfusion injury by inhibiting HMGB1 expression in a rat model.
Chen, ZB; Li, D; Ma, XX; Qiu, T; Wang, ZS; Zhang, L; Zhou, JQ, 2016
)
"Treatment with allopurinol reduced cardiac levels of TGF-β1, Smad3, and increased Smad7 expression."( Allopurinol attenuates oxidative stress and cardiac fibrosis in angiotensin II-induced cardiac diastolic dysfunction.
Dai, Q; Dong, P; Jia, N; Qian, C; Ye, Y, 2012
)
"Treatment with allopurinol was independently associated with improved survival (HR 0.79, 95% CI 0.64-0.98; P < .05)."( Changes in uric acid levels and allopurinol use in chronic heart failure: association with improved survival.
Gotsman, I; Keren, A; Lotan, C; Zwas, DR, 2012
)
"Treatment with allopurinol was associated with improved survival."( Changes in uric acid levels and allopurinol use in chronic heart failure: association with improved survival.
Gotsman, I; Keren, A; Lotan, C; Zwas, DR, 2012
)
"Treatment with allopurinol and nimesulide significantly decreased the MDA and MPO levels whereas increased the SOD and CAT levels when compared I/R group in both non-diabetic and diabetic rats."( Neuroprotective effect of allopurinol and nimesulide against cerebral ischemic reperfusion injury in diabetic rats.
Ansari, MA; Goli, D; Hussain, SK; Mudagal, MP, 2013
)
"Pretreatment with allopurinol had no significant effect on any of our study parameters."( The role of allopurinol in human liver ischemia/reperfusion injury: a prospective randomized clinical trial.
Harinck, HI; Marinelli, A; van de Velde, CJ; Vriens, MR; Zwinderman, KH,
)
"Pretreatment with allopurinol or pentoxifilline resulted in significantly lower hepatic enzyme elevation than that in controls in the rat liver ischaemia/reperfusion model. "( Allopurinol plus pentoxifilline in hepatic ischaemia/reperfusion injury.
Baykan, A; Erdem, L; Köksal, H; Tok, H; Yildirim, S, 2002
)
"Pretreatment with allopurinol attenuated the tissue content MDA in the colon by more than 60 per cent."( Allopurinol and superoxide dismutase protect against leucocyte-endothelium interactions in a novel model of colonic ischaemia-reperfusion.
Dawson, P; Jeppsson, B; Menger, MD; Riaz, AA; Schäfer, T; Thorlacius, H; Wan, MX, 2002
)
"Pretreatment with allopurinol improved renal function after repetitive brief ischemia-reperfusion compared with the allopurinol-untreated repetitive brief ischemia-reperfusion group."( Repetitive brief ischemia: intermittent reperfusion during ischemia ameliorates the extent of injury in the perfused kidney.
Endre, ZH; Gobé, GC; Kadkhodaee, M; Willgoss, DA; Zhang, B, 2003
)
"Treatment with allopurinol, adequate hydration, urinary alkalization, and a low-purine diet was started."( Eighteen-year follow-up of a patient with partial hypoxanthine phosphoribosyltransferase deficiency and a new mutation.
Gregoric, A; Kokalj Vokac, N; Rabelink, GM; Varda, NM; Zagradisnik, B, 2005
)
"Treatment with allopurinol and antipruritic ointment was given."( [Acquired reactive perforating collagenosis after curettage of seborrheic keratoses].
Hagedorn, M; Matthes, T, 2004
)
"Treatment with allopurinol was associated to a mean reduction of serum urate concentration of 50%, and was normalized in all patients."( Efficacy and safety of allopurinol in patients with the Lesch-Nyhan syndrome and partial hypoxanthine- phosphoribosyltransferase deficiency: a follow-up study of 18 Spanish patients.
Prior, C; Puig, JG; Torres, RJ, 2006
)
"Pretreatment with allopurinol partly prevented generation of free oxygen radicals in the pancreas of dogs with experimental acute pancreatitis. "( Antiradical effect of allopurinol at early stages of experimental acute pancreatitis.
Milyakova, MN; Minyailov, NA; Shabanov, VV, 2006
)
"Treatment with allopurinol normalized serum urate level in all patients and resulted in a mean reduction in serum urate of 47%."( Efficacy and safety of allopurinol in patients with hypoxanthine-guanine phosphoribosyltransferase deficiency.
Prior, C; Puig, JG; Torres, RJ, 2007
)
"Treatment with allopurinol increased significantly Johnsen's score in both the ischemic (7.3 +/- 0.5 vs 5.6 +/- 0.5, P < 0.05) and contralateral (8.9 +/- 0.1 vs 8.3 +/- 0.2, P < 0.05) testis, compared to IR-animals."( Effect of allopurinol on germ cell apoptosis following testicular ischemia-reperfusion injury in a rat.
Coran, AG; Meyer, G; Mogilner, JG; Nativ, O; Shiloni, E; Sukhotnik, I; Voskoboinik, K, 2008
)
"Pretreatment with allopurinol has been shown to be beneficial in shock; however, it is unlikely that allopurinol by itself if given following shock would have any salutary effects."( The use of substrates and energy in the treatment of shock.
Baue, AE; Chaudry, IH, 1980
)
"Pretreatment with allopurinol did not reduce the toxicity of 5-FU administered as an intravenous bolus."( Effect of allopurinol on the toxicity of high-dose 5-fluorouracil administered by intermittent bolus injection.
Howell, SB; Pfeifle, CE; Wung, WE, 1983
)
"Treatment with Allopurinol inhibits the formation of uric acid and qualitatively renal excretion of oxypurines modifies."( [Xanthine lithiasis in a case of Lesch-Nyhan syndrome treated with allopurinol].
Heras Gironella, M; Izaguirre Zugazaga, C; Lázaro Castillo, J; Loris Pablo, C; March, A; Martínez Escribano, MP; Oliván del Cacho, MJ; Sierra Sirvant, J, 1983
)
"Treatment with allopurinol resulted ina significant reduction of ammonium excretion, a phenomenon which could not be readily explained."( Allopurinol treatment and its effect on renal function in gout: a controlled study.
Gibson, T; Potter, C; Rodgers, V; Simmonds, HA, 1982
)
"Treatment with allopurinol did not affect the HGRPT and APRT activities."( [Erythrocyte purine phosphoribosyltransferase activity in girls with the Lesch-Nyhan syndrome].
Aleksandrova, LA; Shaposhnikov, AM, 1981
)
"Pretreatment with allopurinol did not alter the effects of endothelin-1."( Endothelin-1-induced oedema in rat and guinea-pig isolated perfused lungs.
Ercan, ZS; Kilinç, M; Korkusuz, P; Türker, RK; Yazar, O,
)
"Treatment with allopurinol was unsuccessful at reducing the xanthine excretion."( Acute renal failure due to xanthine stones.
Bradbury, MG; Brocklebank, JT; Henderson, M; Simmonds, HA, 1995
)
"Pretreatment with allopurinol prevented this further increase (p < 0.01)."( The effect of allopurinol pretreatment before detorting testicular torsion.
Akgür, FM; Aktuğ, T; Kilinç, K; Olguner, M, 1994
)
"Pretreatment with allopurinol (100 mg kg-1, i.p.) also reduced the mucosal injury induced by local intra-arterial infusion of the nitrosothiol, S-nitroso-N-acetyl-penicillamine (40 micrograms kg-1 min-1), but not that induced by local infusion of endothelin-1 (5 pmol kg-1 min-1), indicating specificity of action."( Involvement of superoxide and xanthine oxidase in neutrophil-independent rat gastric damage induced by NO donors.
Lamarque, D; Whittle, BJ, 1995
)
"The treatment with allopurinol demonstrates of on benefit or phosphocreatine and ATP kinetics."( [Effects of allopurinol on damage caused by ischemia and reperfusion of skeletal muscles: an in vivo spectroscopic analysis (31P-MR) in rats].
Erhard, P; Gürke, L; Heberer, M; Kuhrmeier, A; Martinoli, S; Sutter, PM,
)
"Treatment with allopurinol did not alter this pattern, such that the ratio of oxidised to total glutathione in plasma was higher among the 16 patients than 8 controls (P < 0.025)."( A pilot study of blood antioxidant and free radical marker profiles in patients awaiting coronary artery bypass grafting.
Braganza, JM; Gu, M; Love, H; Odom, N; Schofield, D; Turkie, W, 1996
)
"Pre-treatment with allopurinol prevented damage to tissues whereas untreated or allopurinol solvent-treated showed severe damage following reperfusion. "( The effects of allopurinol on the ultrastructure of ischaemic and reperfused large intestine of sheep.
Ahmadinejad, M; Cribb, B; Pollitt, CC; Rex, M; Sutton, RH, 1996
)
"Pretreatment with allopurinol also prevented the cytotoxicity associated with LPS but, in contrast to DMSO, did not alter induction of MnSOD mRNA."( Effect of antioxidants on lipopolysaccharide-stimulated induction of mangano superoxide dismutase mRNA in bovine pulmonary artery endothelial cells.
Berry, L; Jiang, H; Meyrick, B; Mitchell, J, 1996
)
"Pretreatment with allopurinol (150 mg/kg iv) did not significantly influence regional cerebral blood flow, intracranial pressure, and brain water content in pneumococci-injected rats."( Mannitol, but not allopurinol, modulates changes in cerebral blood flow, intracranial pressure, and brain water content during pneumococcal meningitis in the rat.
Koedel, U; Lorenzl, S; Pfister, HW, 1996
)
"Pretreatment with allopurinol, 10 mg/kg, significantly reduced malondialdehyde responses to tachykinin challenge in intestinal tissues (P < 0.001)."( Tachykinins stimulate lipid peroxidation mediated by free radicals in gastrointestinal tract of rat.
Hellström, PM; Lördal, M; Söder, O, 1997
)
"Pre-treatment with allopurinol, a xanthine oxidase inhibitor and free radical scavenger, suppressed NF-kappaB activation by WY-14 643 almost completely."( WY-14 643 rapidly activates nuclear factor kappaB in Kupffer cells before hepatocytes.
Rusyn, I; Thurman, RG; Tsukamoto, H, 1998
)
"Treatment with allopurinol controls formation of DHA stones by inhibiting XDH activity."( Chronic renal failure in a mouse model of human adenine phosphoribosyltransferase deficiency.
Boivin, GP; Lorenz, JN; Sahota, A; Smith, FN; Stambrook, PJ; Stockelman, MG; Tischfield, JA, 1998
)
"Treatment with allopurinol did not show any beneficial effects (37.5% SD 14.2)."( Free radical scavengers to prevent reperfusion injury following experimental warm liver ischaemia. Is there a real physiological benefit?
Chavez-Cartaya, R; Jamieson, NV; Marin, J; Pino-Chavez, G; Ramirez, P, 1999
)
"Treatment with allopurinol and a low-purine diet led to improvement and stabilization of renal function."( Adenine phosphoribosyltransferase deficiency and renal allograft dysfunction.
Benedetto, B; Braden, G; Freeman, J; Kurbanov, A; Lipkowitz, GS; Madden, R, 2001
)
"Treatment with allopurinol results in a significant reduction in serum creatinine in patients with gout and in those with hyperuricemia and renal impairment."( Hyperuricemia, gout, and renal function after liver transplantation.
Alexander, GJ; Gibbs, P; Gimson, AE; Neal, DA; Tom, BD, 2001
)
"Pretreatment with allopurinol prevented the mitochondrial oxidant stress and liver injury due to acetaminophen toxicity but had no effect on Jo-mediated apoptosis."( Acetaminophen-induced inhibition of Fas receptor-mediated liver cell apoptosis: mitochondrial dysfunction versus glutathione depletion.
Jaeschke, H; Knight, TR, 2002
)
"Pretreatment with allopurinol prevented prolongation of GATT and returned the number of CPIMM to the level of sham treatment (P < 0.01)."( Short-term intestinal ischemia-reperfusion alters intestinal motility that can be preserved by xanthine oxidase inhibition.
Akgür, FM; Aktuğ, T; Ateş, O; Hakgüder, G; Olguner, M; Ozer, E, 2002
)
"Treatment with allopurinol and clofibrate did not alter the rate of elimination of warfarin from plasma."( The effects of allopurinol and clofibrate on the elimination of coumarin anticoagulants in man.
Graham, GG; Pond, SM; Sudlow, G; Wade, DN, 1975
)
"Pretreatment with allopurinol, dibenzyline, methylprednisolone, glucagon, ATP-MgCl2 and aspartic acid reduced the overall mortality of ischemic liver injury."( Ischemic damage of the liver. Part II: In vivo investigation of the prevention of the ischemic lesion of the liver.
Kokas, P; Kupcsulik, P, 1979
)
"Treatment with allopurinol alone yielded a cure rate of 80 percent (P less than 0.001)."( Allopurinol in the treatment of American cutaneous leishmaniasis.
Marr, JJ; Martinez, S, 1992
)
"Pretreatment with allopurinol did not significantly affect 51Cr-EDTA leakage at any time during the experiment."( Role of oxygen-derived free radicals in indomethacin-induced gastric injury.
Meddings, JB; Vaananen, PM; Wallace, JL, 1991
)
"Pretreatment with allopurinol (146 mumols/kg, i.p.) given at 16 hr and at 30 min before ethanol (2.3 g/kg) or with desferrioxamine (152 mumols/kg, i.p.) 30 min before ethanol failed to prevent the ethanol-induced decrease in CK activity."( Disturbances in myocardial creatine kinase following ethanol administration to rats--trials of prevention by allopurinol, desferrioxamine and propranolol.
Hininger, I; Nordmann, R; Ribiere, C, 1991
)
"Pretreatment with allopurinol, a xanthine oxidase inhibitor, produced a significant reduction in the number and size of lesions (p < 0.0001)."( [The etiopathogenesis of the acute stress ulcer. The role of oxygen free radicals].
Aracena, M; de la Fuente, G; Mancinelli, S; Manríquez, V; Múñoz, R; Múñoz, S, 1990
)
"Pretreatment with allopurinol, a competitive inhibitor of xanthine oxidase, prevented considerably the gastric injury (a) induced by burn shock, (b) produced by treatment with compound 48/80, and (c) caused by ischemia-reperfusion."( Role of oxygen-derived free radicals in the pathogenesis of gastric mucosal lesions in rats.
Kondo, M; Naito, Y; Oyamada, H; Sugino, S; Takemura, T; Ueda, S; Yoshida, N; Yoshikawa, T, 1990
)
"Pretreatment with allopurinol (0, 0.01, 0.02, 0.05, 0.10, 0.20, or 0.50 g.kg-1.day-1 per os 48, 24, and 1 h before study) reduced VF incidence from its control value of 93 to less than 50% at several doses.(ABSTRACT TRUNCATED AT 250 WORDS)"( Reperfusion arrhythmias: dose-related protection by anti-free radical interventions.
Bernier, M; Hearse, DJ; Manning, AS, 1989
)
"Pre-treatment with allopurinol is able markedly to attenuate the deterioration in blood viscosity (BV) and whole blood filterability (WBF) that occurs after ischaemia during exercise. "( Allopurinol prevents ischaemia-dependent haemorheological changes.
Acciavatti, A; Capecchi, PL; Ceccatelli, L; Di Perri, T; Galigani, C; Orrico, A; Pasini, FL; Pasqui, AL; Pieragalli, D, 1988
)
"Pretreatment with allopurinol did not significantly reduce the postoperative increase in serum creatinine and sodium excretion, but the urine osmolality returned to normal more rapidly than in the control group."( Kidney protection by pretreatment with free radical scavengers and allopurinol: renal function at recirculation after warm ischaemia in rabbits.
Hansson, R; Johansson, S; Jonsson, O; Pettersson, S; Scherstén, T; Waldenström, J, 1986
)
"Pretreatment with allopurinol produced a significant (p less than 0.01) preventive effect on PAF induced hypotension."( Role of oxygen derived free radicals in platelet activating factor induced bowel necrosis.
Cueva, JP; Hsueh, W, 1988
)
"Treatment with allopurinol within the first minutes after coronary occlusion was ineffective in limiting tissue necrosis in this model of permanent coronary occlusion, therefore, long pretreatment with allopurinol is necessary for cardioprotection."( Myocardial salvage with allopurinol during 24 h of permanent coronary occlusion: importance of pretreatment.
Downey, JM; Hearse, DJ; Kingma, JG; Miura, T; Yellon, DM, 1988
)
"Pretreatment with allopurinol (a xanthine oxidase inhibitor) reduced the absorption of hypoxanthine, increased the retention of label in the tissue 4-fold or more, and elevated nucleotide formation 10-fold or more."( Effect of nutritional state and allopurinol on purine metabolism in the rat small intestine.
Gross, CJ; Savaiano, DA; Stiles, JE, 1988
)
"Pretreatment with allopurinol (50.0 mg kg-1 i.v.), 60 min before inducing haemorrhagic shock, had no significant effect upon the haemodynamic response to shock, but did prevent the gradual decline seen following reinfusion in the untreated animals."( The protective action of allopurinol in an experimental model of haemorrhagic shock and reperfusion.
Allan, G; Cambridge, D; Lee-Tsang-Tan, L; Van Way, CW; Whiting, MV, 1986
)

Toxicity

Allopurinol is an efficacious urate-lowering therapy (ULT), but is associated with rare serious adverse drug reactions of Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) HLA-B*5801 carriers are at higher risk.

ExcerptReference
" However, these conclusions are different from those of a study where 3 was tested in the presence of a generated toxic oxygen species that can cause mutagenic changes of the environment."( A critical evaluation of the present status of toxicity of aminoxyl radicals.
Sosnovsky, G, 1992
)
" None of the nonresponders responded to the addition of folinic acid, on the contrary toxicity was increased and 2 toxic deaths were reported."( Continuous 24-hour infusion of folinic acid does not increase the response rate of 5-fluorouracil but only the toxicity.
Karvounis, N; Kosmidis, P; Tsavaris, N; Tzannou, I, 1992
)
"We investigated whether or not the generation of reactive oxygens and toxic photoproducts participated in the cutaneous phototoxicity mechanisms induced by the quinolone derivatives, ofloxacin (OFLX), enoxacin, lomefloxacin, ciprofloxacin and DR-3355 (the s-isomer of OFLX) in a mouse model."( Important role of oxygen metabolites in quinolone antibacterial agent-induced cutaneous phototoxicity in mice.
Tawara, K; Wagai, N, 1991
)
"It has been suggested that the generation of toxic radicals plays an important role in toxicity by Adriamycin (ADR) on cancer cell lines and in vivo."( Cytotoxic effect of adriamycin and agarose-coupled adriamycin on glomerular epithelial cells: role of free radicals.
Bertelli, R; Ghiggeri, GM; Ginevri, F; Gusmano, R, 1991
)
"The toxic potential of sodium orthovanadate towards isolated perfused rat livers was investigated at a dose of 2 mmol/l."( Vanadate-induced toxicity towards isolated perfused rat livers: the role of lipid peroxidation.
Strubelt, O; Younes, M, 1991
)
" We conclude that in vitro oxygen metabolites, extracellularly generated, have a direct toxic effect on gastric mucosal cells; hydrogen peroxide is a major mediator of oxygen metabolite-induced gastric cell injury; the oxygen-derived superoxide and hydroxyl radicals are less toxic to gastric mucosal cells than hydrogen peroxide; and intracellular glutathione, which detoxifies hydrogen peroxide, may be involved in antioxidant defense mechanisms."( Oxygen metabolite-induced cytotoxicity to cultured rat gastric mucosal cells.
Hiraishi, H; Ivey, KJ; Ota, S; Sugimoto, T; Terano, A, 1987
)
"To provide a systematic analysis of how adverse symptoms of disease and side effects of cancer therapy relate to patient noncompliance with treatment, we interviewed 107 patients with hematologic malignancies at the initiation of therapy and 6 months later to collect information on the type, frequency, and difficulty of unpleasant physical effects experienced."( The influence of symptoms of disease and side effects of treatment on compliance with cancer therapy.
Levine, A; Marks, G; Richardson, JL, 1988
)
"In order to elucidate toxic and protective mechanisms responsible for allopurinol-induced nephrotoxicity in rats, we investigated changes in plasma creatinine concentration, renal lipid peroxidation, and renal activities of xanthine oxidase, superoxide dismutase and catalase, as enzymatic factors in producing and scavenging oxygen radicals."( Possible mechanism responsible for allopurinol-nephrotoxicity: lipid peroxidation and systems of producing- and scavenging oxygen radicals.
Sudo, J; Suzuki, Y, 1987
)
" We report a new case of serious toxic manifestations with acute interstitial nephritis."( [Allopurinol toxicity. Apropos of 1 case].
Berthoux, F; Genin, C; Guérin, C; Leroy, G; Sabatier, JC; Toulon, J, 1986
)
" Toxic effects are specially considered in this paper, where effects in 20 advanced gastrointestinal patients are evaluated."( [5-fluorouracil in high doses. Principles and toxicity].
Fleischer, I; Milano, MC; Wainstein, R, 1985
)
" A 60-min incubation in the presence of the enzyme systems resulted in a dose-dependent toxic effect with evidence of cytolysis (increased LDH release) and cell loss (decrease in DNA and protein content), when these indexes were measured 24 hr after completion of the enzyme reaction."( Effect of variable glutathione peroxidase activity on H2O2-related cytotoxicity in cultured aortic endothelial cells.
Junod, AF; Ody, C, 1985
)
" Toxic effects limited the dose of azathioprine in 27 patients (42%) and led to discontinuation of therapy in 13 (20%)."( Azathioprine toxicity in neuromuscular disease.
Griggs, RC; Kissel, JT; Levy, RJ; Mendell, JR, 1986
)
" It is concluded that sulfite oxidase is instrumental in counteracting the toxic systemic effects of bisulfite, either injected or derived from respired SO(2)."( Molecular basis of the biological function of molybdenum: the relationship between sulfite oxidase and the acute toxicity of bisulfite and SO2.
Cohen, HJ; Drew, RT; Johnson, JL; Rajagopalan, KV, 1973
)
" These results denote that the minimal toxic dose ranges between 10 and 30 mg/kg/day, and that the kidney is more sensitive than the liver."( Allopurinol toxicity: its toxic organ-specificity between the liver and the kidney in the rat.
Sudo, J; Suzuki, Y; Tanabe, T, 1984
)
" Gastrointestinal and hematologic toxic effects were mild and infrequent."( High-dose allopurinol modulation of 5-FU toxicity: phase I trial of an outpatient dose schedule.
Campbell, TN; House, BA; Howell, SB; Pfeifle, C, 1982
)
" For this reason we rate the development of this disease in both cases as a rare but significant side effect of allopurinol."( [Granuloma anulare disseminatum as a rare side effect of allopurinol].
Becker, D; Bräuninger, W; Enk, A; Knop, J, 1995
)
" In summary, in this series, routine human liver procurement using exclusive aortic perfusion seemed to be at least as safe as using a combined aortic and portal perfusion technique."( Liver procurement without in situ portal perfusion. A safe procedure for more flexible multiple organ harvesting.
Barker, A; de Ville de Goyet, J; Hausleithner, V; Jamart, J; Lerut, J; Malaise, J; Otte, JB; Reding, R, 1994
)
" Using the xanthine/xanthine oxidase reaction to generate superoxide radicals, we have attempted to examine the role of the Fenton reaction in SOD toxicity observing that high SOD levels along with micromolar concentrations of Fe2+ greatly increased the production of the highly toxic hydroxyl radical."( Superoxide dismutase (SOD)-catalase conjugates. Role of hydrogen peroxide and the Fenton reaction in SOD toxicity.
Lopaschuk, GD; Mao, GD; Poznansky, MJ; Thomas, PD, 1993
)
" Vitamin E neutralized the toxic effect of free radicals in vitro."( Toxicity of free radicals to mesothelial cells and peritoneal membrane.
Breborowicz, A; Martis, L; Oreopoulos, DG; Serkes, KD; Wieczorowska, K; Witowski, J, 1993
)
"p injection of the ribosome-inactivating proteins ricin or saporin, or a Ber-H2 (anti-CD30)-saporin immunotoxin at a dose corresponding to three times the LD50 calculated for mice."( Hepatoxicity of ricin, saporin or a saporin immunotoxin: xanthine oxidase activity in rat liver and blood serum.
Battelli, MG; Bolognesi, A; Buonamici, L; Polito, L; Stirpe, F, 1996
)
" These results suggest that H2O2 is more toxic to colonic epithelial cells than 02."( Hydrogen peroxide-mediated cytotoxicity to cultured colonic epithelial cells.
Hata, Y; Hiraishi, H; Ivey, KJ; Kawabe, T; Ota, S; Terano, A, 1997
)
" RINm5F cells were also susceptible to butylalloxan, a lipophilic alloxan derivative that is selectively toxic to pancreatic beta-cells."( Complementary action of antioxidant enzymes in the protection of bioengineered insulin-producing RINm5F cells against the toxicity of reactive oxygen species.
Lenzen, S; Lortz, S; Munday, R; Tiedge, M, 1998
)
" However, when used in patients with renal insufficiency it may have life-threatening toxic effects known as allopurinol hypersensitivity syndrome (AHS)."( Nephrotoxic effects of allopurinol in dinitrofluorobenzene-sensitized mice: comparative studies on TEI-6720.
Horiuchi, H; Kaneko, H; Kasahara, Y; Komoriya, K; Ohta, T; Ota, M, 1999
)
"We investigated the relationship between the toxic effect of allopurinol and pyrimidine metabolism in mice."( Allopurinol induces renal toxicity by impairing pyrimidine metabolism in mice.
Horiuchi, H; Kaneko, H; Kasahara, Y; Komoriya, K; Nishimura, S; Ohta, T; Ota, M, 2000
)
" However, it induces nephrotoxicity, a severe side effect in which oxygen free radicals have been implicated to play an important role."( Potentiation of cisplatin-induced nephrotoxicity in rats by allopurinol.
Erdinç, L; Erdinç, M; Işik, B; Nergiz, Y, 2000
)
"These results suggest that reactive oxygen metabolites can contribute significantly to the development of intestinal lesions, and that R(-)-ketoprofen present in racemic preparations can enhance the toxic intestinal effects of S (+)-enantiomer via modification of neutrophil migration and oxidative stress."( Intestinal toxicity of ketoprofen-trometamol vs its enantiomers in rat. Role of oxidative stress.
Cabré, F; de la Lastra, CA; Herrerías, JM; Martín, MJ; Mauleón, D; Motilva, V; Nieto, A, 2000
)
" The potent free radical scavenger erdosteine may have protective potential in this process and it will become a promising drug in the prevention of this undesired side-effect of cisplatin, but further studies are needed to illuminate the exact protection mechanism of erdosteine against cisplatin-induced nephrotoxicity."( In vivo evidence suggesting a role for purine-catabolizing enzymes in the pathogenesis of cisplatin-induced nephrotoxicity in rats and effect of erdosteine against this toxicity.
Kotuk, M; Ozyurt, H; Söğüt, S; Ulu, R; Yildirim, Z; Yilmaz, HR,
)
"Allopurinol is generally considered to be a safe and well tolerated drug."( [Side effects off allopurinol].
Kvande, KT; Rødevand, E; Sletvold, O, 2004
)
" Although not uncommon, adverse events were mild and self-limited, and no deaths or serious adverse events were observed."( Febuxostat (TMX-67), a novel, non-purine, selective inhibitor of xanthine oxidase, is safe and decreases serum urate in healthy volunteers.
Becker, MA; Hunt, B; Joseph-Ridge, N; Khosravan, R; Kisicki, J; MacDonald, P; Mulford, D; Wu, J, 2004
)
" A total of five adverse events were reported with all mild in severity."( PK/PD and safety of a single dose of TMX-67 (febuxostat) in subjects with mild and moderate renal impairment.
Hoshide, S; Hosoya, T; Ishikawa, T; Komoriya, K; Kubo, J; Ohno, I; Takahashi, Y; Tsuchimoto, M, 2004
)
"Cisplatin ototoxicity has been associated with the generation of toxic levels of reactive oxygen species (ROS) which can lead to injury or loss of outer hair cells in the organ of Corti, damage to the stria vascularis, and loss of spiral ganglion cells, resulting in permanent hearing loss."( Reduction of acute cisplatin ototoxicity and nephrotoxicity in rats by oral administration of allopurinol and ebselen.
Gu, R; Kil, J; Lynch, ED; Pierce, C, 2005
)
" Incidences of treatment-related adverse events were similar in the febuxostat and placebo groups."( Febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase: a twenty-eight-day, multicenter, phase II, randomized, double-blind, placebo-controlled, dose-response clinical trial examining safety and efficacy in patients with gout.
Becker, MA; Eustace, D; Joseph-Ridge, N; MacDonald, PA; Palo, WA; Schumacher, HR; Vernillet, L; Wortmann, RL, 2005
)
" Febuxostat therapy was safe and well tolerated."( Febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase: a twenty-eight-day, multicenter, phase II, randomized, double-blind, placebo-controlled, dose-response clinical trial examining safety and efficacy in patients with gout.
Becker, MA; Eustace, D; Joseph-Ridge, N; MacDonald, PA; Palo, WA; Schumacher, HR; Vernillet, L; Wortmann, RL, 2005
)
" We now demonstrate that this osteogenic combination of oxysterols prevents the adverse effects of oxidative stress on differentiation of M2 cells into mature osteoblastic cells."( Osteogenic oxysterols inhibit the adverse effects of oxidative stress on osteogenic differentiation of marrow stromal cells.
Amantea, CM; Hahn, TJ; Kha, HT; Parhami, F; Richardson, JA; Shouhed, D, 2005
)
"The genotoxicity of benzoquinone (BQ), a toxic benzene metabolite, is greatly enhanced by the presence of fetal calf serum (FCS) in the incubation medium."( Involvement of oxygen free radicals in the serum-mediated increase of benzoquinone genotoxicity.
De Bartolomeo, A; Fabiani, R; Morozzi, G, 2005
)
" Febuxostat 80 mg once daily appears to be generally safe and well tolerated in mildly and moderately impaired hepatic function groups, and dose adjustment is not required in subjects with mild to moderate hepatic impairment."( The effect of mild and moderate hepatic impairment on pharmacokinetics, pharmacodynamics, and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase.
Grabowski, BA; Joseph-Ridge, N; Khosravan, R; Mayer, MD; Vernillet, L; Wu, JT, 2006
)
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
"Reactive oxygen species (ROS) generated by xanthine oxidoreductase (XOR) were toxic to B lymphoma-derived Raji cells (positive for 8A monoclonal antibody, mAb)."( Toxicity of xanthine oxidoreductase to malignant B lymphocytes.
Battelli, MG; Bolognesi, A; Falà, F; Musiani, S; Polito, L; Stirpe, F; Tazzari, PL,
)
" The majority of adverse events were mild-to-moderate in intensity."( Pharmacokinetics, pharmacodynamics and safety of febuxostat, a non-purine selective inhibitor of xanthine oxidase, in a dose escalation study in healthy subjects.
Grabowski, BA; Joseph-Ridge, N; Khosravan, R; Vernillet, L; Wu, JT, 2006
)
" However, the boundary between cancer-protecting and toxic levels of selenium is extremely narrow."( Extracellular production of hydrogen selenide accounts for thiol-assisted toxicity of selenite against Saccharomyces cerevisiae.
Barbier, F; Blanquet, S; Dauplais, M; Grigoras, I; Ha-Duong, NT; Lazard, M; Plateau, P; Tarze, A, 2007
)
" Safety was assessed by recording adverse events."( Efficacy and safety of allopurinol in patients with hypoxanthine-guanine phosphoribosyltransferase deficiency.
Prior, C; Puig, JG; Torres, RJ, 2007
)
" Drug adverse effects and the lack of efficacy, however, commonly require withdrawal of therapy."( Thiopurine hepatotoxicity in inflammatory bowel disease: the role for adding allopurinol.
Gearry, RB; Leong, RW; Sparrow, MP, 2008
)
"The addition of low dose allopurinol to dose-reduced thiopurine analogue seems safe but careful monitoring for adverse effects and profiling of thiopurine metabolites is essential."( Thiopurine hepatotoxicity in inflammatory bowel disease: the role for adding allopurinol.
Gearry, RB; Leong, RW; Sparrow, MP, 2008
)
" It appears safe and effective for long-term use, but requires monitoring for myelotoxicity."( Long-term outcome of using allopurinol co-therapy as a strategy for overcoming thiopurine hepatotoxicity in treating inflammatory bowel disease.
Ansari, A; Baburajan, B; Chocair, P; Duley, J; Elliott, T; Mayhead, P; O'Donohue, J; Sanderson, J, 2008
)
" Overall adverse event rates (including cardiovascular adverse event rates), adjusted for 10-fold greater febuxostat than allopurinol exposure, did not differ significantly among treatment groups."( Clinical efficacy and safety of successful longterm urate lowering with febuxostat or allopurinol in subjects with gout.
Becker, MA; Lademacher, C; Lloyd, E; MacDonald, PA; Schumacher, HR, 2009
)
" Adverse effects of TAM include hepatotoxicity."( Caffeic acid phenethyl ester protects against tamoxifen-induced hepatotoxicity in rats.
Abdel-Naim, AB; Albukhari, AA; El-Beshbishy, HA; Gashlan, HM; Nagy, AA, 2009
)
" Moreover, the administration of MK-801 to rats as a pretreatment resulted in a complete prevention of the QUIN-induced NAD(P)H activation, suggesting that this toxic event is completely dependent on N-methyl-D-aspartate receptor overactivation."( NAD(P)H oxidase contributes to neurotoxicity in an excitotoxic/prooxidant model of Huntington's disease in rats: protective role of apocynin.
Galván-Arzate, S; Maldonado, PD; Molina-Jijón, E; Pedraza-Chaverrí, J; Santamaría, A; Villeda-Hernández, J, 2010
)
" The safety of miltefosine-allopurinol combination therapy was confirmed by lack of effect on renal and hepatic parameters and adverse reactions."( Multicentric, controlled clinical study to evaluate effectiveness and safety of miltefosine and allopurinol for canine leishmaniosis.
Bianciardi, P; Cañavate, C; Cruz, I; Miró, G; Mortarino, M; Oliva, G; Vischer, C, 2009
)
" Safety assessments included blinded adjudication of each cardiovascular (CV) adverse event (AE) and death."( The urate-lowering efficacy and safety of febuxostat in the treatment of the hyperuricemia of gout: the CONFIRMS trial.
Becker, MA; Espinoza, LR; Lademacher, C; Lloyd, E; MacDonald, P; Schumacher, HR; Wells, AF, 2010
)
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
"Allopurinol has been presented as a safe and effective adjunct to thiopurine therapy in inflammatory bowel disease (IBD)."( Combination of thiopurines and allopurinol: adverse events and clinical benefit in IBD.
Govani, SM; Higgins, PD, 2010
)
" No serious adverse events were observed."( Using allopurinol above the dose based on creatinine clearance is effective and safe in patients with chronic gout, including those with renal impairment.
Barclay, ML; Chapman, PT; Frampton, C; James, J; O'Donnell, JL; Stamp, LK; Zhang, M, 2011
)
" Our results indicated that ZEN induced several toxic effects and significant alterations mediated by oxidative stress mechanism."( Protective effect of aqueous extract of Allium sativum against zearalenone toxicity mediated by oxidative stress.
Abid-Essefi, S; Bacha, H; Bouaziz, C; Kaderi, R; Salem, IB; Zaied, C, 2012
)
" Allopurinol is efficacious and safe in most patients, but intolerance is estimated to occur in up to 10% of treated patients."( Safety and efficacy of febuxostat treatment in subjects with gout and severe allopurinol adverse reactions.
Chohan, S, 2011
)
" Rates of adverse events (AEs) were low."( Women with gout: efficacy and safety of urate-lowering with febuxostat and allopurinol.
Becker, MA; Chefo, S; Chohan, S; Jackson, RL; MacDonald, PA, 2012
)
"Despite an increasing incidence of gout in older age patients with multiple metabolic and cardiovascular comorbidities, there are limited data addressing whether currently available urate-lowering therapy is comparably effective and safe in older (≥65 years of age) versus younger (<65 years of age) patients."( Treating hyperuricemia of gout: safety and efficacy of febuxostat and allopurinol in older versus younger subjects.
Becker, MA; Gunawardhana, L; Hunt, B; MacDonald, PA, 2011
)
" Adverse events (AEs) were recorded throughout the study."( African American patients with gout: efficacy and safety of febuxostat vs allopurinol.
Chefo, S; Jackson, RL; MacDonald, PA; Wells, AF, 2012
)
"0 mg/dL at the final visit, overall and by renal function status, percent change in sUA from baseline to final visit, flare rates, and rates of adverse events (AEs)."( The efficacy and safety of febuxostat for urate lowering in gout patients ≥65 years of age.
Hunt, B; Jackson, RL; MacDonald, PA, 2012
)
" Allopurinol hypersensitivity syndrome (AHS) is a rare but potentially fatal adverse event."( Starting dose is a risk factor for allopurinol hypersensitivity syndrome: a proposed safe starting dose of allopurinol.
Dalbeth, N; Dockerty, JL; Drake, J; Frampton, C; Jones, PB; Stamp, LK; Taylor, WJ, 2012
)
" Adverse events were monitored and therapeutic adherence was assessed."( Safety and effectiveness of long-term allopurinol-thiopurine maintenance treatment in inflammatory bowel disease.
Bouma, G; de Boer, NK; Hanauer, SB; Harrell, LE; Hoentjen, F; Rubin, DT; Seinen, ML; van Bodegraven, AA, 2013
)
" VPA is a relatively safe drug, but its use in higher concentrations is associated with idiosyncratic neurotoxicity."( An in vitro approach to assess the neurotoxicity of valproic acid-induced oxidative stress in cerebellum and cerebral cortex of young rats.
Chaudhary, S; Parvez, S, 2012
)
" However, few studies have assessed the possible toxic effects of artichoke extracts."( In vivo genotoxicity evaluation of an artichoke (Cynara scolymus L.) aqueous extract.
Da Silva, J; de Andrade, HH; Dihl, RR; Ferraz, AB; Lehmann, M; Nunes, E; Picada, JN; Richter, MF; Semedo, J; Zan, MA, 2013
)
" Finally, 1000 μg/mL cefazolin showed no adverse effects on porcine kidney endothelial cells."( Antibiotic prophylaxis in (sub)normothermic organ preservation: in vitro efficacy and toxicity of cephalosporins.
Bruinsma, BG; de Boer, L; Heger, M; Post, IC; van Gulik, TM; van Rijssen, LB; Zaat, SA, 2013
)
"Allopurinol, one of the most commonly used uric acid-lowering agents, can cause serious adverse events."( Clinical risk factors for adverse events in allopurinol users.
Kim, HW; Kim, JH; Lee, EB; Lee, EY; Lee, YJ; Ryu, HJ; Song, R; Song, YW, 2013
)
" Diabetics and non-diabetics reported self-limiting diarrhoea and URIs as the most common adverse events."( Diabetes and gout: efficacy and safety of febuxostat and allopurinol.
Becker, MA; Hunt, BJ; Jackson, RL; MacDonald, PA, 2013
)
"Despite higher co-morbidity rates in diabetic patients, febuxostat and allopurinol were safe in both groups at the doses tested."( Diabetes and gout: efficacy and safety of febuxostat and allopurinol.
Becker, MA; Hunt, BJ; Jackson, RL; MacDonald, PA, 2013
)
"Heavy metals become toxic when they are not metabolized by the body and accumulate in the soft tissue."( Beneficial effect of sesame oil on heavy metal toxicity.
Chandrasekaran, VR; Hsu, DZ; Liu, MY, 2014
)
"Gout management with allopurinol in patients with CKD can be challenging because of the risk of adverse events and uncertain efficacy."( Safety and efficacy of allopurinol in chronic kidney disease.
Bourg, CA; Phillips, BB; Thurston, MM, 2013
)
" In inflammatory bowel disease patients who shunt thiopurine metabolism towards more toxic and less desirable pathways, allopurinol is proving to be an effective add on therapy with good resultant disease control and less treatment side effects."( Allopurinol use in pregnancy in three women with inflammatory bowel disease: safety and outcomes: a case series.
Andrews, JM; Bampton, PA; Doogue, MP; Fazal, MW; Leong, RW, 2013
)
"We report three cases of safe use of allopurinol in pregnancy for women with inflammatory bowel disease."( Allopurinol use in pregnancy in three women with inflammatory bowel disease: safety and outcomes: a case series.
Andrews, JM; Bampton, PA; Doogue, MP; Fazal, MW; Leong, RW, 2013
)
" The patients' comorbidities and concomitant medications may contribute to the risk of adverse drug reactions with anti-gout therapies."( Safety profile of anti-gout agents: an update.
Stamp, LK, 2014
)
" Allopurinol and febuxostat have similar adverse effect profiles."( Safety profile of anti-gout agents: an update.
Stamp, LK, 2014
)
"In general, treatments for gout are well tolerated, although clinicians must keep in mind the potential for drug interactions and the contribution of comorbidities to the potential for adverse effects with gout therapies."( Safety profile of anti-gout agents: an update.
Stamp, LK, 2014
)
"To study the toxic effects of phthalate esters on the aquatic creatures, carps were exposed to dibutyl phthalate (DBP) and di-2-ethylhexyl phthalate (DEHP) of six different concentrations for 96 h-LC50 measurements."( Toxicity of phthalate esters exposure to carp (Cyprinus carpio) and antioxidant response by biomarker.
Gao, Y; Qi, M; Zhao, X, 2014
)
"The available scientific data indicate that the pathomechanism of Parkinson's disease (PD) involves the accumulation of endogenous and exogenous toxic substances."( Assessment of the role of multidrug resistance-associated proteins in MPTP neurotoxicity in mice.
Klivényi, P; Plangár, I; Szalárdy, L; Vécsei, L; Zádori, D, 2013
)
" The explanation of these findings would be that the stimulation of MRP1- and MRP2-mediated transport of glutathione conjugates of toxic substances may have slight beneficial effects, while stimulation of MRP4-mediated efflux of brain urate, which has an important antioxidant potency, may worsen the effects of oxidative stress."( Assessment of the role of multidrug resistance-associated proteins in MPTP neurotoxicity in mice.
Klivényi, P; Plangár, I; Szalárdy, L; Vécsei, L; Zádori, D, 2013
)
"0 mg/dL), estimated glomerular filtration rates in allografts, and adverse events were retrospectively analyzed in the FX, NFX, and NPTHU groups."( Efficacy and safety of febuxostat in the treatment of hyperuricemia in stable kidney transplant recipients.
Hara, T; Hayashida, Y; Inui, M; Kakehi, Y; Kohno, M; Moriwaki, K; Nishijima, Y; Nishiyama, A; Sofue, T; Ueda, N, 2014
)
" None of the patients in the FX group experienced any severe adverse effects, such as pancytopenia or attacks of gout, throughout the entire study period."( Efficacy and safety of febuxostat in the treatment of hyperuricemia in stable kidney transplant recipients.
Hara, T; Hayashida, Y; Inui, M; Kakehi, Y; Kohno, M; Moriwaki, K; Nishijima, Y; Nishiyama, A; Sofue, T; Ueda, N, 2014
)
"Treatment with febuxostat sufficiently lowered uric acid levels without severe adverse effects in stable kidney transplant recipients with PTHU."( Efficacy and safety of febuxostat in the treatment of hyperuricemia in stable kidney transplant recipients.
Hara, T; Hayashida, Y; Inui, M; Kakehi, Y; Kohno, M; Moriwaki, K; Nishijima, Y; Nishiyama, A; Sofue, T; Ueda, N, 2014
)
" All patients were maintained on febuxostat without serious adverse events, except for 1 patient, who discontinued febuxostat because of numbness in the arms."( Efficacy and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase for the treatment of hyperuricemia in kidney transplant recipients.
Fuchinoue, S; Nakajima, I; Teraoka, S; Tojimbara, T; Yashima, J, 2014
)
" None of the extracts are toxic against brine shrimp larvae in the test concentration."( Enzyme inhibition, antioxidant and immunomodulatory activities, and brine shrimp toxicity of extracts from the root bark, stem bark and leaves of Terminalia macroptera.
Barsett, H; Diallo, D; Ho, GT; Inngjerdingen, KT; Le, NH; Malterud, KE; Michaelsen, TE; Paulsen, BS; Zou, YF, 2014
)
"To investigate the prevalence of xanthine oxidase (XO) inhibitors prescription at admission and discharge in elderly hospital in-patients, to analyze the appropriateness of their use in relation to evidence-based indications, to evaluate the predictors of inappropriate prescription at discharge and the association with adverse events 3 months after hospital discharge."( Inappropriate prescription of allopurinol and febuxostat and risk of adverse events in the elderly: results from the REPOSI registry.
Brucato, AL; Corrao, S; Di Corato, P; Djade, CD; Franchi, C; Ghidoni, S; Mannucci, PM; Marcucci, M; Marengoni, A; Nobili, A; Pasina, L; Salerno, F; Tettamanti, M, 2014
)
" Prescription of XO inhibitors was associated with a higher risk of adverse clinical events in univariate and multivariate analysis."( Inappropriate prescription of allopurinol and febuxostat and risk of adverse events in the elderly: results from the REPOSI registry.
Brucato, AL; Corrao, S; Di Corato, P; Djade, CD; Franchi, C; Ghidoni, S; Mannucci, PM; Marcucci, M; Marengoni, A; Nobili, A; Pasina, L; Salerno, F; Tettamanti, M, 2014
)
"rate of adverse events and death."( Safety of allopurinol compared with other urate-lowering drugs in patients with gout: a systematic review and meta-analysis.
Carmona, L; Castrejon, I; Loza, E; Pérez-Ruiz, F; Rosario, MP; Toledano, E, 2015
)
" The incidence of adverse events was similar in the three treatment groups."( A phase 3, multicenter, randomized, allopurinol-controlled study assessing the safety and efficacy of oral febuxostat in Chinese gout patients with hyperuricemia.
Chen, S; Ji, H; Ji, Q; Lin, J; Liu, B; Liu, H; Liu, P; Liu, X; Lu, Y; Ming, J; Peng, Y; Wang, J; Wang, Y; Xu, S; Zhang, Y, 2015
)
" Febuxostat, at a daily dose of 40 or 80 mg, was safe and well tolerated."( A phase 3, multicenter, randomized, allopurinol-controlled study assessing the safety and efficacy of oral febuxostat in Chinese gout patients with hyperuricemia.
Chen, S; Ji, H; Ji, Q; Lin, J; Liu, B; Liu, H; Liu, P; Liu, X; Lu, Y; Ming, J; Peng, Y; Wang, J; Wang, Y; Xu, S; Zhang, Y, 2015
)
" The objective of the current study was to test for association of this haplotype with other, less severe adverse effects (AEs) of allopurinol therapy in a large New Zealand gout cohort."( A human leukocyte antigen locus haplotype confers risk for allopurinol-related adverse effects in Caucasian patients with gout.
Dalbeth, N; Harrison, A; Merriman, TR; Roberts, RL; Stamp, LK; Wallace, MC, 2015
)
" Treatment-emergent adverse events possibly related to allopurinol occurred in 15."( An open-label, 6-month study of allopurinol safety in gout: The LASSO study.
Baumgartner, S; Becker, MA; Choi, HK; Cravets, M; Dalbeth, N; Fitz-Patrick, D; Storgard, C, 2015
)
"Allopurinol is an efficacious urate-lowering therapy (ULT), but is associated with rare serious adverse drug reactions of Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), with higher risk among HLA-B*5801 carriers."( Cost-effectiveness analysis of genotyping for HLA-B*5801 and an enhanced safety program in gout patients starting allopurinol in Singapore.
Dong, D; Finkelstein, E; Sung, C; Tan-Koi, WC; Teng, GG, 2015
)
"The risk of skin reaction with febuxostat seems moderately increased in patients with a history of cutaneous adverse events with allopurinol."( Risk of cutaneous adverse events with febuxostat treatment in patients with skin reaction to allopurinol. A retrospective, hospital-based study of 101 patients with consecutive allopurinol and febuxostat treatment.
Bardin, T; Chalès, G; Clerson, P; Delayen, A; Flipo, RM; Korng Ea, H; Pascart, T; Roujeau, JC, 2016
)
" Following an initial 2-week washout period, over the next 12 weeks we made five measurements of serum urate levels along with assessments of adverse events (AEs)."( Safety and efficacy of oral febuxostat for treatment of HLA-B*5801-negative gout: a randomized, open-label, multicentre, allopurinol-controlled study.
Chen, CJ; Chen, DY; Hsu, PN; Lai, JH; Lin, HY; Yu, KH, 2016
)
"Oxidative stress (OS) is thought to play an important role in the pharmacological and toxic effects of various drugs of abuse."( Cardiovascular and Hepatic Toxicity of Cocaine: Potential Beneficial Effects of Modulators of Oxidative Stress.
Antonilli, L; Badiani, A; Grassi, MC; Graziani, M; Saso, L; Togna, AR, 2016
)
" There were no meaningful differences in adverse events (AEs) between groups, and there were no serious AEs related to arhalofenate."( A Randomized, Double-Blind, Active- and Placebo-Controlled Efficacy and Safety Study of Arhalofenate for Reducing Flare in Patients With Gout.
Boudes, PF; Choi, YJ; Davis, CS; Martin, RL; McWherter, CA; Poiley, J; Steinberg, AS, 2016
)
" Incidences of overall adverse events (AEs) in the topiroxostat groups were comparable to those in the placebo group; however, the incidence of AEs in the 120-mg group was statistically lower than that in the placebo group."( Clinical efficacy and safety of topiroxostat in Japanese male hyperuricemic patients with or without gout: an exploratory, phase 2a, multicentre, randomized, double-blind, placebo-controlled study.
Hashimoto, H; Hosoya, T; Ohashi, T; Sakamoto, R; Sasaki, T, 2016
)
"HLA-B*5801 allele carriage (a strong determinant of allopurinol hypersensitivity syndrome) varies substantially among races, which may lead to racial disparities in the risk of Stevens-Johnson Syndrome (SJS) and toxic epidermal necrolysis (TEN) in the context of urate-lowering drug adverse events (ULDAEs)."( Racial disparities in the risk of Stevens-Johnson Syndrome and toxic epidermal necrolysis as urate-lowering drug adverse events in the United States.
Choi, HK; Kim, SC; Lu, N; Menendez, ME; Rai, SK; Terkeltaub, R, 2016
)
" Specific information about the dose, effect on serum urate, adverse effects and liver function tests after commencing benzbromarone was recorded."( The safety and efficacy of benzbromarone in gout in Aotearoa New Zealand.
Cathro, A; Corkill, M; Dalbeth, N; Frampton, C; Gardner, D; Grainger, R; Haslett, J; Kain, T; Kumar, R; Kumar, S; Metcalfe, S; Porter, D; Stamp, LK; Stebbings, S; Taylor, G; White, D; Wyeth, J, 2016
)
" Benzbromarone-related adverse events included rash (n = 4), diarrhoea (n = 9), nausea (n = 6) and urate stones (n = 3)."( The safety and efficacy of benzbromarone in gout in Aotearoa New Zealand.
Cathro, A; Corkill, M; Dalbeth, N; Frampton, C; Gardner, D; Grainger, R; Haslett, J; Kain, T; Kumar, R; Kumar, S; Metcalfe, S; Porter, D; Stamp, LK; Stebbings, S; Taylor, G; White, D; Wyeth, J, 2016
)
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
" No significant difference in the incidence of adverse events was observed among all groups, including the allopurinol group."( Clinical efficacy and safety of topiroxostat in Japanese hyperuricemic patients with or without gout: a randomized, double-blinded, controlled phase 2b study.
Hosoya, T; Ohashi, T; Sasaki, T, 2017
)
" The serum uric acid (UA) concentrations of the patients in each group were recorded and compared from week 2 through week 24 after the treatments, and all adverse events were evaluated to determine the safety of the various treatment regimens."( A study comparing the safety and efficacy of febuxostat, allopurinol, and benzbromarone in Chinese gout patients: a retrospective cohort study
.
Chen, X; Su, J; Tian, J; Zhou, Q; Zhou, T; Zhu, J, 2017
)
" However, the total number of patients experiencing adverse events was significantly higher in the febuxostat 80-mg group."( A study comparing the safety and efficacy of febuxostat, allopurinol, and benzbromarone in Chinese gout patients: a retrospective cohort study
.
Chen, X; Su, J; Tian, J; Zhou, Q; Zhou, T; Zhu, J, 2017
)
"Chinese patients treated with the 40-mg dose of febuxostat experienced a treatment effect and total rate of adverse events similar to those produced by allopurinol or benzbromarone."( A study comparing the safety and efficacy of febuxostat, allopurinol, and benzbromarone in Chinese gout patients: a retrospective cohort study
.
Chen, X; Su, J; Tian, J; Zhou, Q; Zhou, T; Zhu, J, 2017
)
" The primary endpoints were reduction in SU and adverse events (AEs)."( A randomised controlled trial of the efficacy and safety of allopurinol dose escalation to achieve target serum urate in people with gout.
Barclay, ML; Chapman, PT; Dalbeth, N; Drake, J; Frampton, C; Horne, A; Stamp, LK; Tan, P, 2017
)
" The results of the safety study showed that no organ toxicity and no treatment-related adverse effects were observed in mice treated with high doses of MFEs."( Evaluating the urate-lowering effects of different microbial fermented extracts in hyperuricemic models accompanied with a safety study.
Chen, HM; Chen, MH; Chen, RJ; Chen, SJ; Chen, YL; Hsiao, CM; Wang, YJ; Wu, MD; Yech, YJ; Yuan, GF, 2017
)
" No other adverse events were reported."( Efficacy and Safety of Febuxostat in Kidney Transplant Patients.
Baek, CH; Han, DJ; Kim, H; Park, SK; Yang, WS, 2018
)
"Febuxostat reduced serum uric acid levels effectively in kidney transplant patients without severe adverse events."( Efficacy and Safety of Febuxostat in Kidney Transplant Patients.
Baek, CH; Han, DJ; Kim, H; Park, SK; Yang, WS, 2018
)
" The effect of baseline kidney function on urate lowering and adverse effects was investigated."( The effect of kidney function on the urate lowering effect and safety of increasing allopurinol above doses based on creatinine clearance: a post hoc analysis of a randomized controlled trial.
Barclay, M; Chapman, PT; Dalbeth, N; Drake, J; Frampton, C; Horne, A; Stamp, LK; Tan, P, 2017
)
" Adverse events were similar among groups."( The effect of kidney function on the urate lowering effect and safety of increasing allopurinol above doses based on creatinine clearance: a post hoc analysis of a randomized controlled trial.
Barclay, M; Chapman, PT; Dalbeth, N; Drake, J; Frampton, C; Horne, A; Stamp, LK; Tan, P, 2017
)
"Allopurinol is effective at lowering urate even though and accepting that there were small numbers of participants with CrCL <30 ml/min, these data indicate that allopurinol dose escalation to target SU is safe in people with severe CKD."( The effect of kidney function on the urate lowering effect and safety of increasing allopurinol above doses based on creatinine clearance: a post hoc analysis of a randomized controlled trial.
Barclay, M; Chapman, PT; Dalbeth, N; Drake, J; Frampton, C; Horne, A; Stamp, LK; Tan, P, 2017
)
" The presence of liver alterations following the introduction of a new drug must suggest an adverse drug reaction."( [A rare case of hepatotoxicity in geriatrics].
El Kahi, C; Martinet, V; Pepersack, T; Praet, JP,
)
" To adjust for treatment duration, treatment-emergent adverse events (TEAEs) were expressed as exposure-adjusted incidence rates (patients with events per 100 person-years)."( Integrated safety studies of the urate reabsorption inhibitor lesinurad in treatment of gout.
Baumgartner, S; Goldfarb, DS; Jalal, D; Pillinger, M; Saag, KG; Schechter, BM; Terkeltaub, R; Valiyil, R; White, WB, 2019
)
" Major adverse cardiovascular events were 3, 4 and 9 with XOI, LESU200+XOI and LESU400+XOI, respectively."( Integrated safety studies of the urate reabsorption inhibitor lesinurad in treatment of gout.
Baumgartner, S; Goldfarb, DS; Jalal, D; Pillinger, M; Saag, KG; Schechter, BM; Terkeltaub, R; Valiyil, R; White, WB, 2019
)
"At the approved dose of 200 mg once-daily combined with an XOI, LESU did not increase renal, cardiovascular or other adverse events compared with XOI alone, except for sCr elevations."( Integrated safety studies of the urate reabsorption inhibitor lesinurad in treatment of gout.
Baumgartner, S; Goldfarb, DS; Jalal, D; Pillinger, M; Saag, KG; Schechter, BM; Terkeltaub, R; Valiyil, R; White, WB, 2019
)
" Liver and blood functions were monitored and other adverse events were recorded."( Comparison of efficacy and safety between febuxostat and allopurinol in early post-renal transplant recipients with new onset of hyperuricemia.
Chen, P; Chen, X; Fu, Q; Gao, X; Li, J; Liu, L; Shen, X; Wang, C, 2019
)
"Despite morbidities and fatalities, nationwide epidemiologic data for severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and drug reaction with eosinophilia and systemic symptoms (DRESS), are not widely available."( Analysis of Individual Case Safety Reports of Severe Cutaneous Adverse Reactions in Korea.
Kang, DY; Kang, HR; Kang, MG; Lee, JY; Park, HK; Sohn, KH; Yang, MS, 2019
)
"We analyzed individual case safety reports (ICSRs) of SCARs in the Korea Adverse Event Reporting System from 1988 to 2013."( Analysis of Individual Case Safety Reports of Severe Cutaneous Adverse Reactions in Korea.
Kang, DY; Kang, HR; Kang, MG; Lee, JY; Park, HK; Sohn, KH; Yang, MS, 2019
)
" The number of SCAR ICSRs has been increasing with increasing ICSRs for overall adverse drug events."( Analysis of Individual Case Safety Reports of Severe Cutaneous Adverse Reactions in Korea.
Kang, DY; Kang, HR; Kang, MG; Lee, JY; Park, HK; Sohn, KH; Yang, MS, 2019
)
"Older drugs for ULT like allopurinol are well studied and extensively described from typical adverse effects (mild skin rash) to unusual fatal reactions, while febuxostat seems to be overall well tolerated."( Safety and tolerability of available urate-lowering drugs: a critical review.
Cicero, AF; Fogacci, F; Strilchuk, L, 2019
)
" The difference in incidence of adverse events among patients with stage 1-3 CKD, those with stage 4-5 CKD, and those on dialysis was not significant."( Renal safety and urate-lowering efficacy of febuxostat in gout patients with stage 4-5 chronic kidney disease not yet on dialysis.
Kim, JM; Kim, SH; Lee, SY; Son, CN, 2020
)
" The serum levels of uric acid (UA), creatinine, other biochemical parameters, estimated glomerular filtration rate (eGFR), and adverse events were measured at baseline as well as at 1, 3, and 6 months after the switch to febuxostat."( Switching from allopurinol to febuxostat: efficacy and safety in the treatment of hyperuricemia in renal transplant recipients.
Li, Y; Liu, M; Lu, Y; Meng, J; Zhang, X, 2019
)
" Data on the incidence of clinical and laboratory adverse events (AEs), including hepatotoxicity and myelotoxicity resulting in imposing LDTA therapy cessation and associated risk factors were collected."( Real-life study of safety of thiopurine-allopurinol combination therapy in inflammatory bowel disease: myelotoxicity and hepatotoxicity rarely affect maintenance treatment.
de Boer, NK; de Jong, DJ; de Veer, RC; de Vries, AC; Dijkstra, G; Kreijne, JE; Moorsel, SAW; van der Woude, CJ; West, R, 2019
)
"LDTA therapy is a safe and beneficial optimisation strategy in IBD patients."( Real-life study of safety of thiopurine-allopurinol combination therapy in inflammatory bowel disease: myelotoxicity and hepatotoxicity rarely affect maintenance treatment.
de Boer, NK; de Jong, DJ; de Veer, RC; de Vries, AC; Dijkstra, G; Kreijne, JE; Moorsel, SAW; van der Woude, CJ; West, R, 2019
)
"Febuxostat had the best efficacy and safety results among the tested agents, and topiroxostat and allopurinol appeared to have fewer adverse events."( Efficacy and safety of urate-lowering treatments in patients with hyperuricemia: A comprehensive network meta-analysis of randomized controlled trials.
Lin, CJ; Lin, JY; Shi, Y; Sun, SS; Zhang, DH, 2020
)
" Safety outcomes included total adverse events (AEs), serious AEs, withdrawals due to AEs, and AEs per organ system."( Comparison of efficacy and safety of urate-lowering therapies for hyperuricemic patients with gout: a meta-analysis of randomized, controlled trials.
Fan, M; Gu, J; Li, X; Liu, J; Schlesinger, N; Wu, X; Zhao, B, 2021
)
" Allopurinol was well tolerated, without significant adverse events."( Allopurinol use during pediatric acute lymphoblastic leukemia maintenance therapy safely corrects skewed 6-mercaptopurine metabolism, improving inadequate myelosuppression and reducing gastrointestinal toxicity.
Annesley, C; Bhuiyan, M; Brown, P; Cohen, G; Cooper, S; Sison, EA, 2020
)
"Thiopurines are important for treating inflammatory bowel disease, but are often discontinued due to adverse effects."( Influence of allopurinol on thiopurine associated toxicity: A retrospective population-based cohort study.
de Boer, A; Egberts, ACG; Houwen, JPA; Houwen, RHJ; Lalmohamed, A; van Maarseveen, EM, 2021
)
" In the febuxostat group, 222 (7·2%) of 3063 patients died and 1720 (57·3%) of 3001 in the safety analysis set had at least one serious adverse event (with 23 events in 19 [0·6%] patients related to treatment)."( Long-term cardiovascular safety of febuxostat compared with allopurinol in patients with gout (FAST): a multicentre, prospective, randomised, open-label, non-inferiority trial.
De Caterina, R; Findlay, E; Ford, I; Hallas, J; Hawkey, CJ; MacDonald, TM; Mackenzie, IS; McMurray, JJV; Nuki, G; Perez-Ruiz, F; Ralston, SH; Robertson, M; Walters, M; Webster, J, 2020
)
"Febuxostat is non-inferior to allopurinol therapy with respect to the primary cardiovascular endpoint, and its long-term use is not associated with an increased risk of death or serious adverse events compared with allopurinol."( Long-term cardiovascular safety of febuxostat compared with allopurinol in patients with gout (FAST): a multicentre, prospective, randomised, open-label, non-inferiority trial.
De Caterina, R; Findlay, E; Ford, I; Hallas, J; Hawkey, CJ; MacDonald, TM; Mackenzie, IS; McMurray, JJV; Nuki, G; Perez-Ruiz, F; Ralston, SH; Robertson, M; Walters, M; Webster, J, 2020
)
" In terms of the adverse events, the pooling overall adverse events data did achieve advantage in the febuxostat group (RR=0."( Efficacy and safety of Febuxostat Versus Allopurinol in Hyperuricemic patients with or without Gout: A meta-analysis.
Fan, B; Li, X; Zhang, P, 2020
)
"A retrospective pharmacovigilance disproportionality analysis was conducted using the Japanese Adverse Drug Event Report database."( Safety profiles of new xanthine oxidase inhibitors: A post-marketing study.
Hirai, T; Hosohata, K; Inada, A; Iwanaga, K; Kambara, H; Nakatsuji, T; Niinomi, I; Oyama, S; Ueno, S; Wakabayashi, T, 2021
)
"Among 7,305 reports of adverse events associated with XO inhibitors, 64."( Safety profiles of new xanthine oxidase inhibitors: A post-marketing study.
Hirai, T; Hosohata, K; Inada, A; Iwanaga, K; Kambara, H; Nakatsuji, T; Niinomi, I; Oyama, S; Ueno, S; Wakabayashi, T, 2021
)
"The strength of the associations of XO inhibitors with adverse events is variable, and further studies are required to evaluate the identified signals."( Safety profiles of new xanthine oxidase inhibitors: A post-marketing study.
Hirai, T; Hosohata, K; Inada, A; Iwanaga, K; Kambara, H; Nakatsuji, T; Niinomi, I; Oyama, S; Ueno, S; Wakabayashi, T, 2021
)
" Elevated levels of 6MMP have been associated with toxic effects that may interfere with therapy."( Allopurinol to Prevent Mercaptopurine Adverse Effects in Children and Young Adults With Acute Lymphoblastic Leukemia.
Bostrom, B; Kamojjala, R, 2021
)
" Initiation of febuxostat in patients was not associated with an increased risk of death or serious cardiovascular related adverse events compared with allopurinol."( Cardiovascular safety of febuxostat compared to allopurinol for the treatment of gout: A systematic and meta-analysis.
Cheng, R; Gao, L; Lu, Y; Pan, Y; Wang, B, 2021
)
" The three outcomes used to assess the safety of uric acid lowering medications were treatment-related adverse events, liver damage, and major adverse cardiovascular events (MACE)."( The association between urate-lowering therapies and treatment-related adverse events, liver damage, and major adverse cardiovascular events (MACE): A network meta-analysis of randomized trials.
Chen, J; Deng, Q; Guo, J; Xie, Q; Xie, S; Yu, Y; Zhang, S; Zhong, L, 2021
)
" We found no statistically significant differences in their effects on treatment-related adverse events and MACE."( The association between urate-lowering therapies and treatment-related adverse events, liver damage, and major adverse cardiovascular events (MACE): A network meta-analysis of randomized trials.
Chen, J; Deng, Q; Guo, J; Xie, Q; Xie, S; Yu, Y; Zhang, S; Zhong, L, 2021
)
" Diagnostic tools, treatment protocols, seroconversion rates and adverse events were investigated."( Monotherapy and combination chemotherapy for Chagas disease treatment: a systematic review of clinical efficacy and safety based on randomized controlled trials.
Cardoso Santos, E; Dias Novaes, R; Lima, GDA; Oliveira Silva, R; Santana Nogueira, S; Vilela Gonçalves, R, 2022
)
" We examined the toxic effects of BPS on gastric and renal functions, as well as the efficacy of allopurinol as a treatment."( Evaluation of the therapeutic role of allopurinol on bisphenol S gastric and renal toxicity in adult male albino rats: An in vivo study.
Fattah, AA; Hosny, SA; Khalifa, FN; Matter, LM; Moawad, AM; Ramadan, NM, 2022
)
" Besides, the drug-related adverse events (AEs) were recorded."( Low-dose febuxostat exhibits a superior renal-protective effect and non-inferior safety profile compared to allopurinol in chronic kidney disease patients complicated with hyperuricemia: A double-centre, randomized, controlled study.
Cao, B; Yang, N, 2022
)
"To evaluate the influence of febuxostat on adverse events and mortality in gout."( Effect of febuxostat on adverse events and mortality in gout in Taiwan: An interrupted time series analysis.
Kuo, CF; Li, PR; Liu, JR; See, LC; Tsai, PH, 2023
)
" An interrupted time series analysis with adjustments for demographics, comorbidities, and comedication by propensity score-based stabilized weights was used to compare the trend of adverse events and mortality before vs after febuxostat was introduced in 2012."( Effect of febuxostat on adverse events and mortality in gout in Taiwan: An interrupted time series analysis.
Kuo, CF; Li, PR; Liu, JR; See, LC; Tsai, PH, 2023
)
" The slope of the 1-year incidence rate of Stevens-Johnson syndrome (SJS) or toxic epidermal necrolysis (TEN) (per 10 000 patients) significantly reduced after 2012 in those with and without comorbidities (-0."( Effect of febuxostat on adverse events and mortality in gout in Taiwan: An interrupted time series analysis.
Kuo, CF; Li, PR; Liu, JR; See, LC; Tsai, PH, 2023
)
" The latter shows higher efficacy but a higher side effect rate, suggesting the use of split-dose regimen as the first-line approach."( Safety and Efficacy of Split-Dose Thiopurine vs Low-Dose Thiopurine-Allopurinol Cotherapy in Pediatric Inflammatory Bowel Disease.
Borrelli, O; Buckingham, R; Chadokufa, S; Cococcioni, L; El-Kouly, S; Gaynor, E; Kiparissi, F; Pensabene, L; Puoti, MG; Saliakellis, E, 2023
)
"To determine the risk of adverse events associated with colchicine or non-steroidal anti-inflammatory drug (NSAID) prophylaxis when initiating allopurinol for gout."( Safety of colchicine and NSAID prophylaxis when initiating urate-lowering therapy for gout: propensity score-matched cohort studies in the UK Clinical Practice Research Datalink.
Bajpai, R; Clarson, LE; Forrester, H; Mallen, CD; Muller, S; Padmanabhan, N; Partington, RJ; Roddy, E; Whittle, R, 2023
)
" Weighted Cox proportional hazards models investigated associations between colchicine/NSAID and specified adverse events."( Safety of colchicine and NSAID prophylaxis when initiating urate-lowering therapy for gout: propensity score-matched cohort studies in the UK Clinical Practice Research Datalink.
Bajpai, R; Clarson, LE; Forrester, H; Mallen, CD; Muller, S; Padmanabhan, N; Partington, RJ; Roddy, E; Whittle, R, 2023
)
" Adverse event incidence rates were <200/10 000 patient-years except diarrhoea (784."( Safety of colchicine and NSAID prophylaxis when initiating urate-lowering therapy for gout: propensity score-matched cohort studies in the UK Clinical Practice Research Datalink.
Bajpai, R; Clarson, LE; Forrester, H; Mallen, CD; Muller, S; Padmanabhan, N; Partington, RJ; Roddy, E; Whittle, R, 2023
)

Pharmacokinetics

Three open-label, multiple-dose studies in healthy subjects investigated possible pharmacokinetic interactions between aliskiren 300 mg od and three drugs. In this randomized, crossover evaluation in healthy volunteers, probenecid reduces the renal clearance of allopurinol riboside. The purpose of this investigation was to determine the pharmacokinetics disposition of intravenous alloparinol in neonates with the hypoplastic left heart syndrome (HLHS)

ExcerptReference
" This was accomplished by generating parent drug and metabolite plasma level profiles assuming formation and excretion rate-limited pharmacokinetic models with absorption rate constants obtained from bivariate normal distributions and designated random errors."( The role of metabolites in bioequivalency assessment. I. Linear pharmacokinetics without first-pass effect.
Chen, ML; Jackson, AJ, 1991
)
"6 hours after administration, has an elimination half-life of 3 hours, and steady-state concentrations in the therapeutic range."( Pharmacokinetics and metabolism of allopurinol riboside.
Danso, K; Desjardins, RE; Nelson, DJ; Pamplin, CL; Shapiro, TA; Were, JB, 1991
)
" Pharmacokinetic absorption behavior of a sustained-release preparation of theophylline after repetitive oral administration was adequately evaluated using MFA-MULTI."( Pharmacokinetic analysis of single- or multiple-dose plasma drug concentration data with a microcomputer using multi-fraction absorption models.
Murata, K; Noda, K; Samejima, M; Tagawa, K, 1989
)
" The pharmacokinetic absorption behavior of a sustained-release preparation of diltiazem hydrochloride was studied using a multi-fraction absorption model."( Pharmacokinetic analysis of concentration data of drugs with irregular absorption profiles using multi-fraction absorption models.
Kohno, K; Murata, K; Noda, K; Samejima, M, 1987
)
" Furthermore, the plasma oxipurinol half-life was increased from 27."( Sustained reductions in oxipurinol renal clearance during a restricted diet.
Berlinger, WG; Kitt, TM; Park, GD; Spector, R; Tsalikian, E, 1987
)
" Allopurinol controlled release tablets (Sigapurol CR), containing 200 mg of the drug characterized by rapid absorption and 100 mg characterized by pH-dependent delivery, were identified as a formulation with advantages pharmacokinetic properties."( [Clinical pharmacokinetics of allopurinol. 3. Allopurinol/oxipurinol pharmacokinetics following administration of a controlled release allopurinol preparation].
Fenner, H; Gikalov, I; Radivojevich, F; Schiemann, O, 1986
)
"02), and the plasma oxypurinol half-life increased nearly threefold from 17."( The effect of dietary protein on the clearance of allopurinol and oxypurinol.
Berlinger, WG; Park, GD; Spector, R, 1985
)
"In a pharmacokinetic study with 6 healthy volunteers the parameters for allopurinol and oxipurinol were compared following a single dose of allopurinol and multiple application of the drug."( [The clinical pharmacokinetics of allopurinol. 2. Allopurinol/oxypurinol pharmacokinetics following allopurinol in single doses and multiple application].
Fenner, H; Gikalov, I; Schiemann, O, 1985
)
" The influence of allopurinol on the pharmacokinetic parameters of 6MP was as follows: (a) a 2-fold increase in the half-life and area under the concentration-time curve; (b) a 2-fold decrease in the total body clearance; and (c) an approximate 3-fold decrease in elimination rate constant."( Effect of allopurinol on the pharmacokinetics of 6-mercaptopurine in rabbits.
Brown, DA; Day, JL; Schroeder, EC; Tterlikkis, L, 1983
)
"The aim of this study was to determine the relative bioavailability of five oral allopurinol preparations and evaluation of the pharmacodynamic effect."( [Comparative study of the bioavailability and the pharmacodynamic effect of five allopurinol preparations (author's transl)].
Blome, J; Jaeger, H; Rasper, J; Russmann, D, 1982
)
"4 mg/kg, 200 mg/m2, 200 microCi total) was administered to five patients; the radiolabel in the plasma declined with an initial half-life (t1/2) of 14 min and a terminal t1/2 of 19."( Pharmacokinetics and metabolism of beta-2'-deoxythioguanosine and 6-thioguanine in man.
Benvenuto, JA; Bodey, GP; Gottlieb, JA; Loo, TL; Lu, K; Rosenblum, MG, 1982
)
"In a randomized cross-over study with 10 volunteers two different commercial preparations of allopurinol (Remid and standard) were tested by reversed-phase HPLC with respect to their pharmacokinetic behaviour."( [Pharmacokinetic studies on plasma elimination half-life of oxipurinol (author's transl)].
Bader, B; Harries, EH; Lach, HJ; Schnitker, J, 1982
)
" The possibility of a pharmacokinetic interaction between the anti-viral agent, famciclovir and allopurinol has been investigated in twelve healthy male volunteers following a single oral dose of famciclovir (500 mg) in the presence and absence of steady-state levels of allopurinol (300 mg)."( Lack of a pharmacokinetic interaction between oral famciclovir and allopurinol in healthy volunteers.
Fowles, SE; Laroche, J; Pratt, SK; Prince, WT, 1994
)
"The purpose of this investigation was to determine the pharmacokinetic disposition of intravenous allopurinol and its metabolite oxypurinol in neonates with the hypoplastic left heart syndrome (HLHS) and to evaluate the subsequent degree of xanthine oxidase inhibition using serum uric acid as a marker."( The pharmacokinetics of injectable allopurinol in newborns with the hypoplastic left heart syndrome.
Clancy, RR; Davis, LE; Jacobs, ML; Krawczeniuk, MM; McGaurn, SP; Murphy, JD; Norwood, WI, 1994
)
" Pharmacokinetic parameters were determined for elimination half-life, clearance, volume of distribution, and mean residence time."( The pharmacokinetics of injectable allopurinol in newborns with the hypoplastic left heart syndrome.
Clancy, RR; Davis, LE; Jacobs, ML; Krawczeniuk, MM; McGaurn, SP; Murphy, JD; Norwood, WI, 1994
)
" to healthy male volunteers to evaluate its pharmacokinetic and pharmacodynamic properties."( Pharmacokinetic and pharmacodynamic properties of a novel xanthine oxidase inhibitor, BOF-4272, in healthy volunteers.
Nakashima, M; Uematsu, T, 1994
)
" In this randomized, crossover evaluation in healthy volunteers, probenecid reduces the renal clearance of allopurinol riboside, extends the half-life of allopurinol riboside in plasma, and triples the levels of allopurinol riboside in plasma."( Effects of probenecid on the pharmacokinetics of allopurinol riboside.
Shapiro, TA; Were, JB, 1993
)
"To determine bioavailability and pharmacokinetic parameters for allopurinol and its active metabolite, oxypurinol."( Bioavailability and pharmacokinetics of intravenously and orally administered allopurinol in healthy beagles.
Bartges, JW; Bird, KA; Chen, M; Felice, LJ; Koehler, LA; Osborne, CA; Sawchuk, RJ; Ulrich, LK, 1997
)
" The bioavailability of allopurinol, and pharmacokinetic parameters of allopurinol and oxypurinol after oral administration of allopurinol, are not affected by administration with food."( Bioavailability and pharmacokinetics of intravenously and orally administered allopurinol in healthy beagles.
Bartges, JW; Bird, KA; Chen, M; Felice, LJ; Koehler, LA; Osborne, CA; Sawchuk, RJ; Ulrich, LK, 1997
)
" From these data, pharmacokinetic parameters were calculated."( Influence of two diets on pharmacokinetic parameters of allopurinol and oxypurinol in healthy beagles.
Bartges, JW; Bird, KA; Chen, M; Felice, LJ; Koehler, LA; Osborne, CA; Ulrich, LK, 1997
)
"There is no influence of diet on pharmacokinetic parameters of allopurinol or oxypurinol."( Influence of two diets on pharmacokinetic parameters of allopurinol and oxypurinol in healthy beagles.
Bartges, JW; Bird, KA; Chen, M; Felice, LJ; Koehler, LA; Osborne, CA; Ulrich, LK, 1997
)
" Similar pharmacokinetic profiles for DXG were observed following either route of administration in serum, liver and brain."( Biotransformation and pharmacokinetics of prodrug 9-(beta-D-1,3-dioxolan-4-yl)-2-aminopurine and its antiviral metabolite 9-(beta-D-1,3-dioxolan-4-yl)guanine in mice.
Boudinot, FD; Chu, CK; Manouilov, KK; Manouilova, LS; Schinazi, RF, 1997
)
" The elimination half-life of the distribution phase (t1/2(alpha)) was similar in mice (0."( Pharmacokinetics of BOF-4272, a xanthine oxidase inhibitor, after single intravenous or oral administration to male mice and rats.
Naito, S; Nishimura, M; Nogawa, H, 1999
)
"25) as was the area under the oxipurinol plasma concentration-time curve, AUC (260+/-46 and 166+/-23 microgram ml-1 h, respectively), the pharmacodynamic effect of oxipurinol was smaller in elderly than young subjects (time-dependent decrease of plasma uric acid 83+/-30 microgram ml-1 h in elderly compared with 176+/-21 in young controls)."( Pharmacokinetics and pharmacodynamics of allopurinol in elderly and young subjects.
Krivanek, P; Oberbauer, R; Turnheim, K, 1999
)
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
" Considering the dose, the AUC(obs) and Cmax of unchanged drug in patients with gout and/or hyperuricemia were estimated to be similar to those of healthy male adults."( Pharmacokinetics and pharmacodynamics of febuxostat (TMX-67), a non-purine selective inhibitor of xanthine oxidase/xanthine dehydrogenase (NPSIXO) in patients with gout and/or hyperuricemia.
Hoshide, S; Kamatani, N; Kobayashi, H; Komoriya, K; Kubo, J; Nakachi, T; Takeda, K; Tsuchimoto, M; Yamanaka, H, 2004
)
" Regression analyses indicated that febuxostat tmax and Cmax,u values were not affected by CLcr."( Pharmacokinetics and pharmacodynamics of febuxostat, a new non-purine selective inhibitor of xanthine oxidase in subjects with renal impairment.
Joseph-Ridge, N; Khosravan, R; Mayer, MD; Mulford, DJ; Vernillet, L; Wu, JT,
)
"Quantitative structure-pharmacokinetic relationships (QSPkR) have increasingly been used for the prediction of the pharmacokinetic properties of drug leads."( Quantitative structure-pharmacokinetic relationships for drug clearance by using statistical learning methods.
Chen, YZ; Li, ZR; Yap, CW, 2006
)
" There were no statistically significant differences in the plasma pharmacokinetic parameters for unbound febuxostat and its active metabolites between subjects with mild or moderate hepatic impairment and those with normal hepatic function."( The effect of mild and moderate hepatic impairment on pharmacokinetics, pharmacodynamics, and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase.
Grabowski, BA; Joseph-Ridge, N; Khosravan, R; Mayer, MD; Vernillet, L; Wu, JT, 2006
)
"A simple HPLC method was developed and validated for the determination of uric acid (UA), xanthine (X) and hypoxanthine (HX) concentrations in human serum to support pharmacodynamic (PD) studies of a novel xanthine oxidase inhibitor during its clinical development."( Quantification of uric acid, xanthine and hypoxanthine in human serum by HPLC for pharmacodynamic studies.
Cooper, N; Erdmann, C; Fiene, J; Khosravan, R; Lee, JW, 2006
)
" In the present study, a population pharmacokinetic model was designed and validated for allopurinol in this specific patient group."( Population pharmacokinetics of allopurinol in full-term neonates with perinatal asphyxia.
Benders, MJ; Groenendaal, F; Rademaker, CM; van Bel, F; van Kesteren, C; Ververs, FF, 2006
)
" During the course of the study, blood and urine samples were collected to assess the pharmacokinetics of febuxostat and its metabolites, and its pharmacodynamic effects on uric acid, xanthine and hypoxanthine concentrations after both single and multiple dose administration."( Pharmacokinetics, pharmacodynamics and safety of febuxostat, a non-purine selective inhibitor of xanthine oxidase, in a dose escalation study in healthy subjects.
Grabowski, BA; Joseph-Ridge, N; Khosravan, R; Vernillet, L; Wu, JT, 2006
)
" There appeared to be a linear pharmacokinetic and dose-response (percentage decrease in serum uric acid) relationship for febuxostat dosages within the 10-120 mg range."( Pharmacokinetics, pharmacodynamics and safety of febuxostat, a non-purine selective inhibitor of xanthine oxidase, in a dose escalation study in healthy subjects.
Grabowski, BA; Joseph-Ridge, N; Khosravan, R; Vernillet, L; Wu, JT, 2006
)
" Pharmacokinetic and pharmacodynamic parameters were analysed using two-way ANOVA."( Pharmacokinetic and pharmacodynamic interaction between allopurinol and probenecid in healthy subjects.
Day, RO; Graham, GG; McLachlan, AJ; Stocker, SL; Williams, KM, 2008
)
" This multiple-dose study investigated the potential for pharmacokinetic interactions between aliskiren and three drugs, each predominantly eliminated by a different clearance/metabolic pathway: allopurinol (glomerular filtration), celecoxib (cytochrome P450 metabolism) and cimetidine (P-glycoprotein and organic anion/cation transporters)."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008
)
"Three open-label, multiple-dose studies in healthy subjects investigated possible pharmacokinetic interactions between aliskiren 300 mg od and allopurinol 300 mg od (n = 20), celecoxib 200 mg bid (n = 22), or cimetidine 800 mg od (n = 22)."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008
)
"In this multiple-dose study, aliskiren showed no clinically relevant pharmacokinetic interactions when co-administered with allopurinol, celecoxib or cimetidine in healthy subjects."( A study of the pharmacokinetic interactions of the direct renin inhibitor aliskiren with allopurinol, celecoxib and cimetidine in healthy subjects.
Ayalasomayajula, S; Bizot, MN; Dieterich, HA; Dole, WP; Howard, D; Tchaloyan, S; Yeh, CM, 2008
)
" 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
)
" Following multiple dosing with febuxostat, there were no statistically significant differences in the plasma or urinary pharmacokinetic or pharmacodynamic parameters between subjects aged 18 to 40 years and >or=65 years."( The effect of age and gender on pharmacokinetics, pharmacodynamics, and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase.
Joseph-Ridge, N; Khosravan, R; Kukulka, MJ; Vernillet, L; Wu, JT, 2008
)
"To investigate the pharmacokinetic and pharmacodynamic interaction between probenecid and oxypurinol (the active metabolite of allopurinol) in patients with gout."( Pharmacokinetic and pharmacodynamic interaction between allopurinol and probenecid in patients with gout.
Day, RO; Graham, GG; McLachlan, AJ; Stocker, SL; Williams, KM, 2011
)
"The aims of this study were to develop a population pharmacokinetic model for allopurinol and oxypurinol and to explore the influence of patient characteristics on allopurinol and oxypurinol pharmacokinetics."( The population pharmacokinetics of allopurinol and oxypurinol in patients with gout.
Barclay, ML; Duffull, SB; Holford, NH; Merriman, TR; Stamp, LK; Wright, DF, 2013
)
"The pharmacokinetic model provides a means of predicting the allopurinol dose required to achieve target oxypurinol plasma concentrations for patients with different magnitudes of renal function, different body mass and with or without concomitant diuretic use."( The population pharmacokinetics of allopurinol and oxypurinol in patients with gout.
Barclay, ML; Duffull, SB; Holford, NH; Merriman, TR; Stamp, LK; Wright, DF, 2013
)
" The proposed method was successfully applied to pharmacokinetic studies in humans."( A sensitive LC-MS/MS method for the quantification of febuxostat in human plasma and its pharmacokinetic application.
Inamadugu, JK; Katreddi, HR; Pilli, NR; Ramesh, M; Vaka, VR, 2013
)
"All pharmacokinetic parameters were comparable between the two formulations The observed mean Cmax, AUC(last), and AUC(∞) values for the reference formulation were 3,670 ng/mL, 12,086 ng x h/mL, and 12,880 ng x h/mL, respectively."( Comparison of pharmacokinetics and uric acid lowering effect between two different strength febuxostat formulations (80 mg vs. 40 mg) in healthy subjects.
Kim, KA; Park, JY, 2015
)
" The mean Cmax and AUClast values increased with increasing doses, and exposure to LC350189 was dose proportional."( Pharmacokinetics, pharmacodynamics, and tolerability of LC350189, a novel xanthine oxidase inhibitor, in healthy subjects.
Jang, IJ; Lee, H; Shin, D; Yoon, S; Yu, KS, 2015
)
" The 90% confidence intervals for the ratio of log transformed values of Cmax , AUC0-t , and AUCt-∞ of the two treatments were within the acceptable range (0."( Pharmacokinetics and comparative bioavailability of allopurinol formulations in healthy subjects.
El-Bedaiwy, HM; Helmy, SA, 2014
)
" In order to investigate the pharmacokinetic behavior in vivo, a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for determination the concentration of WSJ-537 in rat plasma was developed."( Development of a selective and fast LC-MS/MS for determination of WSJ-537, an xanthine oxidase inhibitor, in rat plasma: Application to a pharmacokinetic study.
Lin, J; Yang, T; Zhang, D, 2016
)
" Derivatives of imidazole, 1,3-thiazole and pyrimidine proved to be more potent than febuxostat while also displaying/possessing favorable predicted physico-chemical, pharmacokinetic and toxicological properties."( Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
Anderluh, M; Jakopin, Ž; Kocić, G; Petronijević, Ž; Šmelcerović, A; Šmelcerović, Ž; Tomašič, T; Tomović, K, 2017
)
" The developed assay was successfully applied in an oral pharmacokinetic study of allopurinol, oxypurinol and lesinurad in rats."( Ultra-performance hydrophilic interaction liquid chromatography coupled with tandem mass spectrometry for simultaneous determination of allopurinol, oxypurinol and lesinurad in rat plasma: Application to pharmacokinetic study in rats.
Alam, O; Ezzeldin, E; Herqash, RN; Iqbal, M, 2019
)
" The validated lesinurad plasma quantification method was successfully applied for the pharmacokinetic evaluations to support the clinical studies in renal impaired patients."( The Effects of Special Patient Population Plasma on Pharmacokinetic Quantifications Using LC-MS/MS.
Nguyen, M; Sun, L; Wilson, DM; Yeh, LT; Zhou, D, 2019
)
" With the confirmation that there is no impact on quantification from the matrix, the bioanalytical method can be used to support the pharmacokinetic evaluations for clinical studies in special populations."( The Effects of Special Patient Population Plasma on Pharmacokinetic Quantifications Using LC-MS/MS.
Nguyen, M; Sun, L; Wilson, DM; Yeh, LT; Zhou, D, 2019
)
" The purpose of the present study was to standardize and validate a sensitive high-performance liquid chromatography-mass spectrometric (HPLC-MS/MS) method to determine the concentration of allopurinol and its active metabolite oxypurinol in canine urine for clinical pharmacokinetic investigation."( Detection of allopurinol and oxypurinol in canine urine by HPLC/MS-MS: Focus on veterinary clinical pharmacokinetics.
Azeredo, FJ; Barrouin-Melo, SM; de Jesus, C; Godoy, ALPC; Gonçalves, RS; Lanchote, VL; Larangeira, DF; Marques, MP; Rocha, A, 2020
)
"The aim of this study was to quantify identifiable sources of variability, including key pharmacogenetic variants in oxypurinol pharmacokinetics and their pharmacodynamic effect on serum urate (SU)."( Population pharmacokinetics, pharmacodynamics and pharmacogenetics modelling of oxypurinol in Hmong adults with gout and/or hyperuricemia.
Brundage, RC; Culhane-Pera, KA; Roman, YM; Straka, RJ; Wen, YF, 2023
)
" A sequential population pharmacokinetic pharmacodynamics (PKPD) analysis with non-linear mixed effects modelling was performed."( Population pharmacokinetics, pharmacodynamics and pharmacogenetics modelling of oxypurinol in Hmong adults with gout and/or hyperuricemia.
Brundage, RC; Culhane-Pera, KA; Roman, YM; Straka, RJ; Wen, YF, 2023
)

Compound-Compound Interactions

The aim of this 6-month, randomized, blinded, controlled clinical trial was to compare the efficacy and safety of aminosidine-allo. In this review we will explore the history, pharmacology, recent studies and give recommendations for the utilisation of azathioprine combined with allopurinol.

ExcerptReference
"Rats with an experimental solitary liver tumor of a nitrosoguanidine-induced colonic adenocarcinoma were subjected to hepatic artery ligation (HAL) alone or in combination with 5-fluorouracil (5-FU) in three different doses, with or without the addition of allopurinol."( Effect on liver tumor growth in rats of allopurinol and 5-fluorouracil in combination with hepatic artery ligation.
Carlsson, G; Gustavsson, B; Hafström, L, 1989
)
"2 per day) combined with a fixed dose of interferon-alpha 2b (5 million units) and allopurinol (300 mg."( 5-fluorouracil and allopurinol combined with recombinant interferon-alpha 2b in the treatment of patients with advanced prostate cancer: a phase I/II study.
Amdur, RJ; Ernstoff, MS; Fukui, I; Glazier, DB; Harris, R; Heaney, JA; Schned, AR, 1996
)
" Cohorts of patients received a 5-day constant infusion of 5-fluorouracil combined with subcutaneous interferon-alpha 2b 3 times weekly and allopurinol for 1 week during 5-fluorouracil infusion."( 5-fluorouracil and allopurinol combined with recombinant interferon-alpha 2b in the treatment of patients with advanced prostate cancer: a phase I/II study.
Amdur, RJ; Ernstoff, MS; Fukui, I; Glazier, DB; Harris, R; Heaney, JA; Schned, AR, 1996
)
" In ROP kidneys, however, TAN were less reduced, suggesting that even during CS, TAN can still be regenerated in the injured kidneys when ROP is combined with UW solution."( Retrograde oxygen persufflation in combination with UW solution enhances adenine nucleotide contents in ischemically damaged rat kidney during cold storage.
Booster, MH; Buurman, WA; Kootstra, G; Maessen, JG; van der Vusse, GJ; Yin, M, 1996
)
" Two patients with advanced stages of the disease were treated with polychemotherapy (pentamidine and allopurinol) combined with recombinant human interferon-gamma (rIFN-gamma)."( The efficacy of pentamidine combined with allopurinol and immunotherapy for the treatment of patients with diffuse cutaneous leishmaniasis.
Becker, I; Berzunza-Cruz, M; Dominguez, JS; Morales-Vargas, A; Perez-Montfort, R; Ruiz-Remigio, A; Salaiza-Suazo, N; Velasco-Castrejon, O; Volkow, P, 1999
)
" I show how such biochemical information may be combined with genetic information, thus demonstrating the usefulness of biochemical data."( Biochemical data in ornithine transcarbamylase deficiency (OTCD) carrier risk estimation: logistic discrimination and combination with genetic information.
Oexle, K, 2006
)
" The potential for drug-drug interactions with febuxostat was examined in the following three in vitro systems: the characteristics of the binding of febuxostat to human plasma proteins; identification of the cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes participating in the metabolism of febuxostat; and the potential inhibitory effects of febuxostat on typical CYP reactions."( In vitro drug-drug interaction studies with febuxostat, a novel non-purine selective inhibitor of xanthine oxidase: plasma protein binding, identification of metabolic enzymes and cytochrome P450 inhibition.
Hoshide, S; Kanou, M; Mukoyoshi, M; Muroga, H; Nishimura, S; Taniguchi, K; Umeda, S, 2008
)
"Electroacupuncture combined with local blocking is an effective method for treatment of acute gouty arthritis and it can decrease blood uric acid level."( [Observation on therapeutic effect of electroacupuncture combined with local blocking therapy on acute gouty arthritis].
Liu, B; Wang, FY; Wang, HM, 2008
)
" However, allopurinol drastically induced apoptosis of PC-3 and DU145 in combination with tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), which is a promising candidate for anticancer agent but its efficacy is limited by the existence of resistant cancer cells."( Anti-gout agent allopurinol exerts cytotoxicity to human hormone-refractory prostate cancer cells in combination with tumor necrosis factor-related apoptosis-inducing ligand.
Goda, AE; Horinaka, M; Miki, T; Mizutani, Y; Sakai, T; Shiraishi, T; Wakada, M; Yano, K; Yasuda, T; Yoshida, T, 2008
)
"To study the effect of retention enema of Chinese herbal medicine combined with allopurinol in treating hyperuricaemia (HUE)."( Clinical study on treatment of hyperuricaemia by retention enema of Chinese herbal medicine combined with allopurinol.
Akebaier, W; Chen, Q; Ma, L, 2009
)
"Seventy-eight patients with HUE were assigned to two: groups, the 40 patients in the treated group were treated with retention enema of Chinese herbal medicine combined with oral intake of allopurinol, and the 38 patients in the control group were treated with allopurinol alone."( Clinical study on treatment of hyperuricaemia by retention enema of Chinese herbal medicine combined with allopurinol.
Akebaier, W; Chen, Q; Ma, L, 2009
)
"Retention enema with: Chinese herbal medicine combined with allopurinol could obviously reduce the uric acid level in blood, improve patients' renal function and lipid metabolism, and alleviate the clinical symptoms in patients with HUE."( Clinical study on treatment of hyperuricaemia by retention enema of Chinese herbal medicine combined with allopurinol.
Akebaier, W; Chen, Q; Ma, L, 2009
)
" The efficacy of miltefosine and marbofloxacin alone or in combination with allopurinol against clinical strains of Leishmania infantum was assessed in vitro by incubating increasing concentrations of the drugs with a standard parasite inoculum."( Canine leishmaniosis: in vitro efficacy of miltefosine and marbofloxacin alone or in combination with allopurinol against clinical strains of Leishmania infantum.
Badino, P; Farca, AM; Ferroglio, E; Miniscalco, B; Monticelli, P; Odore, R; Trisciuoglio, A, 2012
)
"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
)
"In this study, a new method based on ultrafiltration liquid chromatography-mass spectrometry (UF-LC-MS) combined with enzyme channel blocking (ECB) was developed to discover bioactive components from herbal medicines."( Screening for selective inhibitors of xanthine oxidase from Flos Chrysanthemum using ultrafiltration LC-MS combined with enzyme channel blocking.
Chen, J; Fu, Y; Li, P; Mo, HY; Song, HP; Zhang, H; Zhang, M, 2014
)
" Therefore, ultrafiltration liquid chromatography combined with high-speed countercurrent chromatography is not only a powerful tool for screening and isolating α-glucosidase and xanthine oxidase inhibitors in complex samples but is also a useful platform for discovering bioactive compounds for the prevention and treatment of diabetes mellitus and gout."( Ultrafiltration liquid chromatography combined with high-speed countercurrent chromatography for screening and isolating potential α-glucosidase and xanthine oxidase inhibitors from Cortex Phellodendri.
Guo, L; Li, S; Liu, C; Ma, B; Qin, Y; Ren, J; Tang, Y; Wang, J; Wang, Y; Yang, X; Zhang, Y, 2014
)
" Probenecid alone or in combination with furosemide reduced XO protein expression significantly."( Molecular mechanism of an adverse drug-drug interaction of allopurinol and furosemide in gout treatment.
Bahn, A; Knake, C; Stamp, L, 2014
)
"The aims of this study are to evaluate prevalence and characteristics of adverse drug reactions (ADRs) and to evaluate the potential contribution of specific medications, therapeutic categories and drug-drug interactions (DDIs) in older adults."( Understanding adverse drug reactions in older adults through drug-drug interactions.
Bettoni, D; Brognoli, F; Concoreggi, C; Marengoni, A; Martini, G; Nobili, A; Onder, G; Pasina, L, 2014
)
" Thus, application of ursodeoxycholic acid, rosuvastatin and allopurinol in these study patients with NAFLD dosages in combination with hyperuricemia improves the clinical symptoms and normalization of biochemical parameters and normalizes the spectrum of biliary acids."( [CORRECTION OF BILE FLOW CHARACTERISTICS IN PATIENTS WITH NON-ALCOHOLIC FATTY LIVER DISEASE IN COMBINATION WITH HYPERURICEMIA].
Barabanchyk, OV; Kozak, NP; Svintsits'kyĭ, AS, 2014
)
" The results demonstrate that UF-LC-MS combined with HSCCC might provide not only a powerful tool for screening and isolating xanthine oxidase inhibitors in complex samples but also a useful platform for discovering bioactive compounds for the prevention and treatment of gout."( Development of a method to screen and isolate potential xanthine oxidase inhibitors from Panax japlcus var via ultrafiltration liquid chromatography combined with counter-current chromatography.
Guo, L; Li, J; Li, S; Liu, C; Tang, Y; Zhang, Y, 2015
)
"To assess the efficacy and tolerability of lesinurad, an oral selective uric acid reabsorption inhibitor, in combination with allopurinol versus allopurinol alone in patients with gout and an inadequate response to allopurinol."( Lesinurad in combination with allopurinol: results of a phase 2, randomised, double-blind study in patients with gout with an inadequate response to allopurinol.
Cravets, M; Miner, JN; Perez-Ruiz, F; Storgard, C; Sundy, JS, 2016
)
"Patients (N=227) with an inadequate response to allopurinol, defined as serum urate (sUA) ≥6 mg/dL on ≥2 occasions ≥2 weeks apart despite ≥6 weeks of allopurinol, were randomised 2:1 to 4 weeks of double-blind treatment with lesinurad (200, 400 or 600 mg/day) or matching placebo in combination with their prestudy allopurinol dose (200-600 mg/day)."( Lesinurad in combination with allopurinol: results of a phase 2, randomised, double-blind study in patients with gout with an inadequate response to allopurinol.
Cravets, M; Miner, JN; Perez-Ruiz, F; Storgard, C; Sundy, JS, 2016
)
" Lesinurad 200, 400 and 600 mg in combination with allopurinol produced significant mean percent reductions from baseline sUA of 16%, 22% and 30%, respectively, versus a mean 3% increase with placebo (p<0."( Lesinurad in combination with allopurinol: results of a phase 2, randomised, double-blind study in patients with gout with an inadequate response to allopurinol.
Cravets, M; Miner, JN; Perez-Ruiz, F; Storgard, C; Sundy, JS, 2016
)
"Lesinurad achieves clinically relevant and statistically significant reductions in sUA in combination with allopurinol in patients who warrant additional therapy on allopurinol alone."( Lesinurad in combination with allopurinol: results of a phase 2, randomised, double-blind study in patients with gout with an inadequate response to allopurinol.
Cravets, M; Miner, JN; Perez-Ruiz, F; Storgard, C; Sundy, JS, 2016
)
"Lesinurad is a selective uric acid reabsorption inhibitor used for the treatment of gout in combination with a xanthine oxidase inhibitor."( Lesinurad Combined With Allopurinol: A Randomized, Double-Blind, Placebo-Controlled Study in Gout Patients With an Inadequate Response to Standard-of-Care Allopurinol (a US-Based Study).
Adler, S; Baumgartner, S; Becker, MA; Bhakta, N; Fitz-Patrick, D; Fung, M; Kopicko, J; Saag, KG; Storgard, C, 2017
)
" We aimed to describe our center's experience with thiopurine optimization through the use of reduced thiopurine dosing in combination with allopurinol upon hepatotoxicity, drug metabolite levels, and clinical outcomes in children with IBD."( Thiopurine Optimization Through Combination With Allopurinol in Children With Inflammatory Bowel Diseases.
Boyle, B; Bricker, J; Crandall, W; Dotson, JL; Kim, SC; Maltz, R; Serpico, MR, 2018
)
"Low-dose thiopurines in combination with allopurinol improved hepatotoxicity and increased 6-TG levels in children with IBD."( Thiopurine Optimization Through Combination With Allopurinol in Children With Inflammatory Bowel Diseases.
Boyle, B; Bricker, J; Crandall, W; Dotson, JL; Kim, SC; Maltz, R; Serpico, MR, 2018
)
"The objective of the study was to evaluate the effect of lesinurad, a selective uric acid uptake inhibitor, alone and in combination with the xanthine oxidase inhibitor allopurinol, on serum uric acid and urinary urate excretion in patients with gout and hyperuricemia."( The Effect of Lesinurad in Combination With Allopurinol on Serum Uric Acid Levels in Patients With Gout.
Baumgartner, S; Kerr, B; Manhard, K; Quart, B; Shen, Z; Yeh, LT, 2018
)
"We aimed to assess the relative efficacy and safety of once-daily administration of lesinurad in combination with xanthine oxidase inhibitor (XOI) in hyperuricemic patients with gout."( Comparative efficacy and safety of lesinurad 200 mg and 400 mg combined with a xanthine oxidase inhibitor in hyperuricemic patients with gout: A Bayesian network meta-analysis of randomized controlled trials
.
Lee, YH; Song, GG, 2019
)
"A method based on enzyme blocking combined with ultrafiltration liquid chromatography-mass spectrometry (LC-MS) has been developed to identify xanthine oxidase (XOD) inhibitors in the roots of Lindera reflexa Hemsl (LR) and determine their binding positions."( Screening, and identification of the binding position, of xanthine oxidase inhibitors in the roots of Lindera reflexa Hemsl using ultrafiltration LC-MS combined with enzyme blocking.
Chen, S; Fu, Y; Sun, X; Xie, Z; Yang, J; Zhao, P, 2019
)
"Both tioguanine and low-dose thiopurines combined with allopurinol (LDTA) can be considered for the treatment of inflammatory bowel disease (IBD) when conventional thiopurines fail due to adverse events."( A comparative analysis of tioguanine versus low-dose thiopurines combined with allopurinol in inflammatory bowel disease patients.
Biemans, VBC; de Boer, NKH; Dijkstra, G; Gabriëls, RY; Hoentjen, F; Pierik, MJ; Savelkoul, E; Simsek, M; West, RL, 2020
)
"The aim of this 6-month, randomized, blinded, controlled clinical trial was to compare the efficacy and safety of aminosidine-allopurinol combination with that of meglumine antimoniate-allopurinol combination for the treatment of leishmaniosis in dogs without stage III or IV chronic kidney disease."( A randomized, blinded, controlled clinical trial comparing the efficacy of aminosidine (paromomycin)-allopurinol combination with the efficacy of meglumine antimoniate-allopurinol combination for the treatment of canine leishmaniosis due to Leishmania inf
Apostolidis, K; Athanasiou, LV; Chatzis, MK; Ikonomopoulos, J; Kasabalis, D; Leontides, LS; Mataragka, A; Petanides, T; Saridomichelakis, MN; Xenoulis, PG, 2020
)
" In this review we will explore the history, pharmacology, recent studies and give recommendations for the utilisation of the usual duo of azathioprine combined with allopurinol."( Low-Dose Azathioprine in Combination with Allopurinol: The Past, Present and Future of This Useful Duo.
Sparrow, MP; Turbayne, AK, 2022
)
"Adverse drug events due to drug-drug interactions can be prevented by avoiding concomitant use of causative drugs; therefore, it is important to understand drug combinations that cause drug-drug interactions."( Possibility of Multiple Drug-Drug Interactions in Patients Treated with Statins: Analysis of Data from the Japanese Adverse Drug Event Report (JADER) Database and Verification by Animal Experiments.
Horii, N; Inoue, N; Kobayashi, D; Mutoh, M; Negishi, A; Numajiri, S; Ohshima, S; Oshima, S, 2022
)

Bioavailability

Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms. It is not absorbed rectally from any of the dosage forms to any significant extent.

ExcerptReference
" Accumulation of caffeine, with its subsequent metabolism to theophylline, in patients, who consume average quantities of caffeine-containing beverages relative to those patients who avoid such drinks could interfere with bioavailability studies in normal volunteers."( The human metabolism of caffeine to theophylline.
Hossie, RD; McGilveray, IJ; Sved, S, 1976
)
" This was accomplished by generating parent drug and metabolite plasma level profiles assuming formation and excretion rate-limited pharmacokinetic models with absorption rate constants obtained from bivariate normal distributions and designated random errors."( The role of metabolites in bioequivalency assessment. I. Linear pharmacokinetics without first-pass effect.
Chen, ML; Jackson, AJ, 1991
)
" The bioavailability of breast milk Mo seems to be higher than formula Mo according to the Mo levels and to their statistical link with uric acid excretion which could be proposed as a functional index of Mo status."( Molybdenum in the premature infant.
Bougle, D; Bureau, F; Duhamel, JF; Foucault, D; Voirin, J, 1991
)
" Recently, wide variability in the bioavailability of oral mercaptopurine has been demonstrated, and there is concern that this may affect the risk of relapse."( Systemic exposure to mercaptopurine as a prognostic factor in acute lymphocytic leukemia in children.
Ferrazini, G; Giesbrecht, E; Greenberg, M; Kapelushnik, J; Klein, J; Koren, G; Langevin, AM; Soldin, S; Sulh, H, 1990
)
"The bioavailability of 6-mercaptopurine (6-MP) administered orally for maintenance therapy of children with acute lymphoblastic leukemia is highly variable."( Milk could decrease the bioavailability of 6-mercaptopurine.
David, M; Leclerc, JM; Lin, KT; Rivard, GE, 1989
)
" The authors conclude that the procedures are useful and effective for potentiating the bioavailability of pharmacologically active natural products."( Activation of antioxidant activity in natural medicinal products by heating, brewing and lipophilization. A new drug delivery system.
Kanoh, T; Kasama, T; Negishi, M; Niwa, Y, 1988
)
" Studies of oral 6-MP indicate that, contrary to previous information, the bioavailability of this drug is relatively poor after oral administration, and that plasma 6-MP concentrations achieved after uniform oral dosing are highly variable."( The pharmacology of orally administered chemotherapy. A reappraisal.
Balis, FM; Poplack, DG; Zimm, S, 1986
)
" 6-Deoxyacyclovir, an analog of acyclovir, is well absorbed when given orally, and is converted to acyclovir by xanthine oxidase which is present in the gut and liver."( The disposition of 6-deoxyacyclovir, a xanthine oxidase-activated prodrug of acyclovir, in the isolated perfused rat liver.
Hoofnagle, JH; Jones, DB; Jones, EA; Kornhauser, DM; Quinn, R; Rustgi, VK; Woods, A,
)
"Nonlinear regression analysis of plasma drug concentration data with irregular or stepwise absorption profiles was studied using multi-fraction absorption models in which drugs in the gastrointestinal tract were assumed to be divided into several fractions each with its respective lag time and absorption rate constant."( Pharmacokinetic analysis of concentration data of drugs with irregular absorption profiles using multi-fraction absorption models.
Kohno, K; Murata, K; Noda, K; Samejima, M, 1987
)
"Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms to humans and rabbits; however, it is not absorbed rectally from any of the dosage forms to any significant extent."( Allopurinol absorption from different sites of the rat gastrointestinal tract.
Kramer, WG; Patel, VS, 1986
)
"Studies of the Clinical Pharmacokinetics of Allopurinol/3rd Communication: Allopurinol/oxipurinol bioavailability and pharmacokinetics following the administration of a controlled release allopurinol formulation."( [Clinical pharmacokinetics of allopurinol. 3. Allopurinol/oxipurinol pharmacokinetics following administration of a controlled release allopurinol preparation].
Fenner, H; Gikalov, I; Radivojevich, F; Schiemann, O, 1986
)
" A capacity limited absorption process for allopurinol, suggested from the results of a study on the allopurinol bioavailability from different formulations, could not be proved in the range of single doses between 200 and 600 mg resp."( [The clinical pharmacokinetics of allopurinol. 1. Allopurinol absorption sites and dose proportionality of allopurinol/oxipurinol bioavailability].
Fenner, H; Gikalov, I; Haertel, M; Hugemann, B; Schiemann, O; Schuster, O, 1985
)
" After a single oral dose of 100 mg atenolol combined with 1 gm ampicillin, the bioavailability of atenolol was reduced to 36 +/- 5% compared to 60 +/- 8% after monotherapy."( Atenolol interaction with aspirin, allopurinol, and ampicillin.
Axthelm, T; Kirch, W; Köhler, H; Mutschler, E; Schäfer-Korting, M, 1983
)
"The aim of this study was to determine the relative bioavailability of five oral allopurinol preparations and evaluation of the pharmacodynamic effect."( [Comparative study of the bioavailability and the pharmacodynamic effect of five allopurinol preparations (author's transl)].
Blome, J; Jaeger, H; Rasper, J; Russmann, D, 1982
)
" The absolute systemic bioavailability of the oral tablet was 67% +/- 23%, while the allopurinol rectal suppositories produced no measurable plasma concentrations of allopurinol or oxipurinol in any of the subjects."( Allopurinol kinetics and bioavailability. Intravenous, oral and rectal administration.
Appelbaum, SJ; Dorr, RT; Mayersohn, M; Perrier, D, 1982
)
" The bioavailability of oral allopurinol computed from plasma data was 90."( Kinetics of allopurinol after single intravenous and oral doses. Noninteraction with benzbromarone and hydrochlorothiazide.
Breithaupt, B; Tittel, M, 1982
)
"The relative bioavailability of two commercial preparations of 100 mg and 300 mg allopurinol tablets was examined in two groups of 16 healthy human subjects, one for each dosage level."( The bioavailability of two commercial preparations of allopurinol tablets.
Kleinberg, SI; Marcus, M; Tse, FL, 1982
)
"The bioavailability of allopurinol from orally administered tablets and rectally administered suppositories is reported."( Bioavailability of allopurinol oral and rectal dosage forms.
Ballentine, R; Chang, SL; Feldman, S; Frankel, LS; Kramer, WG, 1981
)
" Its high content in soybeans and relatively high bioavailability favor genistein as a promising candidate for the prevention of human cancers."( Antioxidant and antipromotional effects of the soybean isoflavone genistein.
Barnes, S; Bowen, R; Cai, Q; Wang, Y; Wei, H, 1995
)
" The bioavailability of the prodrug after oral administration was 60."( Enhanced brain delivery of an anti-HIV nucleoside 2'-F-ara-ddI by xanthine oxidase mediated biotransformation.
Chu, CK; Du, J; Gallo, JM; Koudriakova, T; Nampalli, S; Schinazi, RF; Shanmuganathan, K, 1994
)
" The CI of Cmax of allopurinol slightly exceeded the upper limit of 130%, so that bioequivalence was not confirmed with regard to the rate of bioavailability of the parent compound."( Bioequivalence of allopurinol preparations: to be assessed by the parent drug or the active metabolite?
de Vries, JX; Ittensohn, A; Kreiner, C; Stenzhorn, G; Voss, A; Walter-Sack, I; Weber, E, 1993
)
" The bioavailability of allopurinol was low (14."( The pharmacokinetics or oral and intravenous allopurinol and intravenous oxypurinol in the horse.
Dunnett, M; Mills, PC; Smith, NC, 1995
)
"Oxipurinol is well absorbed and sufficiently effective in hyperuricemic patients when administered as a rapid release preparation of oxipurinol sodium."( Uric acid lowering effect of oxipurinol sodium in hyperuricemic patients - therapeutic equivalence to allopurinol.
de Vries, JX; Ernst, B; Frei, M; Kolb, S; Kosmowski, J; Priebe, U; Schroder, HE; Slotty, C; Voss, A; Walter-Sack, I; Weber, A; Wegscheider, K, 1996
)
"To determine bioavailability and pharmacokinetic parameters for allopurinol and its active metabolite, oxypurinol."( Bioavailability and pharmacokinetics of intravenously and orally administered allopurinol in healthy beagles.
Bartges, JW; Bird, KA; Chen, M; Felice, LJ; Koehler, LA; Osborne, CA; Sawchuk, RJ; Ulrich, LK, 1997
)
" The bioavailability of allopurinol, and pharmacokinetic parameters of allopurinol and oxypurinol after oral administration of allopurinol, are not affected by administration with food."( Bioavailability and pharmacokinetics of intravenously and orally administered allopurinol in healthy beagles.
Bartges, JW; Bird, KA; Chen, M; Felice, LJ; Koehler, LA; Osborne, CA; Sawchuk, RJ; Ulrich, LK, 1997
)
"We studied the effects of 5-MTHF on NO bioavailability in vivo in 10 patients with FH and 10 matched control subjects by venous occlusion plethysmography, using serotonin and nitroprusside as endothelium-dependent and -independent vasodilators."( 5-methyltetrahydrofolate, the active form of folic acid, restores endothelial function in familial hypercholesterolemia.
Kastelein, JJ; Koomans, HA; Rabelink, TJ; van Dam, T; Verhaar, MC; Wever, RM, 1998
)
" The relative bioavailability with respect to a reference preparation for AUC related to oxipurinol was 98."( [The bioequivalence of a new allopurinol tablet formulation in comparison to a reference formulation].
Buchberger, D; Läuter, J; Metzner, JE; Pech, R, 1997
)
" In summary, the bioavailability of components of preservation solutions at 4 degrees C is lower than at physiological temperatures, so that the application of cytoprotectants at 37 degrees C to organ donors, rather than simple addition to the cold storage solution, might improve cold storage preservation of livers and kidneys."( Effect of temperature on hepatic and renal uptake of components from University of Wisconsin solution.
Büchler, MW; Schilling, M; Tian, YH, 1998
)
"The relative bioavailability of allopurinol from two tablet preparations (Uribenz vs."( Bioequivalence of allopurinol-containing tablet preparations.
Barthel, W; Haustein, KO; Hüller, G, 1999
)
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
" Nitrate tolerance increased bioavailability of NO in the heart without increasing formation of reactive oxygen species."( Nitrate tolerance does not increase production of peroxynitrite in the heart.
Baxter, GF; CsonkA, C; Csont, T; Dux, L; Ferdinandy, P; Görbe, A; Onody, A; Schulz, R, 2002
)
" Because of their unique chemical versatility and unusually high bioavailability these two transition metals have been incorporated into the active sites of enzymes over the course of evolution."( Molybdenum and tungsten in biology.
Hille, R, 2002
)
" Thus to further improve the NAC bioavailability a single oral administration of 1200 mg NAC has been recently proposed."( Human neutrophil oxidative bursts and their in vitro modulation by different N-acetylcysteine concentrations.
Allegra, L; Bovio, C; Braga, PC; Dal Sasso, M; Fonti, E; Massoni, C, 2002
)
" These results suggest that prolonged exposure of rabbits to oral arsenate may impair the bioavailability of BH(4) in endothelial cells and, as a consequence, disrupt the balance between NO and O2(."( A potential mechanism for the impairment of nitric oxide formation caused by prolonged oral exposure to arsenate in rabbits.
Hayashi, T; Horiguchi, S; Itoh, K; Kumagai, Y; Nikaido, M; Pi, J; Shimojo, N; Sun, G; Sun, Y; Waalkes, MP; Yamamoto, M; Yamauchi, H, 2003
)
" Superoxide production in the aorta was reduced by sepiapterin and by L-NAME, suggesting that reduced bioavailability of tetrahydrobiopterin and uncoupling of nitric oxide synthase were the origin of increased reactive oxygen species in this model."( Effect of hyperhomocystinemia and hypertension on endothelial function in methylenetetrahydrofolate reductase-deficient mice.
Amiri, F; Iglarz, M; Neves, MF; Rozen, R; Schiffrin, EL; Touyz, RM; Virdis, A, 2003
)
"Mthfr+/- mice show endothelial dysfunction of mesenteric vessels probably attributable to a reduced nitric oxide bioavailability caused by oxidative excess due to uncoupling of nitric oxide synthase without vascular structural alterations."( Effect of hyperhomocystinemia and hypertension on endothelial function in methylenetetrahydrofolate reductase-deficient mice.
Amiri, F; Iglarz, M; Neves, MF; Rozen, R; Schiffrin, EL; Touyz, RM; Virdis, A, 2003
)
" Y-700 (1 mg/kg) was absorbed rapidly by the oral route with high bioavailability (84."( Y-700 [1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid]: a potent xanthine oxidoreductase inhibitor with hepatic excretion.
Eger, BT; Fukunari, A; Kamezawa, M; Kato, N; Nishino, T; Okamoto, K; Pai, EF; Yamada, I, 2004
)
" These results suggested that Y-700 is a new effective inhibitor of XO in rats and humans with high oral bioavailability being predominantly eliminated via the liver unlikely to allopurinol."( Pharmacokinetics/pharmacodynamics of Y-700, a novel xanthine oxidase inhibitor, in rats and man.
Fukunari, A; Iwane, J; Kamezawa, M; Mori, H; Osajima, T; Yamada, I, 2004
)
" These observations reveal that XO-derived reactive oxygen species significantly contribute to impaired coronary NO bioavailability in CAD and that XO inhibition represents an additional treatment concept for inflammatory vascular diseases that deserves further investigation."( Oxypurinol improves coronary and peripheral endothelial function in patients with coronary artery disease.
Baldus, S; Berger, J; Chumley, P; Freeman, BA; Heitzer, T; Koss, K; Köster, R; Meinertz, T; Münzel, T; Ostad, MA; Rudolph, V; Staude, HJ; Thuneke, F; Warnholtz, A, 2005
)
"This is the first demonstration in the rat myocardium that 3-NP induces pharmacological preconditioning, thereby limiting infarct size, and that this effect is associated with increased NO bioavailability and reduced peroxynitrite formation due to inhibition of superoxide formation by XO and NADH oxidase."( The role of peroxynitrite in chemical preconditioning with 3-nitropropionic acid in rat hearts.
Bencsik, P; Cakici, I; Csonka, C; Csont, T; Ferdinandy, P; Fodor, G; Giricz, Z; Gyöngyösi, M; Turan, N, 2006
)
" We suggest that potassium depletion and hyperuricemia in rats exacerbates endothelial dysfunction and lowers the bioavailability of nitric oxide, which blocks insulin activity and causes insulin resistance during thiazide usage."( Thiazide diuretics exacerbate fructose-induced metabolic syndrome.
Johnson, RJ; Mu, W; Nakagawa, T; Reungjui, S; Roncal, CA; Sirivongs, D; Srinivas, TR, 2007
)
" Since it is inactivated by xanthine oxidase (XO), concurrent intake of substances containing XO may potentially reduce bioavailability of mercaptopurine."( Interaction between mercaptopurine and milk.
de Lemos, ML; Hamata, L; Jennings, S; Leduc, T, 2007
)
"In cirrhotic livers, decreased nitric oxide (NO) bioavailability is a major factor increasing intrahepatic vascular tone."( Increased oxidative stress in cirrhotic rat livers: A potential mechanism contributing to reduced nitric oxide bioavailability.
Bosch, J; Fernández, M; García-Calderó, H; García-Pagán, JC; Gracia-Sancho, J; Laviña, B; Rodríguez-Vilarrupla, A, 2008
)
"Our data show that oxidative stress may contribute to reduced NO bioavailability in cirrhotic livers, supporting the evaluation of O(2) (-) reduction as a potential mechanism to restore NO content."( Increased oxidative stress in cirrhotic rat livers: A potential mechanism contributing to reduced nitric oxide bioavailability.
Bosch, J; Fernández, M; García-Calderó, H; García-Pagán, JC; Gracia-Sancho, J; Laviña, B; Rodríguez-Vilarrupla, A, 2008
)
" Animal studies suggest that (single-dose) allopurinol (xanthine oxidase inhibitor with high oral bioavailability and long-lasting active metabolites) may reduce this risk; human study results are conflicting."( Allopurinol to prevent pancreatitis after endoscopic retrograde cholangiopancreatography: a randomized placebo-controlled trial.
Bain, VG; Bass, S; Cole, M; Fedorak, RN; Hilsden, R; Love, J; May, G; McKaigney, J; Romagnuolo, J; Sandha, GS, 2008
)
" Diminished antioxidant capacity increases vascular superoxide levels, which reduce NO bioavailability and promote peroxynitrite generation."( Vascular oxidative stress and nitric oxide depletion in HIV-1 transgenic rats are reversed by glutathione restoration.
Dikalov, S; Guidot, DM; Hart, CM; Jones, DP; Kleinhenz, DJ; Kline, ER; Liang, B; Sutliff, RL, 2008
)
" Bioavailability of thiopurines may be competitively inhibited by dietary purines."( Influence of xanthine oxidase on thiopurine metabolism in Crohn's disease.
Ansari, A; Aslam, Z; De Sica, A; Duley, J; Fairbanks, L; Gilshenan, K; Marinaki, A; Sanderson, J; Smith, M, 2008
)
" Thus, ET-1 may augment its vasoconstrictive effects through the formation of superoxide, which may impair the bioavailability of nitric oxide in the retinal microvasculature."( Involvement of NADPH oxidase and protein kinase C in endothelin-1-induced superoxide production in retinal microvessels.
Ikeda, T; Kanbara, Y; Kobayashi, T; Matsuo, J; Oku, H; Sugiyama, T, 2009
)
"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
)
"Endothelial dysfunction and impaired nitric oxide bioavailability have been implicated in the pathogenesis of sickle cell anemia."( Sickle cell anemia and vascular dysfunction: the nitric oxide connection.
Akinsheye, I; Klings, ES, 2010
)
"An abnormal production of reactive oxygen species (ROS) and the subsequent decrease in vascular bioavailability of nitric oxide (NO) have long been proposed to be the common pathogenetic mechanism of the endothelial dysfunction, resulting from diverse cardiovascular risk factors such as hypercholesterolaemia, diabetes mellitus, chronic smoking, metabolic syndrome, and hypertension."( Is oxidative stress a therapeutic target in cardiovascular disease?
Bruno, RM; Gori, T; Münzel, T; Taddei, S, 2010
)
" Reactive oxygen species (ROS) may directly alter vascular function or cause changes in vascular tone by several mechanisms including altered nitric oxide (NO) bioavailability or signaling."( Oxidative stress and endothelial dysfunction in hypertension.
Gori, T; Münzel, T; Schulz, E, 2011
)
" We evaluated the antihypertensive effects of sodium nitrite given in drinking water for 4 weeks in two-kidney one-clip (2K1C) hypertensive rats and the effects induced by nitrite on NO bioavailability and oxidative stress."( Sodium nitrite downregulates vascular NADPH oxidase and exerts antihypertensive effects in hypertension.
Amaral, JH; Ferreira, GC; Marçal, DM; Montenegro, MF; Pereira, RP; Pinheiro, LC; Reis, RI; Sakamoto, EK; Tanus-Santos, JE, 2011
)
"5 μmol/l, 24 h) of DES resulted in a marked reduction in endothelial NO• bioavailability determined by ESR (electron spin resonance), while 17β-oestradiol instead increased NO• production as expected."( Inhibition of XO or NOX attenuates diethylstilbestrol-induced endothelial nitric oxide deficiency without affecting its effects on LNCaP cell invasion and apoptosis.
Cai, H; Nguyen, A; Youn, JY, 2012
)
" Thus, in skeletal muscle arterioles, in the presence of ADMA, we investigated the dilator effect of an NO donor and increases in flow and aimed to elucidate the underlying mechanisms, including the role of oxidative stress, which is known to reduce the bioavailability of NO."( Asymmetric dimethylarginine reduces nitric oxide donor-mediated dilation of arterioles by activating the vascular renin-angiotensin system and reactive oxygen species.
Debreczeni, B; Hamar, J; Kaminski, PM; Koller, A; Veresh, Z; Wolin, MS, 2012
)
"We suggest that by activating the vascular renin-angiotensin-NAD(P)H oxidase pathway, ADMA elicits oxidative stress, which interferes with the bioavailability of NO and consequently reduces NO-mediated dilations."( Asymmetric dimethylarginine reduces nitric oxide donor-mediated dilation of arterioles by activating the vascular renin-angiotensin system and reactive oxygen species.
Debreczeni, B; Hamar, J; Kaminski, PM; Koller, A; Veresh, Z; Wolin, MS, 2012
)
"The unilateral, permanent femoral artery ligation model of hind-limb ischemia was performed in C57BL/6J wild-type and endothelial NO synthase-knockout mice to evaluate exogenous H(2)S effects on NO bioavailability and ischemic revascularization."( Hydrogen sulfide stimulates ischemic vascular remodeling through nitric oxide synthase and nitrite reduction activity regulating hypoxia-inducible factor-1α and vascular endothelial growth factor-dependent angiogenesis.
Bir, SC; Kevil, CG; Kolluru, GK; McCarthy, P; Pardue, S; Pattillo, CB; Shen, X, 2012
)
"These data demonstrate that H(2)S differentially regulates NO metabolism during chronic tissue ischemia, highlighting novel biochemical pathways to increase NO bioavailability for ischemic vascular remodeling."( Hydrogen sulfide stimulates ischemic vascular remodeling through nitric oxide synthase and nitrite reduction activity regulating hypoxia-inducible factor-1α and vascular endothelial growth factor-dependent angiogenesis.
Bir, SC; Kevil, CG; Kolluru, GK; McCarthy, P; Pardue, S; Pattillo, CB; Shen, X, 2012
)
" The bioavailability and efficacy of antioxidants in human corneal limbal epithelial (HCLE) cells were measured to determine whether antioxidants might be beneficial constituents of lubricant eye drops."( Bioavailability of antioxidants applied to stratified human corneal epithelial cells.
Koetje, LR; Mitchell, AK; Schotanus, MP; Stoddard, AR; Ubels, JL, 2013
)
" Taken together, the results demonstrated that the studied derivatives had optimal properties for bioavailability and oral absorption."( Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
Alba-Soto, CD; Briñón, MC; Gualdesi, MS; Novoa, MM; Raviolo, MA; Solana, ME, 2013
)
" Hydrophobic substitution such as isopropyl at 1-position of the indole moiety without any substitution at 2-position has an essential role for enhancing bioavailability and therefore for high in vivo efficacy."( Design and synthesis of novel 2-(indol-5-yl)thiazole derivatives as xanthine oxidase inhibitors.
Choi, SP; Jung, CK; Jung, SH; Kim, GT; Kim, TH; Lee, JY; Song, JU, 2015
)
" Of the many processes involved in the pathophysiology of hypertension, vascular damage due to oxidative stress (excess bioavailability of reactive oxygen species [ROS]) is particularly important."( Oxidative stress and human hypertension: vascular mechanisms, biomarkers, and novel therapies.
Briones, AM; Dulak-Lis, M; Harvey, A; Montezano, AC; Touyz, RM; Tsiropoulou, S, 2015
)
"The serum CUPRAC level increased after treatment with both concentrations, indicating that there was sufficient bioavailability of the extract which contributed to the total antioxidant capacity."( Lentinus squarrosulus (Mont.) mycelium enhanced antioxidant status in rat model.
Abdulla, MA; Abdullah, N; Abdullah, S; Kuppusamy, UR; Mhd Omar, NA; Sabaratnam, V, 2015
)
" Reductions in NO bioavailability (eNOS), lower anti-oxidant capacity (SOD-1) and higher pro-oxidant capacity (XO) may contribute to the deficits in NOS signaling in skeletal muscle resistance arteries."( Effects of High-LET Radiation Exposure and Hindlimb Unloading on Skeletal Muscle Resistance Artery Vasomotor Properties and Cancellous Bone Microarchitecture in Mice.
Alwood, JS; Behnke, BJ; Delp, MD; Ghosh, P; Globus, RK; Kilar, CR; Narayanan, A; Park, Y; Schreurs, AS; Shirazi-Fard, Y; Stabley, JN, 2016
)
" This study was undertaken to evaluate the pharmacokinetics and relative bioavailability of two brands of allopurinol tablets."( Pharmacokinetics and comparative bioavailability of allopurinol formulations in healthy subjects.
El-Bedaiwy, HM; Helmy, SA, 2014
)
" According to ADME (absorption, distribution, metabolism, and excretion) simulation in silico, flazin had good oral bioavailability in vivo."( Effect of Soy Sauce on Serum Uric Acid Levels in Hyperuricemic Rats and Identification of Flazin as a Potent Xanthine Oxidase Inhibitor.
Li, H; Lin, L; Su, G; Wang, Y; Zhao, M, 2016
)
"Studies have reported that flavonoids inhibit xanthine oxidase (XO) activity; however, poor solubility and stability in lipophilic media limit their bioavailability and applications."( Kinetic study on the inhibition of xanthine oxidase by acylated derivatives of flavonoids synthesised enzymatically.
Alberto, TG; Carvalho, PO; de Araújo, MEMB; Franco, YEM; Leme, CW; Messias, MCF; Sawaya, ACHF, 2017
)
" In the process of purine metabolism, reactive oxygen species, including superoxide, are generated concomitantly with uric acid production, which may deteriorate endothelial function through the reaction of superoxide with nitric oxide (NO), leading to decreased NO bioavailability and increased production of peroxynitrite, a reactive oxidant."( Hyperuricemia and endothelial function: From molecular background to clinical perspectives.
Higashi, Y; Hisatome, I; Kihara, Y; Maruhashi, T, 2018
)
" In this study, the hypothesis that inorganic nitrite attenuated lipopolysaccharide (LPS)-induced oxidative stress in mice and in macrophage cells by modulating NADPH oxidase activity and NO bioavailability were investigated."( NADPH oxidase is a primary target for antioxidant effects by inorganic nitrite in lipopolysaccharide-induced oxidative stress in mice and in macrophage cells.
Lu, N; Sui, Y; Tian, R, 2019
)
"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
)
" In this study, we used glucosyl hesperidin (GH), which has greater bioavailability than hesperidin, to clarify comprehensive mechanisms underlying the hypouricemic effects of hesperidin in vivo."( Comprehensive analysis of mechanism underlying hypouricemic effect of glucosyl hesperidin.
Harada-Shiba, M; Hirata, H; Ogura, M; Ota-Kontani, A; Tsuchiya, Y, 2020
)
" Dose-restricted tioguanine (thioguanine) could expand treatment options by reducing methylated metabolites, increasing the bioavailability of 6-tioguanine nucleotides and ameliorating thiopurine intolerance or resistance."( Review article: opportunities to improve and expand thiopurine therapy for autoimmune hepatitis.
Czaja, AJ, 2020
)
"The efficacy and safety of thiopurines in autoimmune hepatitis can be improved by investigational efforts that establish monitoring strategies that allow individualisation of dosage and prediction of outcome, increase bioavailability of the active metabolites and demonstrate superiority to alternative agents."( Review article: opportunities to improve and expand thiopurine therapy for autoimmune hepatitis.
Czaja, AJ, 2020
)
" However, BBR exhibits low bioavailability due to its extensive metabolism and limited absorption."( Berberrubine attenuates potassium oxonate- and hypoxanthine-induced hyperuricemia by regulating urate transporters and JAK2/STAT3 signaling pathway.
Chen, J; Huang, Z; Jiang, L; Li, Y; Lin, G; Lin, Z; Liu, Y; Mai, L; Su, Z; Xie, J; Xu, L; Yu, Q, 2021
)
" The bioavailability of Spartinin F2 was 63."( Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
Jiao, QC; Liu, J; Qin, P; Wang, B; Yang, YS; Zhou, KM, 2022
)

Dosage Studied

Allopurinol at higher dosage diminished the noradrenaline-induced decrease of heart rate and increase of blood pressure. Dose-response curves with and without allopur inol pretreatment showed an almost constant 0.5 mg/dl. Plasma oxipurinOL concentrations correlated directly with both alloparinol dosage and with renal glomerular function.

ExcerptReference
" It is concluded that allopurinol should be used only in select patients, and the dosage should be modified if renal disease exists."( Severe hypersensitivity reactions to allopurinol.
Lang, PG, 1979
)
" Preexisting renal disease was present in 97% of patients, and, in the majority of these, the dosage of allopurinol was not reduced despite instructions contained in the package insert for this drug."( The allopurinol hypersensitivity syndrome.
Lupton, GP; Odom, RB, 1979
)
" It is concluded that the arthralgia was often self-limiting, that aspirin had a small beneficial effect, that allopurinol, in the dosage studied, may have had a slightly deleterious effect, but that it would be worth studying larger dosages of allopurinol because the dosage studied did not affect the serum uric acid concentration."( Double blind controlled comparison of aspirin, allopurinol and placebo in the management of arthralgia during pyrazinamide administration.
Allan, WG; Fox, W; Girling, DJ; Horsfall, PA; Nunn, AJ; Plummer, J, 1979
)
"At the high dosage of 600 mg daily, the uric-acid reducing effect of allopurinol depends on the initial level of uric-acid concentration in the same manner as at the usual dosage of 300 mg daily, but is more marked at the entire hyperuricaemic concentration range of 65--71 mumol/l (11--12 mg/l)."( [Uric-acid reduction with high allopurinol dosages (author's transl)].
Loewer, H; Mertz, DP, 1979
)
" These results suggest a possible role for superoxide anion in the establishment of IFN-mediated antiviral effect, especially in the dose-response region in which the inverse relationship between the generation of the IFN-alpha-mediated antiviral state and CuZnSOD activity was observed."( The role of superoxide anions in the establishment of an interferon-alpha-mediated antiviral state.
Carlson, EJ; Epstein, CJ; Epstein, LB; Huang, TT, 1992
)
" Oral dosing of nilvadipine suppressed carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen."( Inhibition by nilvadipine of ischemic and carrageenan paw edema as well as of superoxide radical production from neutrophils and xanthine oxidase.
Oyanagui, Y; Sato, S, 1991
)
"The administration to rats of tryptophan (CAS 73-22-3) in high dosage causes a significant increase in pain threshold values."( Potentiation of the analgesic effects of tryptophan by allopurinol in rats.
Malvezzi, L; Pinelli, A; Trivulzio, S; Zecca, L, 1991
)
" The difference in dosage form may partly account for this difference, but the benzbromarone also seems to be involved."( Kinetics of allopurinol and its metabolite oxypurinol after oral administration of allopurinol alone or associated with benzbromarone in man. Simultaneous assay of hypoxanthine and xanthine by gas chromatography-mass spectrometry.
Bargnoux, H; Berger, JA; Bussiere, JL; Chabard, JL; Lartigue-Mattei, C; Petit, J; Ristori, JM, 1991
)
" The dramatic response of our patients to cyclophosphamide, which is known to inhibit cell-mediated cytotoxicity by inhibiting both the recognition and lethal hit stages, together with the rapid regrowth of the epidermis within 4 days to a week in patients who received adequate dosage of the drug, supports the preceding concepts."( Efficacy of cyclophosphamide in toxic epidermal necrolysis. Clinical and pathophysiologic aspects.
Allen, SG; Heng, MC, 1991
)
" This could be completely blocked by combination dosing with allopurinol, an inhibitor of xanthine oxidase."( Hyperuricemia induced by the uricosuric drug probenecid in rats.
Shinosaki, T; Yonetani, Y, 1991
)
"This study was performed to investigate the possible influence of repeated omeprazole dosing on the metabolism of caffeine, which has been shown to reflect the activity of one specific enzyme within the hepatic cytochrome P450 family, P450IA2."( Omeprazole treatment does not affect the metabolism of caffeine.
Andersson, T; Bergstrand, R; Cederberg, C; Eriksson, S; Lagerström, PO; Skånberg, I, 1991
)
" In 2 of the remaining 6 patients, the initial improvement disappeared during the course of treatment but control was regained by increasing the dosage of allopurinol."( Clinical effects of allopurinol on intractable epilepsy.
Arimoto, K; Matsuo, T; Morooka, K; Tada, H,
)
" Dosing with theophylline was used to produce 1MX as an intermediate metabolite in six healthy volunteers."( 1-Methylxanthine derived from theophylline as an in vivo biochemical probe of allopurinol effect.
Birkett, DJ; Day, RO; Miners, JO, 1991
)
"This study examined dosage prescribing patterns and steady-state oxipurinol plasma concentrations in 66 patients receiving chronic allopurinol therapy."( Dosage prescribing and plasma oxipurinol levels in patients receiving allopurinol therapy.
Boyle, RR; Francis, HW; Oliver, NW; Paterson, J; Peterson, GM; Taylor, GR; von Witt, RJ, 1990
)
" In other groups of rabbits, the effect of the same dosage of verapamil on the size of myocardial infarct after 20 or 30 min ischaemia and 72 h reperfusion was examined."( Does verapamil limit myocardial infarct size in a heart deficient in xanthine oxidase?
Adachi, T; Goto, M; Iimura, O; Iwamoto, T; Miura, T; Noto, T; Ogawa, T; Ooiwa, H; Tsuchida, A, 1990
)
" These corresponded to 600 or 900 mg/day of allopurinol for 60 days and benznidazole or nifurtimox at conventional dosage regimens."( Therapeutic efficacy of allopurinol in patients with chronic Chagas' disease.
Gallerano, RH; Marr, JJ; Sosa, RR, 1990
)
"After a brief review of the history of allopurinol therapy the mechanism of action, interactions with other drugs, side-effects, indications and contra-indications of Milurit (100 mg allopurinol per tab, EGIS Pharmaceuticals, Budapest) in adults and children, and the dosage of the drug have been discussed."( Milurit's place in therapy.
Gömör, B; Szebenyi, B, 1990
)
" Animals (donors and recipients) were pretreated with allopurinol given orally at a dosage of 50 mg/kg for 4 days."( Response to allopurinol pretreatment in a swine model of heart-lung transplantation.
Germann, E; Godin, DV; Jamieson, WR; Ko, KM; Lam, S; Qayumi, AK; Van den Broek, J, 1990
)
" The repeated dosing of allopurinol at higher doses (20 and 50 mg/kg) significantly retarded the elimination of DPH from the circulation and dramatically decreased the urinary excretion of p-hydroxyphenytoin (HPPH), a major metabolite of DPH."( Drug interaction between phenytoin and allopurinol.
Ito, Y; Iwaki, M; Ogiso, T; Tsunekawa, K, 1990
)
" Cisplatin was administered at a dosage of 100 mg/m2 iv bolus and 5-fluorouracil was continuously infused iv at a dosage of 1000 mg/m2/day for 4 days."( A phase II trial of cisplatin and 5-fluorouracil with allopurinol for recurrent or metastatic carcinoma of the uterine cervix: a Southwest Oncology Group trial.
Alberts, DS; Boutselis, JG; Green, S; Hannigan, EV; Surwit, EA; Wallace, DL; Weiss, GR, 1990
)
" In ensuing dose-response studies, the concentrations of lactobionate, glutahione, dexamethasone in UW solution proved to be optimal."( Rat liver preservation. I. The components of UW solution that are essential to its success.
Bitter-Suermann, H; Coddington, D; Yu, WM, 1990
)
" Increased OXY dosage (15 mg/kg) or allopurinol (40 mg/kg) had no greater effects."( Effects of xanthine oxidase inhibition on ischemic acute renal failure in the rat.
Gmur, DJ; Zager, RA, 1989
)
", throughout the experiment) reduced the incidence of reperfusion-induced ventricular fibrillation (VF), the dose-response characteristics describing an asymmetric U-shaped curve."( Reperfusion arrhythmias: dose-related protection by anti-free radical interventions.
Bernier, M; Hearse, DJ; Manning, AS, 1989
)
" The neutrophil dose-response curve for increase in XO paralleled closely the curve for neutrophil-mediated RPAEC cytotoxicity."( Xanthine oxidase activity in rat pulmonary artery endothelial cells and its alteration by activated neutrophils.
Gannon, DE; Phan, SH; Ryan, US; Varani, J; Ward, PA, 1989
)
" All rats were fed on a low-Fe diet for 3 d before dosing in order to standardize the Fe status of the intestinal mucosal cells."( Effects of dietary iron deficiency and tungsten supplementation on 59Fe absorption and gastric retention from 59Fe compounds in rats.
Ledward, DA; Neale, RJ; Shears, GE, 1989
)
" An ischemia control group received NS, whereas experimental groups were given Nx, SOD, APL, or DEF with the same previous dosage schedule."( Experimental pharmacologic cerebroprotection.
Donovan, DL; Fink, JA; Pigott, JP; Sharp, WV, 1988
)
" It was apparent that many patients were taking unnecessarily high daily doses of allopurinol and that renal status was not always considered when deciding dosage regimens of allopurinol."( Allopurinol dosage selection: relationships between dose and plasma oxipurinol and urate concentrations and urinary urate excretion.
Birkett, DJ; Day, RO; Hayes, J; Miners, JO; Naidoo, D; Savdie, E; Whitehead, A, 1988
)
" Studies of oral 6-MP indicate that, contrary to previous information, the bioavailability of this drug is relatively poor after oral administration, and that plasma 6-MP concentrations achieved after uniform oral dosing are highly variable."( The pharmacology of orally administered chemotherapy. A reappraisal.
Balis, FM; Poplack, DG; Zimm, S, 1986
)
" Allopurinol inhibits the metabolism of 6-mercaptopurine and azathioprine, which require dosage modifications."( Clinical pharmacokinetics of allopurinol.
Murrell, GA; Rapeport, WG,
)
" The animals were killed 5 min after dosing to minimize the conversion of alpha-tocopheryl acetate to alpha-tocopherol."( Comparison of the antioxidant properties of alpha-tocopherol and alpha-tocopheryl acetate in newborn rabbit lung.
Cook, J; Knight, M; Roberts, RJ; Wispe, J, 1987
)
" Plasma oxipurinol concentrations correlated directly with both allopurinol dosage and with renal glomerular function as reflected by the plasma creatinine concentration."( Plasma oxipurinol concentrations during allopurinol therapy.
Cross, M; Emmerson, BT; Gordon, RB; Thomson, DB, 1987
)
"Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms to humans and rabbits; however, it is not absorbed rectally from any of the dosage forms to any significant extent."( Allopurinol absorption from different sites of the rat gastrointestinal tract.
Kramer, WG; Patel, VS, 1986
)
" We stress the need to adapt the daily dosage of the drug to the glomerular filtration rate and to interrupt drug administration rapidly if allergic manifestations develop."( [Allopurinol toxicity. Apropos of 1 case].
Berthoux, F; Genin, C; Guérin, C; Leroy, G; Sabatier, JC; Toulon, J, 1986
)
" Monitoring of plasma oxipurinol levels (ideally less than 100 mumol/l) by high-pressure liquid chromatography is helpful for adjusting dosage in renal failure."( Allopurinol in renal failure and the tumour lysis syndrome.
Cameron, JS; Davies, PM; Morris, GS; Simmonds, HA, 1986
)
" No changes in pharmacokinetics were seen with repeated dosing in mice or with administration of the protective agent phenyl AIC."( CB 1954 revisited. I. Disposition kinetics and metabolism.
Talbot, K; White, RA; Workman, P, 1986
)
" 5-FU infusions with allopurinol as used in this regimen appear to offer no therapeutic advantage over a conventional dosing schedule."( Phase II trial of high-dose continuous infusion 5-fluorouracil with allopurinol modulation in colon cancer.
Ahmann, FR; Garewal, H; Greenberg, BR, 1986
)
" Each patient was allocated, according to his/her baseline values of serum uric acid or serum creatinine to four different sulphinpyrazone incremental dosage schedules."( Sulphinpyrazone dose schedule in hyperuricemic patients with cardiovascular diseases: tolerability assessment.
Bertoli, L; Borghi, C; Busnardo, I; Zagnoni, P, 1985
)
" We studied the dose-response effect of DDS (10-1 mM) on the generation of oxygen intermediates (OI:O2-, H2O2, OH."( Dissociation of the inhibitory effect of dapsone on the generation of oxygen intermediates--in comparison with that of colchicine and various scavengers.
Miyachi, Y; Niwa, Y; Sakane, T, 1984
)
" In rats dosed orally with 6- deoxyacyclovir , absorption was extensive and the major urinary metabolite was acyclovir."( 6-Deoxyacyclovir: a xanthine oxidase-activated prodrug of acyclovir.
Beauchamp, LM; de Miranda, P; Hall, WW; Krenitsky, TA; Schaeffer, HJ; Whiteman, PD, 1984
)
" at two dosage levels (2."( Effect of allopurinol on the pharmacokinetics of 6-mercaptopurine in rabbits.
Brown, DA; Day, JL; Schroeder, EC; Tterlikkis, L, 1983
)
" Although the uridine dosage (0."( Purine and pyrimidine metabolism in hereditary orotic aciduria: some unexpected effects of allopurinol.
Becroft, DM; Potter, CF; Simmonds, HA; Webster, DR, 1980
)
" Current use of rectal dosage forms as an adjunct in cancer chemotherapy should therefore be re-examined."( Allopurinol kinetics and bioavailability. Intravenous, oral and rectal administration.
Appelbaum, SJ; Dorr, RT; Mayersohn, M; Perrier, D, 1982
)
"The relative bioavailability of two commercial preparations of 100 mg and 300 mg allopurinol tablets was examined in two groups of 16 healthy human subjects, one for each dosage level."( The bioavailability of two commercial preparations of allopurinol tablets.
Kleinberg, SI; Marcus, M; Tse, FL, 1982
)
" Allopurinol at higher dosage diminished the noradrenaline-induced decrease of heart rate and increase of blood pressure."( [Effect of allopurinol on adrenergically induced changes in serum lipid levels, heart rate and blood pressure in normal and ischemic rabbits (author's transl)].
Förster, W; Lohse, M; Riedel, H; Sziegoleit, W, 1982
)
" Muscle relaxants do not cause measurable muscle relaxation following usual oral dosage regimens."( Effects of exercise performance on drugs used in musculoskeletal disorders.
Day, RO, 1981
)
" CAT, SOD, or both together, at a dosage of 5,000 U/kg each."( Oxygen radical scavengers are protective against indomethacin-induced intestinal ulceration in the rat.
Dinari, G; Fisher, S; Heckelman, B; Kiro, A; Marcus, H; Zahavi, I, 1995
)
" After obtaining dose-response curves to phenylephrine (PE) and carbachol or sodium nitroprusside (SNP), we exposed rings to the FR generating system or H2O2 for 30 min, either with or without a range of potentially protective agents."( Effects of a xanthine oxidase/hypoxanthine free radical and reactive oxygen species generating system on endothelial function in New Zealand white rabbit aortic rings.
Dowell, FJ; Hamilton, CA; McMurray, J; Reid, JL, 1993
)
" On the other hand, when normal lymphocytes were incubated with the xanthine-xanthine oxidase system (X-XO), a known superoxide anion generator, this elicited a dose-response positive angiogenic reaction in normal recipient mice."( Inhibition of lymphocyte-induced angiogenesis by free radical scavengers.
Davel, LE; de Lustig, ES; Monte, M, 1994
)
"To evaluate the appropriateness of allopurinol dosage according to renal function in patients at Dunedin and Wakari hospitals."( A survey of allopurinol dosage prescribing.
Egan, AJ; McClintock, AD; Pillans, PI; Woods, DJ, 1995
)
" Dosage prescribed was compared with established guidelines."( A survey of allopurinol dosage prescribing.
Egan, AJ; McClintock, AD; Pillans, PI; Woods, DJ, 1995
)
" Although information regarding the allopurinol hypersensitivity syndrome and individualised allopurinol dosage is available, it is evident that many practitioners remain unaware of the recommendations."( A survey of allopurinol dosage prescribing.
Egan, AJ; McClintock, AD; Pillans, PI; Woods, DJ, 1995
)
" On oral dosing of famciclovir to humans, only penciclovir and BRL 42359 can be detected consistently in the plasma; thus, attention was focused on the oxidation reaction."( Role of aldehyde oxidase in the in vitro conversion of famciclovir to penciclovir in human liver.
Chenery, RJ; Clarke, SE; Harrell, AW, 1995
)
" Animals (five per group) were dosed with OOS-TMP at 40 mg/kg and sacrificed on the 1st, 3rd or 7th day after treatment."( Enhanced levels of lipid peroxidation and xanthine oxidase activity in the lung of male Sprague-Dawley rats following treatment with O,O,S-trimethyl phosphorothioate.
Koizumi, A; Ohtaka, K,
)
"To perform and evaluate an educational intervention program aimed at improving the dosage prescribing of allopurinol by general practitioners and based on the application of academic detailing."( Educational program to improve the dosage prescribing of allopurinol.
Peterson, GM; Sugden, JE, 1995
)
" The area under the concentration time curve (aucH) of BOF-4272 was proportional to the dosing amount, and the mean transit time was constant from 62."( Local disposition of a new xanthine oxidase/xanthine dehydrogenase inhibitor, BOF-4272, in rat liver.
Naito, S; Nakagawa, T; Nishimura, M; Yamaoka, K; Yasui, H, 1994
)
" Allopurinol is more frequently used than uricosuric agents such as probenecid, and toxicity may be largely avoided by tailoring dosage schedules according to renal function."( Risks and benefits of drugs used in the management and prevention of gout.
Conaghan, PG; Day, RO, 1994
)
" This study investigates in a canine model of single-lung allotransplantation whether cardiopulmonary bypass adversely affects early graft function and whether a heparin-coated cardiopulmonary bypass circuit with reduced systemic heparin dosage improves results compared with standard uncoated cardiopulmonary bypass systems."( Deleterious effects of cardiopulmonary bypass on early graft function after single lung allotransplantation: evaluation of a heparin-coated bypass circuit.
Aeba, R; Francalancia, NA; Griffith, BP; Marrone, GC; Yousem, SA,
)
" The vessels were resuspended in Krebs buffer and cumulative dose-response curves to norepinephrine reevaluated."( Effects of reactive oxygen metabolites on norepinephrine-induced vasoconstriction.
Benoit, JN; Gao, H; Korthuis, RJ, 1994
)
" Allopurinol dosage was 150 mg daily for children weighing < 20 kg and 300 mg daily for other patients."( Allopurinol as add-on therapy in refractory epilepsy: a double-blind placebo-controlled randomized study.
Bianchi, A; Canger, R; Cornaggia, C; D'Alessandro, P; DeMarco, P; Gianelli, M; Pisani, F; Verzé, L; Zagnoni, PG; Zolo, P,
)
" However, plasma UN and creatinine levels decreased inversely with the dose of 4APP when a different dosage of 4APP was administered together with adenine."( Nephrotoxicity induced by a single dose of adenine: effects of 4-aminopyrazolo[3,4-d]pyrimidine and allopurinol.
Ichii, M; Kadota, E; Minami, T; Nakagawa, H; Okazaki, Y, 1994
)
" Unfortunately a bell-shaped dose-response curve has been observed, whereby SOD at higher concentrations loses its effectiveness and may even enhance the extent of reperfusion injury."( Superoxide dismutase (SOD)-catalase conjugates. Role of hydrogen peroxide and the Fenton reaction in SOD toxicity.
Lopaschuk, GD; Mao, GD; Poznansky, MJ; Thomas, PD, 1993
)
" The following information, when available, was analyzed: (1) patient data (age, gender, medical history), (2) treatment data (daily dosage of allopurinol, duration of treatment, indications, concomitant medications, and (3) adverse-event data."( Allopurinol hypersensitivity syndrome: a review.
Arellano, F; Sacristán, JA, 1993
)
" We present the case of a 72 year-old woman with erythema multiforme, liver and renal failure due to a unknown dosage of allopurinol self-medication for two weeks."( [Hypersensitivity syndrome caused by allopurinol. A case of massive hepatic necrosis].
González, U; Kershenovich, J; Orozco-Topete, RL; Reyes, E,
)
"It is widely recommended that, during concurrent therapy with allopurinol, the azathioprine dosage should be decreased by at least two thirds."( Myelosuppression associated with azathioprine-allopurinol interaction after heart and lung transplantation.
Banner, N; Cummins, D; Halil, O; Sekar, M, 1996
)
"The stability of drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied."( Stability of acetazolamide, allopurinol, azathioprine, clonazepam, and flucytosine in extemporaneously compounded oral liquids.
Allen, LV; Erickson, MA, 1996
)
" The dosage was titrated to 200 mg/d over the following 2 weeks."( Azathioprine and allopurinol: the price of an avoidable drug interaction.
Hayney, MS; Kennedy, DT; Lake, KD, 1996
)
" However, Pt was detected in the cerebral cortex of mice pretreated with either a low dosage of allopurinol or heat-denatured catalase."( Free radical scavengers suppress the accumulation of platinum in the cerebral cortex.
Ichii, M; Kawaki, H; Minami, T; Okazaki, J; Okazaki, Y,
)
" In renal insufficiency, the drug must be used cautiously and in reduced dosage because increased serum concentration of oxipurinol, active metabolite of allopurinol, may induce severe side effect."( [Metabolic disorder of purine nucleotide in patients with renal disease].
Hosoya, T; Ichida, K; Ohno, I; Sakai, O, 1996
)
" In the group composed of patients with normal kidney function (CCr > or = 80 ml/min), increase in the dosage of allopurinol was associated with a linear increase in the serum concentration of oxipurinol."( [A study of serum oxipurinol concentration and renal function in patients administered allopurinol].
Saji, M, 1996
)
" To clarify the actions of SAM during different stages of ischemia/ reperfusion, we have compared its benefit in five dosage regimens, using perfused rat livers after sequential periods of 24 hr cold and 20 min rewarming ischemia."( Treatment of experimental ischemia/reperfusion injury with S-adenyosylmethionine: evidence that donor pretreatment complements other regimens.
Dunne, JB; Piratvisuth, T; Tredger, JM; Williams, R, 1997
)
" orally in divided dosage for 30 days."( Combination therapy in Kala-azar.
Jha, S; Jha, TK; Singh, IJ; Singh, NK, 1995
)
"In the first part of the study, allopurinol was administered IV at a dosage of 10 mg/kg of body weight to 3 dogs and 5 mg/kg to 3 dogs; the sequence was then reversed."( Bioavailability and pharmacokinetics of intravenously and orally administered allopurinol in healthy beagles.
Bartges, JW; Bird, KA; Chen, M; Felice, LJ; Koehler, LA; Osborne, CA; Sawchuk, RJ; Ulrich, LK, 1997
)
" They were fed the diets containing 100 or 200 ppm ACA for 5 weeks, starting 1 week before the first dosing of AOM."( A xanthine oxidase inhibitor 1'-acetoxychavicol acetate inhibits azoxymethane-induced colonic aberrant crypt foci in rats.
Hara, A; Kawabata, K; Kawamori, T; Koshimizu, K; Makita, H; Mori, H; Murakami, A; Ohigashi, H; Satoh, K; Tanaka, T, 1997
)
" Although up to approximately 15% of the EHS matrix proteins were released into the supernatant in a ROS dose-response relationship, the residual insoluble matrix was partially cross-linked by ROS."( Reactive oxygen species cause direct damage of Engelbreth-Holm-Swarm matrix.
Kerjaschki, D; Riedle, B, 1997
)
" Preincubation with the antithyroid drug methimazole, at concentrations ranging from 0-25 microM, prevented superoxide-induced fibroblast proliferation in a dose-response pattern."( Superoxide radical production stimulates retroocular fibroblast proliferation in Graves' ophthalmopathy.
Bahn, RS; Barnes, S; Burch, HB; Lahiri, S, 1997
)
" Moreover, the assessment of cellular functions in parasites treated with increasing concentrations of drugs certified the capacity of these techniques to establish dose-response curves and to permit the detection of side effects."( Leishmania infantum promastigotes: flow cytometry as a possible tool for assessing the effects of drugs on cellular functions.
Azas, N; Delmas, F; Di Giorgio, C; Gasquet, M; Timon-David, P, 1997
)
" They were fed diet containing 100 or 500 ppm ACA for 4 weeks, starting one week before the first dosing of AOM (the initiation feeding)."( Chemoprevention of azoxymethane-induced rat colon carcinogenesis by a xanthine oxidase inhibitor, 1'-acetoxychavicol acetate.
Hara, A; Kakumoto, M; Kawabata, K; Koshimizu, K; Makita, H; Matsunaga, K; Mori, H; Murakami, A; Ohigashi, H; Satoh, K; Tanaka, T, 1997
)
"To study the effect of a safe dosage of allopurinol on ischemia-reperfusion damage following aortic surgery, 24 patients undergoing either elective or acute aortic reconstruction, were randomized to receive allopurinol or placebo, yielding four groups: elective/placebo (EP), elective/allopurinol (EA), acute/placebo (AP) and acute/allopurinol (AA)."( Allopurinol dosage and effect on ischemia-reperfusion damage in elective and acute aortic surgery.
Berger, HM; Camps, J; Dulfer, FT; Hermans, J; Kievit, J; Smeets, HJ; Van Bockel, JH; van Milligen de Wit, AW,
)
"A dosage of 300 mg/d of allopurinol was not effective in reducing pain or improving activities of daily living in chronic pancreatitis."( Does allopurinol reduce pain of chronic pancreatitis?
Banks, PA; Ferrante, M; Hughes, M; Noordhoek, EC; Ramagopal, V; Slivka, A, 1997
)
" A daily dosage of 300 mg allopurinol was given over a period of 4-7 months as single drug therapy."( [Allopurinol in treatment of cutaneous sarcoidosis].
Karrer, S; Landthaler, M; Pfau, A; Stolz, W; Szeimies, RM, 1998
)
" The same dosage of caffeine was given to 10 premenopausal white women during the midfollicular and midluteal phases of three complete menstrual cycles."( Quantitation of three-month intraindividual variability and influence of sex and menstrual cycle phase on CYP1A2, N-acetyltransferase-2, and xanthine oxidase activity determined with caffeine phenotyping.
Bertino, JS; Gotschall, R; James, AW; Kashuba, AD; Kearns, GL; Leeder, JS; Nafziger, AN, 1998
)
" As there is no way to identify the risk group of patients or to make effective treatment for AHS, the only means of minimizing the incidence of AHS is to limit the allopurinol therapy to accepted indications and to adjust the dosage for the patient's renal function."( Allopurinol hypersensitivity syndrome.
Lee, SS; Lin, HY; Tsai, YY; Wang, SR, 1994
)
" Allopurinol was used at a dosage of 10 mg/kg/day PO to treat 10 dogs naturally infected with Leishmania infantum for a period of 2-24 months."( Clinical, serologic, and parasitologic follow-up after long-term allopurinol therapy of dogs naturally infected with Leishmania infantum.
Arnold, P; Cavaliero, T; Deplazes, P; Glaus, T; Hofmann-Lehmann, R; Mathis, A,
)
" Four of these individuals were additionally dosed with 200 mg allopurinol intravenously."( Pharmacokinetics and pharmacodynamics of allopurinol in elderly and young subjects.
Krivanek, P; Oberbauer, R; Turnheim, K, 1999
)
"Allopurinol was formulated into injectable and suppository dosage forms."( Formulation development of allopurinol suppositories and injectables.
Lee, DK; Wang, DP, 1999
)
" The addition of superoxide dismutase (SOD), 100 U/ml produced a shift to the left in the antiaggregant dose-response curve for XOR."( Inhibition of platelet aggregation with glyceryl trinitrate and xanthine oxidoreductase.
Benjamin, N; Blake, D; Millar, T; O'Byrne, S; Shirodaria, C; Stevens, C, 2000
)
" Stone prevention is based on drug withdrawal or change in dosage with additional measures including an increase of diuresis and, if necessary, changes in the urine pH."( [Drug-induced urinary calculi in 1999].
Daudon, M, 1999
)
" In addition, TEI-6720 and allopurinol showed similar dose-response curves for the decrease in uric acid or allantoin concentration, and the associated increase in xanthine concentration, indicating that TEI-6720 and allopurinol have similar pharmacological characteristics although the dosage required differs."( A comparative study on the hypouricemic activity and potency in renal xanthine calculus formation of two xanthine oxidase/xanthine dehydrogenase inhibitors: TEI-6720 and allopurinol in rats.
Horiuchi, H; Kaneko, H; Kasahara, Y; Kobayashi, M; Komoriya, K; Kondo, S; Nishimura, S; Ota, M, 1999
)
" Allopurinol dosing guidelines and a therapeutic range for plasma oxypurinol levels have been published."( The optimal use of allopurinol: an audit of allopurinol use in South Auckland.
Gow, P; Raill, B; Sharples, K; Stamp, L, 2000
)
"We aimed to determine the appropriateness of allopurinol dosing according to current guidelines and to assess the relationship between plasma creatinine, oxypurinol and urate."( The optimal use of allopurinol: an audit of allopurinol use in South Auckland.
Gow, P; Raill, B; Sharples, K; Stamp, L, 2000
)
"There is poor adherence to the current recommended dosing guidelines for allopurinol."( The optimal use of allopurinol: an audit of allopurinol use in South Auckland.
Gow, P; Raill, B; Sharples, K; Stamp, L, 2000
)
"The pharmaceutical utility of the allopurinol gel (APNgel) which consists of allopurinol (APN), carrageenan (kappa-CG or iota-CG) and polyethylene (oxide) (Alkox) was investigated as a possible material for an oral dosage preparation for ease in handling and/or swallowing."( [Development of patient-friendly preparations(II): Preparation and characterization of carrageenan gel containing polyethylene (oxide)].
Hanawa, K; Hanawa, T; Ito, A; Kasai, I; Kawata, K; Mohri, K; Nakajima, S; Suzuki, M; Tsuchiya, T, 2000
)
" After drug-induced hepatitis, a caffeine test might be used to check the total recovery or to choose an adapted dosage of medicines."( Caffeine metabolism differences in acute hepatitis of viral and drug origin.
Bechtel, PR; Bechtel, YC; Brientini, MP; David-Laroche, M; Lelouët, H; Miguet, JP; Paintaud, G,
)
" Twenty-eight patients completed the desensitization procedure to a target allopurinol dosage of 50-100 mg/day, 21 without deviation from the protocol for a mean of 30."( Efficacy and safety of desensitization to allopurinol following cutaneous reactions.
Dunne, SM; Fam, AG; Iazzetta, J; Paton, TW, 2001
)
" Although pruritic skin eruptions may recur both during and after desensitization, most of these cutaneous reactions can be managed by temporary withdrawal of allopurinol and dosage adjustment."( Efficacy and safety of desensitization to allopurinol following cutaneous reactions.
Dunne, SM; Fam, AG; Iazzetta, J; Paton, TW, 2001
)
"A randomized clinical trial of low dosage combination of pentamidine and allopurinol was carried out with objectives to assess the efficacy and toxicity as compared to full dosage of pentamidine in antimony unresponsive visceral leishmaniasis (VL) patients."( A randomized clinical trial of low dosage combination of pentamidine and allopurinol in the treatment of antimony unresponsive cases of visceral leishmaniasis.
Das, VN; Gupta, AK; Kar, SK; Lal, CS; Ranjan, A; Siddiqui, NA; Sinha, AN; Verma, N, 2001
)
" After constricting the vessels with phenylephrine, an acetylcholine dose-response curve was obtained while monitoring changes in diameter by videomicroscopy."( Perivascular superoxide anion contributes to impairment of endothelium-dependent relaxation: role of gp91(phox).
Carretero, OA; Garvin, JL; Li, XC; Pagano, PJ; Rey, FE, 2002
)
" The dose-response effects of HA on the viability of normal cultures were identified."( The effect of hyaluronan on CD44-mediated survival of normal and hydroxyl radical-damaged chondrocytes.
Abatangelo, G; Brun, P; Cortivo, R; Daga Gordini, D; Panfilo, S, 2003
)
" Dogs of group 1 were treated by use of meglumine antimonate (100 mg/kg, SC, q 24 h) administered concurrently with allopurinol (15 mg/kg, PO, q 12 h) for 20 days and then with allopurinol alone at the same dosage for the subsequent 30 days."( Serum concentrations of acute-phase proteins in dogs with leishmaniosis during short-term treatment.
Bernal, LJ; Cerón, JJ; Martínez-Subiela, S, 2003
)
" The presence of lipoperoxides in the guinea pig cochleae exposed to noise-induced oxidative stress was determined by means of the dosage of malondialdhyde, evaluated by measuring the content of thiobarbituric acid reactive substances in perilymph samples."( Effect of superoxide dismutase and allopurinol on impulse noise-exposed guinea pigs--electrophysiological and biochemical study.
Attanasio, G; Barbara, M; Cassandro, E; Filipo, R; Mondola, P; Sequino, L, 2003
)
"Stomatitis is a harmful side effect induced by high and/or multiple dosing of cytotoxic drugs such as 5-fluorouracil."( Development of patient-friendly preparations: preparation of a new allopurinol mouthwash containing polyethylene(oxide) and carrageenan.
Hanawa, T; Kawata, K; Masuda, N; Mohri, K; Nakajima, S; Suzuki, M, 2004
)
" No statistically significant difference was observed in the activity of the three enzymes between those at baseline, and on day 1 after dosing with TJ-29 or placebo."( The in-vivo effect of bakumondo-to (TJ-29), a traditional Japanese medicine used for treatment of chronic airway disease, on cytochrome P450 1A2, xanthine oxidase and N-acetyltransferase 2 activity in man.
Higa, Y; Hisaeda, S; Ishizaki, T; Nakagawa, K; Saruwatari, J; Tomiyasu, Y, 2004
)
" A single oral dosing of Y-700 (5, 20 or 80 mg) to volunteers caused a dose-dependent reduction of serum uric acid levels indicating close relationship to plasma concentrations of the compound."( Pharmacokinetics/pharmacodynamics of Y-700, a novel xanthine oxidase inhibitor, in rats and man.
Fukunari, A; Iwane, J; Kamezawa, M; Mori, H; Osajima, T; Yamada, I, 2004
)
" Gout flares occurred with similar frequency in the placebo (37%) and 40-mg febuxostat (35%) groups and with increased frequency in the higher dosage febuxostat groups (43% taking 80 mg; 55% taking 120 mg)."( Febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase: a twenty-eight-day, multicenter, phase II, randomized, double-blind, placebo-controlled, dose-response clinical trial examining safety and efficacy in patients with gout.
Becker, MA; Eustace, D; Joseph-Ridge, N; MacDonald, PA; Palo, WA; Schumacher, HR; Vernillet, L; Wortmann, RL, 2005
)
"This investigation involved the evaluation of the effect of hexacosanol (HC, ceryl alcohol), a new hydrophobic wax modifier (WM) in comparison with conventional modifiers, on the development of sustained-release allopurinol (AP) solid lipospheres (SLS) intended for use in a suspension formulation and other oral dosage forms."( Effect of hexacosanol on the characteristics of novel sustained-release allopurinol solid lipospheres (SLS): factorial design application and product evaluation.
Abdel-Ghaffar, SK; El-Gibaly, I, 2005
)
" These indicators were developed to assess: (i) dosing in renal impairment; (ii) concomitant use with azathioprine or 6-mercaptopurine; and (iii) use in the treatment of asymptomatic hyperuricaemia."( Suboptimal physician adherence to quality indicators for the management of gout and asymptomatic hyperuricaemia: results from the UK General Practice Research Database (GPRD).
Bilker, WB; Farrar, JT; Fernandes, S; Mikuls, TR; Saag, KG, 2005
)
"Approved dosage regimens for prescription drug products are developed with a view to obtaining a favourable therapeutic index in the overall exposed population."( Appropriate dosing regimen of allopurinol in Japanese patients.
Gunji, T; Kawato, N; Kotake, T; Nakai, M; Okada, H; Saito, M; Shibakawa, M; Takada, M, 2005
)
" Prescription information, including mean dose and the distribution of doses, was extracted for each hospital and the data compared with the dosage recommended in the approved labelling for the product."( Appropriate dosing regimen of allopurinol in Japanese patients.
Gunji, T; Kawato, N; Kotake, T; Nakai, M; Okada, H; Saito, M; Shibakawa, M; Takada, M, 2005
)
"7 mg/day, was lower than the approved dosage of 200-300 mg/day."( Appropriate dosing regimen of allopurinol in Japanese patients.
Gunji, T; Kawato, N; Kotake, T; Nakai, M; Okada, H; Saito, M; Shibakawa, M; Takada, M, 2005
)
"Dose of 100-300 mg/day was an effective and commonly used dosing regimen for allopurinol in Japanese patients."( Appropriate dosing regimen of allopurinol in Japanese patients.
Gunji, T; Kawato, N; Kotake, T; Nakai, M; Okada, H; Saito, M; Shibakawa, M; Takada, M, 2005
)
"To minimize serious DHS, proper indications for treatment and dosage adjustment should be closely observed when starting allopurinol therapy in patients with chronic kidney disease."( Hypersensitivity syndrome and pure red cell aplasia following allopurinol therapy in a patient with chronic kidney disease.
Chao, SC; Lee, JY; Yang, CC, 2005
)
"Data from a cohort database of 484 gouty patients were used to calculate estimated allopurinol doses using CrCl and estimation of the clearance of creatinine using the equation of Cockroft and Gault (CrCl-CG) if, as a hypothesis, a dosage of 300 mg/d would be prescribed in any patient with Pcr <2."( Correction of allopurinol dosing should be based on clearance of creatinine, but not plasma creatinine levels: another insight to allopurinol-related toxicity.
Hernando, I; Nolla, JM; Perez-Ruiz, F; Villar, I, 2005
)
" Animals in Groups V and VI were treated exactly the same as those in Groups III and IV, respectively except that they were pretreated with oral GE for 5 days at a dosage of 5 ml/kg."( Protective role of natural antioxidant supplementation on testicular tissue after testicular torsion and detorsion.
Avci, A; Cimentepe, E; Derya Balbay, M; Durak, I; Eroglu, M; Guven, C; Unsal, A, 2006
)
"Allopurinol dosage reduction is recommended in patients with renal dysfunction because drug toxicity risk is increased."( Frequency of serum creatinine monitoring during allopurinol therapy in ambulatory patients.
Chan, KA; Feldstein, AC; Gunter, MJ; Harrold, L; Lafata, JE; McClure, DL; Nelson, WW; Platt, R; Raebel, MA; Simon, SR, 2006
)
" Lack of monitoring and lack of subsequent possible dosage adjustment put patients at increased risk of allopurinol toxicity."( Frequency of serum creatinine monitoring during allopurinol therapy in ambulatory patients.
Chan, KA; Feldstein, AC; Gunter, MJ; Harrold, L; Lafata, JE; McClure, DL; Nelson, WW; Platt, R; Raebel, MA; Simon, SR, 2006
)
" Quality control samples were prepared in control serum from individuals not dosed with the xanthine oxidase inhibitor."( Quantification of uric acid, xanthine and hypoxanthine in human serum by HPLC for pharmacodynamic studies.
Cooper, N; Erdmann, C; Fiene, J; Khosravan, R; Lee, JW, 2006
)
" To develop rational dosing schemes for future studies, knowledge of the pharmacokinetics in this patient group is essential."( Population pharmacokinetics of allopurinol in full-term neonates with perinatal asphyxia.
Benders, MJ; Groenendaal, F; Rademaker, CM; van Bel, F; van Kesteren, C; Ververs, FF, 2006
)
" We investigated whether such dosing provides adequate control of hyperuricemia."( Dose adjustment of allopurinol according to creatinine clearance does not provide adequate control of hyperuricemia in patients with gout.
Dalbeth, N; Gow, P; Kumar, S; Stamp, L, 2006
)
"9% were taking recommended doses, based on published allopurinol dosing guidelines."( Dose adjustment of allopurinol according to creatinine clearance does not provide adequate control of hyperuricemia in patients with gout.
Dalbeth, N; Gow, P; Kumar, S; Stamp, L, 2006
)
"Adherence to published allopurinol dosing guidelines led to suboptimal control of hyperuricemia in this population of patients with gout."( Dose adjustment of allopurinol according to creatinine clearance does not provide adequate control of hyperuricemia in patients with gout.
Dalbeth, N; Gow, P; Kumar, S; Stamp, L, 2006
)
"88 mg/dL) for all doses and was dose linear for the 10-120 mg/day dosage range."( Pharmacokinetics, pharmacodynamics and safety of febuxostat, a non-purine selective inhibitor of xanthine oxidase, in a dose escalation study in healthy subjects.
Grabowski, BA; Joseph-Ridge, N; Khosravan, R; Vernillet, L; Wu, JT, 2006
)
" There appeared to be a linear pharmacokinetic and dose-response (percentage decrease in serum uric acid) relationship for febuxostat dosages within the 10-120 mg range."( Pharmacokinetics, pharmacodynamics and safety of febuxostat, a non-purine selective inhibitor of xanthine oxidase, in a dose escalation study in healthy subjects.
Grabowski, BA; Joseph-Ridge, N; Khosravan, R; Vernillet, L; Wu, JT, 2006
)
" Future studies involving different doses and the dose-response relationship could promise better results."( Neuroprotection by resveratrol against traumatic brain injury in rats.
Altinoz, E; Ates, O; Cayli, S; Gurses, I; Kocak, A; Sener, M; Yologlu, S; Yucel, N, 2007
)
" Allopurinal dosage should be reduced or discontinued if xanthine nephropathy is suspected."( Acute renal failure from xanthine nephropathy during management of acute leukemia.
Bakdash, S; Ellis, D; Krishnamurti, L; LaRosa, C; McMullen, L; Moritz, ML; Wu, HY, 2007
)
" This study aimed to establish its mechanism of action and to construct a dose-response curve for the effect of allopurinol."( High-dose allopurinol improves endothelial function by profoundly reducing vascular oxidative stress and not by lowering uric acid.
Belch, JJ; Carr, E; Davies, J; George, J; Struthers, A, 2006
)
"For the first time, we have shown that a steep dose-response relationship exists between allopurinol and its effect on endothelial function."( High-dose allopurinol improves endothelial function by profoundly reducing vascular oxidative stress and not by lowering uric acid.
Belch, JJ; Carr, E; Davies, J; George, J; Struthers, A, 2006
)
" The addition of allopurinol enabled a reduction in mean daily prednisone dosage from 17."( Effect of allopurinol on clinical outcomes in inflammatory bowel disease nonresponders to azathioprine or 6-mercaptopurine.
Cao, D; Friedman, S; Hanauer, SB; Hande, SA; Sparrow, MP, 2007
)
"Our results indicate that TJ-19 at the generally recommended dosage is unlikely to cause pharmacokinetic interaction with co-administered medications primarily dependent on the CYP1A2, CYP2D6, CYP3A, XO, and NAT2 pathways for elimination."( The effect of Shoseiryuto, a traditional Japanese medicine, on cytochrome P450s, N-acetyltransferase 2 and xanthine oxidase, in extensive or intermediate metabolizers of CYP2D6.
Fukushima, Y; Hisadome, M; Muramoto, Y; Nakagawa, K; Nakao, M; Saruwatari, J; Shoji, M; Yamano, N, 2007
)
" This article reviews the clinical efficacy, side effect profile, dosing and administration of rasburicase, an intravenous recombinant urate oxidase used in patients at risk of Tumour lysis syndrome due to a high tumour burden or where treatment is required."( Rasburicase in the prevention and treatment of tumour lysis syndrome.
Keady, S; Mayne, N; Thacker, M, 2008
)
" Aim of our study was to assess the effect of low dosage of recombinant urate oxidase on hyperuricemia in renal failure patients that already receiving allopurinol."( Is rasburicase an effective alternative to allopurinol for management of hyperuricemia in renal failure patients? A double blind-randomized study.
Cianci, R; De Angelis, S; De Lorenzo, A; Di Renzo, L; Giarrizzo, GF; Giordano, F; Naticchia, A; Noce, A; Splendiani, G; Tozzo, C,
)
" There is now sufficient evidence to justify dedicated studies to determine the clinical benefits, dosing and duration of XO inhibition before and after gastrointestinal surgery."( The potential role for xanthine oxidase inhibition in major intra-abdominal surgery.
Loveday, B; Mittal, A; Phillips, AR; Windsor, JA, 2008
)
" Venous blood samples were collected predose (at 0 hours) and 1, 2, 3, 4, 6, 8, 10 and 12 hours after dosage for determination of oxypurinol and/or probenecid concentrations."( Pharmacokinetic and pharmacodynamic interaction between allopurinol and probenecid in healthy subjects.
Day, RO; Graham, GG; McLachlan, AJ; Stocker, SL; Williams, KM, 2008
)
" Multiple factors contribute to refractory gout, and they often relate to delayed or insufficient dosing with allopurinol."( Refractory gout: what is it and what to do about it?
Fels, E; Sundy, JS, 2008
)
" Brandis is an important component of commonly dispensed traditional dosage forms."( Pharmacological basis for use of Pistacia integerrima leaves in hyperuricemia and gout.
Ahmad, NS; Farman, M; Hasan, A; Mian, KB; Najmi, MH, 2008
)
"The increased uptake of allopurinol 100 mg suggests greater adherence to dosing guidelines and that there is value in educational programmes to optimize drug usage."( Utilization of allopurinol in the Australian community.
Chung, Y; Day, RO; Graham, GG; Lu, CY; Mant, A, 2008
)
" The dosage of allopurinol in the D group was significantly lower than in the A and B groups."( [Usefulness of combination treatment using allopurinol and benzbromarone for gout and hyperuricemia accompanying renal dysfunction: kinetic analysis of oxypurinol].
Gomi, H; Hikita, M; Hosoya, T; Ichida, K; Ohno, I; Okabe, H; Saikawa, H; Uetake, D; Yamaguchi, Y, 2008
)
" Following multiple dosing with febuxostat, there were no statistically significant differences in the plasma or urinary pharmacokinetic or pharmacodynamic parameters between subjects aged 18 to 40 years and >or=65 years."( The effect of age and gender on pharmacokinetics, pharmacodynamics, and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase.
Joseph-Ridge, N; Khosravan, R; Kukulka, MJ; Vernillet, L; Wu, JT, 2008
)
"Any sampling interval at least 4 h after caffeine dosing is suitable for NAT2 and XO activity assessments."( Phenotyping of N-acetyltransferase type 2 and xanthine oxidase with caffeine: when should urine samples be collected?
Fuhr, U; Jetter, A; Kinzig, M; Rodamer, M; Sörgel, F; Tomalik-Scharte, D, 2009
)
" Limiting allopurinol dosing to < or = 300 mg/d suboptimally controls hyperuricemia and fails to adequately prevent hypersensitivity reactions."( A critical reappraisal of allopurinol dosing, safety, and efficacy for hyperuricemia in gout.
Chao, J; Terkeltaub, R, 2009
)
" After a 20-week 4-n-NP treatment orally at the dosage of 10 and 50 muM in the drinking water, phenylephrine- and potassium chloride-induced concentration-dependent responsiveness assessed by wire myograph were both significantly higher in aorta isolated from 4-n-NP-treated rats compared with control rats, but acetylcholine-induced vasorelaxation was similar between these two groups."( Effects of chronic 4-n-nonylphenol treatment on aortic vasoconstriction and vasorelaxation in rats.
Hsieh, CC; Hsieh, CY; Miaw, CL; Tseng, HC; Yang, YH; Yen, CH, 2009
)
" The allopurinol dosage must be adjusted to achieve therapeutic fetal allopurinol/oxypurinol concentrations."( Maternal allopurinol during fetal hypoxia lowers cord blood levels of the brain injury marker S-100B.
Baquero, H; Benders, MJ; Bos, AF; Buonocore, G; Derks, JB; Longini, M; Rademaker, CM; Torrance, HL; Van Bel, F; Van Den Berg, P; Venegas, M; Visser, GH, 2009
)
" The dosage schedule of these patients was recorded."( Drug dosage protocol for calcium oxalate stone.
Marickar, YM; Salim, A, 2009
)
" Shorter courses or smaller doses of rasburicase than those recommended may be effective in reducing hyperuricemia in some patients, but it is important to recognize that the alternative dosing still awaits validation."( Rasburicase for the prevention and treatment of hyperuricemia in tumor lysis syndrome.
Ajiboye, VO; Kennedy, LD, 2010
)
" Dosing was guided by measuring thiopurine methyltransferase (for UK patients) or thioguanine nucleotides and methyl-6MP (Australian patients)."( Low-dose azathioprine or mercaptopurine in combination with allopurinol can bypass many adverse drug reactions in patients with inflammatory bowel disease.
Ansari, A; Duley, JA; Florin, TH; O'Donohue, J; Patel, N; Sanderson, J, 2010
)
" The 1 mM dosage of homocysteine in staurosporine-differentiated RGC-5 cells also did not induce cell death above control levels, although 18 hr treatment of non-differentiated RGC-5 cells with 5 mM homocysteine decreased survival by 50%."( Sensitivity of staurosporine-induced differentiated RGC-5 cells to homocysteine.
Allen, JB; Bozard, BR; Dun, Y; Duplantier, J; Farooq, A; Ganapathy, PS; Ha, Y; Smith, SB, 2010
)
" Clinical trials found that 40 mg/d of febuxostat was noninferior to conventionally dosed allopurinol (300 mg/d) in the percentage of subjects achieving the primary end point of serum urate <6."( Febuxostat: a selective xanthine-oxidase/xanthine-dehydrogenase inhibitor for the management of hyperuricemia in adults with gout.
Ernst, ME; Fravel, MA, 2009
)
" New recommendations have been presented on appropriate dosing of colchicine for acute gout flares and potential toxicities of combining colchicine with medications such as clarithromycin."( Progress in the pharmacotherapy of gout.
Sundy, JS, 2010
)
" HaCaT cells treatment with a cocaine concentration of 2 mM for 24 h (as was chosen by dose-response experiments) markedly enhanced superoxide radicals and peroxides formation."( Cocaine induces oxidative damage to skin via xanthine oxidase and nitric oxide synthase.
Kohen, R; Numa, R; Portugal-Cohen, M; Yaka, R, 2010
)
" Dosage adjustment in mild-to-moderate renal insufficiency is unnecessary; however, data are lacking on the safety of febuxostat in patients with severe renal impairment."( Urate-lowering therapy for gout: focus on febuxostat.
Barrons, R; Love, BL; Snider, KM; Veverka, A, 2010
)
" The purpose of this study was to examine a simple method to evaluate whether optional variables are appropriate as factors to improve dosing algorithms."( Application of Akaike information criterion to evaluate warfarin dosing algorithm.
Ariyoshi, N; Harada, T; Imamaki, M; Ishii, I; Kitada, M; Kobayashi, Y; Miyazaki, M; Sato, Y; Shimura, H; Takahashi, K; Yamagata, S; Yokoyama, I, 2010
)
" Dosing algorithms were constructed by multivariate linear regression analyses and were evaluated by the Akaike Information Criterion (AIC)."( Application of Akaike information criterion to evaluate warfarin dosing algorithm.
Ariyoshi, N; Harada, T; Imamaki, M; Ishii, I; Kitada, M; Kobayashi, Y; Miyazaki, M; Sato, Y; Shimura, H; Takahashi, K; Yamagata, S; Yokoyama, I, 2010
)
" We evaluated the adequacy of these variables as factors to improve the dosing algorithm using the AIC."( Application of Akaike information criterion to evaluate warfarin dosing algorithm.
Ariyoshi, N; Harada, T; Imamaki, M; Ishii, I; Kitada, M; Kobayashi, Y; Miyazaki, M; Sato, Y; Shimura, H; Takahashi, K; Yamagata, S; Yokoyama, I, 2010
)
" To prevent severe bone marrow depletion, the dosage of azathioprine, an immunosupressant drug, was reduced by 50% to prevent interaction with allopurinol."( Gout in pediatric renal transplant recipients.
Goetschel, P; Laube, GF; Trück, J; von Vigier, RO, 2010
)
" All treatments at the same dosage (100 mmol/kg) were administered to the abdominal cavity of PO-induced hyperuricemic mice, and serum uric acid level was measured at 3 h after administration."( Phytochemicals from Acacia confusa heartwood extracts reduce serum uric acid levels in oxonate-induced mice: their potential use as xanthine oxidase inhibitors.
Chang, ST; Chen, CS; Hsu, CA; Huang, CC; Tung, YT; Yang, SC, 2010
)
" Furthermore, after reviewing allopurinol dosing and administration, it was found that 50 mg/kg is statistically the most effective dose in attenuating liver ischemia reperfusion injury."( Allopurinol and xanthine oxidase inhibition in liver ischemia reperfusion.
Anaya-Prado, R; Lopez-Neblina, F; Peglow, S; Toledo, AH; Toledo-Pereyra, LH, 2011
)
" The goals when treating gout are no different in these patients, but the choice and dosage of drugs may need to be modified."( Managing gout: how is it different in patients with chronic kidney disease?
El-Zawawy, H; Mandell, BF, 2010
)
" The effect of chronic aspirin and HCTZ dosing taken together upon the efficacy of chronic allopurinol therapy in patients with hyperuricaemia needs to be investigated."( Lack of effect of hydrochlorothiazide and low-dose aspirin on the renal clearance of urate and oxypurinol after a single dose of allopurinol in normal volunteers.
Day, RO; Graham, GG; Ng, DY; Stocker, SL; Williams, KM, 2011
)
" A dose-response relationship between serum uric acid and early decline in renal function has recently been demonstrated in patients with type-1 diabetes."( Serum uric acid as a new player in the development of diabetic nephropathy.
Hovind, P; Johnson, RJ; Parving, HH; Rossing, P, 2011
)
" Dosage of allopurinol prescription(s) and number of gout flares were determined from claims data."( Relationship between physician specialty and allopurinol prescribing patterns: a study of patients with gout in managed care settings.
Becker, LK; Dabbous, O; Hariri, A; Krishnan, E; Pandya, BJ; Riedel, AA; Swindle, JP, 2011
)
" Change in allopurinol dosage from initial to final dose was more frequent among patients prescribed by rheumatologists and nephrologists."( Relationship between physician specialty and allopurinol prescribing patterns: a study of patients with gout in managed care settings.
Becker, LK; Dabbous, O; Hariri, A; Krishnan, E; Pandya, BJ; Riedel, AA; Swindle, JP, 2011
)
" Data were analyzed using the dosage of allopurinol (mg/day) greater than the recommended dosage, as defined by the Hande criteria."( Using allopurinol above the dose based on creatinine clearance is effective and safe in patients with chronic gout, including those with renal impairment.
Barclay, ML; Chapman, PT; Frampton, C; James, J; O'Donnell, JL; Stamp, LK; Zhang, M, 2011
)
" All doses except the 250 mg daily dose were divided and dosing was twice daily."( Pharmacokinetic and pharmacodynamic interaction between allopurinol and probenecid in patients with gout.
Day, RO; Graham, GG; McLachlan, AJ; Stocker, SL; Williams, KM, 2011
)
" The recommended starting dosage is 40 mg orally once daily."( Febuxostat for treatment of chronic gout.
Gray, CL; Walters-Smith, NE, 2011
)
"A dose-response for canakinumab was not apparent with any of the four predefined dose-response models."( Canakinumab reduces the risk of acute gouty arthritis flares during initiation of allopurinol treatment: results of a double-blind, randomised study.
Arulmani, U; Balfour, A; De Meulemeester, M; Krammer, G; Lin, HY; Mysler, E; Rovensky, J; Sallstig, P; Schlesinger, N; So, A, 2011
)
" The better results of lowering serum uric acid and protecting against renal failure were at the dosage of Que between 10 and 20 mg/kg."( [Preventive and therapeutic effects of quercetin on hyperuricemia and renal injury in rats].
Fu, R; He, W; Yao, F; Zhang, R, 2011
)
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
"A multicenter study with randomized, placebo-controlled, double-blind, parallel, intergroup comparison was carried out to evaluate the dose-response relationship, efficacy, and safety of febuxostat in 202 patients with hyperuricemia (including patients with gout) in Japan."( Placebo-controlled double-blind dose-response study of the non-purine-selective xanthine oxidase inhibitor febuxostat (TMX-67) in patients with hyperuricemia (including gout patients) in japan: late phase 2 clinical study.
Fujimori, S; Hada, T; Hisashi, Y; Hosoya, T; Kamatani, N; Kenjiro, K; Kohri, K; Matsuzawa, Y; Nakamura, T; Naoyuki, K; Shin, F; Takanori, U; Tatsuo, H; Tetsuya, Y; Toshikazu, H; Toshitaka, N; Ueda, T; Yamamoto, T; Yamanaka, H; Yuji, M, 2011
)
" A statistically significant dose-response relationship was found."( Placebo-controlled double-blind dose-response study of the non-purine-selective xanthine oxidase inhibitor febuxostat (TMX-67) in patients with hyperuricemia (including gout patients) in japan: late phase 2 clinical study.
Fujimori, S; Hada, T; Hisashi, Y; Hosoya, T; Kamatani, N; Kenjiro, K; Kohri, K; Matsuzawa, Y; Nakamura, T; Naoyuki, K; Shin, F; Takanori, U; Tatsuo, H; Tetsuya, Y; Toshikazu, H; Toshitaka, N; Ueda, T; Yamamoto, T; Yamanaka, H; Yuji, M, 2011
)
"In a 52-week, multicenter, open-label trial, febuxostat was initially administered at 10 mg/d; then, the dosage was increased in a stepwise fashion to 40 mg/d."( Multicenter, open-label study of long-term administration of febuxostat (TMX-67) in Japanese patients with hyperuricemia including gout.
Fujimori, S; Hada, T; Hosoya, T; Kamatani, N; Kohri, K; Matsuzawa, Y; Nakamura, T; Ueda, T; Yamamoto, T; Yamanaka, H, 2011
)
" There was no marked difference between the 2 dosage groups in terms of the incidence of adverse events."( Multicenter, open-label study of long-term administration of febuxostat (TMX-67) in Japanese patients with hyperuricemia including gout.
Fujimori, S; Hada, T; Hosoya, T; Kamatani, N; Kohri, K; Matsuzawa, Y; Nakamura, T; Ueda, T; Yamamoto, T; Yamanaka, H, 2011
)
" Almost all gastroenterologists (97%) used weight-based dosing that was gradually escalated."( How are thiopurines used and monitored by Swedish gastroenterologists when treating patients with inflammatory bowel disease?
Andersson, P; Hindorf, U, 2011
)
"To study the prevalence of chronic kidney disease (CKD) and its impact on allopurinol dosing and uric acid control among patients with gout."( Chronic kidney disease in gout in a managed care setting.
Dabbous, O; Fuldeore, MJ; Krishnan, E; Pandya, BJ; Riedel, AA; Zarotsky, V, 2011
)
" During preservation, in the periods of zero, 12, 18 and 24 hours, were conducted evaluating the degree of mucosal injury and dosage of malondialdehyde acid (MDA)."( Effects of ischemic preconditioning associated to different preservation solutions in protecting the intestinal graft.
Abrahão, Mde S; Gonzalez, AM; Montero, EF; Neves, Jde S; Salzedas Netto, AA, 2011
)
" Twelve patients were under allopurinol dosage adjustment according to creatinine clearance."( Cutaneous adverse drug reactions to allopurinol: 10 year observational survey of the dermatology department--Cagliari University (Italy).
Aste, N; Atzori, L; Ferreli, C; Mantovani, L; Mulargia, M; Pau, M; Pinna, AL, 2012
)
" 13 adverse events occurred, including 6 specific to co-therapy (3 rash, 2 abnormal liver function tests, 1 dosing error)."( Optimising outcome on thiopurines in inflammatory bowel disease by co-prescription of allopurinol.
Anderson, SH; Blaker, P; Irving, PM; Marinaki, AM; Sanderson, JD; Smith, MA, 2012
)
" Dosing guidelines based on creatinine clearance have been proposed based on the recognition that dosages of ≥300 mg/day may be associated with AHS, particularly in patients with renal impairment."( Starting dose is a risk factor for allopurinol hypersensitivity syndrome: a proposed safe starting dose of allopurinol.
Dalbeth, N; Dockerty, JL; Drake, J; Frampton, C; Jones, PB; Stamp, LK; Taylor, WJ, 2012
)
" Allopurinol can be used for the prophylactic management of chronic hyperuricemia in patients with CKD, but the recommended decreased dosage may limit efficacy and serious hypersensitivity reactions may preclude its use."( Challenges associated with the management of gouty arthritis in patients with chronic kidney disease: a systematic review.
Curiel, RV; Guzman, NJ, 2012
)
" Exposure of BAECs (bovine aortic endothelial cells) to pharmacologically relevant dosage (12."( Inhibition of XO or NOX attenuates diethylstilbestrol-induced endothelial nitric oxide deficiency without affecting its effects on LNCaP cell invasion and apoptosis.
Cai, H; Nguyen, A; Youn, JY, 2012
)
" In the dose-response experiment, ACN accelerated the conversion of XD to XO, with a significant depletion of gastric GSH in a dose-related manner."( Acrylonitrile-induced gastric toxicity in rats: the role of xanthine oxidase.
Al-Abbasi, FA, 2012
)
"ULT prescription and dosing are key modifiable factors associated with achieving SU target."( Prescription and dosing of urate-lowering therapy, rather than patient behaviours, are the key modifiable factors associated with targeting serum urate in gout.
Dalbeth, N; Horne, A; House, ME; McQueen, FM; Petrie, KJ; Taylor, WJ, 2012
)
" No dose-response relationship was noted, except for NF-κB expression in normal tissue."( A randomized, placebo-controlled, preoperative trial of allopurinol in subjects with colorectal adenoma.
Argusti, A; Bandelloni, R; Benelli, R; Boccardo, S; Branchi, D; Coccia, G; Crosta, C; De Roberto, G; DeCensi, A; Gatteschi, B; Meroni, E; Michetti, P; Minetti, E; Mori, M; Munizzi, F; Puntoni, M; Salvi, S; Sonzogni, A; Turbino, L; Zanardi, S, 2013
)
" As the dosage was increased (40, 80, 120 mg/d), the proportion of patients who achieved target sUA in the febuxostat-treated group increased gradually (50."( Efficacy and tolerability of febuxostat in hyperuricemic patients with or without gout: a systematic review and meta-analysis.
Chen, S; Cheng, Q; Li, Q; Liu, L; Luo, T; Lv, Q; Mei, M; Yang, S; Ye, P; Zhang, W, 2013
)
" The model provides a basis for the rational dosing of allopurinol in clinical practice."( The population pharmacokinetics of allopurinol and oxypurinol in patients with gout.
Barclay, ML; Duffull, SB; Holford, NH; Merriman, TR; Stamp, LK; Wright, DF, 2013
)
" This meta-analysis study evaluated the efficacy and cost savings of a single-dose rasburicase (SDR) regimen compared with the Food and Drug Administration-approved daily dosing of rasburicase (DDR) for 5 days or the traditional treatment with allopurinol in adult cancer patients with hyperuricaemia or at high risk for TLS."( Efficacy and cost of single-dose rasburicase in prevention and treatment of adult tumour lysis syndrome: a meta-analysis.
Bhutada, NS; Dong, K; Feng, X; Inciardi, J; Pence, S; Pham, D, 2013
)
" To date, however, optimal dosing has not been established."( Low allopurinol doses are sufficient to optimize azathioprine therapy in inflammatory bowel disease patients with inadequate thiopurine metabolite concentrations.
Curkovic, I; Frei, P; Fried, M; Jetter, A; Kullak-Ublick, GA; Rentsch, KM; Rogler, G, 2013
)
" A low dosage of allopurinol over 12 days also stimulated cell growth and increased their number in culture."( Dependence of cell survival on correlative activities of xanthine oxidase and dihydopyrimidine dehydrogenase in human brain-derived cell culture.
Danielyan, KE, 2013
)
"A modest dosage of vitamin C (500 mg/day) for 8 weeks had no clinically significant urate-lowering effects in patients with gout, despite the fact that plasma ascorbate levels increased."( Clinically insignificant effect of supplemental vitamin C on serum urate in patients with gout: a pilot randomized controlled trial.
Chapman, PT; Drake, JM; Frampton, C; O'Donnell, JL; Stamp, LK; Zhang, M, 2013
)
"The incidence of aberrant cells and aberration types (mostly chromatids, breaks and fragments) was reduced with curcumin dosage as compared to irradiated group."( Curcumin protection activities against γ-rays-induced molecular and biochemical lesions.
Abouelella, AM; Shahein, YE; Tawfik, SS, 2013
)
" Literature regarding the safety and efficacy of dosing allopurinol in CKD has shown inconsistent results and is based primarily on retrospective, case cohort or observational data."( Safety and efficacy of allopurinol in chronic kidney disease.
Bourg, CA; Phillips, BB; Thurston, MM, 2013
)
" On 48% of occasions, the time of allopurinol dosing was recorded, while just 79 (19%) blood samples were collected 6-9 hours postdosing, the time window used to establish the therapeutic range for oxypurinol."( An audit of a therapeutic drug monitoring service for allopurinol therapy.
Day, RO; Graham, GG; Jones, G; Kannangara, DR; Ramasamy, SN; Ray, JE; Williams, KM, 2013
)
" Quercetin was administered by gavage daily for 10 days at dosage 50 mg kg(-1) ."( Evaluation of the protective effect of quercetin against cisplatin-induced renal and testis tissue damage and sperm parameters in rats.
Aldemir, M; Avcı, A; Ener, K; Evirgen, O; Gürleyik, E; Kösemehmetoğlu, K; Okulu, E; Topal, F, 2014
)
" However, inadequate dosing and patient nonadherence or intolerance to therapy often lead to treatment failure."( CaseBook challenges: Managing gout, hyperuricemia and comorbidities -- dialogue with the experts.
Bakris, GL; Doghramji, PP; Keenan, RT; Silber, SH, 2014
)
"Following the intraperitoneal administration of silymarin (with MRP1, 2, 4 and 5 inhibitory effects), naringenin (with MRP1, 2 and 4 stimulatory effects), sulfinpyrazone (with MRP1, 4 and 5 inhibitory and MRP2 stimulatory effects) and allopurinol (with MRP4 stimulatory effect in doses of 100 mg/kg, 100 mg/kg, 100 mg/kg and 60 mg/kg, respectively, for one week before and after the administration of MPTP in C57B/6 mice in acute dosing regimen the striatal concentrations of dopamine, 3,4-dihydroxyphenylacetic acid and homovanillic acid has been measured using high-performance liquid chromatography."( Assessment of the role of multidrug resistance-associated proteins in MPTP neurotoxicity in mice.
Klivényi, P; Plangár, I; Szalárdy, L; Vécsei, L; Zádori, D, 2013
)
" Among the TCM patents, 84% contain various dosage formulae for different Chinese medicines, 13% are herbal extracts and only 7 patents are from herbal extract derivatives."( Analysis of patents on anti-gout therapies issued in China.
Meng, L; Wei, JF; Yuan, HY; Zhang, XH; Zhang, XL, 2014
)
"0 mg/dL, despite the low dosage of febuxostat."( Efficacy and safety of febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase for the treatment of hyperuricemia in kidney transplant recipients.
Fuchinoue, S; Nakajima, I; Teraoka, S; Tojimbara, T; Yashima, J, 2014
)
" Conventional weight based dosing of thiopurines in IBD leads to intolerance or inefficacy in many patients."( The role of thiopurine metabolite monitoring in inflammatory bowel disease.
Beswick, L; Friedman, AB; Sparrow, MP, 2014
)
" The high and low dosage of chicory inulin also decreased serum UA levels on days 7, 14, and 28."( Effects of chicory inulin on serum metabolites of uric acid, lipids, glucose, and abdominal fat deposition in quails induced by purine-rich diets.
Jin, R; Lin, Z; Liu, X; Zhang, B; Zhu, W, 2014
)
"In both dosing scenarios, allopurinol-only therapy was cost-saving."( Cost-effectiveness of allopurinol and febuxostat for the management of gout.
Choi, HK; Jutkowitz, E; Kuntz, KM; Pizzi, LT, 2014
)
"-Some of the reasons identified for poor adherence to anti-gout medications include the risk of flare of acute gout with the initiation of urate-lowering therapy (ULT), poor response to ULT and persistence of attacks of acute gout, suboptimal dosing of allopurinol therapy and intolerance of allopurinol."( Adherence and persistence to urate-lowering therapies in the Irish setting.
Bennett, K; McGowan, B; Silke, C; Whelan, B, 2016
)
"The objective of the study was to develop gastroretentive dosage form (GRDF) for allopurinol (ALP) using combined approaches of mucoadhesion and floating systems."( Formulation optimization of gastroretentive drug delivery system for allopurinol using experimental design.
Mehta, TA; Parikh, DC; Shah, MV; Sharma, OP, 2015
)
" Potentially modifiable factors associated with treatment adherence and obtaining the SUA goal in the multivariable analysis included concomitant diuretic use, prescriber specialty, and allopurinol dosing practices."( Modifiable factors associated with allopurinol adherence and outcomes among patients with gout in an integrated healthcare system.
Cheetham, TC; Coburn, BW; Curtis, JR; Mikuls, TR; Rashid, N; Saag, KG; Wu, YL, 2015
)
" Studies have identified the safe and effective dosing strategies for 'old' drugs such as allopurinol and colchicine."( Advances in pharmacotherapy for the treatment of gout.
Dalbeth, N; Robinson, PC, 2015
)
" Dosage change during admission was rarely observed."( Understanding and improving the use of allopurinol in a teaching hospital.
Baysari, MT; Day, RO; Hmar, RC; Kannangara, DR; Ramasamy, SN; Williams, KM, 2015
)
" The dosage of cinacalcet was optimized for each patient in order to obtain a reduction of parathyroid hormone (PTH) within normal limits while enabling the maintenance of adequate calcemic values."( Use of cinacalcet in nephrolithiasis associated with normocalcemic or hypercalcemic primary hyperparathyroidism: results of a prospective randomized pilot study.
Brardi, S; Cevenini, G; Ponchietti, R; Romano, G; Verdacchi, T, 2015
)
" d-1 ) to prepare the hyperuricemia model, and divided into normal, model, Allopurinol, LE high dosage, middle dosage and low dose (200, 100, 50 mg ."( [Regulatory effect of leonurus extracts on hyperuricemia in rats].
An, YT; Li, J; Wang, T; Wu, ZZ; Yan, M, 2014
)
" Urine voided within 7 h after dosing was collected for a high-performance liquid chromatographic analysis of metabolites, and the urinary molar ratio of metabolites was used as marker for enzyme activity."( Distribution of xanthine oxidase activity in a Nigerian population.
Adehin, A; Bolaji, OO, 2015
)
"The Clinical Pharmacogenetics Implementation Consortium (CPIC) Guidelines for HLA-B*58:01 Genotype and Allopurinol Dosing was originally published in February 2013."( Clinical Pharmacogenetics Implementation Consortium (CPIC) guidelines for human leukocyte antigen B (HLA-B) genotype and allopurinol dosing: 2015 update.
Callaghan, JT; Caudle, KE; Goldspiel, BR; Hershfield, MS; Kamatani, N; Klein, TE; Lee, MT; McDonagh, EM; Mushiroda, T; Phillips, EJ; Saito, Y; Stamp, LK; Tassaneeyakul, W, 2016
)
" Suboptimal dosing is a key contributor to poor clinical outcomes, but few data are available on the safety and efficacy of dose-titrated allopurinol, particularly at doses > 300 mg/d."( An open-label, 6-month study of allopurinol safety in gout: The LASSO study.
Baumgartner, S; Becker, MA; Choi, HK; Cravets, M; Dalbeth, N; Fitz-Patrick, D; Storgard, C, 2015
)
"2% of patients; dosing duration was 115."( An open-label, 6-month study of allopurinol safety in gout: The LASSO study.
Baumgartner, S; Becker, MA; Choi, HK; Cravets, M; Dalbeth, N; Fitz-Patrick, D; Storgard, C, 2015
)
" Risk factors for allopurinol hypersensitivity included female sex, age 60 years or older, initial allopurinol dosage exceeding 100 mg/d, renal or cardiovascular comorbidities, and use for treating asymptomatic hyperuricemia."( Allopurinol Use and Risk of Fatal Hypersensitivity Reactions: A Nationwide Population-Based Study in Taiwan.
Chen, CH; Chen, YJ; Chung, WH; Deng, ST; Huang, CS; Hung, SI; Lin, YJ; Wu, CY; Yang, CY, 2015
)
"5% of patients were followed-up > 1 month for second evaluation of uric acid and most of them not receiving dosage up-titration even though not achieving the target."( Outcome of Treatment in Gouty Arthritis Patients: A Retrospective Study.
Hanvivadhanakul, P; Wongdet, R, 2015
)
" The aim of this study was to assess whether appropriate dosage adjustments were made in hospitalized patients with renal impairment."( Drug dosage adjustment in hospitalized patients with renal impairment at Tikur Anbessa specialized hospital, Addis Ababa, Ethiopia.
Getachew, H; Shibeshi, W; Tadesse, Y, 2015
)
" Data regarding serum creatinine level, age, sex and prescribed drugs and their dosage was collected from the patients' medical records."( Drug dosage adjustment in hospitalized patients with renal impairment at Tikur Anbessa specialized hospital, Addis Ababa, Ethiopia.
Getachew, H; Shibeshi, W; Tadesse, Y, 2015
)
"The findings indicate that dosing errors were common among hospitalized patients with renal impairment."( Drug dosage adjustment in hospitalized patients with renal impairment at Tikur Anbessa specialized hospital, Addis Ababa, Ethiopia.
Getachew, H; Shibeshi, W; Tadesse, Y, 2015
)
" Despite the fact that it has been available for over 40 years there is ongoing debate about optimal allopurinol dosing in gout patients with chronic kidney disease."( Allopurinol and kidney function: An update.
Chapman, PT; Palmer, SC; Stamp, LK, 2016
)
"To determine how many ambulatory older adults with chronic kidney disease receive medications that are contraindicated or dosed excessively given their level of renal function."( Use of Renally Inappropriate Medications in Older Veterans: A National Study.
Chang, F; Miao, Y; O'Hare, AM; Steinman, MA, 2015
)
" It remains to be seen whether allopurinol has a dose-response relationship with cardiovascular events at higher doses."( Impact of Urate Level on Cardiovascular Risk in Allopurinol Treated Patients. A Nested Case-Control Study.
Hallas, J; Lindegaard, HM; Pottegård, A; Søltoft Larsen, K, 2016
)
"Arhalofenate at a dosage of 800 mg decreased gout flares significantly compared to allopurinol at a dosage of 300 mg."( A Randomized, Double-Blind, Active- and Placebo-Controlled Efficacy and Safety Study of Arhalofenate for Reducing Flare in Patients With Gout.
Boudes, PF; Choi, YJ; Davis, CS; Martin, RL; McWherter, CA; Poiley, J; Steinberg, AS, 2016
)
" The gene dosage effect of HLA-B*58:01 also influenced the development of allopurinol-induced cutaneous adverse drug reactions (OR = 15."( Impact of the HLA-B(*)58:01 Allele and Renal Impairment on Allopurinol-Induced Cutaneous Adverse Reactions.
Chang, CJ; Chang, WC; Chang, YC; Chen, DY; Chung, WH; Fan, WL; Hui, RC; Hung, SI; Lin, YJ; Ng, CY; Su, SC; Tian, YC; Wang, CW; Wu, YJ; Yang, CH; Yeh, YT, 2016
)
" Although dosing was otherwise well tolerated, two subjects experienced serious adverse events of acute kidney injury."( Acute kidney injury observed during phase 1 clinical trials of a novel xanthine oxidase/URAT1 dual inhibitor PF-06743649.
Dua, P; Gurrell, R; Kirby, S; Loudon, PT; Sudworth, M, 2016
)
" In post-AMI rats, XO activity and UA concentrations were increased, while SalA dosing palliated this increase."( Mechanism-based pharmacokinetic-pharmacodynamic modeling of salvianolic acid A effects on plasma xanthine oxidase activity and uric acid levels in acute myocardial infarction rats.
He, H; Li, X; Liu, X; Liu, Y; Wang, H; Wang, S; Zhang, W, 2017
)
"27 mg/dl, and were receiving an allopurinol dosage of 306."( Lesinurad Combined With Allopurinol: A Randomized, Double-Blind, Placebo-Controlled Study in Gout Patients With an Inadequate Response to Standard-of-Care Allopurinol (a US-Based Study).
Adler, S; Baumgartner, S; Becker, MA; Bhakta, N; Fitz-Patrick, D; Fung, M; Kopicko, J; Saag, KG; Storgard, C, 2017
)
"85]) Conclusions: This study indicated that by changing the treatment strategy from standard weight-based dosing of azathioprine to weight-based low-dose azathioprine in combination with allopurinol, we can increase remission rates in patients with IBD."( Randomized clinical trial: a pilot study comparing efficacy of low-dose azathioprine and allopurinol to azathioprine on clinical outcomes in inflammatory bowel disease.
Kiszka-Kanowitz, M; Mertz-Nielsen, A; Theede, K, 2016
)
" In terms of the effectiveness of topiroxostat in lowering serum urate levels, the dose-response relationship has been evaluated; however, it remains to be verified."( Clinical efficacy and safety of topiroxostat in Japanese hyperuricemic patients with or without gout: a randomized, double-blinded, controlled phase 2b study.
Hosoya, T; Ohashi, T; Sasaki, T, 2017
)
" Expert opinion: The initial dosage of allopurinol should be low, particularly in patients with renal impairment."( Allopurinol: insights from studies of dose-response relationships.
Carland, JE; Day, RO; Graham, GG; Kannangara, DR; Stocker, SL; Williams, KM, 2017
)
" This study examined the changes in risk of CAD in gout patients taking allopurinol and/or benzbromarone, and analyzed the dose-response relationship of both drugs with CAD incidence."( Allopurinol, benzbromarone and risk of coronary heart disease in gout patients: A population-based study.
Chiang, SJ; Daimon, M; Ho, Y; Lin, HC; Uang, YS; Wang, CH; Wang, LH, 2017
)
" However, after adjustment for covariates in dose-response analyses, treatment with over 270 defined daily doses (DDDs) of allopurinol, and over 360 DDDs of benzbromarone, was associated with a significantly reduced risk of CAD."( Allopurinol, benzbromarone and risk of coronary heart disease in gout patients: A population-based study.
Chiang, SJ; Daimon, M; Ho, Y; Lin, HC; Uang, YS; Wang, CH; Wang, LH, 2017
)
"We found that the use of allopurinol and benzbromarone, whether alone or in combination, had a linear dose-response relationship between the numbers of defined daily doses and the risk of CAD, especially in higher DDDs."( Allopurinol, benzbromarone and risk of coronary heart disease in gout patients: A population-based study.
Chiang, SJ; Daimon, M; Ho, Y; Lin, HC; Uang, YS; Wang, CH; Wang, LH, 2017
)
"2%) 19 patients received the recommended starting dosage of 100mg/day."( GOSPEL 3: Management of gout by primary-care physicians and office-based rheumatologists in France in the early 21st century - comparison with 2006 EULAR Recommendations.
Delva, C; Ea, HK; Goossens, J; Guggenbuhl, P; Lambert, C; Lancrenon, S; Lanz, S; Lioté, F; Sahbane, S; Saraux, A, 2017
)
" Genetic data may inform assessment of disease prognosis in individuals with hyperuricaemia or established gout, personalised lifestyle advice, selection and dosing of urate-lowering therapy, and prevention of serious medication adverse effects."( The genetics of gout: towards personalised medicine?
Dalbeth, N; Merriman, TR; Stamp, LK, 2017
)
" Drug metabolism and pharmacogenetics have increasingly played a role in determining dosing and dose optimisation and we review the rationale for this in both thiopurine monotherapy and in combination with biologic agents."( Optimising use of thiopurines in inflammatory bowel disease.
Dart, RJ; Irving, PM, 2017
)
"Simulation results showed a surge in urinary uric acid occurring when dosing is restarted following missed doses."( Impact of non-adherence on the safety and efficacy of uric acid-lowering therapies in the treatment of gout.
Hill-McManus, D; Hughes, D; Lane, S; Marshall, S; Soto, E, 2018
)
"This research aims to evaluate the predictive performance of a published allopurinol dosing tool."( The impact of diuretic use and ABCG2 genotype on the predictive performance of a published allopurinol dosing tool.
Barclay, ML; Dalbeth, N; Drake, J; Horne, A; Merriman, TR; Phipps-Green, AJ; Stamp, LK; Tan, P; Wright, DFB, 2018
)
"The dosing tool produced acceptable maintenance dose predictions for patients not taking diuretics."( The impact of diuretic use and ABCG2 genotype on the predictive performance of a published allopurinol dosing tool.
Barclay, ML; Dalbeth, N; Drake, J; Horne, A; Merriman, TR; Phipps-Green, AJ; Stamp, LK; Tan, P; Wright, DFB, 2018
)
" Indications for switch, dosing and subsequent clinical outcomes (including thiopurine persistence) were recorded."( Low-dose thiopurine with allopurinol co-therapy overcomes thiopurine intolerance and allows thiopurine continuation in inflammatory bowel disease.
Beswick, L; Friedman, AB; Haridy, J; Moltzen, A; Raghunath, A; Sparrow, M; van Langenberg, D; Vasudevan, A, 2018
)
" The main management issues are related to patient adherence, because gout patients have the lowest rate of medication possession ratio at 1 year, but they also include clinical inertia by physicians, meaning XOI dosage is not titrated according to regular serum uric acid level measurements for targeting serum uric acid levels for uncomplicated (6."( Gout: state of the art after a decade of developments.
Lioté, F; Pascart, T, 2019
)
" We aimed to describe our center's experience with thiopurine optimization through the use of reduced thiopurine dosing in combination with allopurinol upon hepatotoxicity, drug metabolite levels, and clinical outcomes in children with IBD."( Thiopurine Optimization Through Combination With Allopurinol in Children With Inflammatory Bowel Diseases.
Boyle, B; Bricker, J; Crandall, W; Dotson, JL; Kim, SC; Maltz, R; Serpico, MR, 2018
)
" When considering allopurinol for elderly patients with impaired kidney function, a full risk-benefit assessment, dosage adjustments, and careful monitoring may be warranted."( Examining the use of allopurinol: Perspectives from recent drug injury relief applications.
Chen, WW; Chu, MP; Huang, CH, 2019
)
" Underutilization of urate-lowering therapy (ULT) is thought to be common, via both suboptimal dosing and poor medication adherence."( Gout prevalence and predictors of urate-lowering therapy use: results from a population-based study.
Dal Grande, E; Gill, TK; Gonzalez-Chica, D; Hill, CL; Lester, S; Longo, M; Pisaniello, HL; Sharplin, GR; Stocks, N; Whittle, SL, 2018
)
" The use of allopurinol has been researched extensively and newer strategies for safer effective dosing are now recommended."( Gout - An update of aetiology, genetics, co-morbidities and management.
Robinson, PC, 2018
)
" Lack of adherence and insufficient dosing contributed to stone recurrence and AKI during pharmacotherapy."( Long-term renal outcomes of APRT deficiency presenting in childhood.
Agustsdottir, IM; Edvardsson, VO; Indridason, OS; Palsson, R; Runolfsdottir, HL, 2019
)
"Allopurinol dosing has frequently been limited based on creatinine clearance (CrCL), resulting in failure to achieve target serum urate (SU)."( How much allopurinol does it take to get to target urate? Comparison of actual dose with creatinine clearance-based dose.
Barclay, ML; Chapman, PT; Dalbeth, N; Drake, J; Frampton, C; Horne, A; Stamp, LK; Tan, P, 2018
)
" We have previously shown that switching 6MP dosing from evening to morning resolved hypoglycemia by reducing 6MMP; however, the reduction of 6MMP was only transient, potentially resulting in return of hypoglycemia."( Allopurinol reverses mercaptopurine-induced hypoglycemia in patients with acute lymphoblastic leukemia.
Bostrom, B; Zhang, M, 2019
)
" We have previously shown that switching 6MP dosing from evening to morning resolved hypoglycemia by reducing 6MMP; however, the reduction of 6MMP was only transient, potentially resulting in return of hypoglycemia."( Allopurinol reverses mercaptopurine-induced hypoglycemia in patients with acute lymphoblastic leukemia.
Bostrom, B; Zhang, M, 2019
)
" Challenges include timing, dosing and administration route for each neuroprotectant."( Novel interventions to reduce oxidative-stress related brain injury in neonatal asphyxia.
Cheung, PY; Schmölzer, GM; Solevåg, AL, 2019
)
"We conducted an imaging study of a 2-year randomized clinical trial that compared immediate allopurinol dose escalation to SU target with conventional dosing for 1 year followed by dose escalation to target, in gout patients who were receiving allopurinol and who had an SU level of ≥0."( Effects of Allopurinol Dose Escalation on Bone Erosion and Urate Volume in Gout: A Dual-Energy Computed Tomography Imaging Study Within a Randomized, Controlled Trial.
Aati, O; Allan, J; Billington, K; Dalbeth, N; Doyle, A; Drake, J; Frampton, C; Horne, A; Stamp, LK; Tan, P, 2019
)
" Mean sU decrement by dosing per CKD groups was determined by CKD stage."( Low-Dose Allopurinol Promotes Greater Serum Urate Lowering in Gout Patients with Chronic Kidney Disease Compared with Normal Kidney Function.
Crittenden, DB; Fisher, MC; Keenan, RT; Krasnokutsky, S; Modjinou, DV; Oh, C; Pillinger, MH; Toprover, M, 2019
)
" The dose-response relationship between xanthine oxidase inhibitor use and adverse CV outcomes were also determined."( Comparing Cardiovascular Safety of Febuxostat and Allopurinol in the Real World: A Population-Based Cohort Study.
Hsieh, SC; Lin, FJ; Lin, LY; Shen, LJ; Su, CY, 2019
)
" We used World Health Organization's defined daily dose (DDD) as a measure to assess the dosage of colchicine, allopurinol and benzbromarone exposure."( Association of gout medications and risk of cataract: a population-based case-control study.
Li, YJ; Perng, WT; Tseng, KY; Wang, YH; Wei, JC, 2019
)
" Patients with heart disease and chronic kidney disease who were started on an allopurinol dosage of greater than 100 mg/d had an 11-fold higher risk."( Heart disease and the risk of allopurinol-associated severe cutaneous adverse reactions: a general population-based cohort study.
Aviña-Zubieta, JA; Choi, HK; Li, L; Lu, N; McCormick, N; Rai, SK; Xie, H; Yokose, C; Zheng, Y, 2019
)
" There is paucity of data on the dosing of ULT for managing hyperuricaemia in gout patients with chronic kidney disease."( Debates in gout management.
Abhishek, A, 2020
)
" There were significant differences in the maximum dosage, time to corticosteroid tapering, and the total dosage of corticosteroid between the SJS group and the TEN group, as well as among the three groups (P = 0."( Retrospective study of 213 cases of Stevens-Johnson syndrome and toxic epidermal necrolysis from China.
Li, F; Shou, YH; Xu, JH; Yang, L; Yang, YS; Zhu, XH, 2020
)
" Two articles found allopurinol to be protective in patients with gout, 1 found no statistically significant association, and 1 found no statistically significant effect of escalation of allopurinol dosage on all-cause or cardiovascular-related mortality."( Mortality in Patients With Gout Treated With Allopurinol: A Systematic Review and Meta-Analysis.
Belcher, J; Hay, CA; Mallen, CD; Prior, JA; Roddy, E, 2021
)
" Allopurinol, a urate synthesis inhibitor, is generally administered at a reduced dosage to patients with renal impairment."( Recent approaches to gout drug discovery: an update.
Anzai, N; Hisatome, I; Kudo, H; Otani, N; Ouchi, M; Tsuruoka, S, 2020
)
"To describe the metabolic pathways and key factors implicated in the efficacy and toxicity of the thiopurine drugs and to indicate the opportunities to improve outcomes by monitoring and manipulating metabolic pathways, individualising dosage and strengthening the response."( Review article: opportunities to improve and expand thiopurine therapy for autoimmune hepatitis.
Czaja, AJ, 2020
)
" Universal pre-treatment assessment of thiopurine methyltransferase activity and individualisation of dosage to manipulate metabolite thresholds could improve outcomes."( Review article: opportunities to improve and expand thiopurine therapy for autoimmune hepatitis.
Czaja, AJ, 2020
)
"The efficacy and safety of thiopurines in autoimmune hepatitis can be improved by investigational efforts that establish monitoring strategies that allow individualisation of dosage and prediction of outcome, increase bioavailability of the active metabolites and demonstrate superiority to alternative agents."( Review article: opportunities to improve and expand thiopurine therapy for autoimmune hepatitis.
Czaja, AJ, 2020
)
" The effect of uricosuric agents on the decrease in hospitalized stroke risk indicated a dose-response relationship."( Urate-lowering therapy may mitigate the risks of hospitalized stroke and mortality in patients with gout.
Hsu, CC; Hwu, CM; Li, HL; Wei, JC; Yen, FS, 2020
)
" And as febuxostat dosage increased, more patients achieved the target SU level."( Comparison of efficacy and safety of urate-lowering therapies for hyperuricemic patients with gout: a meta-analysis of randomized, controlled trials.
Fan, M; Gu, J; Li, X; Liu, J; Schlesinger, N; Wu, X; Zhao, B, 2021
)
" And as febuxostat dosage increased, more patients achieved the target SU level."( Comparison of efficacy and safety of urate-lowering therapies for hyperuricemic patients with gout: a meta-analysis of randomized, controlled trials.
Fan, M; Gu, J; Li, X; Liu, J; Schlesinger, N; Wu, X; Zhao, B, 2021
)
" The dosage of allopurinol to accomplish full control of gout and to lower serum uric acid to normal or near-normal levels varies with the severity of the disease, and needs to be flexible to permit precise, customized dose titration for individual patients."( Physicochemical Stability of Compounded Allopurinol Suspensions in PCCA Base, SuspendIt.
Bostanian, LA; Graves, RA; Le, G; Mandal, TK; Morris, TC; Pramar, YV,
)
" In the present work, two different highly sensitive, selective and accurate fluorescence spectroscopic methods were developed for quantitative analysis of lesinurad and allopurinol in their pharmaceutical dosage form without any tedious operation procedure."( Application of different spectrofluorimetric methods for determination of lesinurad and allopurinol in pharmaceutical preparation and human plasma.
Abdelazim, AH; Attia, KAM; El-Olemy, A; Hasan, MA; Omar, MKM; Ramzy, S; Shahin, M, 2021
)
"Patients in maintenance were considered for allopurinol treatment who had the following features: (a) Grade ≥3 hepatotoxicity; (b) Grade ≥2 nonhepatic gastrointestinal (GI) toxicity; or (c) persistently elevated absolute neutrophil count (ANC) despite >150% protocol dosing of oral chemotherapy."( Allopurinol use during pediatric acute lymphoblastic leukemia maintenance therapy safely corrects skewed 6-mercaptopurine metabolism, improving inadequate myelosuppression and reducing gastrointestinal toxicity.
Annesley, C; Bhuiyan, M; Brown, P; Cohen, G; Cooper, S; Sison, EA, 2020
)
"Different spectrophotometic quantitative analytical methods have been developed and applied for quantitative determination of lesinurad and allopurinol in their newly FDA approved pharmaceutical dosage form."( Spectrophotometric determination of lesinurad and allopurinol in recently approved FDA pharmaceutical preparation.
Abdelazim, AH; El-Olemy, A; Mohamed, AA; Omar, MKM; Ramzy, S; Shahin, M, 2021
)
" In addition, daily dosing of febuxostat 80 mg had greater efficacy to that of febuxostat 40 mg (RR=1."( Efficacy and safety of Febuxostat Versus Allopurinol in Hyperuricemic patients with or without Gout: A meta-analysis.
Fan, B; Li, X; Zhang, P, 2020
)
" Moreover, our result suggested that dose titration to febuxostat 120 mg daily was superior to other daily dosing with regard to urate-lowering efficacy."( Efficacy and safety of Febuxostat Versus Allopurinol in Hyperuricemic patients with or without Gout: A meta-analysis.
Fan, B; Li, X; Zhang, P, 2020
)
" Every 3 weeks, the dosage of the drug was increased by 50 mg to 300 mg per day under the control of the level of serum uric acid (sUA)."( [Evaluation of a 12-week allopurinol-lowering therapy in combination with the non-steroidal anti-inflammatory drug meloxicam in patients with gout].
Gromova, MA; Kislyak, OA; Malysheva, NV; Tsurko, VV, 2020
)
" From these findings, a strategic SR formulation approach might be an efficacious dosage option for ALP to avoid severe nephrotoxicity in patients with nephropathy."( Biopharmaceutical characterization of a novel sustained-release formulation of allopurinol with reduced nephrotoxicity.
Nihei, T; Onoue, S; Sato, H, 2021
)
"Three chemometric assisted spectrophotometric approaches were designed for precise quantitative analysis of lesinurad and allopurinol, in their recently FDA approved combination pharmaceutical dosage form."( Different chemometric assisted approaches for spectrophotometric quantitative analysis of lesinurad and allopurinol.
Abdelazim, AH; Shahin, M, 2021
)
" The results indicated a dose-response relationship between allopurinol usage and CRC risk (P for trend < ."( Exploring the Relationship Between Colorectal Cancer and Allopurinol: A Taiwanese Population-Based Propensity-Matched Case-Control Study.
Hsieh, YW; Hsu, FG; Huang, CY; Lai, JN; Lin, MC, 2021
)
" Simulations based on the uric acid model were performed to assess dose-response of verinurad in combination with XOI, and to investigate the impact of covariates."( A semi-mechanistic exposure-response model to assess the effects of verinurad, a potent URAT1 inhibitor, on serum and urine uric acid in patients with hyperuricemia-associated diseases.
Aksenov, S; Eriksson, UG; Johansson, S; Leander, J; Parkinson, J; Rekić, D; Sunnåker, M, 2021
)
" The validated HPLC method was successfully applied to the simultaneous determination of both drugs in their tablet dosage forms."( Development and greenness assessment of a stability-indicating HPLC-DAD method for simultaneous determination of allopurinol and benzbromarone.
Abdel-Khalek, MM; Abdelhamid, AG; Belal, TS; El-Kafrawy, DS, 2021
)
" The dosage used and the effect of allopurinol in this population, either or not undergoing therapeutic hypothermia (TH), were evaluated."( Pharmacokinetic/Pharmacodynamic Modelling of Allopurinol, its Active Metabolite Oxypurinol, and Biomarkers Hypoxanthine, Xanthine and Uric Acid in Hypoxic-Ischemic Encephalopathy Neonates.
Allegaert, K; Annink, KV; Bakkali, LE; Benders, MJNL; Chu, WY; Dorlo, TPC; Franz, AR; Hagen, A; Huitema, ADR; Maiwald, CA; Nijstad, AL; Schroth, M; van Bel, F; van Weissenbruch, MM, 2022
)
" The dosing regimen applied in the ALBINO trial leads to the targeted XO inhibition in neonates treated with or without TH."( Pharmacokinetic/Pharmacodynamic Modelling of Allopurinol, its Active Metabolite Oxypurinol, and Biomarkers Hypoxanthine, Xanthine and Uric Acid in Hypoxic-Ischemic Encephalopathy Neonates.
Allegaert, K; Annink, KV; Bakkali, LE; Benders, MJNL; Chu, WY; Dorlo, TPC; Franz, AR; Hagen, A; Huitema, ADR; Maiwald, CA; Nijstad, AL; Schroth, M; van Bel, F; van Weissenbruch, MM, 2022
)
"1% split its dosage but increase administration frequency."( Xanthinuria secondary to allopurinol treatment in dogs with leishmaniosis: Current perspectives of the Iberian veterinary community.
Arenas, C; Domínguez-Ruiz, M; Englar, RE; Jesus, L; Leal, RO; Roura, X; Silvestrini, P, 2022
)
" The top hit Spartinin F2 exhibited inhibition percentages at 10 μM dosage as high as 84."( Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
Jiao, QC; Liu, J; Qin, P; Wang, B; Yang, YS; Zhou, KM, 2022
)
" Drug dose titration (DT) is the process by which dosage is progressively adjusted to the patient till a steady dose is reached."( Modelling and assessing one- and two-drug dose titrations.
Alonso, JR; Kamišalić, A; Pečnik, Š; Riaño, D, 2022
)
"Lesinurad and allopurinol have been formulated in a combined dosage form providing a new challenge for the treatment of gout attacks."( Different spectrophotometric methods for simultaneous determination of lesinurad and allopurinol in the new FDA approved pharmaceutical preparation; additional greenness evaluation.
Abd Elhalim, LM; Abdelazim, AH; Abourehab, MAS; Almrasy, AA; Ramzy, S, 2023
)
"Advantageous application of the validated HPLC method for the concurrent analysis of ALO/THA in their tablet dosage form was accomplished."( Forced Degradation and Stability-Indicating Study for the Binary Mixture of Allopurinol and Thioctic Acid Using Validated HPLC-DAD Method.
Abdel-Khalek, MM; Abdelhamid, AG; Belal, TS; El-Kafrawy, DS, 2023
)
" The aim of this study was to investigate whether anthropometric and socioeconomic factors and comorbidities could explain sex-related differences in concentrations and dosing for metoprolol and oxypurinol, the active metabolite of allopurinol."( Females present higher dose-adjusted drug concentrations of metoprolol and allopurinol/oxypurinol than males.
Busseuil, D; de Denus, S; Dubé, MP; Gaulin, MJ; Hindi, J; Jutras, M; Leclair, G; Meloche, M; Mongrain, I; Oussaïd, E; Pilon, MO; Rouleau, JL; St-Jean, I; Tardif, JC, 2023
)
" The available medications for stone prevention, namely thiazide diuretics, alkali, and allopurinol, are not always prescribed consistently, dosed correctly, or tolerated well by patients."( Breaking the Cycle of Recurrent Calcium Stone Disease.
Ganesan, C; Malieckal, DA; Mendez, DA; Pao, AC, 2023
)
"The proposed allopurinol dosing guide uses individuals' fat-free mass, renal function and SLC22A12 rs505802 and PDZK1 rs12129861 genotypes to achieve target SU."( Population pharmacokinetics, pharmacodynamics and pharmacogenetics modelling of oxypurinol in Hmong adults with gout and/or hyperuricemia.
Brundage, RC; Culhane-Pera, KA; Roman, YM; Straka, RJ; Wen, YF, 2023
)
" ULT dosage is also limited by formularies and clinical inertia."( Mechanisms and rationale for uricase use in patients with gout.
Lioté, F; Pérez-Ruiz, F; Schlesinger, N, 2023
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
antimetaboliteA substance which is structurally similar to a metabolite but which competes with it or replaces it, and so prevents or reduces its normal utilization.
EC 1.17.3.2 (xanthine oxidase) inhibitorAn EC 1.17.3.* (oxidoreductase acting on CH or CH2 with oxygen as acceptor) inhibitor that interferes with the action of xanthine oxidase (EC 1.17.3.2).
radical scavengerA role played by a substance that can react readily with, and thereby eliminate, radicals.
gout suppressantA drug that increases uric acid excretion by the kidney (uricosuric drug), decreases uric acid production (antihyperuricemic), or alleviates the pain and inflammation of acute attacks of gout.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
organic heterobicyclic compound
nucleobase analogueA molecule that can substitute for a normal nucleobase in nucleic acids.
[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]

Pathways (6)

PathwayProteinsCompounds
guanosine nucleotides degradation II125
adenosine nucleotides degradation I327
superpathway of purines degradation in plants745
superpathway of guanosine nucleotides degradation (plants)227
guanosine nucleotides degradation I226
purine nucleotides degradation I (plants)334

Protein Targets (37)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
interleukin 8Homo sapiens (human)Potency74.97800.047349.480674.9780AID651758
TDP1 proteinHomo sapiens (human)Potency5.80480.000811.382244.6684AID686979
AR proteinHomo sapiens (human)Potency1.55180.000221.22318,912.5098AID1259243; AID1259381
thyroid stimulating hormone receptorHomo sapiens (human)Potency5.01190.001318.074339.8107AID926; AID938
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency22.19830.000657.913322,387.1992AID1259378
progesterone receptorHomo sapiens (human)Potency27.94590.000417.946075.1148AID1346784
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency15.08900.000214.376460.0339AID720691
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency39.98190.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
estrogen nuclear receptor alphaHomo sapiens (human)Potency40.38960.000229.305416,493.5996AID1259244; AID743069; AID743075
IDH1Homo sapiens (human)Potency25.92900.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.02510.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.39810.540617.639296.1227AID2364; AID2528
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency0.79430.794321.275750.1187AID624246
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency16.45770.000323.4451159.6830AID743065; AID743067
ras-related protein Rab-9AHomo sapiens (human)Potency1.00000.00022.621531.4954AID485297
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency74.97800.000627.21521,122.0200AID651741
gemininHomo sapiens (human)Potency0.09200.004611.374133.4983AID624296
survival motor neuron protein isoform dHomo sapiens (human)Potency1.00000.125912.234435.4813AID1458
lamin isoform A-delta10Homo sapiens (human)Potency6.30960.891312.067628.1838AID1487
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency70.19700.001557.789015,848.9004AID1259244
Cellular tumor antigen p53Homo sapiens (human)Potency31.62280.002319.595674.0614AID651743
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency70.19700.001551.739315,848.9004AID1259244
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Polyphenol oxidase 2Agaricus bisporusIC50 (µMol)1,000.00000.03403.987110.0000AID1082239
Bile salt export pumpHomo sapiens (human)IC50 (µMol)116.50000.11007.190310.0000AID1443986; AID1473738
Xanthine dehydrogenase/oxidase [Includes: Xanthine dehydrogenase Rattus norvegicus (Norway rat)IC50 (µMol)9.31770.00402.25236.0000AID449301; AID552786; AID722986
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC50 (µMol)10.99680.00132.81389.8200AID1234421; AID1272635; AID1310994; AID1330574; AID1348944; AID1389558; AID1405945; AID1433308; AID1453375; AID1485271; AID1485273; AID1485280; AID1485284; AID1485285; AID1502932; AID1651286; AID1799669; AID1865993; AID1888100; AID1900625; AID219595; AID219739; AID287937; AID295041; AID341681; AID351098; AID378013; AID378145; AID380589; AID384287; AID384323; AID387151; AID387152; AID398996; AID399340; AID406380; AID467250; AID479084; AID590702; AID717724
Xanthine dehydrogenase/oxidaseHomo sapiens (human)Ki2.89170.00011.38097.3000AID1183551; AID1185461; AID1269361; AID1649918; AID1900627; AID219741
Nuclear receptor ROR-gammaMus musculus (house mouse)IC50 (µMol)11.10000.02500.02500.0250AID1064493
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC50 (µMol)13.75200.00303.10159.8000AID1064493; AID1072541; AID1146435; AID1150142; AID1298770; AID1369117; AID1379542; AID1402016; AID1424732; AID1435053; AID1444510; AID1444593; AID1461517; AID1485269; AID1485276; AID1485278; AID1485281; AID1485283; AID1487713; AID1503694; AID1537337; AID1570304; AID1594173; AID1608483; AID1637837; AID1695067; AID1736372; AID1762453; AID1800155; AID1800197; AID1800440; AID1867877; AID1878316; AID219599; AID355479; AID469633; AID552787; AID578685; AID614370; AID660255; AID682403; AID728035
Xanthine dehydrogenase/oxidaseBos taurus (cattle)Ki1.80000.00010.83862.6000AID1146441; AID1146443
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Histamine H3 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)8.69000.00102.90708.6900AID1637837
[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)
Adenosine receptor A2aHomo sapiens (human)Kd77.00000.00020.47319.6000AID1874229
Xanthine dehydrogenase/oxidaseBos taurus (cattle)Kd0.00050.00050.00050.0005AID1485264
[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)
Hypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)Km91.45001.15002.75635.9000AID274549; AID274562
Xanthine dehydrogenase/oxidaseBos taurus (cattle)Km58.37501.80002.78003.7000AID424718; AID424719; AID424720; AID424721
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (272)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
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)
T cell mediated cytotoxicityHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
response to amphetamineHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
purine nucleotide biosynthetic processHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
purine ribonucleoside salvageHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
guanine salvageHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
grooming behaviorHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
locomotory behaviorHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
striatum developmentHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
cerebral cortex neuron differentiationHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
central nervous system neuron developmentHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
GMP salvageHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
IMP salvageHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
dopamine metabolic processHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
hypoxanthine salvageHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
AMP salvageHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
positive regulation of dopamine metabolic processHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
GMP catabolic processHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
IMP metabolic processHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
adenine metabolic processHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
hypoxanthine metabolic processHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
lymphocyte proliferationHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
dendrite morphogenesisHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
protein homotetramerizationHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
dopaminergic neuron differentiationHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
synaptic transmission, dopaminergicAdenosine receptor A2aHomo sapiens (human)
response to amphetamineAdenosine receptor A2aHomo sapiens (human)
regulation of DNA-templated transcriptionAdenosine receptor A2aHomo sapiens (human)
phagocytosisAdenosine receptor A2aHomo sapiens (human)
apoptotic processAdenosine receptor A2aHomo sapiens (human)
inflammatory responseAdenosine receptor A2aHomo sapiens (human)
cellular defense responseAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
cell-cell signalingAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, cholinergicAdenosine receptor A2aHomo sapiens (human)
central nervous system developmentAdenosine receptor A2aHomo sapiens (human)
blood coagulationAdenosine receptor A2aHomo sapiens (human)
sensory perceptionAdenosine receptor A2aHomo sapiens (human)
locomotory behaviorAdenosine receptor A2aHomo sapiens (human)
blood circulationAdenosine receptor A2aHomo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A2aHomo sapiens (human)
response to xenobiotic stimulusAdenosine receptor A2aHomo sapiens (human)
response to inorganic substanceAdenosine receptor A2aHomo sapiens (human)
positive regulation of glutamate secretionAdenosine receptor A2aHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionAdenosine receptor A2aHomo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A2aHomo sapiens (human)
response to purine-containing compoundAdenosine receptor A2aHomo sapiens (human)
response to caffeineAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
positive regulation of urine volumeAdenosine receptor A2aHomo sapiens (human)
vasodilationAdenosine receptor A2aHomo sapiens (human)
eating behaviorAdenosine receptor A2aHomo sapiens (human)
negative regulation of vascular permeabilityAdenosine receptor A2aHomo sapiens (human)
negative regulation of neuron apoptotic processAdenosine receptor A2aHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleepAdenosine receptor A2aHomo sapiens (human)
negative regulation of alpha-beta T cell activationAdenosine receptor A2aHomo sapiens (human)
astrocyte activationAdenosine receptor A2aHomo sapiens (human)
neuron projection morphogenesisAdenosine receptor A2aHomo sapiens (human)
positive regulation of protein secretionAdenosine receptor A2aHomo sapiens (human)
negative regulation of inflammatory responseAdenosine receptor A2aHomo sapiens (human)
regulation of mitochondrial membrane potentialAdenosine receptor A2aHomo sapiens (human)
membrane depolarizationAdenosine receptor A2aHomo sapiens (human)
regulation of calcium ion transportAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
inhibitory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
prepulse inhibitionAdenosine receptor A2aHomo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2aHomo sapiens (human)
positive regulation of long-term synaptic potentiationAdenosine receptor A2aHomo sapiens (human)
positive regulation of apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
allantoin metabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of protein phosphorylationXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of endothelial cell proliferationXanthine dehydrogenase/oxidaseHomo sapiens (human)
guanine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
inosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyinosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
adenosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyadenosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyguanosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
AMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
IMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
lactationXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of gene expressionXanthine dehydrogenase/oxidaseHomo sapiens (human)
iron-sulfur cluster assemblyXanthine dehydrogenase/oxidaseHomo sapiens (human)
amide catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of endothelial cell differentiationXanthine dehydrogenase/oxidaseHomo sapiens (human)
GMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
dGMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
dAMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionXanthine dehydrogenase/oxidaseHomo sapiens (human)
positive regulation of p38MAPK cascadeXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of vascular endothelial growth factor signaling pathwayXanthine dehydrogenase/oxidaseHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of vasculogenesisXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine catabolic processXanthine dehydrogenase/oxidaseBos taurus (cattle)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (82)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
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)
nucleotide bindingHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
magnesium ion bindingHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
hypoxanthine phosphoribosyltransferase activityHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
protein bindingHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
identical protein bindingHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
guanine phosphoribosyltransferase activityHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aHomo sapiens (human)
protein bindingAdenosine receptor A2aHomo sapiens (human)
calmodulin bindingAdenosine receptor A2aHomo sapiens (human)
lipid bindingAdenosine receptor A2aHomo sapiens (human)
enzyme bindingAdenosine receptor A2aHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingAdenosine receptor A2aHomo sapiens (human)
identical protein bindingAdenosine receptor A2aHomo sapiens (human)
protein-containing complex bindingAdenosine receptor A2aHomo sapiens (human)
alpha-actinin bindingAdenosine receptor A2aHomo sapiens (human)
xanthine dehydrogenase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine oxidase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
iron ion bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
protein bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
protein homodimerization activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
molybdopterin cofactor bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
flavin adenine dinucleotide bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
2 iron, 2 sulfur cluster bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine dehydrogenase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine oxidase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
FAD bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine dehydrogenase activityXanthine dehydrogenase/oxidaseBos taurus (cattle)
xanthine oxidase activityXanthine dehydrogenase/oxidaseBos taurus (cattle)
iron ion bindingXanthine dehydrogenase/oxidaseBos taurus (cattle)
molybdenum ion bindingXanthine dehydrogenase/oxidaseBos taurus (cattle)
protein homodimerization activityXanthine dehydrogenase/oxidaseBos taurus (cattle)
molybdopterin cofactor bindingXanthine dehydrogenase/oxidaseBos taurus (cattle)
flavin adenine dinucleotide bindingXanthine dehydrogenase/oxidaseBos taurus (cattle)
2 iron, 2 sulfur cluster bindingXanthine dehydrogenase/oxidaseBos taurus (cattle)
FAD bindingXanthine dehydrogenase/oxidaseBos taurus (cattle)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (53)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
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)
cytoplasmHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
cytosolHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
extracellular exosomeHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
cytosolHypoxanthine-guanine phosphoribosyltransferaseHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
intermediate filamentAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
membraneAdenosine receptor A2aHomo sapiens (human)
dendriteAdenosine receptor A2aHomo sapiens (human)
axolemmaAdenosine receptor A2aHomo sapiens (human)
asymmetric synapseAdenosine receptor A2aHomo sapiens (human)
presynaptic membraneAdenosine receptor A2aHomo sapiens (human)
neuronal cell bodyAdenosine receptor A2aHomo sapiens (human)
postsynaptic membraneAdenosine receptor A2aHomo sapiens (human)
presynaptic active zoneAdenosine receptor A2aHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2aHomo sapiens (human)
cytosolXanthine dehydrogenase/oxidaseHomo sapiens (human)
extracellular spaceXanthine dehydrogenase/oxidaseHomo sapiens (human)
peroxisomeXanthine dehydrogenase/oxidaseHomo sapiens (human)
cytosolXanthine dehydrogenase/oxidaseHomo sapiens (human)
sarcoplasmic reticulumXanthine dehydrogenase/oxidaseHomo sapiens (human)
extracellular spaceXanthine dehydrogenase/oxidaseHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaMus musculus (house mouse)
extracellular spaceXanthine dehydrogenase/oxidaseBos taurus (cattle)
peroxisomeXanthine dehydrogenase/oxidaseBos taurus (cattle)
xanthine dehydrogenase complexXanthine dehydrogenase/oxidaseBos taurus (cattle)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (497)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1867888Nephroprotective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in connective tissue hyperplasia at 20 mg/kg, po administered via gavage and measured after 21 days by hematoxylin-eosin and Ma2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
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.
AID614371Antihyperuricemic activity in Swiss mouse assessed as decrease of potassium oxonate-induced uric acid level in serum at 50 mg/kg, ip after 3 hrs by HPLC analysis (Rvb = 7.80 +/- 0.34 uM)2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors.
AID1888102Anti-hyperuricemic activity against potassium oxonate-induced acute hyperuricemia Sprague-Dawley rat model assessed as reduction in serum uric acid level at 10 mg/kg, po pretreated with potassium oxonate for 1 hr followed by compound treatment and measure2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of N-(3-cyano-1H-indol-5/6-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamides and 5-(6-oxo-1,6-dihydropyrimidin-2-yl)-1H-indole-3-carbonitriles as novel xanthine oxidase inhibitors.
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
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1082231Inhibition of Oryctolagus cuniculus (rabbit) AOX in liver cytosol at IC50 concentration2011Journal of agricultural and food chemistry, May-11, Volume: 59, Issue:9
Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
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).
AID1867911Cytoprotective activity in human HK-2 cells assessed as reduction in uric acid-induced increase in branches and intracellular space at 25 uM by inverted light microscopic analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID722717Antioxidant activity assessed as inhibition DPPH radical production after 15 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Trisubstituted thiophene analogues of 1-thiazolyl-2-pyrazoline, super oxidase inhibitors and free radical scavengers.
AID568568Antioxidant activity assessed as inhibition of xanthine-xanthine oxidase generated superoxide anion radical production2011Journal of natural products, Jan-28, Volume: 74, Issue:1
Radical scavenging and antioxidant activities of isocoumarins and a phthalide from the endophytic fungus Colletotrichum sp.
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).
AID1851311Inhibition of xanthine oxidase (unknown origin) at 10 uM relative to control2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
AID552787Inhibition of bovine milk xanthine oxidase by spectrophotometry2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis and xanthine oxidase inhibitory activity of 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives.
AID1753482Selectivity index, ratio of CC50 for human MRC-5 SV2 cells to IC50 for antitrypanosomal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC-5 SV2 cells2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID27580Partition coefficient (logP)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID179366Effect of AOS scavenger on ventricular fibrillation (VF), arrhythmias induced by ischemia-reperfusion in anesthetized rat, frequency, times at 20 mg/kg1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids.
AID1461523Anti-hyperuricemic activity in potassium oxonate-induced hyperuricemic Kun-Ming mouse assessed as serum uric acid level at 10 mg/kg/day, ig for 7 days and measured 1 hr post last dose (Rvb = 5.89 +/- 0.36 mg/dl)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia.
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.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID1867896Anti-hyperuricemic activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in serum uric acid level at 20 mg/kg, po administered via gavage once daily for 4 weeks (Rvb = 356.15 +/- 3.31 uM)2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1637841Anti-hyperuricemic effect in Swiss albino mouse model of potassium oxonate-induced hyperuricemia model assessed as serum uric acid level at 10 mg/kg, po treated 1 hr post potassium oxonate addition and measured after 30 mins by ERBA method (Rvb = 5.9 +/- 2019MedChemComm, Jan-01, Volume: 10, Issue:1
Benzoflavone derivatives as potent antihyperuricemic agents.
AID1330574Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation preincubated for 5 mins followed by addition of xanthine substrate measured every minute up to 8 mins2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
AID424729Inhibition of bovine xanthine oxidase assessed as reduction of cytochrome c at 50 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
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]
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID717694Antihyperuricemic activity in fasted rat assessed as reduction in potassium oxonate-induced uric acid level in serum at 10 mg/kg, po administered 1 hr post potassium oxonate-challenge relative to vehicle-treated control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Isocytosine-based inhibitors of xanthine oxidase: design, synthesis, SAR, PK and in vivo efficacy in rat model of hyperuricemia.
AID1389566In vivo inhibition of XOD activity in liver of Kunming mouse model of potassium oxonate-induced hyperuricemia at 10 mg/kg, po treated 1 hr post potassium oxonate addition measured after 1 hr relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID378145Inhibition of xanthine oxidase2005Journal of natural products, Feb, Volume: 68, Issue:2
Bioactive constituents from Boswellia papyrifera.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
AID1330572Uricosuric activity in potassium oxonate-induced Kun Ming mouse model of hyperuricemia assessed as increase in uric acid excretion in urine at 10 mg/kg qd administered 1 hr post potassium oxonate-challenge for 7 days via oral gavage measured up to 24 hrs 2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
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]
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID179375Effect of AOS scavenger on ventricular tachycardia (VT), arrhythmias induced by ischemia-reperfusion in anesthetized rat, frequency, times at 20 mg/kg1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID168363Superoxide dismutase activity measured as inhibition of Cytochrome C reduction by 50% in isolated rat heart muscle subjected to global ischemia2001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Beneficial effects of different flavonoids, on functional recovery after ischemia and reperfusion in isolated rat heart.
AID1878316Inhibition of bovine XO assessed as inhibition of uric acid formation using xanthine as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured for 2 mins by spectrophotometry2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Discovery of 4-(phenoxymethyl)-1H-1,2,3-triazole derivatives as novel xanthine oxidase inhibitors.
AID1874227Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as affinity on-rate by surface plasmon resonance assay2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
AID1608483Inhibition of bovine milk xanthine oxidase using xanthine as substrate incubated for 15 mins followed by substrate addition and measured at 30 sec interval for 2 mins by spectrophotometrically2019European journal of medicinal chemistry, Nov-01, Volume: 181Targeting the subpocket in xanthine oxidase: Design, synthesis, and biological evaluation of 2-[4-alkoxy-3-(1H-tetrazol-1-yl) phenyl]-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives.
AID295041Inhibition of Xanthine oxidase2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).
AID1389570Hypouricemic effect in Kunming mouse assessed as inhibition of hepatic XOD activity at 10 mg/kg, po measured after 1 hr relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1753481Cytotoxicity against human MRC-5 SV2 cells assessed as reduction in cell growth measured after 3 days by resazurin dye based fluorometric analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1485267Inhibition of butter milk xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate by UV-Vis spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID1868686Selectivity index, ratio of CC50 for Cytotoxicity against Swiss mouse peritoneal macrophages to EC50 for intracellular Leishmania infantum MHOM/MA(BE)/67 ITMAP263 amastigotes infected in Swiss mouse peritoneal macrophages2022European journal of medicinal chemistry, Jul-05, Volume: 237Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents.
AID1651290Antiarthritic activity in potassium oxonate-induced hyperuricemia mouse model assessed as reduction in uric acid level in serum at 10 mg/kg2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Development of novel NLRP3-XOD dual inhibitors for the treatment of gout.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1348941Antioxidant activity assessed as DPPH radical scavenging activity at 30 uM after 60 mins by spectrophotometric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1150142Inhibition of bovine xanthine oxidase1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
2-pyridylimidazoles as inhibitors of xanthine oxidase.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1900625Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 15 mins followed by substrate addition by UV spectrophotometric analysis2022European journal of medicinal chemistry, Feb-05, Volume: 229Intramolecular hydrogen bond interruption and scaffold hopping of TMC-5 led to 2-(4-alkoxy-3-cyanophenyl)pyrimidine-4/5-carboxylic acids and 6-(4-alkoxy-3-cyanophenyl)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-ones as potent pyrimidine-based xanthine oxid
AID590702Inhibition of xanthine oxidase activity assessed as uric acid formation pretreated for 15 mins before substrate addition measured after 5 mins2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Antioxidant xanthone derivatives induce cell cycle arrest and apoptosis and enhance cell death induced by cisplatin in NTUB1 cells associated with ROS.
AID424721Activity at bovine xanthine oxidase at 25 uM preincubated for 10 mins2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1453375Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric method2017Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13
Potential anti-gout constituents as xanthine oxidase inhibitor from the fruits of Stauntonia brachyanthera.
AID776267Stability of the compound in simulated gastric fluid assessed as retention time by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID681386TP_TRANSPORTER: uptake in mOat3-expressing oocytes2004Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 32, Issue:5
Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID670364Inhibition of xanthine oxidase- mediated uric acid formation after 5 mins by spectrophotometry2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Xanthine oxidase inhibitory activity of constituents of Cinnamomum cassia twigs.
AID1695067Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate measured for 20 mins by microplate assay2020RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors.
AID1874229Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
AID1500520Inhibition of butter milk XOD (unknown origin) at 1 uM using xanthine as substrate after 8 mins relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Structure-activity relations of rosmarinic acid derivatives for the amyloid β aggregation inhibition and antioxidant properties.
AID768702Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate assessed as uric acid formation preincubated for 5 mins followed by substrate addition measured every minute up to 8 mins by spectrophotometric analysis2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and biological evaluation of pyrazolo[4,3-d]pyrimidine analogues.
AID1389563Anti-hyperuricemic effect in Kunming mouse assessed as inhibition of potassium oxonate-induced serum uric acid level at 10 mg/kg, po treated 1 hr post potassium oxonate addition measured after 1 hr by phosphotungstic acid method relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.
AID1867922Renal protective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in hyperuricemia-induced renal fibrosis by measuring tubular dilation with epithelial atrophy at 20 mg/kg, po administered via 2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1762453Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 15 mins followed by substrate addition measured for every 30 sec by spectrophotometric analysis2021Bioorganic & medicinal chemistry, 05-15, Volume: 38Synthesis and biological evaluation of 2-(4-alkoxy-3-cyano)phenylpyrimidine derivatives with 4-amino or 4-hydroxy as a pharmacophore element binding with xanthine oxidase active site.
AID776277Stability of the compound in 0.05 M SDS-0.01 M NaH2PO4/H3PO4 assessed as compound recovery at 3.5 x 10'-7 mol/ml by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
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]
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1143922Antioxidant activity assessed as superoxide ion scavenging activity measured as formazone formation at 200 ug/ml after 90 mins by spectrophotometry relative to control2014European journal of medicinal chemistry, Jun-23, Volume: 81Design and synthesis of novel indole-chalcone fibrates as lipid lowering agents.
AID776265Dissociation constant, pKa of the compound at 25 degC2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID1272732Inhibition of butter milk xanthine oxidase (unknown origin) assessed as initial velocity of uric acid formation pre-incubated for 3 mins by spectrophotometry analysis2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Structure-based design and biological evaluation of novel 2-(indol-2-yl) thiazole derivatives as xanthine oxidase inhibitors.
AID1900627Competitive inhibition of xanthine oxidase (unknown origin) assessed as inhibitory constant of enzyme-substrate complex using xanthine as substrate at varying concentrations preincubated for 15 mins followed by substrate addition by UV spectrophotometric 2022European journal of medicinal chemistry, Feb-05, Volume: 229Intramolecular hydrogen bond interruption and scaffold hopping of TMC-5 led to 2-(4-alkoxy-3-cyanophenyl)pyrimidine-4/5-carboxylic acids and 6-(4-alkoxy-3-cyanophenyl)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-ones as potent pyrimidine-based xanthine oxid
AID660255Inhibition of bovine xanthine oxidase assessed as uric acid formation using xanthine as substrate after 30 mins by spectrophotometric analysis2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Identification of novel isocytosine derivatives as xanthine oxidase inhibitors from a set of virtual screening hits.
AID660259Inhibition of bovine xanthine oxidase assessed as uric acid formation using xanthine as substrate at 10 uM after 30 mins by spectrophotometric analysis2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Identification of novel isocytosine derivatives as xanthine oxidase inhibitors from a set of virtual screening hits.
AID770340Antioxidant activity assessed as inhibition of superoxide anion generation at 200 ug/mL after 30 mins by NBT reduction assay relative to control2013European journal of medicinal chemistry, Oct, Volume: 68Hybrid benzofuran-bisindole derivatives: new prototypes with promising anti-hyperlipidemic activities.
AID1075874Antihyperuricemic activity in potassium oxonate-induced hyperuricemic Sprague-Dawley rat model assessed as decrease of uric acid level in serum at 30 mg/kg, po measured after 2 hrs relative to vehicle-treated control2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.
AID1487713Inhibition of bovine xanthine oxidase assessed as reduction in uric acid production using xanthine as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Synthesis and evaluation of 1-phenyl-1H-1,2,3-triazole-4-carboxylic acid derivatives as xanthine oxidase inhibitors.
AID424719Activity at bovine xanthine oxidase at 25 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID384288Inhibition of xanthine oxidase at 100 uM2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis of N-aryl-5-amino-4-cyanopyrazole derivatives as potent xanthine oxidase inhibitors.
AID219739Inhibitory activity against Xanthine Oxidase1996Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13
Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase.
AID1330571Antihyperuricemic activity in fasted Kun Ming mouse assessed as inhibition of potassium oxonate-induced uric acid level in serum at 10 mg/kg qd administered 1 hr post potassium oxonate-challenge for 7 days via oral gavage measured 1 hr post last dose by p2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
AID1234421Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by spectrophotometric analysis2015Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
Discovery of xanthine oxidase inhibitors and/or α-glucosidase inhibitors by carboxyalkyl derivatization based on the flavonoid of apigenin.
AID1330576Antihyperuricemic activity in potassium oxonate-induced Kun Ming mouse model of hyperuricemia assessed as reduction in uric acid level in serum at 10 mg/kg, po qd administered via oral gavage 1 hr post potassium oxonate-challenge for 7 consecutive days by2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
AID334218Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes infected in human HeLa cells assessed as inhibition of amastigotes proliferation at 1 ug/mL after 4 days by HeLa cell-infection assay2002Journal of natural products, Apr, Volume: 65, Issue:4
Monoterpene hydroperoxides with trypanocidal activity from Chenopodium ambrosioides.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1485281Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 3 hrs followed by substrate addition by UV-Vis spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID424725Ratio of kcat to km for bovine xanthine oxidase at 25 uM preincubated for 10 mins2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1183551Inhibition of xanthine oxidase (unknown origin)2014European journal of medicinal chemistry, Sep-12, Volume: 84Flavones: an important scaffold for medicinal chemistry.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1867890Nephroprotective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in tubular-interstitial lesion development at 20 mg/kg, po administered via gavage and measured after 21 days by hematoxylin-eo2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1146436Inhibition of bovine milk xanthine oxidase using xanthine as substrate at 10 times I50 preincubated for 1 hr at 4 degC measured after 10 fold dilution relative to control1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID1082237Inhibition of xanthine oxidase2011Journal of agricultural and food chemistry, May-11, Volume: 59, Issue:9
Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
AID1867889Nephroprotective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in neutrophils infiltrations at 20 mg/kg, po administered via gavage and measured after 21 days by hematoxylin-eosin and Masson2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID396344Antioxidant activity assessed as inhibition of superoxide at 20 ug/mL2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Novel keto-enamine Schiffs bases from 7-hydroxy-4-methyl-2-oxo-2H-benzo[h] chromene-8,10-dicarbaldehyde as potential antidyslipidemic and antioxidant agents.
AID418489Inhibition of xanthine oxidase2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Synthesis, anti-inflammatory, and antioxidant activities of 18beta-glycyrrhetinic acid derivatives as chemical mediators and xanthine oxidase inhibitors.
AID1348939Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 5 mins followed by substrate addition measured every min for 10 mins by spectrophotometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID341681Inhibition of xanthine oxidase2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2',5'-dialkoxylchalcones as cancer chemopreventive agents.
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).
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID351094Cytoprotective activity against H2O2-induced cell death in rat PC12 cells assessed as increase in cell viability at 16 ug/ml preincubated 2 hrs before H2O2 challenge measured after 4 hrs by MTT assay relative to control2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.
AID1485278Inhibition of bovine milk xanthine oxidase assessed using xanthine as substrate after 10 mins by fluorometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1649925Half life in human2019European journal of medicinal chemistry, Mar-15, Volume: 166Pharmacological urate-lowering approaches in chronic kidney disease.
AID1324539Cytotoxicity against African green monkey Vero cells incubated for 24 hrs by neutral red uptake assay2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID449301Inhibition of rat liver xanthine oxidase after 2 hrs by spectrophotometry2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, and examination of neuron protective properties of alkenylated and amidated dehydro-silybin derivatives.
AID776278Stability of the compound in 0.05 M SDS-0.01 M NaH2PO4/H3PO4 assessed as compound recovery at 7.5 x 10'-9 mol/ml by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID625277FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1444596Invivo inhibition of xanthine oxidase in Wistar rat assessed as peak area of 6-MP at 50 mg/kg, ip using 6-mercaptopurine as substrate after 6 hrs by UPLC method (Rvb = 7.3 mAU)2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies.
AID614334Antihyperuricemic activity in Swiss mouse assessed as decrease of potassium oxonate-induced uric acid level in serum at 10 mg/kg, ip after 3 hrs by HPLC analysis (Rvb = 7.80 +/- 0.34 uM)2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors.
AID681371TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Molecular pharmacology, Jul, Volume: 62, Issue:1
Isolation, characterization and differential gene expression of multispecific organic anion transporter 2 in mice.
AID481286Antioxidant activity assessed as inhibition of xanthine-xanthine oxidase generated superoxide anion radical production assessed as formazone formation at 20 ug/ml after 30 mins by spectrophotometric analysis2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Synthesis of novel benzocoumarin derivatives as lipid lowering agents.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID424722Ratio of kcat to km for bovine xanthine oxidase at 10 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID351093Cytoprotective activity against H2O2-induced cell death in rat PC12 cells assessed as increase in cell viability at 8 ug/ml preincubated 2 hrs before H2O2 challenge measured after 4 hrs by MTT assay relative to control2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1867923Renal protective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in extracellular matrix protein deposition by measuring interstitial expansion with collagen accumulation at 20 mg/kg, po admin2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID776295Antimicrobial activity against Trypanosoma cruzi RA amastigotes infected in African green monkey Vero cells assessed as growth inhibition at 1 ug/ml after 72 hrs by Giemsa staining-based light microscopy2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
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).
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1485271Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate after 4 mins by UV-Vis spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID1867883Anti-hyperuricemic activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as blood urea nitrogen level at 20 mg/kg, po administered via gavage once daily for 2 weeks (Rvb = 9.88 +/- 1.21 mM)2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID424718Activity at bovine xanthine oxidase at 10 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
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.
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).
AID1348945Antiproliferative activity against human MCF7 cells at 30 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
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.
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.
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.
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.
AID173963Tested for hypouricemic effect in potassium oxonate (uricase inhibitor) treated (po)rats for 0-6 hr expressed as ED202001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
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.
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.
AID1651325In vivo inhibition of xanthine oxidase in mouse assessed as reduction in enzyme activity in liver at 10 mg/kg relative to control2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Development of novel NLRP3-XOD dual inhibitors for the treatment of gout.
AID1310994Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate assessed as inhibition of uric acid formation after 30 mins by spectrophotometric method2016European journal of medicinal chemistry, Aug-25, Volume: 119On the vasoprotective mechanisms underlying novel β-phosphorylated nitrones: Focus on free radical characterization, scavenging and NO-donation in a biological model of oxidative stress.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1594173Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation preincubated for 5 mins followed by xanthine addition and measured after 20 mins by spectrophotometry2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Design, synthesis and bioevaluation of 3-oxo-6-aryl-2,3-dihydropyridazine-4-carbohydrazide derivatives as novel xanthine oxidase inhibitors.
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.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
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).
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1165425Inhibition of buttermilk xanthine oxidase (unknown origin) incubated for 10 mins by spectrophotometry2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
Substituted thieno[2,3-b]thiophenes and related congeners: Synthesis, β-glucuronidase inhibition activity, crystal structure, and POM analyses.
AID776279Octanol-water partition coefficient, log P of the compound by RP-HPLC analysis2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID607703Antioxidant activity assessed as inhibition of xanthine-xanthine oxidase generated superoxide anion radical production assessed as formazone formation at 20 ug/ml after 30 mins by spectrophotometric analysis2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis and anti-inflammatory activity of novel biscoumarin-chalcone hybrids.
AID1444593Inhibition of bovine xanthine oxidase using xanthine as substrate preincubated for 10 mins followed by substrate addition measured for 15 mins by spectrophotometric method2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies.
AID1330578Antihyperuricemic activity in potassium oxonate-induced Kun Ming mouse model of hyperuricemia assessed as uricosuric activity by measuring increase in urinary uric acid excretion at 10 mg/kg, po qd administered via oral gavage 1 hr post potassium oxonate-2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
AID1146437Inhibition of bovine milk xanthine oxidase using xanthine as substrate at 10 times I50 preincubated for 20 mins at 25 degC measured after 10 fold dilution relative to control1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
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.
AID174770Effect of AOS scavenger on ventricular fibrillation (VF),arrhythmias induced by ischemia-reperfusion in anesthetized rat, duration at 20 mg/kg1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids.
AID717724Inhibition of xanthine oxidase using xanthine as substrate at 30 mins by spectrophotometric analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Isocytosine-based inhibitors of xanthine oxidase: design, synthesis, SAR, PK and in vivo efficacy in rat model of hyperuricemia.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1146439Activity at bovine milk xanthine oxidase assessed as reduction of 2,6-dichlorophenol-indophenol1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID1537337Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid production using xanthine as substrate after 10 mins by HPLC analysis2019Journal of natural products, 02-22, Volume: 82, Issue:2
Propolis Components from Stingless Bees Collected on South Sulawesi, Indonesia, and Their Xanthine Oxidase Inhibitory Activity.
AID1867917Renal protective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in urate accumulation in kidney at 20 mg/kg, po administered via gavage for 2 weeks by polarization microscopic analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1753483Antileishmanial activity against amastigote form of Leishmania infantum MHOM/MA(BE)/67 infected in Swiss mouse peritoneal macrophages assessed as reduction in parasite growth treated at 2 hrs post-infection and measured after 5 days by Giemsa staining bas2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID1851314Anti-hyperuricemic activity against hypoxanthine and oteracil potassium induced hyperuricemia in Kunming mouse model assessed as alanine aminotransferase level at 5 mg/kg, IG administered daily (Rvb = 28.05 +/- 8.478 U/L)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1324551Inhibition of Shigella dysenteriae Shiga toxin-induced mortality in Balb/c mouse exposed to 5 x LD50 Shigella toxin assessed as increase in mouse survival at 2 mM, ip dosed 1 after toxin injection measured after 24 to 48 hrs2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID27575HPLC capacity factor (k)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID1637837Inhibition of bovine milk xanthine oxidase using xanthine as substrate preincubated for 5 mins followed by substrate addition by UV-visible spectrophotometry2019MedChemComm, Jan-01, Volume: 10, Issue:1
Benzoflavone derivatives as potent antihyperuricemic agents.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID399340Inhibition of xanthine oxidase assessed as decrease in uric acid production by spectrophotometry1998Journal of natural products, Jan, Volume: 61, Issue:1
Structure-activity relationship and classification of flavonoids as inhibitors of xanthine oxidase and superoxide scavengers.
AID170002Effect of AOS scavenger on premeture ventricular complexes PVCs, arrhythmias induced by ischemia-reperfusion in anesthetized rat, duration at 20 mg/kg; PVSc/min1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids.
AID219599In vitro inhibitory concentration against Xanthine oxidase2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
AID682403Inhibition of bovine milk XO assessed as decrease in uric acid formation after 5 mins by UV-spectrophotometric analysis2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Synthesis, biological evaluation, and molecular docking of N-{3-[3-(9-methyl-9H-carbazol-3-yl)-acryloyl]-phenyl}-benzamide/amide derivatives as xanthine oxidase and tyrosinase inhibitors.
AID26380Dissociation constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID776275Stability of the compound in 0.1 M SDS-0.01 M 7.5% (v/v) 1-propanol-NaH2PO4/H3PO4 assessed as compound recovery at 7.5 x 10'-9 mol/ml by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID274547Inhibition of [3H]hypoxanthine uptake in Plasmodium falciparum 3D72006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1502932Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate pretreated for 10 mins followed by substrate addition measured every 2 mins for 6 mins2017Journal of natural products, 10-27, Volume: 80, Issue:10
Berchemiosides A-C, 2-Acetoxy-ω-phenylpentaene Fatty Acid Triglycosides from the Unripe Fruits of Berchemia berchemiifolia.
AID776273Stability of the compound in 0.1 M SDS-0.01 M 7.5% (v/v) 1-propanol-NaH2PO4/H3PO4 assessed as compound recovery at 3.5 x 10'-7 mol/ml by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID584550Cytotoxicity against mouse J774A1 cells2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Testing nucleoside analogues as inhibitors of Bacillus anthracis spore germination in vitro and in macrophage cell culture.
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).
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1082238Inhibition of Oryctolagus cuniculus (rabbit) AOX in liver cytosol2011Journal of agricultural and food chemistry, May-11, Volume: 59, Issue:9
Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
AID1868685Cytotoxicity against Swiss mouse peritoneal macrophages assessed as reduction in cell viability measured after 5 days by microscopic analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents.
AID418488Antioxidant activity assessed as DPPH radical scavenging activity2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Synthesis, anti-inflammatory, and antioxidant activities of 18beta-glycyrrhetinic acid derivatives as chemical mediators and xanthine oxidase inhibitors.
AID687692Antioxidant activity assessed as inhibition of superoxide anion radical generation at 200 ug/ml by spectrophotometry2012European journal of medicinal chemistry, Nov, Volume: 57Discovery of amide based fibrates as possible antidyslipidemic and antioxidant agents.
AID173961Tested for hypouricemic effect in potassium oxonate (uricase inhibitor) treated (po) rats for 0-24 hr expressed as ED202001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
AID1435053Inhibition of bovine xanthine oxidase assessed as reduction in uric acid levels using xanthine as substrate after 120 mins by spectrophotometry2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Discovery and biological evaluation of some (1H-1,2,3-triazol-4-yl)methoxybenzaldehyde derivatives containing an anthraquinone moiety as potent xanthine oxidase inhibitors.
AID29344Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
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.
AID614335Antihyperuricemic activity in Swiss mouse assessed as decrease of potassium oxonate-induced uric acid level in serum at 20 mg/kg, ip after 3 hrs by HPLC analysis (Rvb = 7.80 +/- 0.34 uM)2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors.
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).
AID334215Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes infected in human HeLa cells assessed as number of amastigotes per infected cell at 1 ug/mL after 4 days by HeLa cell-infection assay2002Journal of natural products, Apr, Volume: 65, Issue:4
Monoterpene hydroperoxides with trypanocidal activity from Chenopodium ambrosioides.
AID1867912Cytoprotective activity in human HK-2 cells assessed as reduction in uric acid-induced cell remodeling at 25 uM by inverted light microscopic analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1348940Antioxidant activity assessed as DPPH radical scavenging activity at 30 uM after 20 mins by spectrophotometric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1485264Binding affinity to bovine milk xanthine oxidase assessed as reduction in conversion of 4-HPP to 4,6-diHPP by measuring cytochrome c reduction by spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID1146449Dissociation constant, pKa of the compound1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID584546Inhibition of inosine/L-alanine-induced Bacillus anthracis Sterne 34F2 spore germination pretreated for 15 mins before inosine/L-alanine challenge2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Testing nucleoside analogues as inhibitors of Bacillus anthracis spore germination in vitro and in macrophage cell culture.
AID491531Binding affinity to Mycobacterium tuberculosis purine nucleoside phosphorylase by spectrophotometric analysis2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Crystallographic and docking studies of purine nucleoside phosphorylase from Mycobacterium tuberculosis.
AID398996Inhibition of xanthine oxidase2005Journal of natural products, Nov, Volume: 68, Issue:11
Free-radical-scavenging and xanthine oxidase inhibitory constituents from Stereospermum personatum.
AID1433308Inhibition of Xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 3 mins followed by substrate addition measured every 15 secs for 7 mins by spectrophotometry2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and evaluation of xanthine oxidase inhibitory and antioxidant activities of 2-arylbenzo[b]furan derivatives based on salvianolic acid C.
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).
AID384287Inhibition of xanthine oxidase2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis of N-aryl-5-amino-4-cyanopyrazole derivatives as potent xanthine oxidase inhibitors.
AID1867879Anti-hyperuricemic activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in serum uric acid level at 20 mg/kg, po administered via gavage once daily for 2 weeks (Rvb = 318.16 +/- 3.31 uM)2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1485276Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 5 mins followed by substrate addition by UV-Vis spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID776290Metabolic stability of the compound in human plasma2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID1651286Inhibition of xanthine oxidase (unknown origin)2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Development of novel NLRP3-XOD dual inhibitors for the treatment of gout.
AID355479Inhibition of cow milk xanthine oxidase
AID1485285Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate after 30 mins by UV-Vis spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID274550Inhibition of Plasmodium falciparum HGXPRT at pH 7.42006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1867887Nephroprotective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as appearance of clear tubular structures at 20 mg/kg, po administered via gavage and measured after 21 days by hematoxylin-eosin and Masson2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID424730Inhibition of bovine xanthine oxidase assessed as reduction of cytochrome c at 25 uM preincubated for 10 mins2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID274562Inhibition of human HGPRT at pH 8.52006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
AID1851315Anti-hyperuricemic activity against hypoxanthine and oteracil potassium induced hyperuricemia in Kunming mouse model assessed as total bilirubin level at 5 mg/kg, IG administered daily (Rvb = 12.05 +/- 4.92 uM)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
AID1234423Hypouricemic activity in ICR mouse assessed as decrease in potassium oxonate-induced serum uric acid level at 10 mg/kg, ip after 1 hr by Uricase colorimetric method2015Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
Discovery of xanthine oxidase inhibitors and/or α-glucosidase inhibitors by carboxyalkyl derivatization based on the flavonoid of apigenin.
AID380589Inhibition of xanthine oxidase by spectrophotometry1999Journal of natural products, Jul, Volume: 62, Issue:7
New guaianolides and xanthine oxidase inhibitory flavonols from ajania fruticulosa
AID274560Antimalarial activity against Plasmodium falciparum2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
AID776294Antimicrobial activity against Trypanosoma cruzi RA amastigotes infected in African green monkey Vero cells assessed as growth inhibition after 72 hrs by Giemsa staining-based light microscopy2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1868684Antileishmanial activity against intracellular Leishmania infantum MHOM/MA(BE)/67 ITMAP263 amastigotes infected in Swiss mouse peritoneal macrophage assessed as inhibition of parasite growth measured after 5 days by geimsa staining based microscopic analy2022European journal of medicinal chemistry, Jul-05, Volume: 237Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID722986Inhibition of Wistar albino rat xanthine oxidase isolated from liver using xanthine as substrate incubated for 15 mins prior to substrate addition by spectrophotometric analysis2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Trisubstituted thiophene analogues of 1-thiazolyl-2-pyrazoline, super oxidase inhibitors and free radical scavengers.
AID584547Antibacterial activity against Bacillus anthracis Sterne 34F2 infected in mouse J774A.1 cells assessed as protection against bacteria-induced cytotoxicity using propidium iodide staining after 3 hrs measured every hours for up to 7 hrs2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Testing nucleoside analogues as inhibitors of Bacillus anthracis spore germination in vitro and in macrophage cell culture.
AID1649924Tmax in human2019European journal of medicinal chemistry, Mar-15, Volume: 166Pharmacological urate-lowering approaches in chronic kidney disease.
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).
AID1324549Inhibition of Shigella dysenteriae Shiga toxin-induced mortality in Balb/c mouse exposed to 5 x LD50 Shigella toxin assessed as reduction in symptomatic effects of toxin at 2 mM, ip preincubated with Stx for 1 hr measured after 0 to 14 days2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID479084Inhibition of xanthine oxidase2010Journal of natural products, May-28, Volume: 73, Issue:5
Glutarimide alkaloids and a terpenoid benzoquinone from Cordia globifera.
AID424724Ratio of kcat to km for bovine xanthine oxidase at 50 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1146443Mixed-type inhibition of bovine milk xanthine oxidase using xanthine as substrate by Lineweaver-Burk plot analysis1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID776276Stability of the compound in 0.05 M SDS-0.01 M NaH2PO4/H3PO4 assessed as compound recovery at 6 x 10'-8 mol/ml by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
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.
AID1500521Inhibition of butter milk XOD (unknown origin) at 10 uM using xanthine as substrate after 8 mins relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Structure-activity relations of rosmarinic acid derivatives for the amyloid β aggregation inhibition and antioxidant properties.
AID399341Antioxidant activity assessed as superoxide-scavenging activity by nitrite method1998Journal of natural products, Jan, Volume: 61, Issue:1
Structure-activity relationship and classification of flavonoids as inhibitors of xanthine oxidase and superoxide scavengers.
AID274549Inhibition of human HGPRT at pH 7.42006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID443181Antioxidant activity assessed as superoxide radical scavenging activity at 200 ug/ml2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis and biological evaluation of N-aryl-1,4-dihydropyridines as novel antidyslipidemic and antioxidant agents.
AID274563Inhibition of Plasmodium falciparum HGXPRT at pH 8.52006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
AID1503694Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 10 mins followed by substrate addition by UV spectrophotometric method2017European journal of medicinal chemistry, Dec-01, Volume: 141Design, synthesis and biological evaluation of N-(4-alkoxy-3-cyanophenyl)isonicotinamide/nicotinamide derivatives as novel xanthine oxidase inhibitors.
AID1865993Inhibition of xanthine oxidase (unknown origin) at 10 uM using xanthine as substrate2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Isolation and biological activity of azocine and azocane alkaloids.
AID1146438Activity at bovine milk xanthine oxidase assessed as reduction of cytochrome c and phenazine methosulfate1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID1424732Inhibition of bovine xanthine oxidase using xanthine as substrate preincubated for 3 mins followed by substrate addition and measured for every 15 secs for 7 mins by spectrophotometric analysis2018European journal of medicinal chemistry, May-10, Volume: 151Design, synthesis and biological evaluation of novel xanthine oxidase inhibitors bearing a 2-arylbenzo[b]furan scaffold.
AID1753485Selectivity index, ratio of CC50 for Swiss mouse peritoneal macrophages to IC50 for antileishmanial activity against amastigote form of Leishmania infantum MHOM/MA(BE)/67 infected in Swiss mouse peritoneal macrophages2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID776274Stability of the compound in 0.1 M SDS-0.01 M 7.5% (v/v) 1-propanol-NaH2PO4/H3PO4 assessed as compound recovery at 6 x 10'-8 mol/ml by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID1608490Hypouricemic activity in Kunming mouse model of potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid level at 10 mg/kg, ig administered after 3 hrs of potassium oxonate challenge and measured after 3 hrs2019European journal of medicinal chemistry, Nov-01, Volume: 181Targeting the subpocket in xanthine oxidase: Design, synthesis, and biological evaluation of 2-[4-alkoxy-3-(1H-tetrazol-1-yl) phenyl]-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives.
AID1485269Inhibition of bovine milk xanthine-oxygen reductase using xanthine as substrate by spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID1272635Inhibition of xanthine oxidase (unknown origin)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Hydroxylated chalcones with dual properties: Xanthine oxidase inhibitors and radical scavengers.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1330584Antihyperuricemic activity in potassium oxonate-induced Kun Ming mouse model of hyperuricemia assessed as oxonate-induced hepatic XOD activity at 10 mg/ kg, po qd administered 1 hr post potassium oxonate-challenge for 7 consecutive days via oral gavage re2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1324542Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by LDH release assay relative to u2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID29363Dissociation constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1444510Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate pretreated for 5 mins followed by substrate addition measured by UV-vis spectrophotometric method2017European journal of medicinal chemistry, May-05, Volume: 131Synthesis, screening and docking of fused pyrano[3,2-d]pyrimidine derivatives as xanthine oxidase inhibitor.
AID521220Inhibition of neurosphere proliferation of 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.
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.
AID1324536Inhibition of Shigella dysenteriae Shiga toxin-induced mortality in Balb/c mouse exposed to 5 x LD50 Shigella toxin assessed as increase in mouse survival at 2 mM, ip preincubated with Stx for 1 hr measured after 0 to 14 days2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1851316Anti-hyperuricemic activity against hypoxanthine and oteracil potassium induced hyperuricemia in Kunming mouse model assessed as blood urea nitrogen level at 5 mg/kg, IG administered daily (Rvb = 53.09 +/- 1.937 mg/dl)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
AID1649918Inhibition of xanthine oxidase (unknown origin)2019European journal of medicinal chemistry, Mar-15, Volume: 166Pharmacological urate-lowering approaches in chronic kidney disease.
AID552788Inhibition of microbial xanthine oxidase by spectrophotometry2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis and xanthine oxidase inhibitory activity of 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives.
AID29421Partition coefficient (logP) (HPLC)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID489931Antioxidant activity assessed as inhibition non-enzymatic reactants generated superoxide anion at 20 ug/ml by spectrophotometry2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Novel coumarin derivatives as potential antidyslipidemic agents.
AID287937Inhibition of human xanthine oxidase2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.
AID1348944Inhibition of xanthine oxidase (unknown origin) at 30 uM using xanthine as substrate preincubated for 5 mins followed by substrate addition measured every min for 10 mins by spectrophotometric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1461521Antioxidant activity assessed as DPPH free radical scavenging activity incubated for 30 mins at 2000 uM2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1736372Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 25 mins followed by substrate addition measured at first 2 mins by spectrophotometric analysis2020European journal of medicinal chemistry, Mar-15, Volume: 190Design, synthesis and biological evaluation of 1-alkyl-5/6-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-1H-indole-3-carbonitriles as novel xanthine oxidase inhibitors.
AID1435052Inhibition of bovine xanthine oxidase assessed as reduction in uric acid levels at 50 uM using xanthine as substrate after 120 mins by spectrophotometry2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Discovery and biological evaluation of some (1H-1,2,3-triazol-4-yl)methoxybenzaldehyde derivatives containing an anthraquinone moiety as potent xanthine oxidase inhibitors.
AID1867874In vivo inhibition of XOD in adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in XOD activity in liver at 20 mg/kg, po administered via gavage once daily for 2 weeks2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1485274Inhibition of butter milk xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate by spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID351097Inhibition of xanthine oxidase assessed as formation of formazan after 2 hrs by spectrophotometry2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.
AID1753480Antitrypanosomal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC-5 SV2 cells assessed as inhibition of parasite growth measured after 7 days by spectrophotometric analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID1298770Inhibition of bovine milk xanthine oxidase using xanthine as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric method2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Anti-gout nor-oleanane triterpenoids from the leaves of Stauntonia brachyanthera.
AID170014Effect of compound on catalase measured as disappearance of H2O2 in isolated rat heart muscle subjected to global ischemia2001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Beneficial effects of different flavonoids, on functional recovery after ischemia and reperfusion in isolated rat heart.
AID1146441Mixed-type inhibition of bovine milk xanthine oxidase using hypoxanthine as substrate by Lineweaver-Burk plot analysis1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID392225Antioxidant activity assessed as reduction in generation of superoxide radicals at 100 ug/mL measured as formazone formation by spectrophotometry relative to control2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Syntheses and evaluation of glucosyl aryl thiosemicarbazide and glucosyl thiosemicarbazone derivatives as antioxidant and anti-dyslipidemic agents.
AID1324540Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by neutral red uptake assay relati2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1867881Anti-hyperuricemic activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in serum creatinine level at 20 mg/kg, po administered via gavage once daily for 2 weeks (Rvb = 87.62 +/- 0.67 uM)2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID351098Inhibition of xanthine oxidase assessed as formation of formazan at 16 ug/ml after 2 hrs by spectrophotometry2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1485273Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate measured at every 1 mins up to 5 mins2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
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.
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]
AID288650Inhibition of superoxide production by xanthine/xanthine oxidase method2007Journal of natural products, Jun, Volume: 70, Issue:6
Anti-inflammatory thiazine alkaloids isolated from the New Zealand ascidian Aplidium sp.: inhibitors of the neutrophil respiratory burst in a model of gouty arthritis.
AID348893Antioxidant activity assessed as inhibition of xanthine-xanthine oxidase generated superoxide anion radical production at 0.5 mM2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and free radical scavenging activity of some new spiropyranocoumarins.
AID776292Intrinsic solubility of the compound in standard phosphate buffer at pH 6.8 at 25 degC after 24 hrs by shake-flask method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID1405945Inhibition of xanthine oxidase (unknown origin)2018European journal of medicinal chemistry, Aug-05, Volume: 156Current progress on antioxidants incorporating the pyrazole core.
AID1851317Anti-hyperuricemic activity against hypoxanthine and oteracil potassium induced hyperuricemia in Kunming mouse model assessed as creatinine level at 5 mg/kg, IG administered daily (Rvb = 59.12 +/- 7.198 uM)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1324544Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by neutral red uptake assay2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1444595Invivo inhibition of xanthine oxidase in Wistar rat assessed as retention time of 6-MP at 50 mg/kg, ip using 6-mercaptopurine as substrate after 6 hrs by UPLC method (Rvb = 4.912 min)2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies.
AID219595Inhibition of Xanthine oxidase2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Novel 3-O-acyl mesquitol analogues as free-radical scavengers and enzyme inhibitors: synthesis, biological evaluation and structure-activity relationship.
AID717696Antihyperuricemic activity in fasted rat assessed as reduction in potassium oxonate-induced uric acid level in serum at 100 mg/kg, ip administered 1 hr post potassium oxonate-challenge relative to vehicle-treated control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Isocytosine-based inhibitors of xanthine oxidase: design, synthesis, SAR, PK and in vivo efficacy in rat model of hyperuricemia.
AID1878317In vivo Hypouricemic activity against potassium oxonate-induced hyperuricemia rat model assessed as reduction in serum uric acid production at 8 mg/kg, po measured after 2 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Discovery of 4-(phenoxymethyl)-1H-1,2,3-triazole derivatives as novel xanthine oxidase inhibitors.
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.
AID670363Inhibition of xanthine oxidase- mediated uric acid formation at 50 ug/mL after 5 mins by spectrophotometry2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Xanthine oxidase inhibitory activity of constituents of Cinnamomum cassia twigs.
AID1082239Inhibition of Agaricus bisporus (mushroom) tyrosinase2011Journal of agricultural and food chemistry, May-11, Volume: 59, Issue:9
Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
AID1867885Nephroprotective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in renal tubule dilation at 20 mg/kg, po administered via gavage and measured after 21 days by hematoxylin-eosin and Masson tri2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID183793Effect of AOS scavenger on ventricular tachycardia (VT),arrhythmias induced by ischemia-reperfusion in anesthetized rat, incidence at 20 mg/kg; 8/81988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids.
AID776268Stability of the compound in simulated intestinal fluid assessed as retention time by micellar liquid chromatography2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID174778Effect of AOS scavenger on ventricular tachycardia (VT),arrhythmias induced by ischemia-reperfusion in anesthetized rat, duration at 20 mg/kg1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids.
AID1461517Inhibition of bovine milk xanthine oxidase pre-incubated for 30 mins followed by xanthine addition and measured every 30 secs for 5 mins by spectrophotometry2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia.
AID219741Inhibitory activity against Xanthine Oxidase1996Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13
Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase.
AID614370Inhibition of bovine milk xanthine oxidase assessed as decrease of uric acid formation preincubated for 5 mins by UV-visible spectrophotometric analysis2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors.
AID1389558Inhibition of Xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 1 to 5 mins followed by substrate addition2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.
AID1330587Decrease in potassium oxonate-induced renal URAT1 expression in Kun Ming mouse model of hyperuricemia at 10 mg/ kg, po qd administered 1 hr post potassium oxonate-challenge for 7 consecutive days via oral gavage by Western blot method relative to oxonate-2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
AID1269361Non-competitive inhibition of xanthine oxidase (unknown origin) by Lineweaver-Burk plot analysis2016Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
9-Benzoyl 9-deazaguanines as potent xanthine oxidase inhibitors.
AID1324550Inhibition of Shigella dysenteriae Shiga toxin-induced mortality in Balb/c mouse exposed to 5 x LD50 Shigella toxin assessed as increase in mouse survival at 2 mM, ip dosed 1 hr before toxin injection measured after 24 to 48 hrs2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1330588Antihyperuricemic activity in potassium oxonate-induced Kun Ming mouse model of hyperuricemia assessed as reduction in hepatic uric acid level at 10 mg/kg, po qd administered via oral gavage 1 hr post potassium oxonate-challenge for 7 consecutive days by 2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic agents.
AID626109Antioxidant activity assessed as xanthine-xanthine oxidase generated superoxide anion scavenging at 200 mg/ml after 30 mins by NBT reduction assay2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Synthesis of novel N-(2-hydroxy-2-p-tolylethyl)-amide and N-(2-oxo-2-p-tolylethyl)-amide derivatives and their antidyslipidemic and antioxidant activity.
AID1146448Inhibition of bovine milk xanthine oxidase using xanthine as substrate assessed as increase of I50 at pH 6.6 to 7.51976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID387152Inhibition of xanthine oxidase assessed as decrease of uric acid generation2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
ortho-dihydroxyisoflavone derivatives from aged Doenjang (Korean fermented soypaste) and its radical scavenging activity.
AID1402016Inhibition of bovine milk xanthine oxidase using xanthine as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by UV-VIS spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Xanthine oxidase inhibitory activity of natural and hemisynthetic flavonoids from Gardenia oudiepe (Rubiaceae) in vitro and molecular docking studies.
AID1867902Anti-hyperuricemic activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as blood urea nitrogen level at 20 mg/kg, po administered via gavage once daily for 4 weeks (Rvb = 15.25 +/- 1.21 mM)2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1867877Inhibition of bovine XOD assessed as inhibition of uric acid formation using xanthine as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured for 30 mins by microplate reader analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1444597Invivo inhibition of xanthine oxidase in Wistar rat at 50 mg/kg, ip using 6-mercaptopurine as substrate after 6 hrs by UPLC method relative to control2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies.
AID467250Inhibition of XOD2009Journal of natural products, Jun, Volume: 72, Issue:6
Chemical constituents from the aerial parts of Artemisia minor.
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.
AID1851312Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
AID1868687Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 3 days by resazurin dye based fluorescence analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents.
AID424723Ratio of kcat to km for bovine xanthine oxidase at 25 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1753484Cytotoxicity against Swiss mouse peritoneal macrophages assessed as cell detachment, lysis and granulation measured after 5 days by microscopic analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID1324537Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID424720Activity at bovine xanthine oxidase at 50 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID660258Antihyperuricemic activity in Sprague-Dawley rat assessed as decrease of potassium oxonate-induced uric acid level in serum at 10 mg/kg, ip administered 1 hr post potassium oxonate challenge measured after 4 hrs by photometric analysis relative to control2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Identification of novel isocytosine derivatives as xanthine oxidase inhibitors from a set of virtual screening hits.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID351095Cytoprotective activity against H2O2-induced cell death in rat PC12 cells assessed as increase in cell viability at 32 ug/ml preincubated 2 hrs before H2O2 challenge measured after 4 hrs by MTT assay relative to control2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.
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]
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1324545Selectivity index, ratio of CC50 for cytotoxicity against African green monkey Vero cells to IC50 for nhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1867899Anti-hyperuricemic activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in creatinine level at 20 mg/kg, po administered via gavage once daily for 4 weeks (Rvb = 76.87 +/- 0.67 uM)2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1082233Inhibition of Agaricus bisporus (mushroom) tyrosinase at IC50 concentration2011Journal of agricultural and food chemistry, May-11, Volume: 59, Issue:9
Neonicotinoid insecticides: oxidative stress in planta and metallo-oxidase inhibition.
AID1324543Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as protection of cell membrane integrity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by LDH release assay relative to un2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID469638Reduction of uric acid level in rat serum at 0.3 mg/kg, po after 2 hrs by phosphotungstic acid method2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected].
AID578685Inhibition of bovine Xanthine oxidase assessed as decrease in uric acid production preincubated at 293 nM of compound for 5 mins by spectrophotometry2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
A rational approach for the design and synthesis of 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles as a new class of potential non-purine xanthine oxidase inhibitors.
AID1185461Inhibition of human xanthine oxidase2014Journal of natural products, Jul-25, Volume: 77, Issue:7
X-ray crystal structure of a xanthine oxidase complex with the flavonoid inhibitor quercetin.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID387151Inhibition of xanthine oxidase assessed as decrease of superoxide generation2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
ortho-dihydroxyisoflavone derivatives from aged Doenjang (Korean fermented soypaste) and its radical scavenging activity.
AID1485284Inhibition of xanthine oxidase (unknown origin) by SAR analysis2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID183781Effect of AOS scavenger on ventricular fibrillation (VF),arrhythmias induced by ischemia-reperfusion in anesthetized rat, incidence at 20 mg/kg; 4/81988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Studies on scavengers of active oxygen species. 1. Synthesis and biological activity of 2-O-alkylascorbic acids.
AID338970Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes infected in human HeLa cells assessed as infection rate at 1 ug/mL after 4 days by HeLa cell-infection assay2002Journal of natural products, Apr, Volume: 65, Issue:4
Monoterpene hydroperoxides with trypanocidal activity from Chenopodium ambrosioides.
AID1379542Inhibition of cow milk xanthine oxidoreductase using hypoxanthine by spectrophotometry2017European journal of medicinal chemistry, Nov-10, Volume: 140Synthesis and bioevaluation of 1-phenyl-pyrazole-4-carboxylic acid derivatives as potent xanthine oxidoreductase inhibitors.
AID378013Inhibition of xanthine oxidase2006Journal of natural products, Jul, Volume: 69, Issue:7
An apigenin-derived xanthine oxidase inhibitor from Palhinhaea cernua.
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.
AID552786Inhibition of rat liver xanthine oxidase by spectrophotometry2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis and xanthine oxidase inhibitory activity of 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives.
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).
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1461525Anti-hyperuricemic activity in potassium oxonate-induced hyperuricemic Kun-Ming mouse assessed as xanthine oxidase activity per gram of protein at 10 mg/kg/day, ig for 7 days and measured 1 hr post last dose (Rvb = 81.5 +/- 1.4 U/g protein)2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia.
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1348946Antiproliferative activity against NHDF at 30 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID469634Reduction of uric acid level in rat serum at 0.3 mg/kg, po after 6 hrs by phosphotungstic acid method2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected].
AID1651292In vivo inhibition of xanthine oxidase in potassium oxonate-induced hyperuricemia mouse model assessed as reduction enzyme activity in liver at 10 mg/kg relative to control2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Development of novel NLRP3-XOD dual inhibitors for the treatment of gout.
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).
AID1485280Inhibition of xanthine oxidase (unknown origin) assessed as reduction in uric acid formation using xanthine as substrate after 10 mins2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID776293Cytotoxicity against mouse splenocytes assessed as cell viability at 50 times IC50 after 32 hrs by Alamar Blue assay2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
AID1424739Hypouricemic effect in ICR mouse model of potassium oxonate-induced acute hyperuricemia assessed as reduction in serum uric acid levels at 10 mg/kg, iv measured at 1 hr post dose2018European journal of medicinal chemistry, May-10, Volume: 151Design, synthesis and biological evaluation of novel xanthine oxidase inhibitors bearing a 2-arylbenzo[b]furan scaffold.
AID776229Antioxidant activity assessed as decrease in superoxide anions level by measuring formation of formazone at 200 ug/ml after 30 mins by spectrophotometric analysis relative to control2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis of new andrographolide derivatives and evaluation of their antidyslipidemic, LDL-oxidation and antioxidant activity.
AID1324552Toxicity in Balb/c mouse at 2 mM, ip measured after 0 to 14 days2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1210795Inhibition of human liver cytosolic aldehyde oxidase using DACA as substrate by LC-MS/MS analysis relative to control2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Evidence for substrate-dependent inhibition profiles for human liver aldehyde oxidase.
AID469633Inhibition of bovine milk XOR-mediated uric acid formation after 15 mins by spectrophotometer2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected].
AID170013Effect of compound on Glutathione peroxidase measured as disappearance of NADPH in isolated rat heart muscle subjected to global ischemia2001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Beneficial effects of different flavonoids, on functional recovery after ischemia and reperfusion in isolated rat heart.
AID287938Inhibition of human xanthine oxidase at 30 uM2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
The screening and characterization of 6-aminopurine-based xanthine oxidase inhibitors.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1851313Anti-hyperuricemic activity against hypoxanthine and oteracil potassium induced hyperuricemia in Kunming mouse model assessed as uric acid level at 5 mg/kg, IG administered daily (Rvb = 631.6 +/- 103.1 uM)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Discovery of derivatives from Spartina alterniflora-sourced moiety as xanthine oxidase inhibitors to lower uric acid.
AID384323Inhibition of xanthine oxidase assessed as uric acid formation by spectrophotometry2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Schiff base transition metal complexes as novel inhibitors of xanthine oxidase.
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).
AID776266Drug degradation in 0.1 M NaOH at 1 mg/ml at 90 degC after 16 hrs2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID728035Inhibition of bovine xanthine oxidase-mediated uric acid production after 30 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Lead optimization of isocytosine-derived xanthine oxidase inhibitors.
AID406380Inhibition of xanthine oxidase2008Journal of natural products, Jun, Volume: 71, Issue:6
Phloroglucinols with antioxidant activity and xanthonolignoids from the heartwood of Hypericum geminiflorum.
AID1146435Inhibition of bovine milk xanthine oxidase using xanthine as substrate1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.
AID443180Antioxidant activity assessed as superoxide radical scavenging activity at 100 ug/ml2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis and biological evaluation of N-aryl-1,4-dihydropyridines as novel antidyslipidemic and antioxidant agents.
AID1443986Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID374056Antioxidant activity assessed as inhibition of xanthine-xanthine oxidase generated superoxide anion radical production at 20 ug/ml by spectrophotometry2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Antidyslipidemic and antioxidative activities of 8-hydroxyquinoline derived novel keto-enamine Schiffs bases.
AID1330581In vivo inhibition of potassium oxonate-induced hepatic XOD activity in Kun Ming mouse model of hyperuricemia at 10 mg/ kg, po qd administered 1 hr post potassium oxonate-challenge for 7 consecutive days via oral gavage relative to control2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Discovery of novel curcumin derivatives targeting xanthine oxidase and urate transporter 1 as anti-hyperuricemic 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).
AID1461520Antioxidant activity assessed as ABTS free radical scavenging activity by measuring trolox equivalents after 6 mins2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia.
AID424728Inhibition of bovine xanthine oxidase assessed as reduction of cytochrome c at 20 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1064493Inhibition of bovine milk xanthine oxidase using xanthine as substrate assessed as decrease in uric acid formation preincubated for 5 mins2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Microwave assisted synthesis of naphthopyrans catalysed by silica supported fluoroboric acid as a new class of non purine xanthine oxidase inhibitors.
AID1369117Inhibition of bovine milk xanthine oxidase using xanthine as substrate pretreated for 15 mins followed by substrate addition measured after 8 mins2018Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
Synthesis, structure-activity relationships, and mechanistic studies of 5-arylazo-tropolone derivatives as novel xanthine oxidase (XO) inhibitors.
AID1570304Inhibition of bovine xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated with enzyme for 15 mins followed by substrate addition and measured every 30 secs for 2 mins by spectrophotometric method2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of 2-(4-alkoxy-3-cyano)phenyl-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives as novel xanthine oxidase inhibitors.
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.
AID1075876Antihyperuricemic activity in potassium oxonate-induced hyperuricemic Sprague-Dawley rat model assessed as decrease of uric acid level in serum at 30 mg/kg, po measured after 1 hr relative to vehicle-treated control2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.
AID1324541Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by MTT assay relative to untreated2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1570307Anti-hyperuricemic activity in potassium oxonate-induced acute hyperuricemia Sprague-Dawley rat model assessed as reduction in AUC of uric acid in serum at 10 mg/kg, ig pretreated for 1 hr followed by potassium oxonate challenge and measured at 2 hrs post2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of 2-(4-alkoxy-3-cyano)phenyl-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives as novel xanthine oxidase inhibitors.
AID424727Inhibition of bovine xanthine oxidase assessed as reduction of cytochrome c at 10 uM2009Journal of natural products, Apr, Volume: 72, Issue:4
Inhibition studies of bovine xanthine oxidase by luteolin, silibinin, quercetin, and curcumin.
AID1874228Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as affinity off-rate by surface plasmon resonance assay2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
AID776291Intrinsic solubility of the compound in standard phosphate buffer at pH 6.8 at 37 degC after 24 hrs by shake-flask method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID1485283Inhibition of bovine milk xanthine oxidase assessed as reduction in uric acid formation using xanthine as substrate preincubated for 3 hrs followed by substrate addition measured after 1 min by UV spectrophotometric assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity.
AID1867886Nephroprotective activity against adenine and potassium oxonate-induced hyperuricemia Kunming mouse model assessed as reduction in cytoplasmic vacuolation of renal tubular epithelial cells at 20 mg/kg, po administered via gavage and measured after 21 days2022European journal of medicinal chemistry, Jul-05, Volume: 237Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1874230Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
AID1888100Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate incubated for 15 mins followed by substrate addition by spectrophotometric analysis2022European journal of medicinal chemistry, Jan-05, Volume: 227Design, synthesis, and biological evaluation of N-(3-cyano-1H-indol-5/6-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamides and 5-(6-oxo-1,6-dihydropyrimidin-2-yl)-1H-indole-3-carbonitriles as novel xanthine oxidase inhibitors.
AID1072541Inhibition of bovine xanthine oxidase using xanthine as substrate measured for 6 mins at 25 degC by spectrophotometry2014European journal of medicinal chemistry, Mar-21, Volume: 75Design, synthesis and molecular modeling of aloe-emodin derivatives as potent xanthine oxidase inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC 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.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347151Optimization of GU AMC 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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1346020Human xanthine dehydrogenase (Nucleoside synthesis and metabolism)1996Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13
Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1800197Xanthine Oxidase Activity from Article 10.1111/cbdd.12205: \\Antioxidant, a-glucosidase and xanthine oxidase inhibitory activity of bioactive compounds from maize (Zea mays L.).\\2014Chemical biology & drug design, Jan, Volume: 83, Issue:1
Antioxidant, α-glucosidase and xanthine oxidase inhibitory activity of bioactive compounds from maize (Zea mays L.).
AID1800155XO inhibitory activity from Article 10.1111/cbdd.12141: \\In vitro evaluation of selected benzimidazole derivatives as an antioxidant and xanthine oxidase inhibitors.\\2013Chemical biology & drug design, Sep, Volume: 82, Issue:3
In vitro evaluation of selected benzimidazole derivatives as an antioxidant and xanthine oxidase inhibitors.
AID1799669Inhibition Assay from Article 10.1080/14756360290019944: \\2-styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study.\\2002Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 17, Issue:1
2-styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study.
AID1800440XO inhibitory assay from Article 10.1016/j.bioorg.2014.08.007: \\Synthesis and xanthine oxidase inhibitory activity of 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives.\\2014Bioorganic chemistry, Dec, Volume: 57Synthesis and xanthine oxidase inhibitory activity of 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14,279)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904200 (29.41)18.7374
1990's3616 (25.32)18.2507
2000's2795 (19.57)29.6817
2010's2822 (19.76)24.3611
2020's846 (5.92)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials743 (4.92%)5.53%
Reviews1,098 (7.27%)6.00%
Case Studies953 (6.31%)4.05%
Observational45 (0.30%)0.25%
Other12,257 (81.19%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (175)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-Blind, Parallel Group Study to Evaluate the Safety and Efficacy of Tranilast in Combination With Allopurinol in Patients With Moderate to Severe Gout (TAnGO)[NCT01109121]Phase 2112 participants (Actual)Interventional2010-06-30Completed
PERL (Preventing Early Renal Loss in Diabetes) Continuous Glucose Monitoring (CGM) Study[NCT03334318]175 participants (Actual)Observational2017-10-01Completed
A Randomized, Double-Blind, Crossover, Pharmacodynamic and Pharmacokinetic Drug Interaction Study of Tranilast in Combination With Allopurinol Compared With Tranilast Alone and Allopurinol Alone in Healthy Subjects With Hyperuricemia[NCT01052987]Phase 224 participants (Anticipated)Interventional2010-01-31Completed
Effect of Hyperuricemia Treatment on Hypertension and Metabolic Syndrome[NCT01157936]Phase 240 participants (Anticipated)Interventional2010-07-31Completed
Allogeneic Hematopoietic Stem Cell Transplantation Using Reduced Intensity Conditioning (RIC) With Post-Transplant Cytoxan (PTCy) for the Treatment of Hematological Diseases[NCT05805605]Phase 256 participants (Anticipated)Interventional2023-05-01Recruiting
Effect of Allopurinol on Left Ventricular Function in Children With Dilated Cardiomyopathy[NCT05193838]100 participants (Anticipated)Observational2022-05-01Not yet recruiting
Effect of Allopurinol or Febuxostat to Prevent Contrast Induced Acute Kidney Injury (CI-AKI)[NCT03767322]Phase 2558 participants (Anticipated)Interventional2018-12-05Not yet recruiting
The Effect of Antioxidants on Skin Blood Flow During Local Heating[NCT03680638]Phase 144 participants (Actual)Interventional2016-09-07Completed
Prednisone in Uric Acid Lowering in Symptomatic Heart Failure PATients With Hyperuricemia (PUSH-PATH Study 2)[NCT02129764]Phase 2/Phase 3205 participants (Actual)Interventional2013-12-31Completed
Evaluation of a Treatment With Allopurinol on Autistic Disorders and Epilepsy in Adenylosuccinate Lyase Deficiency (ADSL)[NCT03776656]Phase 28 participants (Actual)Interventional2019-10-14Completed
The Effects of BCRP Q141K on Allopurinol Pharmacokinetics and Dynamics[NCT02956278]Phase 427 participants (Actual)Interventional2016-11-30Completed
To Examine the Percentage of Cases of Acute Treatment With Allopurinol in Gout Patients as Secondary Treatment[NCT03601260]700 participants (Anticipated)Interventional2018-08-31Not yet recruiting
The Potential Role of Allopurinol Versus Atorvastatin to Prevent Complications of Liver Cirrhosis: A Quadruple Blind Clinical Study[NCT05511766]Phase 2/Phase 3150 participants (Anticipated)Interventional2022-11-15Recruiting
A Phase 3, Randomized, Multicenter Study Comparing the Safety and Efficacy of Oral Febuxostat Versus Allopurinol in Subjects With Gout[NCT00102440]Phase 3760 participants (Actual)Interventional2002-07-31Completed
Evaluation of Single Agent Rasburicase for 5 Days Versus Sequential Treatment With Rasburicase From Day 1 Through 3 Followed by Oral Allopurinol From Day 3 Through 5 (Overlap on Day 3) Versus Single Agent Oral Allopurinol for 5 Days in the Management of P[NCT00230178]Phase 3280 participants (Actual)Interventional2004-04-30Completed
Evaluating the Safety and Efficacy of Chemotherapy in Patients With Relapsed Small Cell Lung Cancer in Combination With Allopurinol and MycoPhenolate (CLAMP Trial)[NCT05049863]Phase 1/Phase 236 participants (Anticipated)Interventional2023-02-27Recruiting
In Vitro-In Vivo Relationship Study to Assess the Impact of the In Vitro Dissolution Profile on the Pharmacokinetic Parameters Used to Establish Bioequivalence[NCT02398448]Phase 120 participants (Actual)Interventional2015-04-30Completed
Comparative Clinical Efficacy and Safety of Coded Polyherbal Medicine Arthitec 1 and Arthitec 2 With Allopathic Medicine for the Management of Arthritis[NCT03506919]Phase 1/Phase 2200 participants (Anticipated)Interventional2018-01-01Recruiting
The Effect of Antioxidants on Skin Blood Flow-BH4[NCT03680573]Phase 116 participants (Actual)Interventional2018-01-08Completed
Allopurinol in Schizophrenia: A Randomized Trial Administering Allopurinol vs Placebo as add-on Antipsychotics in Patients With Schizophrenia[NCT00864825]Phase 4248 participants (Actual)Interventional2009-08-31Completed
Does Allopurinol Regress Left Ventricular Hypertrophy in Patients With Treated Essential Hypertension?[NCT02237339]Phase 472 participants (Actual)Interventional2014-09-30Completed
Treat-to-Target Serum Urate Versus Treat-to-Avoid Symptoms in Gout: A Randomized Controlled Trial[NCT04875702]650 participants (Anticipated)Interventional2023-11-15Not yet recruiting
A Single-Centre, Randomised, Double-Blind, Placebo-Controlled, 3-Period, Cross-Over Phase I Study to Investigate the Effect on the QTcF Interval of a Single Dose of 2 Different Doses of Verinurad, Each in Combination With Allopurinol 300 mg, Compared With[NCT04256629]Phase 124 participants (Actual)Interventional2020-03-03Completed
Uric Acid, Klotho and Salt Sensitivity in Young Adults Born Preterm[NCT04026776]Early Phase 1165 participants (Anticipated)Interventional2020-09-02Recruiting
Low-dose Azathioprine and Allopurinol- Versus Azathioprine Monotherapy in Patients With Ulcerative Colitis: An Investigator-initiated, Open, Multicentre, Parallel-arm, Randomised Controlled Trial[NCT03101800]Phase 384 participants (Anticipated)Interventional2016-12-14Recruiting
Gender Differences in the Metabolic Effects of Uric Acid[NCT03076684]Early Phase 10 participants (Actual)Interventional2017-03-03Withdrawn(stopped due to Preliminary data collected and diets developed. Funding has ended and data used to support a larger application to test the hypothesis.)
Crossover Clinical Trial, Randomized, Double Blind, Placebo Controlled Trial. Modulation of Cellular Mediators and Repair Endothelial Damage in Patients With Chronic Renal Disease Through Inhibition of Xanthine Oxidase[NCT04983160]Phase 222 participants (Actual)Interventional2014-02-26Completed
Allopurinol in the Treatment of Patients With Diabetes Mellitus and Multivessel Coronary Artery Disease Treated by Either PCI or CABG: Pilot Study[NCT03700645]Phase 4100 participants (Anticipated)Interventional2018-12-01Not yet recruiting
Effect of Allopurinol on Markers of Mineral and Bone Metabolism in Patients in With Chronic Kidney Disease: a Randomized Double-blind Study[NCT05601271]50 participants (Actual)Interventional2021-03-01Active, not recruiting
A Multicentre, Randomized, Double-blind, Allopurinol Controlled Study to Evaluate the Efficacy and Safety of SHR4640 in Subjects With Gout[NCT04956432]Phase 3780 participants (Actual)Interventional2021-06-15Active, not recruiting
Sarcoma Alliance for Research Through Collaboration (SARC) Multicenter Trial: A Phase II Trial of Perifosine in Patients With Chemo-Insensitive Sarcomas[NCT00401388]Phase 272 participants (Actual)Interventional2006-11-30Completed
The Effect of Local Antioxidant Therapy on Racial Differences in Vasoconstriction[NCT03680404]Phase 124 participants (Actual)Interventional2018-10-01Completed
A Phase3, Multicentre, Randomized, Double-Blind, Allopurinol and Placebo-Controlled Study to Evaluate the Efficacy and Safety of SHR4640 Monotherapy in Subjects With Gout[NCT04052932]Phase 3594 participants (Actual)Interventional2019-07-16Completed
Allopurinol for Mania: A Randomized Trial Administering Allopurinol vs. Placebo as add-on to Mood Stabilizers and/or Antipsychotics in Patients in a Bipolar Manic Episode.[NCT01092221]Phase 3180 participants (Actual)Interventional2010-05-31Completed
Randomized, Double-Blind, Multicenter, Placebo-Controlled, Combination Study to Evaluate the Safety, Efficacy and Potential Pharmacokinetic Interaction of RDEA594 and Allopurinol in Gout Patients With an Inadequate Hypouricemic Response With Standard Dose[NCT01001338]Phase 2227 participants (Actual)Interventional2009-10-31Completed
A Randomized, Double-Blind, Multi-center, Placebo-Controlled, Combination Study to Evaluate the Urate-Lowering Activity, Safety, and Potential Pharmacokinetic Interaction of Oral BCX4208 and Allopurinol Administered in Subjects With Gout[NCT01129648]Phase 287 participants (Actual)Interventional2010-05-31Completed
Allopurinol as a Possible Oxygen Sparing Agent During Exercise in Peripheral Arterial Disease[NCT01147705]Phase 450 participants (Actual)Interventional2011-02-28Completed
Study of Sequential Perfusion of Liver Grafts With Low-viscosity and High-viscosity Preservation Solutions to Decrease the Incidence of Nonanastomotic Biliary Strictures After Liver Transplantation[NCT01271179]141 participants (Actual)Interventional2004-07-31Completed
Inflammatory Mediators in Obstructive Sleep Apnoea Syndrome; Mechanisms of Production and the Effect of Long Term Antioxidants Administration[NCT01188005]30 participants (Anticipated)Interventional2010-08-31Recruiting
Optimal Administration of Allopurinol in Dialysis Patients : A Chronotherapy Trial[NCT02477488]Phase 450 participants (Actual)Interventional2015-06-30Completed
Phase 2/3 Study of Effect of AT1RB Versus ACE Inhibitor in Addition to XO Inhibitor on Progression of LV Remodeling and Dysfunction in Diabetic Patients With Acute MI.[NCT01052272]Phase 2/Phase 372 participants (Actual)Interventional2005-07-31Completed
A Double-Blind, Placebo Controlled Augmentation Study With Allopurinol for Treatment Resistant Mania[NCT00643123]Phase 440 participants (Actual)Interventional2007-09-30Completed
Allopurinol Impact on Cirrhosis Related Complications[NCT05545670]Phase 2/Phase 3100 participants (Actual)Interventional2022-06-15Completed
Xanthine Oxidase Inhibition for Improvement of Long-term Outcomes Following Ischaemic Stroke and Transient Ischaemic Attack[NCT02122718]Phase 4464 participants (Actual)Interventional2014-05-31Completed
A Phase II Study of Double Induction Chemotherapy for Newly Diagnosed Non-L3 Adult Acute Lymphoblastic Leukemia With Investigation of Minimal Residual Disease and Risk of Relapse Following Maintenance Chemotherapy[NCT00109837]Phase 279 participants (Actual)Interventional2005-04-30Completed
Effect of Allopurinol on Mono and Co-administration With Statins on Platelets Reactivity on Diabetic Patiets Treated With Aspirin and Insulin[NCT03195153]Phase 4200 participants (Anticipated)Interventional2017-03-28Recruiting
the Impact of Allopurinol of HRQOL in Cirrhotic Patients[NCT05828836]Phase 2/Phase 3100 participants (Actual)Interventional2022-06-15Completed
CSP #594 - Comparative Effectiveness in Gout: Allopurinol vs. Febuxostat[NCT02579096]Phase 4950 participants (Actual)Interventional2017-03-06Completed
A Novel Assay for the Determination of Urinary 2,8-Dihydroxyadenine and Other Key Urinary Purine Metabolites: Effect of Allopurinol and Febuxostat on Urinary 2,8-Dihydroxyadenine Excretion in APRT Deficient Patients[NCT02752633]Phase 49 participants (Actual)Interventional2013-05-31Completed
A Randomized, Multi-regional, Double-blind, Double-dummy Parallel-group, Placebo and Allopurinol-controlled Phase 3 Study to Assess the Efficacy and Safety of Tigulixostat in Gout Patients With Hyperuricemia[NCT05586971]Phase 32,542 participants (Anticipated)Interventional2023-03-30Recruiting
Uric Acid Reduction as a Novel Treatment for Pediatric Chronic Kidney Disease[NCT03865407]Phase 217 participants (Actual)Interventional2019-03-10Terminated(stopped due to inability to achieve recruitment goals at a single center and given the current pandemic conditions)
A Phase 3, Randomized, Multicenter, Allopurinol and Placebo-Controlled Study Assessing the Safety and Efficacy of Oral Febuxostat in Subjects With Gout.[NCT00174915]Phase 31,072 participants (Actual)Interventional2003-02-28Completed
Time-limited Triplet Combination of Pirtobrutinib, Venetoclax, and Obinutuzumab for Patients With Treatment-naïve Chronic Lymphocytic Leukemia (CLL) or Richter Transformation (RT)[NCT05536349]Phase 260 participants (Anticipated)Interventional2022-12-20Recruiting
A Phase I/II Dose Escalation Study of Subcutaneous Campath-1H (NSC #715969, IND #10864) During Intensification Therapy in Adults With Untreated Acute Lymphoblastic Leukemia (ALL)[NCT00061945]Phase 1/Phase 2302 participants (Actual)Interventional2003-06-30Completed
A Double-blind, Placebo-controlled, Cross-over Study of the Effects of Allopurinol on Oxidative Metabolism, Peripheral Blood Flow and Immune Function in Patients With Advanced Chronic Heart Failure (CHF).[NCT00997542]Phase 416 participants (Actual)InterventionalCompleted
Phase I Study of Infusion of Umbilical Cord Blood (UCB) Derived CD25+CD4+ T-Regulatory (Treg) Cells After Nonmyeloablative Cord Blood Transplantation[NCT00602693]Phase 141 participants (Actual)Interventional2007-07-23Completed
[NCT02797028]Phase 4320 participants (Anticipated)Interventional2015-01-31Recruiting
Allopurinol Improves Diastolic Function in African Americans With Resistant Hypertension[NCT05888233]Phase 250 participants (Anticipated)Interventional2023-08-02Recruiting
Phase 2 Study to Determine if Allopurinol Blocks Features of Metabolic Syndrome Induced by Fructose Ingestion[NCT00639756]Phase 260 participants (Anticipated)Interventional2008-06-30Completed
A Phase 2a, Open-Label Study to Evaluate the Safety and Efficacy of AR882 Administered Alone or in Combination With Febuxostat or Allopurinol in Gout Patients[NCT04155918]Phase 230 participants (Actual)Interventional2020-02-03Completed
Involvement of Reactive Oxygen Species Produced by the Xanthine Oxidase in Mitochondrial Alterations in Skeletal Muscle of Type 2 Diabetic Patients[NCT02533648]Phase 331 participants (Actual)Interventional2011-09-16Completed
Rasburicase to Prevent Graft -Versus-Host Disease[NCT00513474]Phase 146 participants (Actual)Interventional2008-01-31Completed
Prospective Study of Allopurinol Treatment That Improves Endothelial Function by Decreasing Uric Acid Levels of Patients With Chronic Kidney Disease[NCT00978653]20 participants (Actual)Interventional2008-04-30Completed
Therapy for Acute Gout: Does Initial Use of Allopurinol Effect Duration and/or Recurrence Rate of Acute Attacks[NCT01310673]Phase 457 participants (Actual)Interventional1998-01-31Completed
A 24-week, Dose-ranging, Multicenter, Double-blind, Double-dummy, Active-controlled Core Study to Evaluate Canakinumab for Prophylaxis of Signs and Symptoms of Acute Flares in Chronic Gout Patients Initiating Allopurinol Therapy and a 24-week Open-label, [NCT00819585]Phase 2432 participants (Actual)Interventional2008-12-31Completed
Does Antenatal Allopurinol Administration Improve Maternal and Neonatal Outcome in Intrauterine Growth Restriction?[NCT00346463]50 participants (Anticipated)Interventional2006-07-31Not yet recruiting
Febuxostat (Zurig) Efficacy & Safety Trial in Comparison With Allopurinol in Hyperuricemic Subjects With or Without Gout[NCT02600780]Phase 450 participants (Actual)Interventional2013-11-30Completed
A Randomized Phase 2 Study to Evaluate the Efficacy of Rasburicase in Patients at Risk for TLS During Two Cycles of Chemotherapy[NCT01200485]Phase 255 participants (Actual)Interventional2011-04-30Completed
MT2007-19R: WCC #53 Allogeneic Natural Killer Cells in Patients With Recurrent Ovarian Cancer, Fallopian Tube, and Primary Peritoneal Cancer[NCT00652899]Phase 214 participants (Actual)Interventional2008-03-31Terminated(stopped due to Withdrawn due to toxicity)
A Single-center, Randomized, Double-blind, Placebo-controlled Study of the Efficacy and Safety of Allopurinol in Improving Ischemic Symptoms in Patients With Refractory Angina.[NCT04368819]Phase 2/Phase 340 participants (Anticipated)Interventional2021-03-03Recruiting
Effects of Allopurinol on Inflammatory Markers and Morphostructural Changes Evidenced by Musculoskeletal Ultrasound in Individuals With Asymptomatic Hyperuricemia. A Proof of Concept[NCT04012294]Phase 3200 participants (Anticipated)Interventional2019-08-30Recruiting
A Double-blind, Randomized, Placebo-controlled 4-week Study on the Efficacy and Safety of the Purinergic Agents Allopurinol and Dipyridamole in Acute Bipolar Mania.[NCT00560079]Phase 4180 participants (Actual)Interventional2003-11-30Completed
A Phase 1, Randomized, Open-Label, Crossover Study to Assess the Relative Bioavailability of Lesinurad/Allopurinol Fixed Dose Combination Tablets and Coadministered Lesinurad and Allopurinol Tablets and the Effect of Food on the Pharmacokinetics of Lesinu[NCT02581553]Phase 1116 participants (Actual)Interventional2015-10-31Completed
A Prospective, Randomized Controlled Study of Uric Acid on the Progression of IgA Nephropathy[NCT00793585]40 participants (Actual)Interventional2007-07-31Completed
A Multicenter, Randomized, Double-Blind, Placebo and Allopurinol Controlled, Phase 2 Study to Evaluate Febuxostat in the Medical Management of Subjects With Hyperuricosuria and Calcium Oxalate Stones[NCT01077284]Phase 299 participants (Actual)Interventional2010-02-28Completed
A Double-blind, Randomized, Placebo Controlled Trial of Allopurinol in Patients With Type 1 Diabetes and Microalbuminuria[NCT02829177]Phase 430 participants (Actual)Interventional2014-09-30Completed
Randomised Phase III Trial of Effectivity and Safety of Rasburicase Compared With Allopurinol for Treatment of Hyperuricemia in Patients With Acute Lymphoblastic Leukemia or High-Grade NHL With High Risk of Tumorlysis Syndrome (> 15 Yrs)[NCT00199043]Phase 380 participants (Actual)Interventional2003-05-31Completed
An Open Label, Naturalistic Study With Allopurinol Augmentation for Prevention of Mania in Bipolar Disorder[NCT00732251]Phase 415 participants (Actual)Interventional2008-08-31Terminated(stopped due to The outpatient area of the department of psychiatry at CSMC closed.)
A Phase 3, Randomized, Multicenter, Double-Blind, Allopurinol-Controlled Study Assessing the Efficacy and Safety of Oral Febuxostat in Subjects With Gout.[NCT00430248]Phase 32,269 participants (Actual)Interventional2007-02-28Completed
Effects of Xanthine Oxidase Inhibition on Mechano-Energetic Coupling in Heart Failure[NCT00181155]Phase 218 participants (Actual)Interventional2004-11-30Completed
The Effect of Allopurinol on Malondialdehyde, Nitric Oxide, Kidney Injury Molecule-1 Urine Levels, Resistive Index and Renal Elastography in Kidney Stone Patients After Extra Corporeal Shockwave Lithotripsy[NCT05414669]Phase 435 participants (Actual)Interventional2020-08-06Completed
Does ALlopurinol Regress lefT Ventricular Hypertrophy in End Stage REnal Disease: The ALTERED Study[NCT01951404]Phase 480 participants (Actual)Interventional2013-09-30Completed
Effect of Allopurinol Administration on the Prevention of Muscle Mass Loss in Subject Immobilized.[NCT01987570]Phase 353 participants (Actual)Interventional2012-04-30Completed
Allopurinol Versus Febuxostat: A New Approach for Management of Hepatic Steatosis in Metabolic-Associated Fatty Liver Disease[NCT05474560]Phase 490 participants (Actual)Interventional2022-01-01Completed
[NCT02008968]130 participants (Anticipated)Interventional2013-12-31Recruiting
A Phase 3, Open-Label, Randomized, Allopurinol-Controlled Study to Assess the Long-Term Safety of Oral Febuxostat in Subjects With Gout[NCT00175019]Phase 31,086 participants (Actual)Interventional2003-07-31Completed
A Randomized, Double-blind, Placebo-controlled Study Evaluating the Effect of Allopurinol on the Risk of Cardiovascular Events in Patients With High and Very High Cardiovascular Risk, Including the Presence of Long-COVID Syndrome.[NCT05943821]Phase 31,116 participants (Anticipated)Interventional2023-09-01Recruiting
A Multicenter, Randomized, Double-blind, Controlled, Phase 2b/3 Study to Assess the Efficacy and Safety of ABP-671 in Participants With Gout[NCT05818085]Phase 2/Phase 3580 participants (Anticipated)Interventional2023-08-11Recruiting
Allogeneic Hematopoietic Stem Cell Transplantation Using Reduced Intensity Conditioning (RIC) for the Treatment of Hematological Diseases [MT2015-32][NCT02661035]Phase 2156 participants (Actual)Interventional2017-03-09Completed
A Randomized, Open Label, Two-Period, Two-Treatment, Two-Sequence, Single Dose, Crossover Comparative Bioequivalence Study of Allopurinol 300 mg Tablets USP With Zyloprim® 300 mg in Normal, Healthy, Adult, Human Male Subjects Under Fasting Condition.[NCT01603134]Phase 132 participants (Actual)Interventional2007-11-30Completed
Placebo-controlled Trial to Determine the Effectiveness of a 3% Allopurinol-base Topical Agent for Prevention of Capecitabine-induced Hand-foot Syndrome[NCT01609166]Phase 260 participants (Actual)Interventional2011-07-31Completed
Modifiable Effectors of Renin System Activation: Treatment Evaluation (MODERATE)[NCT01320722]Phase 3242 participants (Actual)Interventional2011-03-31Completed
Evaluating Pharmacokinetics and Whole Blood Bactericidal Activity Against Mycobacterium Tuberculosis of Pyrazinamide Boosted With Allopurinol in Healthy Volunteers[NCT02700347]Phase 112 participants (Actual)Interventional2016-02-29Completed
A Multicenter, Randomized, Active-Control, Phase 3B Study to Evaluate the Cardiovascular Safety of Febuxostat and Allopurinol in Subjects With Gout and Cardiovascular Comorbidities[NCT01101035]Phase 36,198 participants (Actual)Interventional2010-04-23Completed
A Phase I, Randomized, Open-label Study to Evaluate the Potential Pharmacokinetic Interactions Between D-0120 and Allopurinol in Healthy Adult Subjects[NCT05360628]Early Phase 120 participants (Actual)Interventional2021-11-01Completed
Nonmyeloablative Stem Cell Transplantation With or Without Lenalidomide for Chronic Lymphocytic Leukemia (RV-CLL-PI-0294)[NCT00899431]Phase 239 participants (Actual)Interventional2009-05-06Terminated(stopped due to Terminated per PI's request at the time of continuing review)
A Phase 1, Randomized, Open-Label, Replicate, Crossover Study to Assess the Bioequivalence of Lesinurad/Allopurinol Fixed-Dose Combination Tablets and Coadministered Lesinurad and Allopurinol Tablets in Fed Healthy Adult Subjects[NCT02888054]Phase 128 participants (Actual)Interventional2016-08-30Completed
Dose-effect Relationship Between Allopurinol, Azathioprine and 6-thioguanine Nucleotide Levels (6-TGN) in Inflammatory Bowel Disease Patients.[NCT00849368]Phase 16 participants (Actual)Interventional2009-01-31Completed
Do Xanthine Oxidase Inhibitors Reduce Both Left Ventricular Hypertrophy and Endothelial Dysfunction in Cardiovascular Patients With Renal Dysfunction?[NCT00688480]Phase 467 participants (Actual)Interventional2008-01-31Completed
A Multi-center, Randomized, Open-label, Active-controlled Clinical Trial to Evaluate the Efficacy and Safety of Rasburicase (Fasturtec®) in the Prevention and Treatment of Hyperuricemia in Patients With Hematological Malignancies[NCT00607152]Phase 310 participants (Actual)Interventional2007-10-31Terminated(stopped due to the patient enrollment is too difficult)
Cerebrum and Cardiac Protection With Allopurinol in Neonates With Critical Congenital Heart Disease Requiring Cardiac Surgery With Cardiopulmonary Bypass[NCT04217421]Phase 3236 participants (Anticipated)Interventional2020-01-01Recruiting
Prednisone Versus Allopurinol for Symptomatic Heart Failure Patients With Hyperuricemia[NCT00919243]Phase 440 participants (Anticipated)Interventional2009-02-28Completed
Effects of Allopurinol on Diastolic Function in Chronic Heart Failure Patients[NCT00477789]Phase 40 participants InterventionalCompleted
APEX Study: Effects of Allopurinol on Coronary and Peripheral Endothelial Function in Patients With Cardiac Syndrome X[NCT00512057]Phase 440 participants (Anticipated)Interventional2008-06-30Completed
A Trial Comparing Single Agent Melphalan to Carmustine, Etoposide, Cytarabine and Melphalan (BEAM) as a Preparative Regimen for Patients With Multiple Myeloma Undergoing High Dose Therapy Followed by Autologous Stem Cell Reinfusion[NCT03570983]Phase 2100 participants (Anticipated)Interventional2018-09-05Recruiting
A Randomized, Double-Blind, Active and Placebo-Controlled Study to Evaluate the Efficacy and Safety of Arhalofenate for Preventing Flares and Reducing Serum Uric Acid in Gout Patients[NCT02063997]Phase 2248 participants (Actual)Interventional2014-03-31Completed
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Study of the Safety and Efficacy of Long-Term Rilonacept Treatment for the Prevention of Gout Flares[NCT01459796]Phase 3220 participants (Actual)Interventional2011-11-30Terminated
Randomized Double-blinded, Placebo-controlled, Cross-over Trial of Allopurinol for the Treatment of Newly Diagnosed Essential Hypertension in Adolescents[NCT00288184]Phase 230 participants (Actual)Interventional2004-09-30Completed
A Randomized, Open-Label, Multiple-Dose Phase II Study to Evaluate Efficacy and Safety of D-0120 Administered in Combination With Allopurinol in Subjects With Gout[NCT05665699]Phase 280 participants (Anticipated)Interventional2023-04-17Recruiting
Phase II Study Of Rituximab And Short Duration, High Intensity Chemotherapy With G-CSF Support In Previously Untreated Patients With Burkitt Lymphoma/Leukemia[NCT00039130]Phase 2105 participants (Actual)Interventional2002-05-31Completed
A Phase 2, Randomized, Open-Label, Allopurinol-Controlled, Multicenter Study With Optional Extension to Evaluate the Safety and Efficacy of AR882 Alone or in Combination With Allopurinol in Tophaceous Gout Patients[NCT05253833]Phase 242 participants (Actual)Interventional2022-08-12Active, not recruiting
A Randomized, Open-label, Replicate, Crossover, 4-period Study to Assess the Bioequivalence of Lesinurad/Allopurinol Fixed-dose Combination 200/300 mg Tablets From Ardea Biosciences, Inc. (Test Drug) Versus Lesinurad, 200 mg Tablet From AstraZeneca (Compa[NCT03272425]Phase 132 participants (Actual)Interventional2017-08-14Completed
Treatment of Cutaneous Leishmaniasis With Meglumine Antimoniate 20 Mg/Kg/Day Versus Meglumine Antimoniate 10 Mg/Kg/Day And Tablet Allopurinol 20 Mg/Kg/Day[NCT00480883]400 participants (Anticipated)Interventional2008-01-31Completed
A Phase 2 Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of MBX-102 in Combination With Allopurinol in Gout Patients With an Inadequate Hypouricemic Response to Allopurinol Alone[NCT01399008]Phase 2100 participants (Actual)Interventional2011-06-30Completed
Effect of ALlopurinol in Addition to Hypothermia for Hypoxic-ischemic Brain Injury on Neurocognitive Outcome - a Blinded Randomized Placebo-controlled Parallel Group Multicenter Trial for Superiority (Phase III)[NCT03162653]Phase 3760 participants (Anticipated)Interventional2018-03-25Recruiting
An Open-label, 3-Treatment, 3-Period, Fixed Sequence Study in Healthy Subjects to Assess the Pharmacokinetics of Verinurad and Allopurinol When Administered Alone, and in Combination With Single Doses of Cyclosporine or Rifampicin[NCT04532918]Phase 114 participants (Actual)Interventional2020-09-10Completed
A Pilot Study of Allopurinol As A Modifier of 6-MP Metabolism in Pediatric ALL[NCT02046694]Early Phase 134 participants (Actual)Interventional2014-01-06Completed
A Prospective Study to Evaluate the Effect of Allopurinol on Muscle Energetics in Primary Sarcopenia[NCT01550107]Phase 4124 participants (Actual)Interventional2015-02-01Completed
The Impact of Urate-lowering Therapy on Kidney Function in Patients With/Without Gout[NCT03336203]Phase 42 participants (Anticipated)Interventional2017-10-30Enrolling by invitation
INST Phase II Trial of Gemcitabine and Irinotecan in Patients With Relapsed or Refractory Lymphoma.[NCT00276003]Phase 222 participants (Actual)Interventional2002-08-31Completed
Non-Myeloablative Allogeneic Hematopoietic Cell Transplantation For Patients With Disease Relapse Or Myelodysplasia After Prior Autologous Transplantation[NCT00053196]Phase 282 participants (Actual)Interventional2002-12-31Completed
Influence of Xanthine Oxidase Inhibition on Vascular Function in Obstructive Sleep Apnea[NCT00214084]0 participants (Actual)InterventionalWithdrawn
Does Antenatal Allopurinol Administration Reduce Post-hypoxic-ischemic Reperfusion Damage During Fetal Hypoxia in the Newborn?[NCT00189007]Phase 3222 participants (Actual)Interventional2009-10-31Active, not recruiting
Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines- Probenecid vs Allopurinol[NCT04746989]294,878 participants (Actual)Observational2021-02-01Active, not recruiting
University of Alabama at Birmingham CORT Project 2: The Effects of Urate Lowing Therapy (ULT) in Inflammation, Endothelial Function, and Blood Pressure[NCT02038179]Phase 2/Phase 399 participants (Actual)Interventional2014-07-31Completed
A Phase I Randomized Double-blind Placebo-controlled Study With 2 Separate Cohorts to Assess the Safety, Tolerability and Pharmacokinetics of Verinurad and Allopurinol in Healthy Asian and Chinese Subjects[NCT03836599]Phase 16 participants (Actual)Interventional2019-01-16Completed
A Phase III Trial to Evaluate the Efficacy of the Addition of Inotuzumab Ozogamicin (a Conjugated Anti-CD22 Monoclonal Antibody) to Frontline Therapy in Young Adults (Ages 18-39 Years) With Newly Diagnosed Precursor B-Cell ALL[NCT03150693]Phase 3310 participants (Anticipated)Interventional2017-06-01Suspended(stopped due to Unacceptable Toxicity)
Randomized Double-blinded, Placebo-controlled, Cross-over Trial of Allopurinol for the Treatment of Post-renal-transplant Hypertension in Children[NCT00288171]Phase 1/Phase 20 participants (Actual)Interventional2006-02-28Withdrawn(stopped due to insufficient number of eligible subjects)
Xanthine Oxidase Inhibition in Renal Transplant Recipients[NCT01332799]Phase 420 participants (Actual)Interventional2011-02-28Terminated(stopped due to Study was not funded)
Allopurinol and Cardiac Function Pilot Study in Idiopathic Dilated Cardiomyopathy[NCT00281255]Phase 1/Phase 20 participants (Actual)Interventional2003-06-30Withdrawn(stopped due to Infeasible)
[NCT00288158]Phase 260 participants (Actual)Interventional2008-09-30Completed
Role of Allopurinol in Prevention of Post-Endoscopic Retrograde Cholangiopancreatography Pancreatitis[NCT02992652]100 participants (Actual)Interventional2011-01-31Completed
A Randomized, Open Label, Multicenter, Allopurinol- Controlled Study to Assess the Safety and Efficacy of Oral Febuxostat in Patients With Gout[NCT01736514]Phase 3109 participants (Actual)Interventional2011-03-31Completed
Allopurinol in Acute Gout The Title Will Not be Change as the Study as Been Closed.[NCT01775098]0 participants (Actual)InterventionalWithdrawn(stopped due to because of a lack of funding)
Genomic Guided Assessment of Drug Therapy Effectiveness in Managing Hmong Adults With Hyperuricemia or Gout.[NCT02371421]80 participants (Actual)Observational2014-06-30Completed
A Phase 4, Study to Evaluate the Safety and Efficacy of Lesinurad 200 mg in Combination With a Xanthine Oxidase Inhibitor (XOI), Compared With an XOI Alone, in Subjects With Gout and Estimated Creatinine Clearance (eCrCl) 30 to <60 mL/Min Who Have Not Ach[NCT03226899]Phase 4242 participants (Actual)Interventional2017-07-19Terminated(stopped due to This action was a business decision & not related to any efficacy, safety or clinical concerns with lesinurad.)
A Phase 3 Randomized, Double-Blind, Multicenter, Placebo-Controlled, Combination Study to Evaluate the Efficacy and Safety of Lesinurad and Allopurinol Compared to Allopurinol Alone in Subjects With Gout Who Have Had an Inadequate Hypouricemic Response to[NCT01510158]Phase 3607 participants (Actual)Interventional2012-01-31Completed
Febuxostat for Tumor Lysis Syndrome Prevention in Hematologic Malignancies: a Randomized, Double Blind, Phase III Study Versus Allopurinol[NCT01724528]Phase 3346 participants (Actual)Interventional2012-10-31Completed
Documentation of Patient Outcomes for the Combination Treatment of Sodium Stibogluconate and Allopurinol in Complicated Cutaneous Leishmaniasis in Ethiopia[NCT04699383]105 participants (Actual)Observational2021-02-15Completed
A Phase 2b, Multicentre, Randomised, Double-blind, Placebo-controlled Study of Verinurad and Allopurinol in Patients With Chronic KIdney Disease and Hyperuricaemia[NCT03990363]Phase 2861 participants (Actual)Interventional2019-07-23Completed
Phase II Randomized Study of Allopurinol Versus Glucantime Versus Allopurinol/Glucantime for Cutaneous Leishmaniasis in Brazil[NCT00004755]Phase 2375 participants Interventional1995-09-30Completed
A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Single Rising Dose Study of AR882, a Potent Uricosuric Agent, in Healthy Adult Male Volunteers[NCT04347005]Phase 164 participants (Actual)Interventional2019-01-22Completed
Xanthine Oxidase Inhibition for Hyperuricemic Heart Failure Patients[NCT00987415]Phase 2253 participants (Actual)Interventional2010-05-31Completed
Is Uric Acid a Mediator of Endothelial Dysfunction in Patients With Chronic Kidney Disease?[NCT01228903]80 participants (Actual)Interventional2010-10-31Completed
A Phase III Randomized Trial of Low-Dose Versus Standard-Dose mBACOD Chemotherapy With rGM-CSF for Treatment of AIDS-Associated Non-Hodgkin's Lymphoma[NCT00000658]Phase 3250 participants InterventionalCompleted
Phase II Study in Adults With Untreated Acute Lymphoblastic Leukemia Testing Increased Doses of Daunorubicin During Induction, and Cytarabine During Consolidation, Followed by High-Dose Methotrexate and Intrathecal Methotrexate in Place of Cranial Irradia[NCT00003700]Phase 2163 participants (Actual)Interventional1999-01-31Completed
A Randomised, Single Dose, 5-period, 5-treatment, Crossover Study to Assess the Relative Bioavailability of 4 Different Formulations of Verinurad and Allopurinol in Healthy Subjects[NCT04550234]Phase 125 participants (Actual)Interventional2021-04-13Completed
A Randomized, Double-Blind, Multicenter, Placebo-Controlled, Parallel Group, 24-Week Phase II Study to Evaluate Efficacy and Safety of RDEA3170 5 mg, 7.5 mg, 10 mg, 12.5 mg and 15 mg Versus Placebo and Open-Label Allopurinol 200 mg as a Reference Arm in J[NCT02078219]Phase 2204 participants (Actual)Interventional2014-01-05Completed
Long-term Allopurinol Safety Study Evaluating Outcomes in Gout Patients (LASSO)[NCT01391325]Phase 41,735 participants (Actual)Interventional2011-07-31Completed
Oxidative Stress and Cardiovascular Denervation in Diabetes: An Interventional Trial[NCT00116207]Phase 344 participants (Actual)Interventional2000-01-31Completed
The Effect of Intensive Urate Lowering Therapy (ULT) With Febuxostat in Comparison With Allopurinol on Cardiovascular Risk in Patients With Gout Using Surrogate Markers: a Randomized, Controlled Trial[NCT02500641]Phase 4196 participants (Actual)Interventional2015-08-17Completed
Allopurinol and Trimetazidine as a Preventive of Contrast-associated Acute Kidney Injury in Patients Undergoing Percutaneous Coronary Intervention[NCT05540184]Phase 4124 participants (Anticipated)Interventional2022-09-19Recruiting
Allopurinol as a Possible New Therapy for Acute Coronary Syndromes:The Next Steps[NCT01457820]Phase 426 participants (Actual)Interventional2012-04-30Terminated(stopped due to slow recruitment: stopped early)
Chemotherapy and Azidothymidine, With or Without Radiotherapy, for High Grade Lymphoma in AIDS-Risk Group Members[NCT00000703]45 participants InterventionalCompleted
Pharmacologic Interventions for Cardiovascular Disease in Obstructive Sleep Apnea[NCT01637623]Phase 287 participants (Actual)Interventional2012-06-30Completed
A Phase 1b, Randomized, Open-label Study to Evaluate the Potential Pharmacokinetic and Pharmacodynamic Interactions Between RDEA3170 and Allopurinol in Adult Male Subjects With Gout[NCT02279641]Phase 112 participants (Actual)Interventional2014-11-01Completed
A Phase 2, Multicentre, Double-Blind, Placebo and Active Control Efficacy and Safety Study to Evaluate Verinurad Combined With Allopurinol in Heart Failure With Preserved Ejection Fraction[NCT04327024]Phase 2159 participants (Actual)Interventional2020-05-19Completed
The Predictors of Successful Oral Dissolution Therapy in Radiolucent Renal Stones; A Prospective Evaluation[NCT02373384]Phase 4182 participants (Actual)Interventional2015-02-28Completed
A Phase 3 Randomized, Double-Blind, Multicenter, Placebo- Controlled, Combination Study to Evaluate the Efficacy and Safety of Lesinurad and Allopurinol Compared to Allopurinol Alone in Subjects With Gout Who Have Had an Inadequate Hypouricemic Response t[NCT01493531]Phase 3610 participants (Actual)Interventional2011-12-31Completed
[NCT01451645]Phase 482 participants (Actual)Interventional2011-10-31Completed
T-Cell Depleted Double UCB With Post Transplant IL-2 for Refractory Myeloid Leukemia[NCT01464359]Phase 23 participants (Actual)Interventional2011-10-31Terminated(stopped due to Slow accrual)
A Phase 2a, Randomized, Open-Label Study to Evaluate the Pharmacodynamic Effects and Safety of RDEA3170 Administered in Combination With Allopurinol Compared With Allopurinol Administered Alone in Adult Subjects With Gout[NCT02498652]Phase 241 participants (Actual)Interventional2015-07-28Completed
Busulfan and Cyclophosphamide Followed By Allogeneic Hematopoietic Cell Transplantation In Patients With Hematological Malignancies[NCT01685411]5 participants (Actual)Interventional2013-01-31Terminated
Sex-related Differences in Arterial Stiffness in Type 2 Diabetics: Role of Uric Acid[NCT03648996]Phase 234 participants (Actual)Interventional2018-11-01Completed
A Phase 1B Open Label Evaluation of the PK and PD of Dotinurad and Drug-Drug Interaction of Dotinurad and Allopurinol in U.S. Patients With Gout and Hyperuricemia[NCT06056570]Phase 1/Phase 220 participants (Anticipated)Interventional2023-10-31Recruiting
Phentermine/tOpiramate to eND Obesity and Uric Acid Stones Trial (POuND OUT)[NCT04621929]Phase 340 participants (Anticipated)Interventional2021-03-31Recruiting
A Randomized, Double-blind, Placebo-controlled, 9-month, Parallel Group Study of Allopurinol to Reduce Left Ventricular Mass in Living Kidney Donors (AL-DON)[NCT03353298]Phase 271 participants (Actual)Interventional2018-01-17Completed
Impact of ALLopurInol on Endothelial fuNCtion in diabEtic Patients Affected With Coronary Artery Disease[NCT03385135]58 participants (Anticipated)Interventional2017-12-31Recruiting
Optimizing 6-mercaptopurine Therapy in Pediatric Acute Lymphoblastic Leukemia by Using Allopurinol Clinical Study in Children 1-19 Years on Maintenance Therapy for Acute Lymphoblastic Leukemia.[NCT03022747]Phase 260 participants (Anticipated)Interventional2017-01-31Recruiting
A Phase 3, Randomized, Multicenter, Allopurinol-Controlled Study Assessing the Safety and Efficacy of Oral Febuxostat in Subjects With Gout[NCT02082769]Phase 3504 participants (Actual)Interventional2011-07-31Completed
A Single-center, Prospective, Randomized, Double-blind, Controlled Trial for the Effect of Allopurinol Sustained-release Capsules on the Stability of Coronary Plaques in Patients With Acute Coronary Syndrome[NCT03745729]Phase 4162 participants (Actual)Interventional2019-03-01Completed
Uric Acid and Hypertension in African Americans[NCT00241839]Phase 3150 participants (Actual)Interventional2005-08-31Completed
PERL: A Multicenter Clinical Trial of Allopurinol to Prevent GFR Loss in T1D[NCT02017171]Phase 3530 participants (Actual)Interventional2014-02-28Completed
Does Allopurinol Prolong a Treated, Acute Gout Flare?[NCT01988402]Phase 435 participants (Actual)Interventional2007-12-31Completed
Efficacy and Safety of Two Comparable Single Low Doses of Rasburicase Followed by Allopurinol in Adult Patients With Malignancy[NCT01564277]Phase 224 participants (Actual)Interventional2011-09-29Terminated(stopped due to low accrual)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00039130 (3) [back to overview]2 Year Event Free Survival
NCT00039130 (3) [back to overview]2 Year Overall Survival
NCT00039130 (3) [back to overview]Complete Response Rate
NCT00061945 (6) [back to overview]Number of Participants Who Proceed to Course V Within 2-6 Weeks of the Last Dose of Alemtuzumab (Phase II)
NCT00061945 (6) [back to overview]Number of Participants Achieving Complete Remission
NCT00061945 (6) [back to overview]Minimal Residual Disease (MRD) During Treatment With Alemtuzumab (Phase II)
NCT00061945 (6) [back to overview]Disease-free Survival, for Only Complete Response Patients
NCT00061945 (6) [back to overview]Maximum Tolerated Dose (MTD) of Alemtuzumab (Phase I)
NCT00061945 (6) [back to overview]Overall Survival
NCT00102440 (14) [back to overview]Percentage of Subjects With the Last 3 Serum Urate Levels <6.0 Milligrams Per Deciliter (mg/dL)
NCT00102440 (14) [back to overview]Change From Baseline in Total Number of Tophi at Final Visit in Subjects With Palpable Tophi at Screening.
NCT00102440 (14) [back to overview]Change From Baseline in Total Number of Tophi at Week 28 in Subjects With Palpable Tophi at Screening.
NCT00102440 (14) [back to overview]Change From Baseline in Total Number of Tophi at Week 52 in Subjects With Palpable Tophi at Screening.
NCT00102440 (14) [back to overview]Percent Change From Baseline in Serum Urate Levels at Final Visit
NCT00102440 (14) [back to overview]Percent Change From Baseline in Serum Urate Levels at Week 28.
NCT00102440 (14) [back to overview]Percent Change From Baseline in Serum Urate Levels at Week 52.
NCT00102440 (14) [back to overview]Percent Change From Baseline in Tophus Size at Final Visit, as Determined by Physical Measurement, in Subjects With a Palpable Primary Tophus at Screening.
NCT00102440 (14) [back to overview]Percent Change From Baseline in Tophus Size at Week 28, as Determined by Physical Measurement, in Subjects With a Palpable Primary Tophus at Screening.
NCT00102440 (14) [back to overview]Percent Change From Baseline in Tophus Size at Week 52, as Determined by Physical Measurement, in Subjects With a Palpable Primary Tophus at Screening.
NCT00102440 (14) [back to overview]Percentage of Subjects Requiring Treatment for Gout Flares Between Weeks 8 and 52.
NCT00102440 (14) [back to overview]Percentage of Subjects With Serum Urate <6.0 mg/dL at Final Visit
NCT00102440 (14) [back to overview]Percentage of Subjects With Serum Urate <6.0 mg/dL at Week 28 Visit
NCT00102440 (14) [back to overview]Percentage of Subjects With Serum Urate <6.0 mg/dL at Week 52 Visit
NCT00109837 (2) [back to overview]Continuous Complete Remission at 1 Year
NCT00109837 (2) [back to overview]Toxicity
NCT00116207 (4) [back to overview]Global [11C]HED Retention Index (RI)
NCT00116207 (4) [back to overview]Global Coronary Flow Reserve as a Measure of Endothelial Function
NCT00116207 (4) [back to overview]Inflammation
NCT00116207 (4) [back to overview]Systemic Oxidative Stress
NCT00174915 (10) [back to overview]Percentage of Subjects Whose Last Three Serum Urate Levels Are <6.0 Milligram Per Deciliter (mg/dL).
NCT00174915 (10) [back to overview]Percent Change From Baseline in Serum Urate Levels at Final Visit
NCT00174915 (10) [back to overview]Percent Change in Primary Tophus Size at Week 28, as Determined by Physical Measurement in the Subset of Subjects With Palpable Tophi at the Screening Visit.
NCT00174915 (10) [back to overview]Percent Change in Primary Tophus Size at Final Visit, as Determined by Physical Measurement in the Subset of Subjects With Palpable Tophi at the Screening Visit.
NCT00174915 (10) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Week 28
NCT00174915 (10) [back to overview]Change in the Total Number of Tophi at Week 28 in the Subset of Subjects With Palpable Tophi at the Screening Visit.
NCT00174915 (10) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Final Visit
NCT00174915 (10) [back to overview]Percentage of Subjects Requiring Treatment for a Gout Flare Between Weeks 8 and 28 of the Double-Blind Treatment Period.
NCT00174915 (10) [back to overview]Percent Change From Baseline in Serum Urate Levels at Week 28.
NCT00174915 (10) [back to overview]Change in the Total Number of Tophi at Final Visit in the Subset of Subjects With Palpable Tophi at the Screening Visit
NCT00175019 (13) [back to overview]Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 24.
NCT00175019 (13) [back to overview]Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 36.
NCT00175019 (13) [back to overview]Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 12.
NCT00175019 (13) [back to overview]Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Last Visit on Treatment.
NCT00175019 (13) [back to overview]Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 1.
NCT00175019 (13) [back to overview]Percentage of Subjects Requiring Treatment for Gout Flare up to Month 12.
NCT00175019 (13) [back to overview]Percent Change From Baseline in Primary Tophus Size at Month 36 for Subjects With Palpable Tophi Measured at Baseline.
NCT00175019 (13) [back to overview]Percentage of Subjects Requiring Treatment for Gout Flare After Month 12.
NCT00175019 (13) [back to overview]Percent Change in Serum Urate Levels From Baseline to the Last Visit on Treatment.
NCT00175019 (13) [back to overview]Percent Change From Baseline in the Total Number of Tophi for Subjects With Palpable Tophi at Final Visit.
NCT00175019 (13) [back to overview]Percent Change From Baseline in Primary Tophus Size at Month 24 for Subjects With Palpable Tophi Measured at Baseline.
NCT00175019 (13) [back to overview]Percent Change From Baseline in Primary Tophus Size at Month 12 for Subjects With Palpable Tophi Measured at Baseline.
NCT00175019 (13) [back to overview]Percent Change From Baseline in Primary Tophus Size at Final Visit for Subjects With Palpable Tophi Measured at Baseline.
NCT00181155 (4) [back to overview]Myocardial Creatine Kinase (CK) Flux Pre Intravenous Allopurinol Infusion
NCT00181155 (4) [back to overview]Cardiac PCr/ATP Post Intravenous Infusion
NCT00181155 (4) [back to overview]Cardiac PCr/ATP Pre Intravenous Infusion
NCT00181155 (4) [back to overview]Myocardial CK Flux Post Intravenous Allopurinol Infusion.
NCT00230178 (3) [back to overview]Plasma Uric Acid Responder
NCT00230178 (3) [back to overview]Time to Uric Acid Control
NCT00230178 (3) [back to overview]Plasma Uric Acid
NCT00241839 (4) [back to overview]Change in Systolic Blood Pressure by Cuff After 8-10 Weeks Minus Baseline
NCT00241839 (4) [back to overview]Change in Uric Acid (UA) Levels: Baseline Less End of Treatment
NCT00241839 (4) [back to overview]Change in Diastolic Blood Pressure by Cuff 8-10 Weeks Minus Baseline
NCT00241839 (4) [back to overview]Change in Overall Mean BP From Those Obtained by 24 Hour Ambulatory Blood Pressure Measurements (ABPM) 8-10 Weeks Minus Baseline.
NCT00430248 (17) [back to overview]Mean Percent Change From Baseline in Serum Urate Levels at Month 4 Visit
NCT00430248 (17) [back to overview]Mean Percent Change From Baseline in Serum Urate Levels at Month 6 Visit.
NCT00430248 (17) [back to overview]Mean Percent Change From Baseline in Serum Urate Levels at Final Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Level is <6.0 Milligrams Per Deciliter (mg/dL) at the Final Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Final Visit
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Month 2 Visit
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Month 4 Visit
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Month 6 Visit
NCT00430248 (17) [back to overview]Percentage of Renal Impairment Subjects Whose Final Visit Serum Urate Level is <6.0 mg/dl
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Month 2 Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Month 4 Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Month 6 Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Month 2 Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Month 4 Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Month 6 Visit.
NCT00430248 (17) [back to overview]Mean Percent Change From Baseline in Serum Urate Levels at Month 2 Visit.
NCT00430248 (17) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Final Visit.
NCT00513474 (3) [back to overview]Uric Acid Levels
NCT00513474 (3) [back to overview]Number of Participant With Adverse Events (AE)
NCT00513474 (3) [back to overview]Percentage of Participants With Grades II to IV Acute Graft-Versus-Host Disease (aGVHD)
NCT00643123 (1) [back to overview]Young Mania Rating Scale (YMRS)
NCT00652899 (4) [back to overview]Median Overall Survival Number of Days Patients Alive After Treatment
NCT00652899 (4) [back to overview]Median Number of Days to Progression
NCT00652899 (4) [back to overview]Number of Patients With In Vivo Expansion of Infused Allogeneic Natural Killer (NK) Cell Product
NCT00652899 (4) [back to overview]Number of Patients Per Disease Response
NCT00732251 (2) [back to overview]Number of Depressive Episodes Per Patient Visit According to the Hamilton Depression Scale
NCT00732251 (2) [back to overview]Number of Manic Episodes According to the Young Mania Rating Scale
NCT00793585 (2) [back to overview]Change in Renal Function as Measured With eGFR
NCT00793585 (2) [back to overview]The Longitudinal Change in Proteinuria and Blood Pressure(Including Changes in Antihypertensive Drugs Dosing).
NCT00819585 (12) [back to overview]Core Study: Mean Number of Gout Flares Per Participant
NCT00819585 (12) [back to overview]Core Study: Percentage of Participants With at Least 1 Gout Flare Within 16 Weeks After Randomization
NCT00819585 (12) [back to overview]Core Study: Participant's Assessment of Gout Pain on a 0-100 mm Visual Analog Scale up to Day 7 of All Gout Flares
NCT00819585 (12) [back to overview]Core Study: Participant's Assessment of Gout Pain on a 5-point Likert Scale up to Day 7 of All Gout Flares
NCT00819585 (12) [back to overview]Core Study: Percentage of Participants With Gout Flare at Different Time Points
NCT00819585 (12) [back to overview]Extension Study: Amount of Rescue Medication Taken
NCT00819585 (12) [back to overview]Extension Study: Participant's Assessment of Gout Pain on a 100 mm Visual Analog Scale During the First Flare
NCT00819585 (12) [back to overview]Extension Study: Participant's Global Assessment of Response to Treatment on a 5-point Likert Scale
NCT00819585 (12) [back to overview]Extension Study: Physician's Assessment of Tenderness, Swelling, and Erythema in the Most Affected Joint During the First Flare
NCT00819585 (12) [back to overview]Extension Study: Physician's Global Assessment of Response to Treatment on a 5-point Likert Scale
NCT00819585 (12) [back to overview]Core Study: Mean Number of Gout Flares for the Repeat Dose Regimen of Canakinumab as Compared to the Single Doses of Canakinumab
NCT00819585 (12) [back to overview]Core Study: Physician's Global Assessment of Response to Therapy on a 5-point Likert Scale
NCT00899431 (1) [back to overview]Percentage of Participants With GVHD (Graft Versus Host Disease)
NCT00987415 (5) [back to overview]Change in Submaximal Exercise Capacity (6-MWT)
NCT00987415 (5) [back to overview]Change in Quality of Life (KCCQ)
NCT00987415 (5) [back to overview]Change in Quality of Life (KCCQ).
NCT00987415 (5) [back to overview]Change in Submaximal Exercise Capacity (6-MWT)
NCT00987415 (5) [back to overview]A Composite Clinical Endpoint (CCE) That Classifies Subject's Clinical Status as Improved, Worsened, or Unchanged.
NCT01052272 (7) [back to overview]Peak Early Filling Rate Normalized to EDV
NCT01052272 (7) [back to overview]LV End Systolic Maximum Shortening (LVES Max Shortening)
NCT01052272 (7) [back to overview]Left Ventricular End-diastolic Mass Indexed to Left Ventricular End-diastolic Volume (LVED Mass/LVEDV)
NCT01052272 (7) [back to overview]Left Ventricular End Diastolic Volume Indexed to Body Surface Area (LVEDV/BSA)
NCT01052272 (7) [back to overview]Left Ventricular Ejection Fraction (LVEF)
NCT01052272 (7) [back to overview]Left Ventricular End Systolic Volume Indexed to Body Surface Area (LVESV/BSA)
NCT01052272 (7) [back to overview]Left Ventricular End-Diastolic Radius to Wall Thickness (LVED Radius/Wall Thickness)
NCT01077284 (4) [back to overview]Percent Change From Baseline to Month 6 in 24-hour Urine Uric Acid (uUA) Excretion
NCT01077284 (4) [back to overview]Change From Baseline to Month 6 in the Number of Calcium Oxalate Stones
NCT01077284 (4) [back to overview]Change From Baseline to Month 6 in 24-hour Measured Creatinine Clearance
NCT01077284 (4) [back to overview]Percent Change From Baseline to Month 6 in the In-plane Diameter of the Largest Calcium Oxalate (CaOx) Stone
NCT01101035 (7) [back to overview]Percentage of Participants With Non-fatal Myocardial Infarction (MI)
NCT01101035 (7) [back to overview]Percentage of Participants With Antiplatelet Trialists' Collaborative (APTC) Event
NCT01101035 (7) [back to overview]Percentage of Participants With Unstable Angina With Urgent Coronary Revascularization
NCT01101035 (7) [back to overview]Percentage of Participants With Primary Major Adverse Cardiovascular Events (MACE) Composite (75% Interim Analysis)
NCT01101035 (7) [back to overview]Percentage of Participants With Primary MACE Composite (Final Analysis)
NCT01101035 (7) [back to overview]Percentage of Participants With Cardiovascular (CV) Death
NCT01101035 (7) [back to overview]Percentage of Participants With Non-fatal Stroke
NCT01200485 (2) [back to overview]Number of Cycle 2 Participants Normalizing Uric Acid Levels (UAL) Within 24 Hours of Treatment
NCT01200485 (2) [back to overview]Number of Participants (Incidence) of LTLS (Laboratory Tumor Lysis Syndrome)
NCT01228903 (6) [back to overview]Change in Monocyte Chemotactic Protein-1 From Baseline to Week 12
NCT01228903 (6) [back to overview]Change in Oxidized Low Density Lipoprotein From Baseline to Week 12
NCT01228903 (6) [back to overview]Change in Serum Interleukin-6 From Baseline to Week 12
NCT01228903 (6) [back to overview]Change in Serum Uric Acid Levels From Baseline to Week 12
NCT01228903 (6) [back to overview]Change in Endothelial Dependent Dilation From Baseline to Week 12
NCT01228903 (6) [back to overview]Change in C-reactive Protein From Baseline to Week 12
NCT01320722 (9) [back to overview]Plasma Renin Activity (PRA) [Uric Acid]
NCT01320722 (9) [back to overview]Change in Renal Plasma Flow (RPF) Response to Captopril in High Sodium Balance [Uric Acid]
NCT01320722 (9) [back to overview]Change in Renal Plasma Flow (RPF) in Response to Captopril in High Sodium Balance [Vitamin D]
NCT01320722 (9) [back to overview]Angiotensin II (ATII) Concentration [Vitamin D]
NCT01320722 (9) [back to overview]Angiotensin II (ATII) Concentration [Uric Acid]
NCT01320722 (9) [back to overview]Mean 24-Hour Ambulatory Blood Pressure (ABP) Nocturnal Dipping
NCT01320722 (9) [back to overview]Mean 24-Hour Ambulatory Blood Pressure (ABP)
NCT01320722 (9) [back to overview]Change in Endothelium-Dependent Vasodilation (EDV)
NCT01320722 (9) [back to overview]Plasma Renin Activity (PRA) [Vitamin D]
NCT01391325 (4) [back to overview]Safety of Allopurinol
NCT01391325 (4) [back to overview]Proportion of Subjects With Serum Urate (sUA) Less Than 6.0 mg/dL
NCT01391325 (4) [back to overview]Incidence of Gout Flares
NCT01391325 (4) [back to overview]Mean Change From Baseline to Month 6 in SF-36 PCS+MCS
NCT01399008 (1) [back to overview]Serum Uric Acid
NCT01451645 (4) [back to overview]Mean Number of Gout Flare Days Per Participant Assessed From Day 1 to Week 16
NCT01451645 (4) [back to overview]Percentage of Participants With at Least 2 Gout Flares From Day 1 to Week 16
NCT01451645 (4) [back to overview]Number of Gout Flares Per Participant From Day 1 to Week 16
NCT01451645 (4) [back to overview]Percentage of Participants With at Least 1 Gout Flare From Day 1 to Week 16
NCT01459796 (2) [back to overview]Percentage of Participants With Rescue Medication From Day 1 to Day 364 (Week 52)
NCT01459796 (2) [back to overview]Percentage of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT01464359 (9) [back to overview]Duration of Survival
NCT01464359 (9) [back to overview]Duration of Survival
NCT01464359 (9) [back to overview]Incidence of Acute Graft-Versus-Host Disease
NCT01464359 (9) [back to overview]Transplant-Related Mortality
NCT01464359 (9) [back to overview]Incidence of Graft Failure
NCT01464359 (9) [back to overview]Duration of Survival
NCT01464359 (9) [back to overview]Clinical Disease Response
NCT01464359 (9) [back to overview]Clinical Disease Response
NCT01464359 (9) [back to overview]Disease Free Survival
NCT01493531 (3) [back to overview]Gout Flares
NCT01493531 (3) [back to overview]Subjects With ≥ 1 Target Tophus at Baseline Who Experience Complete Resolution of at Least 1 Target Tophus by Month 12
NCT01493531 (3) [back to overview]Subjects With a Serum Urate (sUA) < 6.0 mg/dL by Month 6.
NCT01510158 (3) [back to overview]Proportion of Subjects With an sUA Level That is < 6.0 mg/dL
NCT01510158 (3) [back to overview]Gout Flares
NCT01510158 (3) [back to overview]Tophus
NCT01564277 (6) [back to overview]Safety of Low Single-doses of Rasburicase.
NCT01564277 (6) [back to overview]Probability of Obtaining a Uric Acid Level =< 7.5mg/dL
NCT01564277 (6) [back to overview]Number of Patients Requiring Additional Doses of Rasburicase to Maintain a Uric Acid Level =< 7.5mg/dL
NCT01564277 (6) [back to overview]Area Under the Plasma Uric Acid Concentration-time Curve (AUC) From Baseline (Day 1) to Day 7
NCT01564277 (6) [back to overview]Baseline White Blood Cell Count by Response
NCT01564277 (6) [back to overview]Number of Patients Experiencing a Doubling of Serum Creatinine
NCT01637623 (11) [back to overview]Apnea-Hypopnea Index
NCT01637623 (11) [back to overview]Aortic Augmentation Index
NCT01637623 (11) [back to overview]Mean Change in PERCENT Vasodilation
NCT01637623 (11) [back to overview]Change in Mean 24-Hour Blood Pressure (Mean Arterial Pressure)
NCT01637623 (11) [back to overview]Change in Aortic Pulse Wave Velocity
NCT01637623 (11) [back to overview]Change in Minute Ventilation at Normoxia
NCT01637623 (11) [back to overview]PERCENT Time Spent Below 88 PERCENT Oxygen Saturation
NCT01637623 (11) [back to overview]Forearm Vascular Conductance
NCT01637623 (11) [back to overview]Change in Muscle Sympathetic Nerve Activity Responses During Hypoxia
NCT01637623 (11) [back to overview]Change in Minute Ventilation During Hypoxia
NCT01637623 (11) [back to overview]Cerebrovascular Conductance
NCT01685411 (15) [back to overview]Counts of Participants With Disease Free Survival
NCT01685411 (15) [back to overview]Count of Participants Who Achieved Neutrophil Engraftment
NCT01685411 (15) [back to overview]Count of Participants With Disease Free Survival
NCT01685411 (15) [back to overview]Percentage of Participants With Engraftment Failure
NCT01685411 (15) [back to overview]Percentage of Participants With Chronic Graft-Versus-Host Disease
NCT01685411 (15) [back to overview]Count of Participants With Disease Free Survival
NCT01685411 (15) [back to overview]Percentage of Participants With Acute Graft-Versus-Host Disease by Grade
NCT01685411 (15) [back to overview]Number of Participant Who Were Alive at 7 Years Post Transplant
NCT01685411 (15) [back to overview]Number of Participant Who Were Alive at 5 Years Post Transplant
NCT01685411 (15) [back to overview]Number of Participant Who Were Alive at 2 Years Post Transplant
NCT01685411 (15) [back to overview]Percentage of Participants With Chronic Graft-Versus-Host Disease
NCT01685411 (15) [back to overview]Percentage of Participants With Treatment-Related Toxicity
NCT01685411 (15) [back to overview]Percentage of Participants With Treatment-Related Toxicity
NCT01685411 (15) [back to overview]Percentage of Participants With Relapse
NCT01685411 (15) [back to overview]Percentage of Participants With Relapse
NCT01724528 (5) [back to overview]Assessment of Laboratory Tumor Lysis Syndrome (LTLS)
NCT01724528 (5) [back to overview]Assessment of Clinical Tumor Lysis Syndrome (CTLS)
NCT01724528 (5) [back to overview]Preservation of Renal Function
NCT01724528 (5) [back to overview]Serum Uric Acid (sUA) Level Control
NCT01724528 (5) [back to overview]Treatment Responder Rate
NCT01988402 (4) [back to overview]Resolution of the Acute Gout Attack
NCT01988402 (4) [back to overview]Pain Day 28
NCT01988402 (4) [back to overview]Physician Global Assessment of Gout Activity at Day 28
NCT01988402 (4) [back to overview]Serum Uric Acid Level
NCT02017171 (9) [back to overview]AER at the End of the Treatment Period
NCT02017171 (9) [back to overview]AER at the End of the Wash-out Period
NCT02017171 (9) [back to overview]eGFR at 4 Months of Treatment
NCT02017171 (9) [back to overview]eGFR Time Trajectory
NCT02017171 (9) [back to overview]Fatal or Non-fatal Cardiovascular Events
NCT02017171 (9) [back to overview]iGFR at the End of the Wash-out Period
NCT02017171 (9) [back to overview]iGFR the End of Treatment Period
NCT02017171 (9) [back to overview]iGFR Time Trajectory
NCT02017171 (9) [back to overview]Serum Creatinine Doubling or End Stage Renal Disease (ESRD)
NCT02038179 (3) [back to overview]Change in Flow-mediated Arterial Vasodilation
NCT02038179 (3) [back to overview]Change in Serum Levels of High Sensitivity C-reactive Protein
NCT02038179 (3) [back to overview]Change in Systolic Blood Pressure (SBP)
NCT02078219 (4) [back to overview]Absolute Change of Serum Uric Acid Levels From Baseline Levels
NCT02078219 (4) [back to overview]Percent Changes of Serum Uric Acid Levels From Baseline Levels
NCT02078219 (4) [back to overview]Percent Change in sUA
NCT02078219 (4) [back to overview]Percentage of Subjects With a Serum Uric Acid Level ≤6.0 mg/dL
NCT02082769 (3) [back to overview]Absolute Change in the Serum Urate Level at the Final Visit Relative to Baseline
NCT02082769 (3) [back to overview]Percentage of Subjects Whose Last Three Serum Urate Levels Are <6.0 Milligram Per Deciliter (mg/dL)
NCT02082769 (3) [back to overview]Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Final Visit
NCT02279641 (13) [back to overview]Time of Occurrence of Maximum Observed Concentration (Tmax)
NCT02279641 (13) [back to overview]Renal Clearance of the Drug From Time Zero up to 24 Hours Postdose (CRL0-24)
NCT02279641 (13) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT02279641 (13) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT02279641 (13) [back to overview]Incidence of Treatment-Emergent Adverse Events
NCT02279641 (13) [back to overview]Area Under the Concentration-time Curve From Time Zero up to 24 Hours Postdose (AUC 0-24)
NCT02279641 (13) [back to overview]Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Sampling Timepoint (AUC Last)
NCT02279641 (13) [back to overview]Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Sampling Timepoint (AUC Last)
NCT02279641 (13) [back to overview]Apparent Terminal Half-life (t1/2)
NCT02279641 (13) [back to overview]Amount Excreted in Urine as Unchanged Drug or Metabolite (Ae0-24)
NCT02279641 (13) [back to overview]Amount Excreted in Urine as Unchanged Drug or Metabolite (Ae0-24)
NCT02279641 (13) [back to overview]Area Under the Concentration-time Curve From Time Zero up to 24 Hours Postdose (AUC 0-24)
NCT02279641 (13) [back to overview]Pharmacodynamics (PD) Profile of Uric Acid From Serum and Urine
NCT02498652 (14) [back to overview]Cohort 2 - Concentration of Serum Urate at 24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol.
NCT02498652 (14) [back to overview]Cohort 2 - Maximum Percentage (%) Change in Serum Urate of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (Emax, CB (%))
NCT02498652 (14) [back to overview]Cohort 2 - Renal Hypoxanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeHXO, CB (%))
NCT02498652 (14) [back to overview]Cohort 2 - Renal Xanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeXO, CB (%))
NCT02498652 (14) [back to overview]Maximum Observed Concentration (Cmax)
NCT02498652 (14) [back to overview]Time of Occurrence of Maximum Observed Concentration (Tmax)
NCT02498652 (14) [back to overview]Number of Participants With Treatment-Emergent Adverse Events
NCT02498652 (14) [back to overview]Apparent Terminal Half-life (t1/2)
NCT02498652 (14) [back to overview]Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Sampling Timepoint (AUC Last)
NCT02498652 (14) [back to overview]Area Under the Concentration-time Curve From Time Zero up to 24 Hours Postdose (AUC 0-24)
NCT02498652 (14) [back to overview]Cohort 1 - Concentration of Serum Urate at 24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol.
NCT02498652 (14) [back to overview]Cohort 1 - Maximum Percentage (%) Change in Serum Urate of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (Emax, CB (%))
NCT02498652 (14) [back to overview]Cohort 1 - Renal Hypoxanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeHXO, CB (%))
NCT02498652 (14) [back to overview]Cohort 1 - Renal Xanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeXO, CB (%))
NCT02500641 (1) [back to overview]Pulse Wave Velocity
NCT02579096 (1) [back to overview]Percentage of Participants Experiencing ≥ 1 Gout Flare During Phase 3
NCT02752633 (1) [back to overview]Urinary 2,8-dihydroxyadenine Excretion
NCT02956278 (3) [back to overview]Percent Change Uric Acid
NCT02956278 (3) [back to overview]Oxypurinol AUC
NCT02956278 (3) [back to overview]Oxypurinol Renal Clearance
NCT03226899 (14) [back to overview]Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment
NCT03226899 (14) [back to overview]Percentage of Participants Meeting Criteria (eg, Based on sCr or eCrCl Criteria) for Treatment Discontinuations Over the Study Period
NCT03226899 (14) [back to overview]Percentage of Participants Who Achieve Serum Urate (sUA) < 6.0 mg/dL at Month 6
NCT03226899 (14) [back to overview]Percentage of Participants With Serum Creatinine (sCr) Elevations (≥1.5 × Baseline) Over the Study Period
NCT03226899 (14) [back to overview]Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment
NCT03226899 (14) [back to overview]Percentage of Participants Who Achieve sUA < 6.0 mg/dL Over Time
NCT03226899 (14) [back to overview]Percentage of Participants Who Achieve sUA < 6.0 mg/dL Over Time
NCT03226899 (14) [back to overview]Percentage of Participants Renal-Related and Kidney Stone Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT03226899 (14) [back to overview]Percent Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment
NCT03226899 (14) [back to overview]Percent Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment
NCT03226899 (14) [back to overview]Percent Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment
NCT03226899 (14) [back to overview]Percent Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment
NCT03226899 (14) [back to overview]Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment
NCT03226899 (14) [back to overview]Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment
NCT03648996 (3) [back to overview]Brachial Artery Flow Mediated Dilation (FMD)
NCT03648996 (3) [back to overview]Insulin-stimulated Leg Blood Flow
NCT03648996 (3) [back to overview]Carotid Femoral Pulse Wave Velocity (cfPWV)
NCT03865407 (6) [back to overview]Serum Uric Acid Change
NCT03865407 (6) [back to overview]Systolic Blood Pressure
NCT03865407 (6) [back to overview]Diastolic Blood Pressure
NCT03865407 (6) [back to overview]eGFR Change
NCT03865407 (6) [back to overview]eGFR Change
NCT03865407 (6) [back to overview]Serum High Sensitivity C-reactive Protein (Hs-CRP)
NCT03990363 (10) [back to overview]P-cystatin C (mg/L) Change From Baseline at 6 Months (V8), Repeated Measures Mixed Model (MMRM)
NCT03990363 (10) [back to overview]P-cystatin C (mg/L) Change From Baseline at 12 Months (Visit 10)
NCT03990363 (10) [back to overview]Estimated Glomerular Filtration Rate (eGFR) (mL/Min/1.73 m²) Change From Baseline at 6 Months (V8), Repeated Measures Mixed Model (MMRM)
NCT03990363 (10) [back to overview]Estimated Glomerular Filtration Rate (eGFR) (mL/Min/1.73 m²) Change From Baseline at 12 Months (Visit 10)
NCT03990363 (10) [back to overview]Serum Uric Acid (sUA) Change From Baseline at 12 Months (Visit 10), Repeated Measures Mixed Model (MMRM)
NCT03990363 (10) [back to overview]Urinary Albumin to Creatinine Ratio (uACR) (mg/g) Change From Baseline at 6 Months (Visit 8), Repeated Measures Mixed Model (MMRM)
NCT03990363 (10) [back to overview]Urinary Albumin to Creatinine Ratio (uACR) (mg/g) Change From Baseline at 12 Months (Visit 10), Repeated Measures Mixed Model (MMRM)
NCT03990363 (10) [back to overview]Serum Uric Acid (sUA) (mg/dL) Change From Baseline at 6 Months (Visit 8), Repeated Measures Mixed Model (MMRM)
NCT03990363 (10) [back to overview]S-creatinine (mg/dL) Change From Baseline at 6 Months (V8), Repeated Measures Mixed Model (MMRM)
NCT03990363 (10) [back to overview]S-creatinine (mg/dL) Change From Baseline at 12 Months (Visit 10)
NCT04256629 (25) [back to overview]Model Predicted Baseline-corrected and Placebo-corrected QT Interval Corrected for Heart Rate (HR) Using Fridericia's Formula (QTcF)(ΔΔQTcF) (Derived From Concentration-QTcF Analysis) at Geometric Mean of Cmax of Verinurad
NCT04256629 (25) [back to overview]Apparent Total Body Clearance of Drug From Plasma After Extravascular Administration (Parent Drug Only) (CL/F) for Verinurad and Allopurinol
NCT04256629 (25) [back to overview]Apparent Volume of Distribution at Steady State Following Extravascular Administration (Parent Drug Only) (Vss/F) for Verinurad and Allopurinol
NCT04256629 (25) [back to overview]Apparent Volume of Distribution During the Terminal Phase After Extravascular Administration (Parent Drug Only) (Vz/F) for Verinurad and Allopurinol
NCT04256629 (25) [back to overview]Time to Reach Maximum Plasma Concentration (Tmax) for Verinurad, M1, M8, Allopurinol, and Oxypurinol
NCT04256629 (25) [back to overview]Number of Participants With Adverse Events (AEs)
NCT04256629 (25) [back to overview]Terminal Half-life (t½λz) for Verinurad, M1, M8, Allopurinol, and Oxypurinol
NCT04256629 (25) [back to overview]Time Delay Between Drug Administration and the First Observed Concentration in Plasma (Tlag) for Verinurad, M1, M8, Allopurinol, and Oxypurinol
NCT04256629 (25) [back to overview]Baseline-corrected and Placebo-corrected QTcF Interval (ΔΔQTcF Interval)
NCT04256629 (25) [back to overview]Time of Last Quantifiable Plasma Concentration (Tlast) for Verinurad, M1, M8, Allopurinol, and Oxypurinol
NCT04256629 (25) [back to overview]Baseline-corrected QTcF Interval (ΔQTcF Interval)
NCT04256629 (25) [back to overview]Area Under Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC) for Verinurad, M1, M8, Allopurinol, and Oxypurinol
NCT04256629 (25) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC[0-t]) for Verinurad, M1, M8, Allopurinol, and Oxypurinol
NCT04256629 (25) [back to overview]Baseline-corrected and Placebo-adjusted Heart Rate (ΔΔHR)
NCT04256629 (25) [back to overview]Baseline-corrected and Placebo-adjusted PR Interval (ΔΔPR Interval)
NCT04256629 (25) [back to overview]Baseline-corrected and Placebo-adjusted RR Interval (ΔΔRR Interval)
NCT04256629 (25) [back to overview]Baseline-corrected and Placebo-corrected QRS Interval (ΔΔQRS Interval)
NCT04256629 (25) [back to overview]Baseline-corrected and Placebo-corrected QT Interval (ΔΔQT Interval)
NCT04256629 (25) [back to overview]Baseline-corrected Heart Rate (ΔHR)
NCT04256629 (25) [back to overview]Baseline-corrected PR Interval (ΔPR Interval)
NCT04256629 (25) [back to overview]Baseline-corrected QRS Interval (ΔQRS Interval)
NCT04256629 (25) [back to overview]Baseline-corrected QT Interval (ΔQT Interval)
NCT04256629 (25) [back to overview]Baseline-corrected RR Interval (ΔRR Interval)
NCT04256629 (25) [back to overview]Maximum Observed Plasma Concentration (Cmax) for Verinurad, M1, M8, Allopurinol, and Oxypurinol
NCT04256629 (25) [back to overview]Mean Residence Time of the Unchanged Drug in the Systemic Circulation From Zero to Infinity (MRT) for Verinurad and Oxypurinol
NCT04327024 (4) [back to overview]Change From Baseline at Week 32 in Peak V02 Consumption in Verinurad + Allopurinol Compared to Placebo (ANCOVA Model)
NCT04327024 (4) [back to overview]Change From Baseline at Week 32 in KCCQ-TSS in Verinurad+ Allopurinol Compared to Placebo (MMRM)
NCT04327024 (4) [back to overview]Change From Baseline at Week 32 in KCCQ-TSS in Verinurad+ Allopurinol Compared to Allopurinol Monotherapy (MMRM)
NCT04327024 (4) [back to overview]Change From Baseline at Week 32 in Peak V02 Consumption in Verinurad+ Allopurinol Compared to Allopurinol Monotherapy (ANCOVA Model)
NCT04532918 (21) [back to overview]Area Under Plasma Concentration-time Curve From Zero to 24 Hours Post-dose AUC(0-24) of Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Area Under Plasma Concentration-time Curve From Time Zero to Infinity (AUCinf) for Verinurad
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Area Under the Plasma Concentration-time Curve From Zero to Time of Last Quantifiable Concentration (AUClast) for Verinurad
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUClast for Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUCinf for Verinurad Metabolites: M1 and M8
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUCinf for Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Number of Participants With Adverse Events (AEs) and Serious AEs (SAEs)
NCT04532918 (21) [back to overview]Metabolite:Parent (MP) AUClast Ratios for M1 and M8: Verinurad
NCT04532918 (21) [back to overview]Metabolite:Parent (MP) AUCinf Ratios for M1 and M8: Verinurad
NCT04532918 (21) [back to overview]Metabolite:Parent (MP) Cmax Ratios for M1 and M8: Verinurad
NCT04532918 (21) [back to overview]Mean Residence Time of the Unchanged Drug in the Systemic Circulation (MRTinf) for Verinurad and Allopurinol
NCT04532918 (21) [back to overview]Time to Reach Peak or Maximum Plasma Concentration (Tmax) for Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Apparent Total Body Clearance of Drug From Plasma After Extravascular Administration (CL/F) for Verinurad and Allopurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Maximum Observed Plasma Peak Concentration (Cmax) for Verinurad
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUClast for Verinurad Metabolites: M1 and M8
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Cmax for Verinurad Metabolites: M1 and M8
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Cmax for Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration Time Curve (t½λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Terminal Elimination Rate Constant (λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Based on the Terminal Phase) (Vz/F) of Verinurad and Allopurinol
NCT04532918 (21) [back to overview]Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Vss/F) of Verinurad and Allopurinol
NCT04550234 (17) [back to overview]Vz/F: Apparent Volume of Distribution During Terminal Phase After Extravascular Administration
NCT04550234 (17) [back to overview]Vss/F: Apparent Volume of Distribution at Steady State Following Extravascular Administration
NCT04550234 (17) [back to overview]MRTinf: Mean Residence Time of the Unchanged Drug in the Systemic Circulation From Zero to Infinity
NCT04550234 (17) [back to overview]Cmax: Maximum Observed Plasma Drug Concentration
NCT04550234 (17) [back to overview]Tmax: Time to Reach Maximum Observed Plasma Concentration Following Drug Administration
NCT04550234 (17) [back to overview]Number of Subjects With Adverse Events (AEs) and Serious Adverse Events
NCT04550234 (17) [back to overview]Tlag: Time Delay Between Drug Administration and First Observed Concentration in Plasma
NCT04550234 (17) [back to overview]CL/F: Apparent Total Body Clearance of Drug Clearance of Drug From Plasma After Extravascular Administration
NCT04550234 (17) [back to overview]AUClast: Area Under Plasma Concentration-time Curve From Zero to the Last Quantifiable Concentration in Fasted Condition
NCT04550234 (17) [back to overview]AUCinf: Area Under Plasma Concentration-time Curve From 0 to Infinity in Fasted Condition
NCT04550234 (17) [back to overview]AUClast: Area Under Plasma Concentration-time Curve From Zero to the Last Quantifiable Concentration
NCT04550234 (17) [back to overview]tEmax, CB: Time of Maximum Percentage CB Change From Baseline (CB)
NCT04550234 (17) [back to overview]λz: Terminal Elimination Rate Constant
NCT04550234 (17) [back to overview]t½λz: Half-life Associated With Terminal Slope (λz) of Semi-logarithmic Concentration-time Curve
NCT04550234 (17) [back to overview]Cmax: Maximum Observed Plasma Drug Concentration in Fasted State
NCT04550234 (17) [back to overview]Emax, CB: Maximum Percentage Change From Baseline (CB)
NCT04550234 (17) [back to overview]AUCinf: Area Under Plasma Concentration-time Curve From 0 to Infinity

2 Year Event Free Survival

Percentage of patients who were event free at 2 years. The 2-year event free rate was estimated using the Kaplan Meier method. An event is defined as death, progression or treatment failure. (NCT00039130)
Timeframe: 2 years

Interventionpercentage of participants (Number)
Rituximab With High Intensity Chemotherapy78

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2 Year Overall Survival

Percentage of participants who were alive at 2 years. The 2 year survival, with 95% confidence interval, was estimated using the Kaplan Meier method. (NCT00039130)
Timeframe: 2 years

Interventionpercentage of participants (Number)
Rituximab With High Intensity Chemotherapy80

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Complete Response Rate

Response is assessed by investigator according to Revised Response Criteria for Malignant Lymphoma. Complete response requires disappearance of all evidence of disease. (NCT00039130)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Rituximab With High Intensity Chemotherapy83

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Number of Participants Who Proceed to Course V Within 2-6 Weeks of the Last Dose of Alemtuzumab (Phase II)

The primary endpoint is the number of participants who are able to proceed to course V within two - six weeks of completion of course IV. (NCT00061945)
Timeframe: 8 months

Interventionparticipants (Number)
Phase II - Alemtuzumab and Combination Chemotherapy30

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Number of Participants Achieving Complete Remission

A complete remission (CR) requires the following: an absolute neutrophil count (segs and bands) > 1500/μl, no circulating blasts, platelets > 100,000/μl; bone marrow cellularity > 20% with trilineage hematopoiesis, and < 5% marrow blast cells, none of which appear neoplastic. All previous extramedullary manifestations of disease must be absent (e.g., lymphadenopathy, splenomegaly, skin or gum infiltration, testicular masses, or CNS involvement). (NCT00061945)
Timeframe: 9 years

Interventionparticipants (Number)
Phase I - Alemtuzumab and Combination Chemotherapy92
Phase II - Alemtuzumab and Combination Chemotherapy145

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Minimal Residual Disease (MRD) During Treatment With Alemtuzumab (Phase II)

Minimal Residual Disease measures the presence of of circulating leukemia cells in the body. Patients that report a Complete Response (CR) during treatment are further tested to determine the presence of small amounts of circulating leukemia cells. Here we report the number of patients who were MRD negative. (NCT00061945)
Timeframe: 9 years 4 months

InterventionParticipants (Count of Participants)
Phase II - Alemtuzumab and Combination Chemotherapy16

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Disease-free Survival, for Only Complete Response Patients

Disease Free Survival (DFS) is defined as the time from a Complete Response (CR) until death or relapse. The date of last clinical assesment will be used as the censor date for patients with no death or relapse. The DFS will be estimated using the Kaplan-Meier method with confidence intervals presented. (NCT00061945)
Timeframe: 9 years 4 months

Interventionmonths (Median)
Phase I - Alemtuzumab and Combination Chemotherapy58.6
Phase II - Alemtuzumab and Combination Chemotherapy19.8

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Maximum Tolerated Dose (MTD) of Alemtuzumab (Phase I)

The maximum tolerated dose is defined as the highest alemtuzumab dose at which less than 40% of patients develop the dose limiting toxicity (DLT), where DLT is defined as the inability to proceed (due to medical complications) with the protocol treatment within six weeks of receiving the last dose of alemtuzumab. Groups of six patients will be enrolled into each cohort at the time of re-registration prior to starting Course IV. After a cohort has accrued 6 patients and at least 3 have completed the 2-6 week post alemtuzumab observation period without DLT, the incoming patients will be assigned to the next cohort in the table while the DLT and other toxicities continue to be assessed for the newly closed cohort. If less than 3 out of 6 enrolled patients in a cohort have completed the 2-6 week post alemtuzumab observation period without DLT, additional patients may continue to enroll in that same cohort, i.e., accrual will not be suspended while waiting for patient follow-up data. (NCT00061945)
Timeframe: 6 weeks

Interventionmg (Number)
Phase I - Alemtuzumab and Combination Chemotherapy30

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Overall Survival

Overall Survival is defines as the time from registration to death due to any cause. It is estimated using the Kaplan-Meier method with confidence intervals presented. (NCT00061945)
Timeframe: 9 years 4 months

Interventionmonths (Median)
Phase I - Alemtuzumab and Combination Chemotherapy33.6
Phase II - Alemtuzumab and Combination Chemotherapy23.1

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Percentage of Subjects With the Last 3 Serum Urate Levels <6.0 Milligrams Per Deciliter (mg/dL)

Each subject's serum urate at the last 3 visits determined the subject's response for the primary efficacy variable. A subject who prematurely discontinued without least 3 postbaseline serum urate levels was considered a nonresponder; if at least 3 serum urate were obtained postbaseline, those 3 visits were used. The last 3 visits used may have differed for each subject. (NCT00102440)
Timeframe: Last 3 Visits (up to 52 weeks)

InterventionPercentage of subjects (Number)
Febuxostat 80 mg QD53
Febuxostat 120 mg QD62
Allopurinol 300 mg QD21

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Change From Baseline in Total Number of Tophi at Final Visit in Subjects With Palpable Tophi at Screening.

Change in number of tophi/subject calculated for the subset of subjects with palpable tophi at Screening. If the tophi were not palpable at the Final Visit, total count was assumed to be 0. The timing of the final visit may have differed for each subject. (NCT00102440)
Timeframe: Baseline and Final Visit (up to 52 weeks)

Interventionnumber of tophi (Median)
Febuxostat 80 mg QD0.0
Febuxostat 120 mg QD0.0
Allopurinol 300 mg QD0.0

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Change From Baseline in Total Number of Tophi at Week 28 in Subjects With Palpable Tophi at Screening.

The change from baseline at Week 28 in the total number of tophi per subject was calculated for the subset of subjects with palpable tophi at the Screening Visit. If the tophi were no longer palpable at the Week 28 visit, the total count was assumed to be zero. (NCT00102440)
Timeframe: Baseline and Week 28

Interventionnumber of tophi (Median)
Febuxostat 80 mg QD0.0
Febuxostat 120 mg QD0.0
Allopurinol 300 mg QD0.0

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Change From Baseline in Total Number of Tophi at Week 52 in Subjects With Palpable Tophi at Screening.

The change from baseline at Week 52 in the total number of tophi per subject was calculated for the subset of subjects with palpable tophi at the Screening Visit. If the tophi were no longer palpable at the Week 52 visit, the total count was assumed to be zero. (NCT00102440)
Timeframe: Baseline and Week 52

Interventionnumber of tophi (Median)
Febuxostat 80 mg QD0.0
Febuxostat 120 mg QD-1.0
Allopurinol 300 mg QD0.0

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Percent Change From Baseline in Serum Urate Levels at Final Visit

The percent change in serum urate from baseline to the Final visit was calculated as [(Final Visit - baseline levels/baseline)]*100 and summarized. The Final visit was the last visit with a serum urate value. The timing of the final visit may have differed for each subject. (NCT00102440)
Timeframe: Baseline and Final Visit (up to 52 weeks)

Interventionpercent change from baseline (Mean)
Febuxostat 80 mg QD-44.7
Febuxostat 120 mg QD-51.5
Allopurinol 300 mg QD-33.0

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Percent Change From Baseline in Serum Urate Levels at Week 28.

Serum urate values were obtained at the Week 28 visit. The percent change in serum urate was calculated as [(week 28 - baseline levels/baseline)]*100 and summarized. (NCT00102440)
Timeframe: Baseline and Week 28

Interventionpercent change from baseline (Mean)
Febuxostat 80 mg QD-46.3
Febuxostat 120 mg QD-53.5
Allopurinol 300 mg QD-34.8

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Percent Change From Baseline in Serum Urate Levels at Week 52.

Serum urate values were obtained at the Week 52 visit. The percent change in serum urate was calculated as [(week 52 - baseline levels/baseline)]*100 and summarized. (NCT00102440)
Timeframe: Baseline and Week 52

Interventionpercent change from baseline (Mean)
Febuxostat 80 mg QD-47.7
Febuxostat 120 mg QD-53.0
Allopurinol 300 mg QD-34.8

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Percent Change From Baseline in Tophus Size at Final Visit, as Determined by Physical Measurement, in Subjects With a Palpable Primary Tophus at Screening.

Percent change in primary tophus size was calculated as [(Final Visit - baseline sizes)/baseline]*100 for the subset of subjects with a primary palpable tophus at Screening. If tophus was not palpable at Final visit, the size was assumed to be 0. The timing of the final visit may have differed for each subject. (NCT00102440)
Timeframe: Baseline and Final Visit (up to 52 weeks)

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-51.7
Febuxostat 120 mg QD-43.8
Allopurinol 300 mg QD-39.6

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Percent Change From Baseline in Tophus Size at Week 28, as Determined by Physical Measurement, in Subjects With a Palpable Primary Tophus at Screening.

The percent change from baseline in primary tophus size as determined by physical measurement was calculated as [(Week 28 - baseline sizes)/baseline]*100 for the subset of subjects with a primary palpable tophus at the Screening Visit. If the primary tophus was no longer palpable at the Week 28 visit, the size was assumed to be zero. (NCT00102440)
Timeframe: Baseline and Week 28

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-29.5
Febuxostat 120 mg QD-49.5
Allopurinol 300 mg QD-28.6

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Percent Change From Baseline in Tophus Size at Week 52, as Determined by Physical Measurement, in Subjects With a Palpable Primary Tophus at Screening.

The percent change from baseline in primary tophus size as determined by physical measurement was calculated as [(Week 52 - baseline sizes)/baseline]*100 for the subset of subjects with a primary palpable tophus at the Screening Visit. If the primary tophus was no longer palpable at the Week 52 visit, the size was assumed to be zero. (NCT00102440)
Timeframe: Baseline and Week 52

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-83.4
Febuxostat 120 mg QD-65.5
Allopurinol 300 mg QD-49.7

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Percentage of Subjects Requiring Treatment for Gout Flares Between Weeks 8 and 52.

The percentage of subjects requiring treatment for a gout flare between Weeks 8 and 52 of the double-blind treatment period was summarized. A subject who reported more than 1 gout flare during this period was counted only once. (NCT00102440)
Timeframe: Weeks 8 through 52

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD64
Febuxostat 120 mg QD70
Allopurinol 300 mg QD64

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Percentage of Subjects With Serum Urate <6.0 mg/dL at Final Visit

The percentage of subjects whose serum urate was <6.0 mg/dL at the final visit was summarized. The final visit was the last visit at which a serum urate value was collected. The timing of the final visit may have differed for each subject. (NCT00102440)
Timeframe: Final Visit (up to 52 weeks)

InterventionPercentage of subjects (Number)
Febuxostat 80 mg QD74
Febuxostat 120 mg QD80
Allopurinol 300 mg QD36

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Percentage of Subjects With Serum Urate <6.0 mg/dL at Week 28 Visit

Serum urate values were obtained at the Week 28 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Week 28 visit was summarized. (NCT00102440)
Timeframe: Week 28

InterventionPercentage of subjects (Number)
Febuxostat 80 mg QD72
Febuxostat 120 mg QD82
Allopurinol 300 mg QD42

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Percentage of Subjects With Serum Urate <6.0 mg/dL at Week 52 Visit

Serum urate values were obtained at the Week 52 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Week 52 visit was summarized. (NCT00102440)
Timeframe: Week 52

InterventionPercentage of subjects (Number)
Febuxostat 80 mg QD81
Febuxostat 120 mg QD82
Allopurinol 300 mg QD39

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Continuous Complete Remission at 1 Year

A patient has a continuous complete remission at 1 year if they achieve a CR and are alive 365 days after registering to the study. (NCT00109837)
Timeframe: After induction, after consolidation, every 3 months during maintenance, and every three months after off treatment for up to a year

Interventionparticipants (Number)
Treatment21

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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 (NCT00109837)
Timeframe: Patients were assessed for adverse events after the induction cycle

InterventionParticipants with a given type of AE (Number)
ALT, SGPT (serum glutamic pyruvic transaminase)AST, SGOT (serum glut oxaloacetic transaminase)Albumin, serum-low (hypoalbuminemia)Alkaline phosphataseAnorexiaAscites (non-malignant)Bilirubin (hyperbilirubinemia)Calcium, serum-low (hypocalcemia)CholecystitisCholesterol, serum-high (hypercholesterolemia)Coagulation-Other (Specify)Colitis, infectious (e.g., Clostridium difficile)ConstipationDIC (disseminated intravascular coagulation)Death not assoc with CTCAE term-Multi-organ failEdema: limbFatigue (asthenia, lethargy, malaise)Febrile neutropeniaFever (in the abs of neutropenia)FibrinogenGlucose, serum-high (hyperglycemia)Glucose, serum-low (hypoglycemia)HemoglobinHypertensionHypotensionHypoxiaIleus, GI (functional obstruction of bowel)Infec(doc clin or mibio) w/ Gr 3/4 neut-AnalInfec(doc clin or mibio) w/ Gr 3/4 neut-BladderInfec(doc clin or mibio) w/ Gr 3/4 neut-BloodInfec(doc clin or mibio) w/ Gr 3/4 neut-BronchusIInfec(doc clin or mibio) w/ Gr 3/4 neut-CatheterInfec(doc clin or mibio) w/ Gr 3/4 neut-Eye NOSInfec(doc clin or mibio) w/ Gr 3/4 neut-LungInfec(doc clin or mibio) w/ Gr 3/4 neut-NoseInfec(doc clin or mibio) w/ Gr 3/4 neut-PharynxInfec(doc clin or mibio) w/ Gr 3/4 neut-Ur tractInfec with nor ANC or Gr 1/2 neut-Lung (pneumonia)Infection-Other (Specify)Leukocytes (total WBC)LipaseLiver dysfunction/failure (clinical)LymphopeniaMagnesium, serum-high (hypermagnesemia)Mucositis/stomatitis (clinical exam) - Oral cavityMucositis/stomatitis (funct/symp) - Oral cavityMucositis/stomatitis (func/symp) - PharynxMuscle weak,gen spec area-Whole bodyNauseaNeuropathy: motorNeutrophils/granulocytes (ANC/AGC)Pain - Abdomen NOSPain - BonePain - NeckPancreatic endocrine: glucose intolerancePancreatitisPhosphate, serum-low (hypophosphatemia)PlateletsPotassium, serum-high (hyperkalemia)Potassium, serum-low (hypokalemia)Rash/desquamationRenal failureSodium, serum-low (hyponatremia)Thrombosis/thrombus/embolismThrombotic microangiopathyTriglyceride, serum-high (hypertriglyceridemia)Tumor lysis syndromeTyphlitis (cecal inflammation)Uric acid, serum-high (hyperuricemia)Vomiting
Induction171332216712111211318111161332321111111111122143121912112314711111144171261215111

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Global [11C]HED Retention Index (RI)

"Distal defects in [11C]meta-hydroxyephedrine ([11C]HED) retention involving at least 10 % of the left ventricle was used to define Cardiac Autonomic Neuropathy (CAN). The retention index (RI) is the unit of measure and is expressed as [11C]HEDblood min -1[ml tissue]-1~PET Data of Randomized Subjects at Baseline and 24-Months~The primary outcome was the change in the global [11C]HED RI = measure of cardiac innervation at 24 months in participants taking the active drug compared with those on placebo." (NCT00116207)
Timeframe: Baseline, 24 months

,
InterventionRetention index (Mean)
BASELINE24 MONTHS
ORAL ANTIOXIDANT0.0810.070
Placebo0.0730.074

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Global Coronary Flow Reserve as a Measure of Endothelial Function

global myocardial blood flow reserve as a measure of endothelial function. Measured by PET using [13N]ammonia at rest and during adenosine stimulated coronary vasodilation. (NCT00116207)
Timeframe: Baseline, 24 months

,
Interventionratio (rest:stress) (Mean)
BASELINE24 MONTH
ORAL ANTIOXIDANT2.953.02
Placebo2.943.22

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Inflammation

High Sensitivity CRP (nmol/L) (NCT00116207)
Timeframe: 24 months

Interventionnmol/L (Mean)
ORAL ANTIOXIDANT17.51
Placebo16.95

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Systemic Oxidative Stress

ng of 8-epi prostaglandin F2alpha /G creatinine assessed in 24 hour urine collection (NCT00116207)
Timeframe: 24 months

Interventionng/G creatinine (Mean)
ORAL ANTIOXIDANT2.92
Placebo2.09

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Percentage of Subjects Whose Last Three Serum Urate Levels Are <6.0 Milligram Per Deciliter (mg/dL).

Each subject's serum urate at the last 3 visits determined the subject's response for the primary efficacy variable. A subject who prematurely discontinued without least 3 postbaseline serum urate levels was considered a nonresponder; if at least 3 serum urate were obtained postbaseline, those 3 visits were used. The last 3 visits used may have differed for each subject. (NCT00174915)
Timeframe: Last 3 visits (any last 3 visits up to week 28)

InterventionPercentage of subjects (Number)
Febuxostat 80 mg QD48
Febuxostat 120 mg QD65
Febuxostat 240 mg QD69
Allopurinol QD22
Placebo QD0

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Percent Change From Baseline in Serum Urate Levels at Final Visit

The percent change in serum urate from baseline to the Final visit was summarized. The percent change in serum urate was calculated as [(Final visit - baseline levels)/baseline]*100. The final visit was the last visit at which a serum urate value was collected. The timing of the final visit may have differed for each subject. (NCT00174915)
Timeframe: Baseline and Final Visit (up to 28 weeks)

InterventionPercent change (Mean)
Febuxostat 80 mg QD-45.2
Febuxostat 120 mg QD-51.9
Febuxostat 240 mg QD-66.3
Allopurinol QD-33.7
Placebo QD-3.0

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Percent Change in Primary Tophus Size at Week 28, as Determined by Physical Measurement in the Subset of Subjects With Palpable Tophi at the Screening Visit.

The percent change from baseline in primary tophus size as determined by physical measurement was calculated as [(Week 28 - baseline sizes)/baseline]*100 for the subset of subjects with a primary palpable tophus at the Screening Visit. If the primary tophus was no longer palpable at the Week 28 visit, the size was assumed to be zero. (NCT00174915)
Timeframe: Baseline and Week 28

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-45.6
Febuxostat 120 mg QD-54.2
Febuxostat 240 mg QD-53.2
Allopurinol QD-31.5
Placebo QD-52.0

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Percent Change in Primary Tophus Size at Final Visit, as Determined by Physical Measurement in the Subset of Subjects With Palpable Tophi at the Screening Visit.

Percent change in primary tophus size was calculated as [(Final Visit - baseline sizes)/baseline]*100 for the subset of subjects with a primary palpable tophus at Screening. If tophus was not palpable at Final visit, the size was assumed to be 0. The timing of the final visit may have differed for each subject. (NCT00174915)
Timeframe: Baseline and Final Visit (up to 28 weeks)

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-33.8
Febuxostat 120 mg QD-42.4
Febuxostat 240 mg QD-47.0
Allopurinol QD-22.6
Placebo QD-40.3

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Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Week 28

Serum urate values were obtained at the Week 28 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Week 28 visit was summarized. (NCT00174915)
Timeframe: Week 28

InterventionPercentage of subjects (Number)
Febuxostat 80 mg QD76
Febuxostat 120 mg QD87
Febuxostat 240 mg QD94
Allopurinol QD41
Placebo QD1

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Change in the Total Number of Tophi at Week 28 in the Subset of Subjects With Palpable Tophi at the Screening Visit.

Change from baseline at Week 28 in the total number of tophi per subject was calculated for the subset of subjects with palpable tophi at the Screening Visit. If the tophi were not palpable at the Week 28 visit, the total count was assumed to be 0. (NCT00174915)
Timeframe: Baseline and Week 28

Interventionnumber of tophi (Median)
Febuxostat 80 mg QD0.0
Febuxostat 120 mg QD0.0
Febuxostat 240 mg QD0.0
Allopurinol QD0.0
Placebo QD0.0

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Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Final Visit

The percentage of subjects whose serum urate was <6.0 mg/dL at the final visit was summarized. The final visit was the last visit at which a serum urate value was collected and may have differed by subject. (NCT00174915)
Timeframe: Final Visit (up to 28 weeks).

InterventionPercentage of subjects (Number)
Febuxostat 80 mg QD72
Febuxostat 120 mg QD79
Febuxostat 240 mg QD92
Allopurinol QD39
Placebo QD1

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Percentage of Subjects Requiring Treatment for a Gout Flare Between Weeks 8 and 28 of the Double-Blind Treatment Period.

Percentage of subjects requiring treatment for a gout flare between Weeks 8 and 28 of the double-blind treatment period was summarized. A subject who reported more than 1 gout flare during this period was counted only once. (NCT00174915)
Timeframe: Weeks 8 through 28

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD55
Febuxostat 120 mg QD54
Febuxostat 240 mg QD57
Allopurinol QD46
Placebo QD52

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Percent Change From Baseline in Serum Urate Levels at Week 28.

Serum urate values were obtained at the Week 28 visit. The percent change in serum urate was calculated as [(Week 28 - baseline levels)/baseline]*100 and summarized. (NCT00174915)
Timeframe: Baseline and Week 28

InterventionPercent change (Mean)
Febuxostat 80 mg QD-47.6
Febuxostat 120 mg QD-54.9
Febuxostat 240 mg QD-67.8
Allopurinol QD-34.4
Placebo QD-3.6

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Change in the Total Number of Tophi at Final Visit in the Subset of Subjects With Palpable Tophi at the Screening Visit

Change in number of tophi/subject was calculated for the subset of subjects with palpable tophi at the Screening. If the tophi were not palpable at the Final Visit, total count was assumed to be 0. The timing of the final visit may have differed for each subject. (NCT00174915)
Timeframe: Final Visit (up to 28 weeks)

Interventionnumber of tophi (Median)
Febuxostat 80 mg QD0.0
Febuxostat 120 mg QD0.0
Febuxostat 240 mg QD0.0
Allopurinol QD0.0
Placebo QD0.0

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Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 24.

Serum urate values were obtained at the Month 24 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Month 24 visit was summarized. (NCT00175019)
Timeframe: Month 24

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD89.3
Febuxostat 120 mg QD87.2
Allopurinol QD78.6

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Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 36.

Serum urate values were obtained at the Month 36 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Month 36 visit was summarized. (NCT00175019)
Timeframe: Month 36

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD90.8
Febuxostat 120 mg QD91.5
Allopurinol QD90.0

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Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 12.

Serum urate values were obtained at the Month 12 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Month 12 visit was summarized. (NCT00175019)
Timeframe: Month 12

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD88.9
Febuxostat 120 mg QD86.3
Allopurinol QD82.2

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Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Last Visit on Treatment.

The percentage of subjects whose serum urate was <6.0 mg/dL at the last visit on treatment was summarized. The last visit on treatment was the last visit at which a serum urate value was collected prior to any changes in drug and/or dose from the initial treatment assignment. (NCT00175019)
Timeframe: Last Visit on treatment (up to 40 months).

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD70.8
Febuxostat 120 mg QD82.0
Allopurinol QD32.6

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Percentage of Subjects Whose Serum Urate Level Decreases to < 6.0 mg/dL at Month 1.

Serum urate values were obtained at the Month 1 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Month 1 visit was summarized. (NCT00175019)
Timeframe: Month 1

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD80.8
Febuxostat 120 mg QD87.0
Allopurinol QD46.0

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Percentage of Subjects Requiring Treatment for Gout Flare up to Month 12.

The percentage of subjects requiring treatment for gout flare during the first twelve months of final stable treatment was summarized. (NCT00175019)
Timeframe: Month 12

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD29.4
Febuxostat 120 mg QD42.5
Allopurinol QD28.3

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Percent Change From Baseline in Primary Tophus Size at Month 36 for Subjects With Palpable Tophi Measured at Baseline.

The area of the primary tophus was calculated based on the length and width of the tophus measured at baseline and Month 36 visit. The percent change from baseline in primary tophus size to the Month 36 visit was summarized. (NCT00175019)
Timeframe: Month 36

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-83

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Percentage of Subjects Requiring Treatment for Gout Flare After Month 12.

The percentage of subjects requiring treatment for gout flare after the first 12 months of final stable treatment was summarized. (NCT00175019)
Timeframe: After Month 12 to Final Visit

Interventionpercentage of subjects (Number)
Febuxostat 80 mg QD15.3
Febuxostat 120 mg QD19.8
Allopurinol QD23.2

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Percent Change in Serum Urate Levels From Baseline to the Last Visit on Treatment.

The percent change in serum urate from baseline to the last visit on treatment was summarized. The last visit on treatment was the last visit at which a serum urate value was collected prior to any changes in drug and/or dose from the initial treatment assignment. (NCT00175019)
Timeframe: Last Visit on treatment (up to 40 months).

Interventionpercent change from baseline (Mean)
Febuxostat 80 mg QD-46.69
Febuxostat 120 mg QD-52.99
Allopurinol QD-32.17

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Percent Change From Baseline in the Total Number of Tophi for Subjects With Palpable Tophi at Final Visit.

The number of tophi were counted at baseline and final visits. The percent change from baseline in the number of tophi to the final visit was summarized. (NCT00175019)
Timeframe: Final Visit (up to 40 months).

Interventionpercent change from baseline (Mean)
Febuxostat 80 mg QD-59.9
Febuxostat 120 mg QD-58.3
Allopurinol QD-48.7

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Percent Change From Baseline in Primary Tophus Size at Month 24 for Subjects With Palpable Tophi Measured at Baseline.

The area of the primary tophus was calculated based on the length and width of the tophus measured at baseline and Month 24 visit. The percent change from baseline in primary tophus size to the Month 24 visit was summarized. (NCT00175019)
Timeframe: Month 24

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-100
Febuxostat 120 mg QD-96
Allopurinol QD-87

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Percent Change From Baseline in Primary Tophus Size at Month 12 for Subjects With Palpable Tophi Measured at Baseline.

The area of the primary tophus was calculated based on the length and width of the tophus measured at the Month 12 visit. The percent change from baseline in primary tophus size to the Month 12 visit was summarized. (NCT00175019)
Timeframe: Month 12

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-82
Febuxostat 120 mg QD-79
Allopurinol QD-56

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Percent Change From Baseline in Primary Tophus Size at Final Visit for Subjects With Palpable Tophi Measured at Baseline.

The area of the primary tophus was calculated based on the length and width of the tophus measured at baseline and final visit. The percent change from baseline in primary tophus size to the final visit was summarized. (NCT00175019)
Timeframe: Final Visit (up to 40 months).

Interventionpercent change from baseline (Median)
Febuxostat 80 mg QD-96
Febuxostat 120 mg QD-84
Allopurinol QD-67

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Myocardial Creatine Kinase (CK) Flux Pre Intravenous Allopurinol Infusion

Magnetic resonance spectroscopy (MRS) Measurement of Myocardial CK Flux Pre Intravenous Allopurinol Infusion (NCT00181155)
Timeframe: Onset of imaging acquisition.

Interventionumol/g/sec (Mean)
Baseline2.07

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Cardiac PCr/ATP Post Intravenous Infusion

The mean ratio of creatine phosphate (PCr) to ATP in the heart. This measure, as a ratio, is unitless. (NCT00181155)
Timeframe: acute (within 15 minutes of single infusion)

Interventionratio (Mean)
Intravenous Allopurinol1.75

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Cardiac PCr/ATP Pre Intravenous Infusion

The mean ratio of creatine phosphate (PCr) to ATP in the heart. This measure, as a ratio, is unitless. (NCT00181155)
Timeframe: Onset of image acquisition.

Interventionratio (Mean)
Baseline1.58

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Myocardial CK Flux Post Intravenous Allopurinol Infusion.

The mean rate of adenosine triphosphate (ATP) flux through the creatine kinase reaction in the heart. (NCT00181155)
Timeframe: acute (within 15 minutes of single infusion)

Interventionumol/g/sec (Mean)
Intravenous Allopurinol2.87

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Plasma Uric Acid Responder

Number of patients responding to treatment defined as plasma uric acid levels at Day 3 through Day 7 <7.5 mg/dl. (NCT00230178)
Timeframe: Day 3 through Day 7

,,
InterventionParticipants (Number)
ResponderNon-Responder
Allopurinol6031
Rasburicase8012
Rasburicase + Allopurinol7220

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Time to Uric Acid Control

Time from the first dose of study drug to the time at which plasma uric acid concentrations were determined <=7.5 mg/dl, measured -4, 4, 24, 48, 72, 96, 120, and 144 hours after infusion. (NCT00230178)
Timeframe: Day 1 to Day 7

InterventionHours (Median)
Rasburicase4.1
Rasburicase + Allopurinol4.1
Allopurinol27.0

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Plasma Uric Acid

Area under the curve concentration versus time curve extrapolated to infinity (AUC) of plasma uric acid values (NCT00230178)
Timeframe: Day 1 to Day 7

Interventionmg*h/dL (Mean)
Rasburicase77.25
Rasburicase + Allopurinol108.05
Allopurinol646.22

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Change in Systolic Blood Pressure by Cuff After 8-10 Weeks Minus Baseline

"The systolic BP was taken at Baseline and after 8-10 weeks of treatment on placebo, while on chlorthalidone and potassium chloride. The blood pressure was measured according to Shared Care protocol: 15 minutes of quiet, undisturbed rest with three BP measurements obtained subsequently at 5 minute intervals.~The mean of the second and third reading was the value used for analysis for both the Baseline measurement and the measurement after 8 - 10 weeks of treatment. The dependent variable is baseline value minus ending value.~Measures are in millimeters of mercury (mm hg)" (NCT00241839)
Timeframe: Measured at 8-10 weeks on allopurinol or placebo

Interventionmm Hg (Mean)
A (Allopurinol)0.21
B (Placebo)-0.95

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Change in Uric Acid (UA) Levels: Baseline Less End of Treatment

Subjects on allopurinol are expected to lower their uric acid levels relative to placebo. (NCT00241839)
Timeframe: Baseline UA levels compared to end of treatment levels (8-10 weeks on allopurinol / placebo)

Interventionmg/dl (Mean)
A (Allopurinol)2.29
B (Placebo)0.14

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Change in Diastolic Blood Pressure by Cuff 8-10 Weeks Minus Baseline

"The Diastolic BP was taken at Baseline and after 8-10 weeks of treatment or placebo while on chlorthalidone and potassium chloride. The blood pressure was measured according to Shared Care protocol: 15 minutes of quiet, undisturbed rest with three BP measurements obtained subsequently at 5 minute intervals.~The mean of the second and third reading was the value used for analysis for both the Baseline measurement and the measurement after 8 - 10 weeks of treatment. The dependent variable is baseline value minus ending value.~Measures are in millimeters of mercury (mm hg)" (NCT00241839)
Timeframe: Measured at 8-10 weeks on allopurinol / placebo

Interventionmm Hg (Mean)
A (Allopurinol)3.44
B (Placebo)-0.83

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Change in Overall Mean BP From Those Obtained by 24 Hour Ambulatory Blood Pressure Measurements (ABPM) 8-10 Weeks Minus Baseline.

Subjects had 24 hr blood pressure monitoring (ABPM) at baseline and treatment end. The readings were averaged and the changes from baseline to treatment end were compared. (NCT00241839)
Timeframe: Baseline and end of treatment (8-10 weeks on allopurinol / placebo)

Interventionmm Hg (Mean)
A (Allopurinol)-5.9
B (Placebo)0.90

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Mean Percent Change From Baseline in Serum Urate Levels at Month 4 Visit

Serum urate values were obtained at the Month 4 visit. The percent change in serum urate from baseline to the Month 4 visit was summarized. (NCT00430248)
Timeframe: Baseline and Month 4

Interventionpercent change from baseline (Mean)
Febuxostat 40 mg QD-34.9
Febuxostat 80 mg QD-45.5
Allopurinol 200 mg or 300 mg QD-34.5

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Mean Percent Change From Baseline in Serum Urate Levels at Month 6 Visit.

Serum urate values were obtained at the Month 6 visit. The percent change in serum urate from baseline to the Month 6 visit was summarized. (NCT00430248)
Timeframe: Baseline and Month 6

Interventionpercent change from baseline (Mean)
Febuxostat 40 mg QD-35.6
Febuxostat 80 mg QD-45.1
Allopurinol 200 mg or 300 mg QD-34.4

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Mean Percent Change From Baseline in Serum Urate Levels at Final Visit.

The percent change in serum urate from baseline to the Final visit was summarized. The final visit was the last visit at which a serum urate value was collected. (NCT00430248)
Timeframe: Baseline and Last Visit on treatment (up to 6 months)

Interventionpercent change from baseline (Mean)
Febuxostat 40 mg QD-33.1
Febuxostat 80 mg QD-40.6
Allopurinol 200 mg or 300 mg QD-31.3

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Percentage of Subjects Whose Serum Urate Level is <6.0 Milligrams Per Deciliter (mg/dL) at the Final Visit.

The percentage of subjects whose serum urate level was <6.0 mg/dL at the Final Visit was summarized. The Final Visit was the last visit at which a serum urate value was collected. (NCT00430248)
Timeframe: Last Visit on treatment (up to 6 months)

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD45.2
Febuxostat 80 mg QD67.1
Allopurinol 200 mg or 300 mg QD42.1

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Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Final Visit

The percentage of subjects whose serum urate level was <4.0 mg/dL at the Final Visit was summarized. The Final Visit was the last visit at which a serum urate values was collected. (NCT00430248)
Timeframe: Last Visit on treatment (up to 6 months)

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD2.5
Febuxostat 80 mg QD17.5
Allopurinol 200 mg or 300 mg QD1.5

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Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Month 2 Visit

Serum urate values were obtained at the Month 2 visit. The percentage of subjects whose serum urate was <4.0 mg/dL at the Month 2 visit was summarized. (NCT00430248)
Timeframe: Month 2

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD2.1
Febuxostat 80 mg QD17.5
Allopurinol 200 mg or 300 mg QD1.5

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Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Month 4 Visit

Serum urate values were obtained at the Month 4 visit. The percentage of subjects whose serum urate was <4.0 mg/dL at the Month 4 visit was summarized. (NCT00430248)
Timeframe: Month 4

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD2.0
Febuxostat 80 mg QD18.6
Allopurinol 200 mg or 300 mg QD1.4

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Percentage of Subjects Whose Serum Urate Levels Are <4.0 mg/dL at Month 6 Visit

Serum urate values were obtained at the Month 6 visit. The percentage of subjects whose serum urate was <4.0 mg/dL at the Month 6 visit was summarized. (NCT00430248)
Timeframe: Month 6

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD3.1
Febuxostat 80 mg QD20.3
Allopurinol 200 mg or 300 mg QD1.8

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Percentage of Renal Impairment Subjects Whose Final Visit Serum Urate Level is <6.0 mg/dl

The percentage of subjects with mild-to-moderate renal impairment whose serum urate was <6.0 mg/dL at the final visit was summarized. The final visit was the last visit at which a serum urate value was collected. (NCT00430248)
Timeframe: Last Visit on treatment (up to 6 months)

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD49.7
Febuxostat 80 mg QD71.6
Allopurinol 200 mg or 300 mg QD42.3

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Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Month 2 Visit.

Serum urate values were obtained at the Month 2 visit. The percentage of subjects whose serum urate was <5.0 mg/dL at the Month 2 visit was summarized. (NCT00430248)
Timeframe: Month 2

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD15.4
Febuxostat 80 mg QD45.9
Allopurinol 200 mg or 300 mg QD11.7

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Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Month 4 Visit.

Serum urate values were obtained at the Month 4 visit. The percentage of subjects whose serum urate was <5.0 mg/dL at the Month 4 visit was summarized. (NCT00430248)
Timeframe: Month 4

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD15.0
Febuxostat 80 mg QD51.6
Allopurinol 200 mg or 300 mg QD13.5

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Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Month 6 Visit.

Serum urate values were obtained at the Month 6 visit. The percentage of subjects whose serum urate was <5.0 mg/dL at the Month 6 visit was summarized. (NCT00430248)
Timeframe: Month 6

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD19.3
Febuxostat 80 mg QD49.7
Allopurinol 200 mg or 300 mg QD14.8

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Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Month 2 Visit.

Serum urate values were obtained at the Month 2 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Month 2 visit was summarized. (NCT00430248)
Timeframe: Month 2

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD49.1
Febuxostat 80 mg QD74.1
Allopurinol 200 mg or 300 mg QD43.2

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Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Month 4 Visit.

Serum urate values were obtained at the Month 4 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Month 4 visit was summarized. (NCT00430248)
Timeframe: Month 4

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD47.1
Febuxostat 80 mg QD75.2
Allopurinol 200 mg or 300 mg QD45.5

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Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Month 6 Visit.

Serum urate values were obtained at the Month 6 visit. The percentage of subjects whose serum urate was <6.0 mg/dL at the Month 6 visit was summarized. (NCT00430248)
Timeframe: Month 6

Interventionpercentage of participants (Number)
Febuxostat 40 mg QD48.9
Febuxostat 80 mg QD75.3
Allopurinol 200 mg or 300 mg QD46.6

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Mean Percent Change From Baseline in Serum Urate Levels at Month 2 Visit.

Serum urate values were obtained at the Month 2 visit. The percent change in serum urate from baseline to the Month 2 visit was summarized. (NCT00430248)
Timeframe: Baseline and Month 2

Interventionpercent change from baseline (Mean)
Febuxostat 40 mg QD-35.1
Febuxostat 80 mg QD-44.5
Allopurinol 200 mg or 300 mg QD-33.8

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Percentage of Subjects Whose Serum Urate Levels Are <5.0 mg/dL at Final Visit.

The percentage of subjects whose serum urate level was <5.0 mg/dL at the Final Visit was summarized. The Final Visit was the last visit at which a serum urate values was collected. (NCT00430248)
Timeframe: Last Visit on treatment (up to 6 months)

Interventionpercentage of subjects (Number)
Febuxostat 40 mg QD16.5
Febuxostat 80 mg QD44.0
Allopurinol 200 mg or 300 mg QD13.2

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Uric Acid Levels

Blood was collected and analyzed at a laboratory for serum uric acid levels reported in milligrams(mg)/deciliter(dL). Data is presented for those participants who experienced Grade II to IV aGVHD and those participants who did not experience Grade II to IV aGVHD at pre-transplant and post-transplant. (NCT00513474)
Timeframe: Pre-transplant Day -7 to Day -1 and Post-transplant Day 0 to Day 6

,
Interventionmg/dL (Mean)
Day -7Day -6Day -5Day -4Day -3Day -2Day -1Day 0Day 1Day 2Day 3Day 4Day 5Day 6
Control Group4.1573.4192.9672.5792.3581.8671.712.1632.6712.7782.8052.7582.5792.653
Rasburicase Group0.10.0750.0860.10.0670.0810.4380.9381.6242.0762.2712.5482.5952.705

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Number of Participant With Adverse Events (AE)

An AE is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. (NCT00513474)
Timeframe: Up to 71 months

InterventionParticipants (Count of Participants)
Rasburicase Group21
Control Group21

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Percentage of Participants With Grades II to IV Acute Graft-Versus-Host Disease (aGVHD)

"aGVHD severity was determined using International Bone Marrow Transplant Registry (IBMTR) scale stage and grade of the skin, liver and gut. Stage 1: Skin=maculopapular rash <25% of body surface; Liver=Bilirubin 2-3 mg/dL and Gut=500-999 mL diarrhea/day or peristent nausea with histologic evidence of GvHD. Stage 2: Skin=maculopapular rash 25-50% of body surface; Liver=Bilirubin 3.1-6 mg/dL and Gut=1000-1499 mL diarrhea/day. Stage 3: Skin=maculopapular rash >50% of body surface; Liver=Bilirubin 6.1-15 mg/dL and Gut=≥1500 mL diarrhea/day. Stage 4: Skin=generalized erythroderma with bulla formation; Liver=Bilirubin >15 mg/dL and Gut=severe abdominal pain.~Grade 1: Stage 1-2 rash; no liver or gut involvement. Grade II: Stage 3 rash, or stage 1 liver involvement, or stage 1 gut involvement. Grade III: None to stage 3 skin rash with stage 2-3 liver, or stage 2-4 gut involvement. Grade IV: Stage 4 skin rash, or stage 4 liver involvement." (NCT00513474)
Timeframe: Up to 71 months

Interventionpercentage of participants (Number)
Rasburicase Group24
Control Group57

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Young Mania Rating Scale (YMRS)

"The YMRS is an 11-item, clinician-administered rating scale to assess the severity of manic symptoms before, during and after treatment. There are four items that are graded on a 0 to 8 scale (irritability, speech, thought content, and disruptive/aggressive behavior), while the remaining seven items are graded on a 0 to 4 scale. A score of 0 indicates the behavior is absent, whereas a score of 4 or 8 indicates the behavior is present and severe.~The change in score between Baseline and the Completion Visit will be reported. Ideally, the two time points will be Baseline and 6 Weeks after Baseline, but, if a subject terminates early, his/her last YMRS score will be carried forward to the final visit.~The scores from each question are added together to form a total score ranging from 0 to 60, with higher scores indicating a greater severity of symptoms. A score of 0-12 indicates the absence of mania or a very mild manic state, a score of 13-20 or higher indicates a mild man" (NCT00643123)
Timeframe: 7 weeks (Baseline and 6 weeks (or last visit date) after baseline

Interventionunits on a scale (Mean)
Allopurinol-12.3
Placebo-9.6

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Median Overall Survival Number of Days Patients Alive After Treatment

Median number of days patients alive from date of treatment to date of death or date of last follow-up if censored. (NCT00652899)
Timeframe: From first date on-study (treatment) to date of death

InterventionDays (Median)
Total Body Irradiation171.5
No Total Body Irradiation291

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Median Number of Days to Progression

Median number of days from first date of treatment to date of disease progression (appearance of new metastatic lesions or objective tumor progression). Defined by computated tomography (CT) imaging based on Response Evaluation Criteria In Solid Tumors (RECIST): Progressive Disease (PD) > or = 20% increase in sum of all target or any new lesions. (NCT00652899)
Timeframe: From date of first treatment to disease progression

InterventionDays (Median)
No Total Body Irradiation107
Total Body Irradiation90

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Number of Patients With In Vivo Expansion of Infused Allogeneic Natural Killer (NK) Cell Product

Detection of an absolute donor derived cell count of > or = 100 cells/mL after NK cell infusion. (NCT00652899)
Timeframe: Day 12-14

InterventionPatients (Number)
Ovarian/Fallopian Tube/Peritoneal Cancer Patients0

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Number of Patients Per Disease Response

Response Evaluation Criteria in Solid Tumors (RECIST) criteria: Complete Response (CR)-Disappearance of all target lesions (TL); Partial Response (PR)-< or = 30% decrease in the sum of the longest diameter (LD) of TL, reference baseline sum LD; Stable Disease (SD)-Neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, reference the smallest sum LD since the treatment started; Progressive Disease (PD)- < or = 20% increase in the sum of the LD of TL, reference the smallest sum LD recorded since treatment started or appearance of < or = 1 new lesion. (NCT00652899)
Timeframe: 1 Month After Natural Killer Cell Infusion (Day 30)

,
InterventionPatients (Number)
Complete ResponsePartial ResponseStable DiseaseProgressive Disease
No Total Body Irradiation0241
Total Body Irradiation0140

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Number of Depressive Episodes Per Patient Visit According to the Hamilton Depression Scale

The Hamilton Depression Rating Scale is a tool used to determine a patient's level of depression before, during, and after treatment. The Hamilton Depression Scale form lists 21 items, but the scoring is based on the first 17 questions. Eight items are scored on a 5-point scale, ranging from 0 (min) = not present to 4 (max) = severe. Nine are scored from 0 (min) to 2 (max). The sum of the scores from the first 17 questions is: 0 (min) to 7 (max) = normal, 8 (min) to 13 (max) = mild depression, 14 (min) to 18 (max) = moderate depression, 19 (min) to 22 (max) = severe depression and ≥ 23=very severe depression. A score of 11 or more indicates a depressive episode in terms of this outcome measure. (NCT00732251)
Timeframe: 2 years

Interventionpatient visits (Count of Units)
Allopurinol7

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Number of Manic Episodes According to the Young Mania Rating Scale

"Young Mania Rating Scale is an 11-item, clinician-administered scale to assess severity of manic symptoms before, during and after treatment. Four items are graded on a min. 0 to max. 8 scale (irritability, speech, thought content and disruptive/aggressive behavior) while the remaining 7 items are graded on a min. 0 to max. 4 scale. A score of 0 indicates behavior is absent and score of 4 or 8 indicates the behavior is present and severe.~The change in score between Baseline and the Completion Visit will be reported. Ideally, the two time points will be Baseline and 6 Weeks after Baseline, but if a subject terminates early, the last Young Mania Rating Scale score will be used. The scores from each question are added for a total score ranging from min. 0 to max 60; higher scores indicate greater severity of symptoms. A score of 0-12 indicates the absence of mania or a very mild manic state, a score of 13-20 or higher indicates a mild manic episode, and over 20 indicates a manic state. (NCT00732251)
Timeframe: 2 Years

Interventionpatient visits (Count of Units)
Allopurinol3

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Change in Renal Function as Measured With eGFR

(NCT00793585)
Timeframe: baseline and 6 months

InterventioneGFR(min/ml) (Mean)
Control Group68.9
Allopurinol Group73.2

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The Longitudinal Change in Proteinuria and Blood Pressure(Including Changes in Antihypertensive Drugs Dosing).

(NCT00793585)
Timeframe: baseline and 6 months

InterventionUpro/cr (mg/g) (Mean)
Control Group1170.4
Allopurinol Group1219.3

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Core Study: Mean Number of Gout Flares Per Participant

A gout flare was defined as an increase in participant-reported gout pain in the most affected joint during a gout attack. (NCT00819585)
Timeframe: Baseline of the core study to Week 16

InterventionGout flares (Mean)
Core Study: Canakinumab 25 mg0.5
Core Study: Canakinumab 50 mg0.4
Core Study: Canakinumab 100 mg0.2
Core Study: Canakinumab 200 mg0.4
Core Study: Canakinumab 300 mg0.2
Core Study: Canakinumab q4wk0.7
Core Study: Colchicine 0.5 mg0.7

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Core Study: Percentage of Participants With at Least 1 Gout Flare Within 16 Weeks After Randomization

The percentage of participants experiencing at least 1 gout flare within 16 weeks after randomization. A gout flare was defined as an increase in participant-reported gout pain in the most affected joint during a gout attack. (NCT00819585)
Timeframe: Baseline of the core study to Week 16

InterventionPercentage of participants (Number)
Core Study: Canakinumab 25 mg27.3
Core Study: Canakinumab 50 mg16.7
Core Study: Canakinumab 100 mg14.8
Core Study: Canakinumab 200 mg18.5
Core Study: Canakinumab 300 mg15.1
Core Study: Canakinumab q4wk16.7
Core Study: Colchicine 0.5 mg44.4

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Core Study: Participant's Assessment of Gout Pain on a 0-100 mm Visual Analog Scale up to Day 7 of All Gout Flares

Participants rated the intensity of pain in the most affected joint on a 0-100 mm visual analog scale, which ranged from no pain (left end, 0) to unbearable pain (right end, 100). Participants assessed pain intensity on the day of onset of the gout flare and in the morning of the 6 following days. (NCT00819585)
Timeframe: Baseline of the core study to Week 16

,,,,,,
InterventionUnits on a scale (Mean)
Day 1 (n=15, 9, 8, 9, 8, 9, 48)Day 2 (n=12, 7, 6, 5, 5, 7, 44)Day 3 (n=10, 4, 4, 4, 4, 5, 38)Day 4 (n=7, 3, 2, 3, 3, 6, 31)Day 5 (n=7, 2, 1, 3, 2, 4, 22)Day 6 (n=6, 1, 1, 2, 1, 3, 18)Day 7 (n=6, 0, 1, 2, 1, 2, 16)
Core Study: Canakinumab 100 mg56.346.249.516.50.00.00.0
Core Study: Canakinumab 200 mg53.019.856.763.554.857.535.0
Core Study: Canakinumab 25 mg41.144.831.531.819.319.620.9
Core Study: Canakinumab 300 mg52.243.126.311.013.012.00.0
Core Study: Canakinumab 50 mg44.640.149.546.348.044.0NA
Core Study: Canakinumab q4wk66.159.358.049.441.443.552.0
Core Study: Colchicine 0.5 mg53.142.838.130.531.833.733.0

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Core Study: Participant's Assessment of Gout Pain on a 5-point Likert Scale up to Day 7 of All Gout Flares

Participants assessed the intensity of pain in the most affected joint on a 5-point Likert scale, which ranged from 1 to 5 (1=None, 2=Mild, 3=Moderate, 4=Severe, 5=Extreme). Participants assessed pain intensity on the day of onset of the gout flare and in the morning of the 6 following days. (NCT00819585)
Timeframe: Baseline of the core study to Week 16

,,,,,,
InterventionUnits on a scale (Mean)
Day 1 (n=15, 8, 8, 9, 8, 9, 48)Day 2 (n=12, 6, 6, 5, 5, 7, 44)Day 3 (n=10, 4, 4, 4, 4, 6, 38)Day 4 (n=7, 3, 2, 3, 3, 7, 31)Day 5 (n=7, 2, 1, 3, 2, 4, 22)Day 6 (n=6, 1, 1, 2, 2, 3, 18)Day 7 (n=6, 0, 1, 2, 1, 2, 16)
Core Study: Canakinumab 100 mg3.53.32.31.51.01.01.0
Core Study: Canakinumab 200 mg3.22.23.03.03.23.52.5
Core Study: Canakinumab 25 mg2.82.92.42.62.22.42.4
Core Study: Canakinumab 300 mg3.12.92.31.71.51.51.0
Core Study: Canakinumab 50 mg3.12.63.12.72.53.0NA
Core Study: Canakinumab q4wk3.83.53.43.22.72.93.3
Core Study: Colchicine 0.5 mg3.23.02.72.42.62.52.4

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Core Study: Percentage of Participants With Gout Flare at Different Time Points

A gout flare was defined as an increase in participant-reported gout pain in the most affected joint during a gout attack. (NCT00819585)
Timeframe: Days 2, 4, 6, and Weeks 2, 4, 6, 10, and 16 of the core study

,,,,,,
InterventionPercentage of participants (Number)
2 days post-dose4 days post-dose6 days post-dose2 weeks post-dose4 weeks post-dose6 weeks post-dose10 weeks post-dose16 weeks post-dose
Core Study: Canakinumab 100 mg3.73.73.77.47.49.311.215.1
Core Study: Canakinumab 200 mg3.73.77.411.113.013.016.818.8
Core Study: Canakinumab 25 mg5.510.912.714.514.516.522.528.7
Core Study: Canakinumab 300 mg0.05.75.77.511.411.411.415.3
Core Study: Canakinumab 50 mg3.73.75.67.49.311.113.117.3
Core Study: Canakinumab q4wk3.83.83.811.315.127.9217.017.0
Core Study: Colchicine 0.5 mg5.610.211.116.725.132.637.545.8

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Extension Study: Amount of Rescue Medication Taken

The amount of naproxen and prednisolone taken after receiving treatment for each of the first 3 flares was recorded. (NCT00819585)
Timeframe: Baseline of the extension study until the end of the study (up to 24 weeks)

,
Interventionmg (Mean)
Gout Flare 1: Naproxen (n=68, 24)Gout Flare 1: Prednisolone (68, 24)Gout Flare 2: Naproxen (n=12, 5)Gout Flare 2: Prednisolone (12, 5)Gout Flare 3: Naproxen (n=4, 1)Gout Flare 3: Prednisolone (4, 1)
Extension Study: Group A1086.84.6650.01.3250.00.0
Extension Study: Group C954.64.2200.00.00.00.0

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Extension Study: Participant's Assessment of Gout Pain on a 100 mm Visual Analog Scale During the First Flare

Participant's rated the intensity of pain in the most affected joint during the first flare on a 0-100 mm visual analog scale, which ranged from no pain (left end, 0) to unbearable pain (right end, 100). Assessments were made pre-dose and 24 hours, 3 days, 4 days, and an average of 5-7 days post-dose (NCT00819585)
Timeframe: Baseline of the extension study until 7 days after the onset of the first gout flare (up to 24 weeks)

,
InterventionUnits on a scale (Mean)
Pre-dose (n=65, 19)24 hours (n=65, 18)3 days (n=54, 15)4 days (n=54, 15)5-7 days (n=52, 13)
Extension Study: Group A61.323.812.48.88.1
Extension Study: Group C71.829.06.82.72.1

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Extension Study: Participant's Global Assessment of Response to Treatment on a 5-point Likert Scale

Study participants made a global assessment of their response to treatment on a 5-point Likert scale (Excellent, Good, Acceptable, Slight, Poor) at the control visit 7±2 days following each of their first 3 flares. The number of participants in each of the 5 categories of the Likert scale are reported. (NCT00819585)
Timeframe: Baseline of the extension study until the end of the study (up to 24 weeks)

,
InterventionParticipants (Number)
Gout Flare 1: Excellent (63, 21)Gout Flare 1: Good (63, 21)Gout Flare 1: Acceptable (63, 21)Gout Flare 1: Slight (63, 21)Gout Flare 1: Poor (63, 21)Gout Flare 2: Excellent (11, 5)Gout Flare 2: Good (11, 5)Gout Flare 2: Acceptable (11, 5)Gout Flare 2: Slight (11, 5)Gout Flare 2: Poor (11, 5)Gout Flare 3: Excellent (3, 1)Gout Flare 3: Good (3, 1)Gout Flare 3: Acceptable (3, 1)Gout Flare 3: Slight (3, 1)Gout Flare 3: Poor (3, 1)
Extension Study: Group A40175104610021000
Extension Study: Group C7140004100001000

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Extension Study: Physician's Assessment of Tenderness, Swelling, and Erythema in the Most Affected Joint During the First Flare

"Tenderness was rated on a 0-3 point scale: 0=no pain, 1=patient states that there is pain, 2=patient states there is pain and winces, and 3=patient states there is pain, winces and withdraws on palpation or passive movement of the most affected joint. Swelling was rated on a 0-3 point scale: 0=no swelling, 1=palpable, 2=visible, and 3=bulging beyond the joint margins. Erythema was rated as present, absent, or not assessable. Assessments were performed at the flare and control visits." (NCT00819585)
Timeframe: Baseline of the extension study until the end of the study (up to 24 weeks)

,
InterventionParticipants (Number)
Tenderness Flare Visit: No painTenderness Flare Visit: PainTenderness Flare Visit: Pain and wincesTenderness Flare Visit: Pain, winces and withdrawsTenderness Control Visit: No painTenderness Control Visit: PainTenderness Control Visit: Pain and wincesTenderness Control Visit: Pain, winces and withdraJoint Swelling Flare Visit: No swellingJoint Swelling Flare Visit: PalpableJoint Swelling Flare Visit: VisibleJoint Swelling Flare Visit: Bulging beyond jointJoint Swelling Control Visit: No swellingJoint Swelling Control Visit: PalpableJoint Swelling Control Visit: VisibleJoint Swelling Control Visit: Bulging beyond jointErythema Flare Visit: AbsentErythema Flare Visit: PresentErythema Flare Visit: Not assessedErythema Control Visit: AbsentErythema Control Visit: PresentErythema Control Visit: Not assessed
Extension Study: Group A227231760810520311361620214406630
Extension Study: Group C02101221300021752220042002400

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Extension Study: Physician's Global Assessment of Response to Treatment on a 5-point Likert Scale

The study physician made a global assessment of the participant's response to treatment on a 5-point Likert scale (Very good, Good, Fair, Poor, Very poor) at the control visit 7±2 days following each of the first 3 flares. The category 'Not assessed' includes missing data and 'not done'. The number of participants in each of the 5 categories of the Likert scale are reported. (NCT00819585)
Timeframe: Baseline of the extension study until the end of the study (up to 24 weeks)

,
InterventionParticipants (Number)
Gout Flare 1: Very Good (69, 23)Gout Flare 1: Good (69, 23)Gout Flare 1: Fair (69, 23)Gout Flare 1: Poor (69, 23)Gout Flare 1: Very Poor (69, 23)Gout Flare 2: Very Good (12, 5)Gout Flare 2: Good (12, 5)Gout Flare 2: Fair (12, 5)Gout Flare 2: Poor (12, 5)Gout Flare 2: Very Poor (12, 5)Gout Flare 3: Very Good (3, 1)Gout Flare 3: Good (3, 1)Gout Flare 3: Fair (3, 1)Gout Flare 3: Poor (3, 1)Gout Flare 3: Very Poor (3, 1)
Extension Study: Group A37282205700012000
Extension Study: Group C13100003200001000

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Core Study: Mean Number of Gout Flares for the Repeat Dose Regimen of Canakinumab as Compared to the Single Doses of Canakinumab

(NCT00819585)
Timeframe: up to 16 weeks after randomization

Interventiongout flares per patient (Least Squares Mean)
Canakinumab 25 mg0.48
Canakinumab 50 mg0.43
Canakinumab 100 mg0.22
Canakinumab 200 mg0.38
Canakinumab 300 mg0.21
Canakinumab q4wk0.68

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Core Study: Physician's Global Assessment of Response to Therapy on a 5-point Likert Scale

The study physician made a global assessment of the participant's response to treatment on a 5-point Likert scale (Very good, Good, Fair, Poor, Very poor) at Days 15, 29, 57, 85, 113, and 141. The category 'Not assessed' includes missing data and 'not done'. The number of participants in each of the 5 categories of the Likert scale are reported. (NCT00819585)
Timeframe: Days 15, 29, 57, 85, 113, and 141 of the core study

,,,,,,
InterventionParticipants (Number)
Day 15: Very goodDay 15 - GoodDay 15 - FairDay 15 - PoorDay 15 - Very poorDay 15 - Not assessedDay 29: Very goodDay 29- GoodDay 29 - FairDay 29 - PoorDay 29 - Very poorDay 29 - Not assessedDay 57: Very goodDay 57- GoodDay 57 - FairDay 57 - PoorDay 57 - Very poorDay 57 - Not assessedDay 85: Very goodDay 85 - GoodDay 85 - FairDay 85 - - PoorDay 85 - Very poorDay 85 - Not assessedDay 113 : Very goodDay 113 - GoodDay 113 - FairDay 113 - PoorDay 113 - Very poorDay 113 - Not AssessedDay 141 : Very goodDay 141 - GoodDay 141 - FairDay 141 - PoorDay 141 - Very poorDay 141 - Not Assessed
Core Study: Canakinumab 100 mg242332012522510028166201321551003018210024193301
Core Study: Canakinumab 200 mg232640012426300027214000321640002620310031126010
Core Study: Canakinumab 25 mg192850032623200025215000272030012418520026166100
Core Study: Canakinumab 300 mg272103012723200030184000311721012920110032142011
Core Study: Canakinumab 50 mg232440112422401327203012311720022918300225202103
Core Study: Canakinumab q4wk252034022722220128203201291732113215320232143211
Core Study: Colchicine 0.5 mg4042166223942192134643931443411220550367218413616205

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Percentage of Participants With GVHD (Graft Versus Host Disease)

Acute grade 2 to 4 Graft versus host disease( GVHD )for patients who were able to be analyzed by measuring the T cell counts for increased CD3+ before and after lenalidomide. (NCT00899431)
Timeframe: Up to 6 months after allotransplant

InterventionParticipants (Count of Participants)
Group 10
Group 23
Group 31

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Change in Submaximal Exercise Capacity (6-MWT)

6-Minute Walk Test (NCT00987415)
Timeframe: Baseline to 24 weeks

Interventionmeters (Mean)
Allopurinol18.1
Sugar Pill20.7

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Change in Quality of Life (KCCQ)

Kansas City Cardiomyopathy (KCCQ) overall summary score - The Kansas City Cardiomyopathy Questionnaire is a 23-item, self-administered instrument that quantifies physical function, symptoms (frequency, severity and recent change), social function, self-efficacy and knowledge, and quality of life. In the KCCQ, an overall summary score can be derived from the physical function, symptom (frequency and severity), social function and quality of life domains. Scores are transformed to a range of 0-100, in which higher scores reflect better health status. (NCT00987415)
Timeframe: Baseline to 24 weeks

Interventionunits on a scale (Mean)
Allopurinol1.13
Sugar Pill4.68

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Change in Quality of Life (KCCQ).

Kansas City Cardiomyopathy (KCCQ) overall summary score - The Kansas City Cardiomyopathy Questionnaire is a 23-item, self-administered instrument that quantifies physical function, symptoms (frequency, severity and recent change), social function, self-efficacy and knowledge, and quality of life. In the KCCQ, an overall summary score can be derived from the physical function, symptom (frequency and severity), social function and quality of life domains. Scores are transformed to a range of 0-100, in which higher scores reflect better health status. (NCT00987415)
Timeframe: Baseline to 12 weeks

Interventionunits on a scale (Mean)
Allopurinol4.45
Sugar Pill3.38

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Change in Submaximal Exercise Capacity (6-MWT)

6-Minute Walk Test (NCT00987415)
Timeframe: Baseline to 12 weeks

Interventionmeters (Mean)
Allopurinol9.5
Sugar Pill9.5

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A Composite Clinical Endpoint (CCE) That Classifies Subject's Clinical Status as Improved, Worsened, or Unchanged.

CCE composed of 3-level categorical variable with options that include worsened, unchanged or improved (NCT00987415)
Timeframe: 24 Weeks

,
Interventionparticipants (Number)
WorsenedUnchangedImproved
Allopurinol585416
Sugar Pill584324

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Peak Early Filling Rate Normalized to EDV

The Peak Early Filling Rate Normalized to EDV is calculated from the slope of the volume during the early filling of the heart with respect to time. The higher values indicate a very healthy heart muscle and lower values are indicative of a very stiff muscle. This is a measure of LV Diastolic Function. Since some visits did not occur at the scheduled 6 month intervals, the results have been divided into 3-month visit intervals for reporting purposes. (NCT01052272)
Timeframe: 5 visits per Participant over 2 years (about every 6 months)

,,,
Intervention1/sec (Mean)
Month 0 (n=17,17,18,18)Month 6(n=14,11,11,12)Month 9(n=1,2,0,0)Month 12(n=12,11,11,11)Month 15(n=3,2,1,1)Month 18(n=10,12,8,8)Month 21(n=3,0,0,1)Month 24 (n=11,9,8,10)Month 27 (n=1,1,0,1)
Candesartan Cilexetil2.012.021.131.901.481.93NA1.651.10
Candesartan Cilexetil and Allopurinol2.01.98NA1.772.282.052.501.822.15
Ramipril1.931.742.501.802.021.911.692.051.34
Ramipril and Allopurinol2.112.03NA1.931.561.89NA1.88NA

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LV End Systolic Maximum Shortening (LVES Max Shortening)

By identifying three points in three different planes in the heart muscle, the maximum shortening is the average of the difference between the distance between these three points at the end of filling of the heart and the end of contraction divided by the length at the end of filling times 100. The maximum shortening is a three dimensional analysis. The higher values indicate a healthy heart. This is a measure of LV Systolic Function. Since some visits did not occur at the scheduled 6 month intervals, the results have been divided into 3-month visit intervals for reporting purposes. (NCT01052272)
Timeframe: 5 visits per Participant over 2 years (about every 6 months)

,,,
Interventionpercent of length at end of filling (Mean)
Month 0 (n=17,17,17,18)Month 6(n=14,11,10,12)Month 9(n=1,2,0,0)Month 12(n=11,11,10,10)Month 15(n=3,2,1,1)Month 18(n=10,12,7,8)Month 21(n=3,0,0,1)Month 24 (n=11,9,8,10)Month 27 (n=1,1,0,1)
Candesartan Cilexetil16.6817.5019.0817.1316.2817.55NA16.6220.38
Candesartan Cilexetil and Allopurinol16.0018.50NA18.5116.3617.5217.8917.8516.59
Ramipril15.8116.8818.4314.5717.0617.2616.6815.6713.70
Ramipril and Allopurinol15.8418.72NA17.9614.2217.46NA17.52NA

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Left Ventricular End-diastolic Mass Indexed to Left Ventricular End-diastolic Volume (LVED Mass/LVEDV)

LVED Mass/LVEDV: As an indicator of heart muscle mass and heart blood volume, the mass indexed to end diastolic volume determines whether there is an adequate amount of heart muscle to pump the heart blood volume obtained from a three-dimensional analysis. The values that are too high or too low indicate a diseased myocardium. This is a measure of LV Geometry. Since some visits did not occur at the scheduled 6 month intervals, the results have been divided into 3-month visit intervals for reporting purposes. (NCT01052272)
Timeframe: 5 visits per Participant over 2 years (about every 6 months)

,,,
Interventiong/ml (Mean)
Month 0 (n=17,17,18,18)Month 6(n=14,11,11,12)Month 9(n=1,2,0,0)Month 12(n=12,11,11,11)Month 15(n=3,2,1,1)Month 18(n=10,12,8,8)Month 21(n=3,0,0,1)Month 24 (n=11,9,8,10)Month 27 (n=1,1,0,1)
Candesartan Cilexetil0.950.830.670.780.700.79NA0.800.64
Candesartan Cilexetil and Allopurinol0.870.82NA0.860.680.800.690.820.69
Ramipril0.920.870.750.840.810.790.950.840.93
Ramipril and Allopurinol0.860.71NA0.720.570.83NA0.80NA

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Left Ventricular End Diastolic Volume Indexed to Body Surface Area (LVEDV/BSA)

LVEDV/BSA: As an indicator of heart size, the blood volume of the heart is related to the body size. The relation of heart blood volume to body size is more accurate in determining pathology because larger people require a larger heart blood volume. The values that are too high or too low indicate a diseased myocardium. This is a measure of LV Diastolic Function. Since some visits did not occur at the scheduled 6 month intervals, the results have been divided into 3-month visit intervals. (NCT01052272)
Timeframe: 5 visits per Participant over 2 years (about every 6 months)

,,,
Interventionml/m^2 (Mean)
Month 0 (n=17,17,18,18)Month 6(n=14,11,11,12)Month 9(n=1,2,0,0)Month12(n=12,11,11,11)Month 15(n=3,2,1,1)Month 18(n=10,12,8,8)Month 21(n=3,0,0,1)Month 24 (n=11,9,8,10)Month 27 (n=1,1,0,1)
Candesartan Cilexetil78.0678.6093.5785.4490.2082.74NA84.2876.65
Candesartan Cilexetil and Allopurinol79.0378.01NA79.7563.184.9575.2779.7275.05
Ramipril73.0374.1073.2375.3481.1975.2871.9970.4648.68
Ramipril and Allopurinol78.5286.13NA83.95108.2567.96NA71.63NA

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Left Ventricular Ejection Fraction (LVEF)

LVEF is a calculation of heart pump function determined from the volume after complete filling minus the volume after complete contraction divided by the volume after complete filling. A value of 55% or greater is normal. This is a measure of LV Systolic Function. Since some visits did not occur at the scheduled 6 month intervals, the results have been divided into 3-month visit intervals for reporting purposes (NCT01052272)
Timeframe: 5 visits per Participant over 2 years (about every 6 months)

,,,
Interventionpercent (Mean)
Month 0 (n=17,17,18,18)Month 6(n=14,11,11,12)Month 9(n=1,2,0,0)Month 12(n=12,11,11,11)Month 15(n=3,2,1,1)Month 18(n=10,12,8,8)Month 21(n=3,0,0,1)Month 24 (n=11,9,8,10)Month 27 (n=1,1,0,1)
Candesartan Cilexetil56.3656.8242.6252.3739.8856.33NA51.7054.17
Candesartan Cilexetil and Allopurinol52.6857.28NA56.1154.4657.8256.1755.7954.40
Ramipril52.1954.2064.9852.7652.1355.0251.2757.1850.73
Ramipril and Allopurinol53.3752.80NA51.7434.8954.05NA55.59NA

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Left Ventricular End Systolic Volume Indexed to Body Surface Area (LVESV/BSA)

LVESV/BSA: The end systolic volume is the blood volume of the heart at the end of contraction and is an index of the pump function of the heart. This relation to body size is more accurate in determining pathology because larger people require a larger heart blood volume. The values that are too high or too low indicate a diseased myocardium. This is a measure of LV Systolic Function. Since some visits did not occur at the scheduled 6 month intervals, the results have been divided into 3-month visit intervals. (NCT01052272)
Timeframe: 5 visits per Participant over 2 years (about every 6 months)

,,,
Interventionml/m^2 (Mean)
Month 0 (n=17,17,18,18)Month 6(n=14,11,11,12)Month 9(n=1,2,0,0)Month 12(n=12,11,11,11)Month 15(n=3,2,1,1)Month 18(n=10,12,8,8)Month 21(n=3,0,0,1)Month 24 (n=11,9,8,10)Month 27 (n=1,1,0,1)
Candesartan Cilexetil35.2635.2653.8742.2754.0437.76NA41.7235.13
Candesartan Cilexetil and Allopurinol39.4934.15NA36.0728.7437.1832.9935.9934.22
Ramipril36.2034.7725.6436.8239.4235.3035.2331.1723.98
Ramipril and Allopurinol37.9142.88NA42.3470.4830.39NA31.56NA

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Left Ventricular End-Diastolic Radius to Wall Thickness (LVED Radius/Wall Thickness)

LVED Radius/Wall thickness As an indicator of heart muscle mass and heart volume chamber diameter, the end-diastolic radius indexed to end diastolic wall thickness determines whether there is an adequate amount of heart muscle to pump the heart blood volume obtained from a two-dimensional analysis. The values that are too high or too low indicate a diseased myocardium. This is a measure of LV Geometry. Since some visits did not occur at the scheduled 6 month intervals, the results have been divided into 3-month visit intervals for reporting purposes. (NCT01052272)
Timeframe: 5 visits per Participant over 2 years (about every 6 months)

,,,
Interventionunitless (Mean)
Month 0 (n=17,17,18,18)Month 6(n=14,11,11,12)Month 9(n=1,2,0,0)Month 12(n=12,11,11,11)Month 15(n=3,2,1,1)Month 18(n=10,12,8,8)Month 21(n=3,0,0,1)Month 24 (n=11,9,8,10)Month 27 (n=1,1,0,1)
Candesartan Cilexetil3.143.394.143.684.103.71NA3.584.04
Candesartan Cilexetil and Allopurinol3.453.63NA3.423.903.564.243.564.29
Ramipril3.233.323.423.433.443.602.923.463.12
Ramipril and Allopurinol3.574.04NA4.014.573.60NA3.61NA

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Percent Change From Baseline to Month 6 in 24-hour Urine Uric Acid (uUA) Excretion

The change from Baseline to Month 6 in 24-hour urine uric acid is expressed as a percentage of the Baseline uUA value. (NCT01077284)
Timeframe: Baseline and Month 6

Interventionpercent change (Mean)
Febuxostat-58.6
Allopurinol-36.4
Placebo-12.7

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Change From Baseline to Month 6 in the Number of Calcium Oxalate Stones

Multidetector Computed Tomography (MDCT) was used to visualize and count calcium oxalate kidney stones at Baseline and after 6 months of treatment. All MDCT images were analyzed independently by a Central Reader. (NCT01077284)
Timeframe: Baseline and Month 6

,,
Interventionstones (Mean)
Baseline (n=28, 24, 30)Change from Baseline (n=26, 23, 26)
Allopurinol6.600.28
Febuxostat4.84-0.06
Placebo5.570.10

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Change From Baseline to Month 6 in 24-hour Measured Creatinine Clearance

Creatinine clearance is a measure of how well the kidneys are filtering creatinine, a waste product produced by the muscles. Measured creatinine clearance was calculated according to the following: Urine 24 hour Creatinine/Serum Creatinine x (total Urine volume/elapsed time) x (1.73/body surface area). (NCT01077284)
Timeframe: Baseline and Month 6

,,
InterventionmL/min/1.73m² (Mean)
Baseline (n=33, 33, 33)Change from Baseline (n=30, 29, 30)
Allopurinol146.0-7.7
Febuxostat146.9-9.0
Placebo147.1-19.0

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Percent Change From Baseline to Month 6 in the In-plane Diameter of the Largest Calcium Oxalate (CaOx) Stone

Multidetector Computed Tomography (MDCT) was used to visualize and measure calcium oxalate kidney stones at Baseline and after 6 months of treatment. All MDCT images were analyzed independently by a Central Reader. The change from Baseline to month 6 is expressed as a percentage of the Baseline largest in-plane diameter. (NCT01077284)
Timeframe: Baseline and Month 6

Interventionpercent change (Mean)
Febuxostat-6.50
Allopurinol0.63
Placebo3.20

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Percentage of Participants With Non-fatal Myocardial Infarction (MI)

Events were adjudicated by an independent cardiovascular endpoints committee as non-fatal MI. (NCT01101035)
Timeframe: Up to last dose of study drug (approximately 83 months)

Interventionpercentage of participants (Number)
Febuxostat3.6
Allopurinol3.8

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Percentage of Participants With Antiplatelet Trialists' Collaborative (APTC) Event

APTC events were defined as a composite of cardiovascular death, nonfatal myocardial infarction, and nonfatal stroke; these events were adjudicated by an independent cardiovascular endpoints committee. (NCT01101035)
Timeframe: Up to last dose of study drug (approximately 83 months)

Interventionpercentage of participants (Number)
Febuxostat9.6
Allopurinol8.8

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Percentage of Participants With Unstable Angina With Urgent Coronary Revascularization

Events were adjudicated by an independent cardiovascular endpoints committee as unstable angina with urgent coronary revascularization. (NCT01101035)
Timeframe: Up to last dose of study drug (approximately 83 months)

Interventionpercentage of participants (Number)
Febuxostat1.6
Allopurinol1.8

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Percentage of Participants With Primary Major Adverse Cardiovascular Events (MACE) Composite (75% Interim Analysis)

Major adverse cardiovascular events (MACE) were defined as a composite of cardiovascular (CV) death, non-fatal myocardial infarction (MI), nonfatal stroke and unstable angina with urgent coronary revascularization; these events were adjudicated by an independent cardiovascular endpoints committee. (NCT01101035)
Timeframe: Up to last dose of study drug (approximately 83 months)

Interventionpercentage of participants (Number)
Febuxostat8.0
Allopurinol8.0

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Percentage of Participants With Primary MACE Composite (Final Analysis)

Major adverse cardiovascular events (MACE) were defined as a composite of cardiovascular (CV) death, non-fatal myocardial infarction (MI), nonfatal stroke and unstable angina with urgent coronary revascularization; these events were adjudicated by an independent cardiovascular endpoints committee. (NCT01101035)
Timeframe: Up to last dose of study drug (approximately 83 months)

Interventionpercentage of participants (Number)
Febuxostat10.8
Allopurinol10.4

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Percentage of Participants With Cardiovascular (CV) Death

Events were adjudicated by an independent cardiovascular endpoints committee as CV death. (NCT01101035)
Timeframe: Up to last dose of study drug (approximately 83 months)

Interventionpercentage of participants (Number)
Febuxostat4.3
Allopurinol3.2

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Percentage of Participants With Non-fatal Stroke

Events were adjudicated by an independent cardiovascular endpoints committee as non-fatal stroke. (NCT01101035)
Timeframe: Up to last dose of study drug (approximately 83 months)

Interventionpercentage of participants (Number)
Febuxostat2.3
Allopurinol2.3

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Number of Cycle 2 Participants Normalizing Uric Acid Levels (UAL) Within 24 Hours of Treatment

Number of participants with normalized UAL as determined by a uric acid blood test at either 24 hours. A uric acid blood test, also known as a serum uric acid measurement, determines how much uric acid is present in the blood where normal levels are 2.4-6.0 mg/dL (female) and 3.4-7.0 mg/dL (male). (NCT01200485)
Timeframe: Up to 24 hours of cycle 2 dose delivery

InterventionParticipants (Count of Participants)
Arm A (Rasburicase)20
Arm B (Allopurinol)25

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Number of Participants (Incidence) of LTLS (Laboratory Tumor Lysis Syndrome)

"Number of participants (incidence) of LTLS in the two arms, as defined by the Cairo-Bishop criteria , during cycle 2.~Cairo-Bishop criteria:~Uric acid x ≥ 476 μmol/l or 25% increase from baseline Potassium x ≥ 6·0 mmol/l or 25% increase from baseline Phosphorous x ≥ 2·1 mmol/l (children), x ≥1·45 mmol/l (adults) or 25% increase from baseline Calcium x ≤ 1·75 mmol/l or 25% decrease from baseline Laboratory tumour lysis syndrome (LTLS) is defined as either a 25% change or level above or below normal, as defined above, for any two or more serum values of uric acid, potassium, phosphate, and calcium within 3d before or 7d after the initiation of chemotherapy." (NCT01200485)
Timeframe: Up to two 3-week cycles, 6 weeks

InterventionParticipants (Count of Participants)
Arm A (Rasburicase)1
Arm B (Allopurinol)1

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Change in Monocyte Chemotactic Protein-1 From Baseline to Week 12

(NCT01228903)
Timeframe: Baseline and 12 weeks

Interventionpg/mL (Mean)
Control-4.7
Allopurinol3.6

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Change in Oxidized Low Density Lipoprotein From Baseline to Week 12

(NCT01228903)
Timeframe: Baseline and 12 weeks

Interventionu/L (Mean)
Control-0.08
Allopurinol-2.97

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Change in Serum Interleukin-6 From Baseline to Week 12

(NCT01228903)
Timeframe: Baseline and 12 weeks

Interventionpg/mL (Mean)
Control0.15
Allopurinol0.37

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Change in Serum Uric Acid Levels From Baseline to Week 12

Serum uric acid levels were measured both at baseline and after 12 weeks (NCT01228903)
Timeframe: Baseline and 12 weeks

Interventionmg/dL (Mean)
Control0.05
Allopurinol3.24

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Change in Endothelial Dependent Dilation From Baseline to Week 12

Change in Endothelial Dependent Dilation measured by Flow Mediated Dilation at baseline and week 12 (NCT01228903)
Timeframe: Baseline and 12 weeks

Intervention% change (Mean)
Control0.2
Allopurinol0.9

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Change in C-reactive Protein From Baseline to Week 12

(NCT01228903)
Timeframe: Baseline and 12 weeks

Interventionmg/L (Mean)
Control0.7
Allopurinol00.42

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Plasma Renin Activity (PRA) [Uric Acid]

PRA is a measure of systemic renin angiotensin system (RAS) activation. Blood was collected and plasma PRA was analyzed using a competitive binding radioimmunoassay (RIA) laboratory test. (NCT01320722)
Timeframe: Week 8

Interventionng/mL per hour (Median)
Probenecid0.4
Allopurinol0.3
Placebo- Uric Acid0.2

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Change in Renal Plasma Flow (RPF) Response to Captopril in High Sodium Balance [Uric Acid]

RPF in response to captopril iis a measure of the vasodilator effect from inhibiting angiotensin II (AngII)- mediated vascular tone and therefore the degree of kidney specific Renin Angiotensin System (RAS) activity. Participants consumed a high sodium diet 3 days prior to the test. Following an 8 hour fast, participants remained in a supine (lying down) position and had an intravenous (IV) catheter inserted in each arm, one for infusion and one for blood collection. An 8 milligrams (mg)/kilogram(kg) loading dose of para-aminohippuric acid (PAH) was given, immediately followed by a continuous PAH infusion at 12 mg/minute. After 60 minutes a single dose of 25 mg of captopril was administered. Three pre-captopril measurements and three post-captopril measurements of RPF were made. RPF was normalized to body surface area of 1.73 meters squared (m^2). The change in RPF was calculated as post-captopril RPF- pre-captopril RPF. (NCT01320722)
Timeframe: Week 8 (pre and post captopril)

InterventionmL/min per 1.73 m^2 (Median)
Probenecid33
Allopurinol36
Placebo- Uric Acid30

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Change in Renal Plasma Flow (RPF) in Response to Captopril in High Sodium Balance [Vitamin D]

Change in RPF in response to captopril is a measure of the vasodilator effect from inhibiting angiotensin II (AngII)- mediated vascular tone and therefore the degree of kidney specific Renin Angiotensin System (RAS) activity. Participants consumed a high sodium diet 3 days prior to the test. Following an 8 hour fast, participants remained in a supine (lying down) position and had an intravenous (IV) catheter inserted in each arm, one for infusion and one for blood collection. An 8 milligrams (mg)/kilogram(kg) loading dose of para-aminohippuric acid (PAH) was given, immediately followed by a continuous PAH infusion at 12 mg/minute. After 60 minutes a single dose of 25 mg of captopril was administered. Three pre-captopril measurements and three post-captopril measurements of RPF were made. RPF was normalized to body surface area of 1.73 meters squared (m^2). The change in RPF was calculated as post-captopril RPF- pre-captopril RPF. (NCT01320722)
Timeframe: Week 8 (pre and post captopril)

InterventionmL/min per 1.73 m^2 (Mean)
Vitamin D35.7
Placebo- Vitamin D35.9

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Angiotensin II (ATII) Concentration [Vitamin D]

ATII concentration is a measure of systemic renin angiotensin system (RAS) activation. Blood was collected and plasma ATII was analyzed using a double-antibody radioimmunoassay (RIA) laboratory test. (NCT01320722)
Timeframe: Week 8

Interventionpg/mL (Mean)
Vitamin D19.5
Placebo- Vitamin D19.7

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Angiotensin II (ATII) Concentration [Uric Acid]

ATII concentration is a measure of systemic renin angiotensin system (RAS) activation. Blood was collected and plasma ATII was analyzed using a double-antibody radioimmunoassay (RIA) laboratory test. (NCT01320722)
Timeframe: Week 8

Interventionpg/mL (Median)
Probenecid20.3
Allopurinol21.4
Placebo- Uric Acid19.1

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Mean 24-Hour Ambulatory Blood Pressure (ABP) Nocturnal Dipping

A 24-hour mean ambulatory blood pressure was monitored using a 24 hour ABP device. The ABP device is a small box that is worn on the belt or pant/skirt line with a line that connect under the clothing to the cuff on the upper arm. Blood Pressure was recorded every 30 minutes during the day and every 60 minutes during the night for 24 hours. Nocturnal dipping is the percent change lower between the daytime and nighttime values. (NCT01320722)
Timeframe: Baseline and Week 8

,,,,
Interventionpercent change (Mean)
BaselineWeek 8
Allopurinol7.55.2
Placebo- Uric Acid9.46.9
Placebo- Vitamin D7.88.1
Probenecid8.49.2
Vitamin D7.37.5

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Mean 24-Hour Ambulatory Blood Pressure (ABP)

A 24-hour mean ambulatory blood pressure was monitored using a 24 hour ABP device. The ABP device is a small box that is worn on the belt or pant/skirt line with a line that connect under the clothing to the cuff on the upper arm. Blood Pressure was recorded every 30 minutes during the day and every 60 minutes during the night for 24 hours. (NCT01320722)
Timeframe: Baseline and Week 8

,,,,
InterventionmmHg (Mean)
Overall Systolic Blood Pressure (SBP), BaselineOverall Diastolic Blood Pressure (DBP), BaselineAwake SBP, BaselineAsleep SBP, BaselineOverall SBP, Week 8Overall DBP, Week 8Awake SBP, Week 8Asleep SBP, Week 8
Allopurinol124.172.1126.7117.1123.772.0125.1118.6
Placebo- Uric Acid122.471.9125.5113.9122.972.6124.9116.2
Placebo- Vitamin D123.773.7126.4116.5124.774.7127.6117.4
Probenecid126.973.3130.0119.2125.273.8128.1116.2
Vitamin D120.471.6122.4113.9121.672.0124.2114.7

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Change in Endothelium-Dependent Vasodilation (EDV)

Endothelial function was assessed by EDV using brachial artery ultrasonography. Measurements of brachial artery diameter were made under basal conditions and reactive hyperemia following ischaemic stimulus. A blood pressure cuff on the forearm was pumped up for 5 minutes then released. Images were taken at baseline and after reactive hyperemia (increased blood flow). The maximum diameter was determined by the investigator. Change in EDV was expressed as a percent of brachial luminal diameter calculated as post-ischaemic brachial artery diameter - pre-ischaemic brachial artery diameter/pre-ischaemic brachial artery diameter * 100. (NCT01320722)
Timeframe: Baseline and Week 8 (pre and post ischaemic stimulus)

,,,,
Interventionpercent of brachial luminal diameter (Mean)
BaselineWeek 8
Allopurinol7.66.2
Placebo- Uric Acid6.57.1
Placebo- Vitamin D7.96.8
Probenecid7.48.3
Vitamin D6.36.1

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Plasma Renin Activity (PRA) [Vitamin D]

PRA is a measure of systemic renin angiotensin system (RAS) activation. Blood was collected and plasma PRA was analyzed using a competitive binding radioimmunoassay (RIA) laboratory test. (NCT01320722)
Timeframe: Week 8

Interventionng/mL per hour (Mean)
Vitamin D0.36
Placebo- Vitamin D0.44

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Safety of Allopurinol

Proportion of subjects who experienced at least one Treatment Emergent Adverse Event (TEAE) during the study. (NCT01391325)
Timeframe: Every month for 6 months.

Interventionpercentage of subjects (Number)
Allopurinol55.1

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Proportion of Subjects With Serum Urate (sUA) Less Than 6.0 mg/dL

Proportion of subjects with serum urate (sUA) less than 6.0 mg/dL at Month 6 using Last Observation Carried Forward (LOCF) for subjects with missing values at Month 6. (NCT01391325)
Timeframe: Month 6

Interventionpercentage of subjects (Number)
Allopurinol43.4

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Incidence of Gout Flares

Proportion of subjects who experienced at least one gout flare requiring treatment during the study. (NCT01391325)
Timeframe: Every month for 6 months.

Interventionpercentage of subjects (Number)
Allopurinol33.4

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Mean Change From Baseline to Month 6 in SF-36 PCS+MCS

The SF-36 is a short-form health survey with 36 questions that yields an 8-scale profile of functional health and well-being scores as well as psychometrically-based physical (PCS) and mental health (MCS) summary. Each scale is directly transformed into a 0-100 scale. The lower the score the more disability. The higher the score the less disability. The component scores (PCS and MCS) are norm-based to a standard population with a mean of 50 and a standard deviation of 10. (NCT01391325)
Timeframe: Month 6

Interventionunits on a scale (Mean)
SF-36 Physical Component SummarySF-36 Mental Health Component Summary
Allopurinol3.880.71

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Serum Uric Acid

Percent change from baseline in serum uric acid in Per Protocol population (NCT01399008)
Timeframe: Percent change from baseline in serum uric acid at Week 4

Interventionpercent change (Mean)
Arhalofenate 400 mg-16.0
Arhalofenate 600 mg-9.9
Placebo-9.5

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Mean Number of Gout Flare Days Per Participant Assessed From Day 1 to Week 16

(NCT01451645)
Timeframe: Day 1 to Week 16

Interventiondays (Mean)
Placebo6.6
Colchicine (Colcrys®) 0.6mg1.6

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Percentage of Participants With at Least 2 Gout Flares From Day 1 to Week 16

(NCT01451645)
Timeframe: Day 1 to Week 16

InterventionPercentage of Participants (Number)
Placebo24.4
Colchicine (Colcrys®) 0.6mg4.9

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Number of Gout Flares Per Participant From Day 1 to Week 16

(NCT01451645)
Timeframe: Day 1 to Week 16

Interventiongout flares (Mean)
Placebo1.1
Colchicine (Colcrys®) 0.6mg0.3

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Percentage of Participants With at Least 1 Gout Flare From Day 1 to Week 16

(NCT01451645)
Timeframe: Day 1 to Week 16

InterventionPercentage of Participants (Number)
Placebo43.9
Colchicine (Colcrys®) 0.6mg24.4

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Percentage of Participants With Rescue Medication From Day 1 to Day 364 (Week 52)

Participants who required rescue medication after having 2 or more gout flares during the treatment period were evaluated. (NCT01459796)
Timeframe: Day 1 to Day 364 (Week 52)

Interventionpercentage of participants (Number)
Placebo22.3
Rilonacept 80 mg8.7

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Percentage of Participants With Treatment Emergent Adverse Events (TEAEs)

Any untoward medical occurrence in a participant who received investigational medicinal product (IMP) was considered an AE without regard to possibility of causal relationship with this treatment. TEAEs were defined as AEs that developed or worsened or became serious during on-treatment period (time from the administration of first dose of study drug up to and including 35 days after the last dose of study drug). A serious adverse event (SAE) was defined as any untoward medical occurrence that resulted in any of the following outcomes: death, life-threatening, required initial or prolonged in-patient hospitalization, persistent or significant disability/incapacity, congenital anomaly/birth defect, or considered as medically important event. Any TEAE included participants with both serious and non-serious AEs. (NCT01459796)
Timeframe: Day 1 to Day 392 (Week 56)

,
Interventionpercentage of participants (Number)
With at least one TEAEWith TEAEs related to study drugWith serious TEAEsWith TEAEs resulting in study drug discontinuationWith TEAEs resulting in death
Placebo68.112.85.310.60.0
Rilonacept 80 mg68.319.04.06.30.0

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Duration of Survival

(NCT01464359)
Timeframe: 2 years after Transplantation.

InterventionParticipants (Count of Participants)
Patients With Acute Myelogenous Leukemia0

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Duration of Survival

(NCT01464359)
Timeframe: 6 months after Transplantation.

InterventionParticipants (Count of Participants)
Patients With Acute Myelogenous Leukemia1

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Incidence of Acute Graft-Versus-Host Disease

(NCT01464359)
Timeframe: Day 60

InterventionParticipants (Count of Participants)
Patients With Acute Myelogenous Leukemia0

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Incidence of Graft Failure

Incidence of graft failure defined as an absolute neutrophil count of less than 500/uL and a bone marrow that is less than 5% cellular (marrow aplasia) (NCT01464359)
Timeframe: Day 42

InterventionParticipants (Count of Participants)
Patients With Acute Myelogenous Leukemia0

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Duration of Survival

(NCT01464359)
Timeframe: 1 year after Transplantation.

InterventionParticipants (Count of Participants)
Patients With Acute Myelogenous Leukemia0

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Clinical Disease Response

Defined as leukemia clearance and complete remission. Patients will be followed for disease response for 1 year from transplantation unless: consent is withdrawal, patient is unevaluable - if a patient is not evaluable, follow only until the resolution or stabilization of treatment related toxicity, new anti-cancer treatment is started, patient is discharged to hospice (terminal) care. (NCT01464359)
Timeframe: 1 Year from Transplantation

InterventionParticipants (Count of Participants)
Patients With Acute Myelogenous Leukemia2

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Clinical Disease Response

Defined as leukemia clearance and complete remission. Patients will be followed for disease response for 2 years from transplantation unless: consent is withdrawal, patient is unevaluable - if a patient is not evaluable, follow only untilthe resolution or stabilization of treatment related toxicity, new anti-cancer treatment is started, patient is discharged to hospice (terminal) care. (NCT01464359)
Timeframe: 2 Years from Transplantation

InterventionParticipants (Count of Participants)
Patients With Acute Myelogenous Leukemia2

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Disease Free Survival

The primary endpoint is a disease free survival at 3 months in patients with chemotherapy refractory AML after a double T-cell depleted (TCD) umbilical cord blood (UCB) transplantation where one TCD unit is activated overnight in IL-2 followed by the administration of two courses of IL-2 three times a week for 6 doses beginning on day +3 and on day +60 to expand UCB-derived NK cells in vivo. (NCT01464359)
Timeframe: At 3 months

Interventionparticipants (Number)
Patients With Acute Myelogenous Leukemia1

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Gout Flares

Mean rate of gout flares requiring treatment for the 6-month period from the end of Month 6 to the end of Month 12. (NCT01493531)
Timeframe: 12 Months

InterventionGout Flares (Mean)
Lesinurad 200 mg + Allopurinol0.7
Lesinurad 400 mg + Allopurinol0.8
Placebo + Allopurinol0.9

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Subjects With ≥ 1 Target Tophus at Baseline Who Experience Complete Resolution of at Least 1 Target Tophus by Month 12

Proportion of subjects with ≥ 1 target tophus at Baseline who experience complete resolution of at least 1 target tophus by Month 12 (NCT01493531)
Timeframe: 12 months

InterventionProportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol0.314
Lesinurad 400 mg + Allopurinol0.276
Placebo + Allopurinol0.333

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Subjects With a Serum Urate (sUA) < 6.0 mg/dL by Month 6.

Proportion of subjects with an sUA level that is < 6.0 mg/dL by Month 6. (NCT01493531)
Timeframe: 6 months

InterventionProportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol0.554
Lesinurad 400 mg + Allopurinol0.665
Placebo + Allopurinol0.233

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Proportion of Subjects With an sUA Level That is < 6.0 mg/dL

(NCT01510158)
Timeframe: 6 Months, analysis after all subjects complete 12 months

InterventionProportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol0.542
Lesinurad 400 mg + Allopurinol0.592
Placebo + Allopurinol0.279

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Gout Flares

Mean rate of gout flares requiring treatment for the 6-month period from the end of Month 6 to the end of Month 12 (NCT01510158)
Timeframe: 12 Months

InterventionGout Flares (Mean)
Lesinurad 200 mg + Allopurinol.60
Lesinurad 400 mg + Allopurinol.50
Placebo + Allopurinol.60

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Tophus

Proportion of subjects with ≥ 1 target tophus at Baseline who experience complete resolution of at least 1 target tophus by Month 12 (NCT01510158)
Timeframe: 12 Months

InterventionProportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol0
Lesinurad 400 mg + Allopurinol0.211
Placebo + Allopurinol0.294

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Safety of Low Single-doses of Rasburicase.

The number of patients with any adverse events . (NCT01564277)
Timeframe: up to day 7

InterventionParticipants (Count of Participants)
Arm I (1.5mg Rasburicase)12
Arm II (3 mg Rasburicase)12

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Probability of Obtaining a Uric Acid Level =< 7.5mg/dL

The proportion of patients able to achieve and/or maintain a uric acid level =< 7.5mg/dL for each treatment arm. (NCT01564277)
Timeframe: Within 24 hours of rasburicase treatment

Interventionproportion of participants (Number)
Arm I (1.5mg Rasburicase)0.83
Arm II (3 mg Rasburicase)0.67

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Number of Patients Requiring Additional Doses of Rasburicase to Maintain a Uric Acid Level =< 7.5mg/dL

Count of partcicpants requiring additional doses of rasburicase to maintain a uric acid level =< 7.5mg/dL by treatment arm. (NCT01564277)
Timeframe: Up to day 7

InterventionParticipants (Count of Participants)
Arm I (1.5mg Rasburicase)1
Arm II (3 mg Rasburicase)3

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Area Under the Plasma Uric Acid Concentration-time Curve (AUC) From Baseline (Day 1) to Day 7

The mean area under the plasma uric acid concentration-time curve (AUC) from baseline (Day 1) to Day 7 (NCT01564277)
Timeframe: Up to day 7

Interventiondays*mg/dL (Mean)
Arm I (1.5mg Rasburicase)12.5
Arm II (3 mg Rasburicase)3.5

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Baseline White Blood Cell Count by Response

The mean baseline white blood cell count of patients with a complete response (CR) (patients who achieved uric acid level =< 7.5mg/dL) and no CR (patients with uric acid level > 7.5mg/dL). (NCT01564277)
Timeframe: Up to day 7

,
Interventioncells x 10^9/L (Mean)
Complete ResponseNo Complete Response
Arm I (1.5mg Rasburicase)62.113.9
Arm II (3 mg Rasburicase)29.033.3

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Number of Patients Experiencing a Doubling of Serum Creatinine

Count of participants experiencing a doubling of serum creatinine (NCT01564277)
Timeframe: up to day 6

InterventionParticipants (Count of Participants)
Arm I (1.5mg Rasburicase)0
Arm II (3 mg Rasburicase)0

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Apnea-Hypopnea Index

Severity of sleep apnea assessed before and after study drug treatment (NCT01637623)
Timeframe: baseline and 6 weeks

,,
Interventionevents/hour (Median)
baselineafter six weeks of treatment
Allopurinol3345
Losartan4644
Placebo3526

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Aortic Augmentation Index

assessed before and after study drug treatment (NCT01637623)
Timeframe: baseline and 6 weeks

,,
InterventionPERCENT of the pulse pressure (Mean)
baselinefollowing six weeks of therapy
Allopurinol18.816.7
Losartan17.316.1
Placebo21.522.5

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Mean Change in PERCENT Vasodilation

Flow-mediated vasodilation (FMD) (measurement of vascular endothelial function) assessed before and after study drug treatment (NCT01637623)
Timeframe: baseline and 6 weeks

Intervention% change in Max relative FMD (Mean)
Losartan1.38
Allopurinol0.18
Placebo-1.06

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Change in Mean 24-Hour Blood Pressure (Mean Arterial Pressure)

Change in mean 24 hour blood pressure (mean arterial pressure) (NCT01637623)
Timeframe: baseline and 6 weeks

Interventionmm Hg (Mean)
Losartan-4.73
Allopurinol-2.58
Placebo1.02

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Change in Aortic Pulse Wave Velocity

measurement of vascular stiffness assessed before and after study drug treatment (NCT01637623)
Timeframe: baseline and 6 weeks

Interventionm/s (Mean)
Losartan-0.6
Allopurinol-0.03
Placebo0.2

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Change in Minute Ventilation at Normoxia

assessed before and after study drug treatment (NCT01637623)
Timeframe: baseline and 6 weeks

,,
Interventionnormoxia - L/min (Mean)
baseline - normoxia in L/minsix weeks - normoxia in L/min
Allopurinol9.39.8
Losartan8.98.9
Placebo9.38.8

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PERCENT Time Spent Below 88 PERCENT Oxygen Saturation

assessed before and after study drug treatment (NCT01637623)
Timeframe: baseline and 6 weeks

,,
Interventionpercentage of total sleep time (Median)
baselinefollowing six weeks of therapy
Allopurinol58
Losartan1012
Placebo53

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Forearm Vascular Conductance

Assessment measurements of forearm vascular conductance during basal conditions and during graded hypoxia before and after study drug treatment. (NCT01637623)
Timeframe: baseline and 6 weeks

,,
Interventionml/min^-1 dL^-1 mmHg^-1 (Mean)
baselineAfter 6 weeks of treatment
Allopurinol0.430.55
Losartan0.410.42
Placebo0.490.51

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Change in Muscle Sympathetic Nerve Activity Responses During Hypoxia

The primary outcome variable is the change in the individual slope of the MSNA - SaO2 response curve at 6 weeks and baseline between treatment groups. (NCT01637623)
Timeframe: baseline and 6 weeks

,,
Interventionbursts/minute*%SaO2 (Mean)
BaselineFollowing 6 weeks of therapy
Allopurinol-0.84-0.66
Losartan-0.54-0.69
Placebo-0.71-0.61

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Change in Minute Ventilation During Hypoxia

assessed before and after study drug treatment (NCT01637623)
Timeframe: baseline and 6 weeks

,,
Interventionhypoxia - L/min*%SaO2 (Mean)
hypoxia - baseline in L/min*PERCENTSaO2hypoxia - after six weeks treatment in L/min*%SaO2
Allopurinol-0.53-0.43
Losartan-0.41-0.37
Placebo-0.44-0.48

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Cerebrovascular Conductance

Assessment measures of cerebral blood flow during basal conditions and during graded hypoxia before and after study drug treatment. Cerebrovascular conductance (CVC) was calculated as velocity-time integral/mean arterial pressure. (NCT01637623)
Timeframe: baseline and 6 weeks

,,
Interventioncm/sec/mmHg (Mean)
baselineAfter six weeks treatment
Allopurinol0.270.31
Losartan0.320.36
Placebo0.330.34

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Counts of Participants With Disease Free Survival

The length of time after treatment ends that a patient survives without any signs or symptoms of that cancer or any other type of cancer. In a clinical trial, measuring the disease-free survival is one way to see how well a new treatment works. Patients with leukemia involving the BM and myelodysplastic syndrome will have this assessed by BM biopsy and additional special studies such as cytogenetics or flow cytometry as appropriate. Patients will also have radiology studies such as plain X-rays or CT scans and/or other studies such as blood tumor markers to document presence or absence of disease as clinically indicated. (NCT01685411)
Timeframe: 2 Years

InterventionParticipants (Count of Participants)
Allogeneic Hematopoietic Stem Cell Transplant3

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Count of Participants Who Achieved Neutrophil Engraftment

Neutrophil engraftment is defined as the first day of three consecutive days where the neutrophil count (absolute neutrophil count) is 500 cells/mm^3 (0.5 x 10^9/L) or greater. (NCT01685411)
Timeframe: By Day 42

InterventionParticipants (Count of Participants)
Allogeneic Hematopoietic Stem Cell Transplant5

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Count of Participants With Disease Free Survival

The length of time after treatment ends that a patient survives without any signs or symptoms of that cancer or any other type of cancer. In a clinical trial, measuring the disease-free survival is one way to see how well a new treatment works. Patients with leukemia involving the BM and myelodysplastic syndrome will have this done by BM biopsy and additional special studies such as cytogenetics or flow cytometry as appropriate. Patients will also have radiology studies such as plain X-rays or CT scans and/or other studies such as blood tumor markers to document presence or absence of disease as clinically indicated. (NCT01685411)
Timeframe: 7 Years

InterventionParticipants (Count of Participants)
Allogeneic Hematopoietic Stem Cell Transplant1

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Percentage of Participants With Engraftment Failure

Graft failure is defined as not accepting donated cells. The donated cells do not make the new white blood cells, red blood cells and platelets. (NCT01685411)
Timeframe: Day 42

Interventionpercentage of participants (Number)
Allogeneic Hematopoietic Stem Cell Transplant0

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Percentage of Participants With Chronic Graft-Versus-Host Disease

Chronic Graft-Versus-Host Disease is a severe long-term complication created by infusion of donor cells into a foreign host. Patients will be staged weekly between days 0 and 100 after transplantation using standard criteria used for staging. Patients will be assigned an overall GVHD score based on extent of skin rash, volume of diarrhea and maximum bilirubin level. The stages of individual organ involvement are combined to produce an overall grade. Grade I GVHD is characterized as mild disease, grade II GVHD as moderate, grade III as severe, and grade IV life-threatening. (NCT01685411)
Timeframe: 1 Year

Interventionpercentage of participants (Number)
Allogeneic Hematopoietic Stem Cell Transplant0

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Count of Participants With Disease Free Survival

The length of time after treatment ends that a patient survives without any signs or symptoms of that cancer or any other type of cancer. In a clinical trial, measuring the disease-free survival is one way to see how well a new treatment works. Patients with leukemia involving the BM and myelodysplastic syndrome will have this done by BM biopsy and additional special studies such as cytogenetics or flow cytometry as appropriate. Patients will also have radiology studies such as plain X-rays or CT scans and/or other studies such as blood tumor markers to document presence or absence of disease as clinically indicated. (NCT01685411)
Timeframe: 5 Years

InterventionParticipants (Count of Participants)
Allogeneic Hematopoietic Stem Cell Transplant1

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Percentage of Participants With Acute Graft-Versus-Host Disease by Grade

Acute Graft-Versus-Host Disease is a severe short-term complication created by infusion of donor cells into a foreign host. Patients will be staged weekly between days 0 and 100 after transplantation using standard criteria used for staging. Patients will be assigned an overall GVHD score based on extent of skin rash, volume of diarrhea and maximum bilirubin level. The stages of individual organ involvement are combined to produce an overall grade. Grade I GVHD is characterized as mild disease, grade II GVHD as moderate, grade III as severe, and grade IV life-threatening. (NCT01685411)
Timeframe: Day 100

Interventionpercentage of participants (Number)
Grade 2-4Grade 3-4
Allogeneic Hematopoietic Stem Cell Transplant4020

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Number of Participant Who Were Alive at 7 Years Post Transplant

Overall survival will be defined as time from date of enrollment to date of death or censored at the date of last documented contact for patients still alive. (NCT01685411)
Timeframe: 7 Years

InterventionParticipants (Count of Participants)
Allogeneic Hematopoietic Stem Cell Transplant1

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Number of Participant Who Were Alive at 5 Years Post Transplant

Overall survival will be defined as time from date of enrollment to date of death or censored at the date of last documented contact for patients still alive. (NCT01685411)
Timeframe: 5 Years

InterventionParticipants (Count of Participants)
Allogeneic Hematopoietic Stem Cell Transplant3

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Number of Participant Who Were Alive at 2 Years Post Transplant

Overall survival will be defined as time from date of enrollment to date of death or censored at the date of last documented contact for patients still alive. (NCT01685411)
Timeframe: 2 Years

InterventionParticipants (Count of Participants)
Allogeneic Hematopoietic Stem Cell Transplant4

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Percentage of Participants With Chronic Graft-Versus-Host Disease

Chronic Graft-Versus-Host Disease is a severe long-term complication created by infusion of donor cells into a foreign host. Patients will be assigned an overall GVHD score based on extent of skin rash, volume of diarrhea and maximum bilirubin level. The stages of individual organ involvement are combined to produce an overall grade. Grade I GVHD is characterized as mild disease, grade II GVHD as moderate, grade III as severe, and grade IV life-threatening. (NCT01685411)
Timeframe: 6 Months

Interventionpercentage of participants (Number)
Allogeneic Hematopoietic Stem Cell Transplant0

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Percentage of Participants With Relapse

The return of disease after its apparent recovery/cessation. Patients with leukemia involving the BM and myelodysplastic syndrome will have this assessed by BM biopsy and additional special studies such as cytogenetics or flow cytometry as appropriate. Patients will also have radiology studies such as plain X-rays or CT scans and/or other studies such as blood tumor markers to document presence or absence of disease as clinically indicated. (NCT01685411)
Timeframe: 2 Years

Interventionpercentage of participants (Number)
Allogeneic Hematopoietic Stem Cell Transplant40

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Percentage of Participants With Relapse

The return of disease after its apparent recovery/cessation. Patients with leukemia involving the BM and myelodysplastic syndrome will have this assessed by BM biopsy and additional special studies such as cytogenetics or flow cytometry as appropriate. Patients will also have radiology studies such as plain X-rays or CT scans and/or other studies such as blood tumor markers to document presence or absence of disease as clinically indicated. (NCT01685411)
Timeframe: 1 Year

Interventionpercentage of participants (Number)
Allogeneic Hematopoietic Stem Cell Transplant40

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Assessment of Laboratory Tumor Lysis Syndrome (LTLS)

Assessment of LTLS, from Day 3 to Day 8. According to Cairo-Bishop definition LTLS is defined by the presence of 2 or more laboratory abnormalities including: a 25% increase or levels above normal for serum uric acid, potassium, and phosphate or a 25% decrease or levels below normal for calcium. (NCT01724528)
Timeframe: 6 days

Intervention% of patients with LTLS occurrence (Number)
Febuxostat8.1
Allopurinol9.2

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Assessment of Clinical Tumor Lysis Syndrome (CTLS)

Assessment of CTLS, from Day 3 to Day 8. According to Cairo-Bishop definition, CTLS is defined by the presence of LTLS in addition to 1 or more of the following significant clinical complications: renal insufficiency, cardiac arrhythmias, sudden death and seizures. The grade of CTLS is defined by the maximal grade of the clinical manifestation (NCT01724528)
Timeframe: 6 days

Intervention% of patients with CTLS occurrence (Number)
Febuxostat1.7
Allopurinol1.2

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Preservation of Renal Function

Change in serum creatinine level from baseline (Day 1) to the evaluation visit (Day 8) (NCT01724528)
Timeframe: 8 days

Interventionchange % (Mean)
Febuxostat-0.83
Allopurinol-4.92

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Serum Uric Acid (sUA) Level Control

Area under the curve of sUA from baseline (Day 1) to the evaluation visit (Day 8) (NCT01724528)
Timeframe: 8 days

Interventionmg x hour/dL (Mean)
Febuxostat514.0
Allopurinol708.0

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Treatment Responder Rate

Assessment of treatment responder rate, where treatment response is defined as the maintenance of sUA ≤ 7.5 mg/dL from Day 3 to Day 8 (NCT01724528)
Timeframe: 6 days

Intervention% of patients who fail to respond (Number)
Febuxostat1.7
Allopurinol4.0

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Resolution of the Acute Gout Attack

The primary outcome unit of measurement is time (in days) to resolution of the acute gout attack (NCT01988402)
Timeframe: 1-28 Days

Interventiondays (Mean)
Allopurinol15.4
Sugar Pill (Placebo)13.4

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Pain Day 28

Patient rated pain on a Likert pain score of 0-10 (NCT01988402)
Timeframe: Pateints are assessed at five time intervals over 28 days: days 1, 3-4, 10-15, 20-25, and 28; Day 28 reported

Interventionunits on a Likert scale (Mean)
Allopurinol1.79
Sugar Pill (Placebo)2.0

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Physician Global Assessment of Gout Activity at Day 28

Physician rated gout activity is measured on a Likert scale 0-10. (NCT01988402)
Timeframe: Pateints are assessed at five time intervals over 28 days: days 1, 3-4, 10-15, 20-25, and 28; Day 28 reported

Interventionunits on a Likert scale (Mean)
Allopurinol0
Sugar Pill (Placebo)0

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Serum Uric Acid Level

Blood test (serum) for uric acid level (NCT01988402)
Timeframe: day 28

Interventionmg/dl (Mean)
Allopurinol6.4
Sugar Pill (Placebo)8.2

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AER at the End of the Treatment Period

Geometric mean of urinary albumin excretion rate (AER) during the last three months of the treatment period (Visits 15 and 16), adjusted for the mean urinary AER at baseline. Results are expressed as least square means of the geometric means in each subject in each group. (NCT02017171)
Timeframe: Last three months of treatment period (Weeks 142 and 156)

Interventionug/min (Least Squares Mean)
Allopurinol47.9
Placebo37.4

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AER at the End of the Wash-out Period

Geometric mean of two urinary albumin excretion (AER) measurements at the end of the 2-month wash-out period following the 3-year treatment period, adjusted for the mean urinary AER at baseline. Results are expressed as least square means of the geometric means in each subject in each group. (NCT02017171)
Timeframe: End of the 2-month wash-out period following the 3-year treatment period (week 164)

Interventionug/min (Least Squares Mean)
Allopurinol42.9
Placebo31.7

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eGFR at 4 Months of Treatment

Glomerular filtration rate (GFR) at 4 months after randomization, estimated from serum creatinine and cystatin C and adjusted for the eGFR at baseline. (NCT02017171)
Timeframe: 4 months after randomization (week 16)

Interventionml/min/1.73 m2 (Least Squares Mean)
Allopurinol70.3
Placebo70.0

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eGFR Time Trajectory

Glomerular filtration rate time trajectory from baseline to end of the 2-month wash-out period (week 164) estimated from quarterly serum creatinine measurements (eGFR). eGFR slopes were estimated by a linear mixed-effects model for longitudinal eGFR measures using a multiple imputation technique for missing values. Positive values denote increasing eGFR over time, negative values denote declining eGFR over time. (NCT02017171)
Timeframe: Weeks 0, 4, 16, 32, 48, 64, 80, 96, 112, 128, 156, and 164 (from baseline to the end of washout period)

Interventionml/min/1.73 m2/year (Least Squares Mean)
Allopurinol-2.4
Placebo-2.1

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Fatal or Non-fatal Cardiovascular Events

Risk of cardiovascular events defined as the composite of CVD death (ICD-10 code I10 to I74.9), myocardial infarction, stroke (ischemic or hemorrhagic), coronary artery bypass grafting, or percutaneous coronary intervention in the allopurinol arm as compared to placebo.Results are expressed as the number of participants who experienced an event in each treatment group. The risk of an event in the allopurinol group as compared to the risk in the placebo group is expressed as hazard ratio (estimated by means of proportional hazard regression). (NCT02017171)
Timeframe: Up to the end of the 2-month wash-out period following the 3-year treatment period (week 0 to 164)

InterventionParticipants (Count of Participants)
Allopurinol15
Placebo9

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iGFR at the End of the Wash-out Period

Glomerular filtration rate (GFR) at the end of the 2-month wash-out period following the 3-year treatment period, measured by the plasma disappearance of non-radioactive iohexol (iGFR) and adjusted for the iGFR at baseline. (NCT02017171)
Timeframe: End of the 2-month wash-out period following the 3-year treatment period (week 164)

Interventionml/min/1.73 m^2 (Least Squares Mean)
Allopurinol61.2
Placebo61.2

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iGFR the End of Treatment Period

Glomerular filtration rate (GFR) at the end of the 3-year treatment period, measured by the plasma disappearance of non-radioactive iohexol (iGFR) and adjusted for the iGFR at baseline. (NCT02017171)
Timeframe: End of the 3-yr treatment period (week 156)

Interventionml/min/1.73 m2 (Least Squares Mean)
Allopurinol61.3
Placebo61.0

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iGFR Time Trajectory

Glomerular filtration rate time trajectory estimated from iohexol disappearance GFR (iGFR) measurements at weeks 0, 80, 156, and 164. iGFR slopes were estimated by a linear mixed-effects model for longitudinal iGFR measures using a multiple imputation technique for missing values. Positive values denote increasing GFR over time, negative values denote declining iGFR over time. (NCT02017171)
Timeframe: Weeks 0, 80, 156, and 164 (from baseline to the end of washout period)

Interventionml/min/1.73 m2/year (Least Squares Mean)
Allopurinol-3.0
Placebo-2.5

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Serum Creatinine Doubling or End Stage Renal Disease (ESRD)

Risk of serum creatinine doubling or end stage renal disease (ESRD) in the allopurinol arm as compared to placebo. Results are expressed as the number of participants who experienced an event in each treatment group. The risk of an event in the allopurinol group as compared to the risk in the placebo group is expressed as hazard ratio (estimated by means of proportional hazard regression). (NCT02017171)
Timeframe: Up to the end of the 2-month wash-out period following the 3-year treatment period (Week 0 to Week 164)

InterventionParticipants (Count of Participants)
Allopurinol13
Placebo11

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Change in Flow-mediated Arterial Vasodilation

Compare endothelial function as indexed by flow-mediated arterial vasodilation (FMD) within each phase of treatment (allopurinol 300 mg/day PO or placebo). Percent (%) change in FMD is calculated by comparing FMD (%) at the end of each treatment phase to pre-treatment values. (NCT02038179)
Timeframe: 4 weeks (pre-treatment vs. post-treatment FMD Values (%))

Interventionpercent change (Mean)
Allopurinol Phase2.5
Placebo Phase-0.1

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Change in Serum Levels of High Sensitivity C-reactive Protein

Serum level of high sensitivity C-reactive protein will be reported as a change during treatment phase (allopurinol 300 mg/day PO or placebo). Change in serum level of C-reactive protein is calculated by comparing serum values at the end of each treatment phase to pre-treatment levels. (NCT02038179)
Timeframe: 4 weeks (pre-treatment vs. post-treatment serum levels)

Interventionmg/L (Mean)
Allopurinol Phase0.6
Placebo Phase0.8

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Change in Systolic Blood Pressure (SBP)

Compare systolic blood pressure (SBP) captured by wearing a 24 hour ambulatory blood pressure monitor during each phase of treatment (allopurinol 300 mg/day PO or placebo). Change in systolic blood pressure is calculated by comparing SBP at the end of each treatment phase to pre-treatment values. (NCT02038179)
Timeframe: 4 weeks (pre-treatment vs. post-treatment SBP)

Interventionmm Hg (Mean)
Allopurinol Phase-1.39
Placebo Phase-1.06

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Absolute Change of Serum Uric Acid Levels From Baseline Levels

To compare the absolute change of serum uric acid levels from baseline levels (NCT02078219)
Timeframe: Baseline, Weeks 1,2,4,6,8,10,12,16,18,20,24

,,,,
Interventionmg/dL (Mean)
Week 1Week 2Week 4Week 6Week 8Week 10Week 12Week 16Week 18Week 20Week 24
Allopurinol 200 mg Treatment Group-1.82-1.83-1.83-3.26-3.22-2.96-3.35-3.44-3.40-3.35-3.31
RDEA3170 Placebo Treatment Group-0.05-0.070.06-0.040.02-0.060.02-0.22-0.27-0.22-0.42
RDEA3170 Treatment Group 1-1.68-1.81-2.01-2.78-2.44-2.19-2.44-2.67-2.86-2.87-3.10
RDEA3170 Treatment Group 2-1.74-1.75-1.72-2.66-2.61-3.22-3.85-4.24-4.17-3.98-3.99
RDEA3170 Treatment Group 3-1.68-1.78-2.07-3.00-2.74-3.75-4.33-4.57-4.62-4.52-4.57

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Percent Changes of Serum Uric Acid Levels From Baseline Levels

The primary objective of the study is to compare percent changes of serum uric acid levels from baseline levels after 16 weeks of dosing between RDEA3170 treatment groups and the placebo treatment group. (NCT02078219)
Timeframe: Baseline and Week 16

InterventionPercent change (Mean)
RDEA3170 Treatment Group 1-30.93
RDEA3170 Treatment Group 2-49.91
RDEA3170 Treatment Group 3-54.32
RDEA3170 Placebo Treatment Group-2.05
Allopurinol 200 mg Treatment Group-39.09

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Percent Change in sUA

To compare percent change in sUA at each study visit. (NCT02078219)
Timeframe: Baseline, Weeks 1,2,4,6,8,10,12,16,18,20,24

,,,,
Intervention% Change (Mean)
Week 1Week 2Week 4Week 6Week 8Week 10Week 12Week 16Week 18Week 20Week 24
Allopurinol 200 mg Treatment Group-20.74-20.80-20.60-37.06-36.51-33.42-37.96-39.09-38.59-38.00-37.77
RDEA3170 Placebo Treatment Group-0.25-0.530.97-0.010.55-0.270.43-2.05-2.86-2.27-4.67
RDEA3170 Treatment Group 1-19.72-21.03-22.95-32.05-27.94-24.69-28.08-30.93-32.94-32.96-35.73
RDEA3170 Treatment Group 2-20.29-20.28-19.66-31.26-30.19-37.61-45.77-49.91-49.04-47.20-47.34
RDEA3170 Treatment Group 3-19.93-20.93-24.21-35.24-32.11-44.38-51.17-54.32-54.70-53.60-54.46

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Percentage of Subjects With a Serum Uric Acid Level ≤6.0 mg/dL

To compare the percentage of subjects whose serum uric acid levels are ≤ 6.0 mg/dL between RDEA3170 treatment groups and the placebo treatment group at each study visit (NCT02078219)
Timeframe: Weeks 1,2,4,6,8,10,12,16,18,20,24

,,,,
Intervention% subjects (Number)
Week 1Week 2Week 4Week 6Week 8Week 10Week 12Week 16Week 18Week 20Week 24
Allopurinol 200 mg Treatment Group19.519.517.173.265.961.075.678.073.278.075.6
RDEA3170 Placebo Treatment Group00000000000
RDEA3170 Treatment Group 126.829.326.870.753.746.353.751.263.461.068.3
RDEA3170 Treatment Group 231.734.131.761.056.178.085.495.192.782.982.9
RDEA3170 Treatment Group 339.034.139.082.978.092.792.797.695.192.787.8

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Absolute Change in the Serum Urate Level at the Final Visit Relative to Baseline

(NCT02082769)
Timeframe: Baseline and Final Visit (up to 26 weeks)

Interventionumol/l (Mean)
Febuxostat 40 mg QD182.2
Febuxostat 80 mg QD216.0
Allopurinol 100mg QD170.4

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Percentage of Subjects Whose Last Three Serum Urate Levels Are <6.0 Milligram Per Deciliter (mg/dL)

(NCT02082769)
Timeframe: Last 3 visits (any last 3 visits up to week 26)

Interventionpercentage of participants (Number)
Febuxostat 40 mg QD22.5
Febuxostat 80 mg QD33.5
Allopurinol 100mg QD17.0

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Percentage of Subjects Whose Serum Urate Levels Are <6.0 mg/dL at Final Visit

(NCT02082769)
Timeframe: Final Visit (up to 26 weeks)

Interventionpercentage of participants (Number)
Febuxostat 40 mg QD45.0
Febuxostat 80 mg QD58.9
Allopurinol 100mg QD34.6

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Time of Occurrence of Maximum Observed Concentration (Tmax)

Tmax of Allopurinol/Oxypurinol and RDEA3170 Alone and In Combination (NCT02279641)
Timeframe: 22 days

Interventionhr (Median)
Allopurinol: Allopurinol Alone1.50
Allopurinol: RDEA3170 + Allopurinol1.25
Oxypurinol: Allopurinol Alone4.00
Oxypurinol: RDEA3170 + Allopurinol3.50
RDEA3170: RDEA3170 Alone3.00
RDEA3170: RDEA3170 + Allopurinol3.00

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Renal Clearance of the Drug From Time Zero up to 24 Hours Postdose (CRL0-24)

CLR0-24 of Allopurinol/Oxypurinol and RDEA3170 Alone and In Combination (NCT02279641)
Timeframe: 22 days

InterventionmL/min (Geometric Mean)
Allopurinol: Allopurinol Alone120
Allopurinol: RDEA3170 + Allopurinol103
Oxypurinol: Allopurinol Alone15.1
Oxypurinol: RDEA3170 + Allopurinol29.2
RDEA3170: RDEA3170 Alone9.28
RDEA3170: RDEA3170 + Allopurinol9.75

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Maximum Observed Plasma Concentration (Cmax)

Cmax of RDEA3170 Alone and In Combination with Allopurinol (NCT02279641)
Timeframe: 22 days

Interventionng/mL (Geometric Mean)
RDEA3170: RDEA3170 Alone14.6
RDEA3170: RDEA3170 + Allopurinol14.5

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Maximum Observed Plasma Concentration (Cmax)

Cmax of Allopurinol/Oxypurinol Alone and In Combination with RDEA3170 (NCT02279641)
Timeframe: 22 days

Interventionμg/mL (Geometric Mean)
Allopurinol: Allopurinol Alone1.13
Allopurinol: RDEA3170 + Allopurinol1.51
Oxypurinol: Allopurinol Alone12.8
Oxypurinol: RDEA3170 + Allopurinol8.68

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Incidence of Treatment-Emergent Adverse Events

(NCT02279641)
Timeframe: 22 days

InterventionNumber of participants (Number)
RDEA3170: RDEA3170 Alone2
Oxypurinol: RDEA3170 + Allopurinol1
Allopurinol: Allopurinol Alone3

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Area Under the Concentration-time Curve From Time Zero up to 24 Hours Postdose (AUC 0-24)

AUC 0-24 of RDEA3170 Alone and In Combination with Allopurinol (NCT02279641)
Timeframe: 22 days

Interventionμg*hr/mL (Geometric Mean)
RDEA3170: RDEA3170 Alone120
RDEA3170: RDEA3170 + Allopurinol115

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Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Sampling Timepoint (AUC Last)

AUC last of RDEA3170 Alone and In Combination with Allopurinol (NCT02279641)
Timeframe: 22 days

Interventionng·hr/mL (Geometric Mean)
RDEA3170: RDEA3170 Alone120
RDEA3170: RDEA3170 + Allopurinol115

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Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Sampling Timepoint (AUC Last)

AUC last of Allopurinol/Oxypurinol Alone and In Combination with RDEA3170 (NCT02279641)
Timeframe: 22 days

Interventionμg·hr/mL (Geometric Mean)
Allopurinol: Allopurinol Alone3.50
Allopurinol: RDEA3170 + Allopurinol3.61
Oxypurinol: Allopurinol Alone255
Oxypurinol: RDEA3170 + Allopurinol157

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Apparent Terminal Half-life (t1/2)

t1/2 of Allopurinol/Oxypurinol and RDEA3170 Alone and In Combination (NCT02279641)
Timeframe: 22 days

Interventionhr (Geometric Mean)
Allopurinol: Allopurinol Alone1.06
Allopurinol: RDEA3170 + Allopurinol0.992
Oxypurinol: Allopurinol Alone43.2
Oxypurinol: RDEA3170 + Allopurinol29.1
RDEA3170: RDEA3170 Alone11.5
RDEA3170: RDEA3170 + Allopurinol12.5

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Amount Excreted in Urine as Unchanged Drug or Metabolite (Ae0-24)

Ae0-24 of RDEA3170 Alone and In Combination with Allopurinol (NCT02279641)
Timeframe: 22 days

Interventionug (Geometric Mean)
RDEA3170: RDEA3170 Alone66.8
RDEA3170: RDEA3170 + Allopurinol67.2

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Amount Excreted in Urine as Unchanged Drug or Metabolite (Ae0-24)

Ae0-24 of Allopurinol/Oxypurinol Alone and In Combination with RDEA3170 (NCT02279641)
Timeframe: 22 days

Interventionmg (Geometric Mean)
Allopurinol: Allopurinol Alone25.4
Allopurinol: RDEA3170 + Allopurinol22.7
Oxypurinol: Allopurinol Alone231
Oxypurinol: RDEA3170 + Allopurinol275

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Area Under the Concentration-time Curve From Time Zero up to 24 Hours Postdose (AUC 0-24)

AUC 0-24 of Allopurinol/Oxypurinol Alone and In Combination with RDEA3170 (NCT02279641)
Timeframe: 22 days

Interventionμg·hr/mL (Geometric Mean)
Allopurinol: Allopurinol Alone3.69
Allopurinol: RDEA3170 + Allopurinol3.68
Oxypurinol: Allopurinol Alone255
Oxypurinol: RDEA3170 + Allopurinol157
RDEA3170: RDEA3170 + Allopurinol115

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Pharmacodynamics (PD) Profile of Uric Acid From Serum and Urine

(NCT02279641)
Timeframe: 22 days

,,
InterventionPercentage (%) (Mean)
Serum Urate Maximum % ChangeUrine Uric Acid % Change (0-24h)Renal Clearance of Uric Acid % Change (0-24h)Fract. Excretion of Uric Acid % Change (0-24h)
Allopurinol: Allopurinol Alone-43.0-47.4-8.50-12.0
Oxypurinol: RDEA3170 + Allopurinol-65.2-21.612578.4
RDEA3170: RDEA3170 Alone-50.59.8812277.4

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Cohort 2 - Concentration of Serum Urate at 24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol.

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 2) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

Interventionmg/dL (Mean)
Treatment A16.2
Treatment A2q5.0
Treatment A2b4.6
Treatment R24.8
Treatment R44.1
Treatment R63.5

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Cohort 2 - Maximum Percentage (%) Change in Serum Urate of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (Emax, CB (%))

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 2) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

InterventionMaximum Percentage (%) Change (Mean)
Treatment A1-39.3
Treatment A2q-54.4
Treatment A2b-50.3
Treatment R2-57.8
Treatment R4-66.0
Treatment R6-73.2

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Cohort 2 - Renal Hypoxanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeHXO, CB (%))

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 2) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

InterventionPercentage (%) Change (Mean)
Treatment A1372
Treatment A2q645
Treatment A2b681
Treatment R2268
Treatment R4267
Treatment R6286

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Cohort 2 - Renal Xanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeXO, CB (%))

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 2) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

InterventionPercentage (%) Change (Mean)
Treatment A1952
Treatment A2q2027
Treatment A2b2138
Treatment R2812
Treatment R4797
Treatment R6816

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Maximum Observed Concentration (Cmax)

Cmax of Allopurinol alone or in combination with RDEA3170 (NCT02498652)
Timeframe: Day 7, 14, 21, 28 and 35 (predose through 24 hours postdose)

Interventionµg/mL (Geometric Mean)
Treatment A11.18
Treatment A2q2.43
Treatment A2b1.19
Treatment R11.16
Treatment R21.16
Treatment R31.14
Treatment R41.11
Treatment R51.12
Treatment R61.26

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Time of Occurrence of Maximum Observed Concentration (Tmax)

Tmax of Allopurinol alone or in combination with RDEA3170 (NCT02498652)
Timeframe: Day 7, 14, 21, 28 and 35 (predose through 24 hours postdose)

Interventionhr (Geometric Mean)
Treatment A11.50
Treatment A2q2.98
Treatment A2b2.02
Treatment R12.01
Treatment R22.49
Treatment R31.73
Treatment R42.98
Treatment R51.73
Treatment R61.97

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Number of Participants With Treatment-Emergent Adverse Events

(NCT02498652)
Timeframe: 11 weeks

InterventionNumber of participants (Number)
Cohort 16
Cohort 26

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Apparent Terminal Half-life (t1/2)

t1/2 of Allopurinol alone or in combination with RDEA3170 (NCT02498652)
Timeframe: Day 7, 14, 21, 28 and 35 (predose through 24 hours postdose)

Interventionhr (Geometric Mean)
Treatment A11.21
Treatment A2q1.47
Treatment A2b1.25
Treatment R11.20
Treatment R21.14
Treatment R31.17
Treatment R41.16
Treatment R51.13
Treatment R61.13

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Area Under the Concentration-time Curve From Time Zero to the Last Quantifiable Sampling Timepoint (AUC Last)

AUC last of Allopurinol alone or in combination with RDEA3170 (NCT02498652)
Timeframe: Day 7, 14, 21, 28 and 35 (predose through 24 hours postdose)

Interventionµg·hr/mL (Geometric Mean)
Treatment A13.70
Treatment A2q10.9
Treatment A2b4.25
Treatment R13.59
Treatment R23.76
Treatment R33.71
Treatment R43.53
Treatment R53.74
Treatment R63.74

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Area Under the Concentration-time Curve From Time Zero up to 24 Hours Postdose (AUC 0-24)

AUC 0-24 of Allopurinol alone or in combination with RDEA3170 (NCT02498652)
Timeframe: Day 7, 14, 21, 28 and 35 (predose through 24 hours postdose)

Interventionµg·hr/mL (Geometric Mean)
Treatment A13.94
Treatment A2q11.0
Treatment A2b8.64
Treatment R14.06
Treatment R24.10
Treatment R33.81
Treatment R43.83
Treatment R53.88
Treatment R63.82

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Cohort 1 - Concentration of Serum Urate at 24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol.

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 1) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

Interventionmg/dL (Mean)
Treatment A15.8
Treatment A2q4.8
Treatment A2b4.0
Treatment R15.5
Treatment R34.6
Treatment R53.8

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Cohort 1 - Maximum Percentage (%) Change in Serum Urate of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (Emax, CB (%))

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 1) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

InterventionMaximum Percentage (%) Change (Mean)
Treatment A1-40.2
Treatment A2q-55.0
Treatment A2b-56.8
Treatment R1-48.1
Treatment R3-61.0
Treatment R5-69.5

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Cohort 1 - Renal Hypoxanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeHXO, CB (%))

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 1) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

InterventionPercentage (%) Change (Mean)
Treatment A1400
Treatment A2q517
Treatment A2b827
Treatment R1310
Treatment R3311
Treatment R5305

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Cohort 1 - Renal Xanthine Excretion at 0-24hr of Multiple-dose RDEA3170 Administered in Combination With Allopurinol (AeXO, CB (%))

Pharmacodynamics (PD) profile of multiple-dose RDEA3170 administered in combination with allopurinol (Cohort 1) (NCT02498652)
Timeframe: Screening, Days -1 , 1, 7, 14, 21, 28, and 35 (Pre-dose and Post-dose)

InterventionPercentage (%) Change (Mean)
Treatment A11065
Treatment A2q1827
Treatment A2b2633
Treatment R1899
Treatment R3958
Treatment R5827

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Pulse Wave Velocity

Comparison of the effects of Febuxostat and Allopurinol on Pulse Wave Velocity (PWV) after 36 weeks of treatment. (NCT02500641)
Timeframe: 36 weeks of treatment

Interventionm/s (Mean)
Febuxostat 80/120 mg/Day9.0
Allopurinol 100 up to 600 mg/Day9.05

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Percentage of Participants Experiencing ≥ 1 Gout Flare During Phase 3

"Participants were defined as flaring in Phase 3 if they:~-1) met 3 of 4 following participant-reported criteria:~a) warm joint(s)~b) swollen joint(s)~c) pain (>3) at rest on a scale of 0-10 (10 being the worst pain)~d) self-identified gout flare~OR~-2) reported use of medications to treat flare" (NCT02579096)
Timeframe: Phase III of the study (weeks 49-72 of study duration)

InterventionParticipants (Count of Participants)
Allopurinol / Sham Comparator (Febuxostat)135
Febuxostat / Sham Comparator (Allopurinol)165

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Urinary 2,8-dihydroxyadenine Excretion

(NCT02752633)
Timeframe: 0, 14 and 28 days

Interventionmg/24-h (Median)
BaselineOn allopurinol treatmentOn febuxostat treatment
Allopurinol/Febuxostat Treatment1164513

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Percent Change Uric Acid

Maximum percent change in uric acid after a single dose of allopurinol (NCT02956278)
Timeframe: 24 hours

InterventionPercent Change from Baseline (Mean)
BCRP Q141K CC Genotype26.8
BCRP Q141K CA Genotype23.8
BCRP Q141K AA Genotype21.4

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Oxypurinol AUC

Area under the concentration time curve from 0-24 hours following a single dose of allopurinol (i.e. Day 1 of both protocols) (NCT02956278)
Timeframe: 24 hours (Collections at 0, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 24 hours post-dose)

Interventionmcg*hr/mL (Mean)
BCRP Q141K CC Genotype95.9
BCRP Q141K CA Genotype99.1
BCRP Q141K AA Genotype108.5

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Oxypurinol Renal Clearance

Renal clearance as defined by amount excreted in 24 hours/AUC from 0-24 hours (NCT02956278)
Timeframe: 24 hours (Urine collected 0-4 hrs,4-8 hrs,8-10 hrs,10-24 hrs post-dose)

InterventionL/hr (Mean)
BCRP Q141K CC Genotype1.9
BCRP Q141K CA Genotype1.4
BCRP Q141K AA Genotype1.6

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Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment

The eCrCl was calculated by the Cockcroft-Gault formula using ideal body weight. (NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

InterventionmL/min (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Month 18Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Placebo + XOI0.13-0.69-1.84-0.78-2.140.36-19.0-1.032.33

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Percentage of Participants Meeting Criteria (eg, Based on sCr or eCrCl Criteria) for Treatment Discontinuations Over the Study Period

Kidney function was monitored throughout the study by measuring sCr and calculating eCrCl by Cockcroft-Gault formula using ideal body weight. Treatment discontinuations were required if a participant experienced an absolute sCr ≥4.0 mg/dL or an eCrCl <20 mL/min (based on central laboratory results). (NCT03226899)
Timeframe: up to 18 months

Interventionpercentage of participants (Number)
Placebo + XOI0.0
Lesinurad + XOI0.0

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Percentage of Participants Who Achieve Serum Urate (sUA) < 6.0 mg/dL at Month 6

(NCT03226899)
Timeframe: Month 6

Interventionpercentage of participants (Number)
Placebo + XOI33.8
Lesinurad + XOI58.8

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Percentage of Participants With Serum Creatinine (sCr) Elevations (≥1.5 × Baseline) Over the Study Period

(NCT03226899)
Timeframe: up to 18 months

Interventionpercentage of participants (Number)
Placebo + XOI5.2
Lesinurad + XOI7.3

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Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment

The eCrCl was calculated by the Cockcroft-Gault formula using ideal body weight. (NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

InterventionmL/min (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Lesinurad + XOI-1.29-1.53-1.80-2.10-4.30-6.00-1.91-2.45

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Percentage of Participants Who Achieve sUA < 6.0 mg/dL Over Time

(NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionpercentage of participants (Number)
BaselineMonth 1Month 3Month 6Month 9Month 12Month 15Month 18
Placebo + XOI10.335.136.433.834.042.945.50.0

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Percentage of Participants Who Achieve sUA < 6.0 mg/dL Over Time

(NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionpercentage of participants (Number)
BaselineMonth 1Month 3Month 6Month 9Month 12Month 15
Lesinurad + XOI10.658.852.558.842.956.562.5

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Percent Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment

(NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionpercent change (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Month 18Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Placebo + XOI-11.3-11.4-10.0-12.6-15.2-18.90.00-10.6-16.1

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Percent Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment

(NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionpercent change (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Lesinurad + XOI-24.0-21.2-23.9-18.6-14.7-26.1-24.8-27.3

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Percent Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment

The eCrCl was calculated by the Cockcroft-Gault formula using ideal body weight. (NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionpercent change (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Month 18Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Placebo + XOI1.16-0.18-2.49-0.26-3.383.67-31.7-1.134.14

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Percent Change From Baseline in eCrCl Over the Study Period, Including the Last Value On and Off Treatment

The eCrCl was calculated by the Cockcroft-Gault formula using ideal body weight. (NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionpercent change (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Lesinurad + XOI-2.07-2.14-3.01-3.42-8.1-11.0-3.04-5.35

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Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment

(NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionµmol/L (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Month 18Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Placebo + XOI-57.0-59.8-54.6-70.6-78.7-92.60.00-57.0-70.7

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Change From Baseline in sUA Over Time, Including the Last Value On and Off Treatment

(NCT03226899)
Timeframe: Baseline, Months 1, 3, 6, 9, 12, 15, 18

Interventionµmol/L (Mean)
Change at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12Change at Month 15Change at Last On-Treatment VisitChange at Last Off-Treatment Visit
Lesinurad + XOI-120.3-106.8-125.8-95.9-69.6-116.6-125.5-156.6

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Brachial Artery Flow Mediated Dilation (FMD)

Brachial artery FMD will be assessed at baseline and final. FMD is a measurement of conduit artery endothelial function. FMD is assessed immediately after each PWV measurement. Shear rate AUC until peak diameter is calculated as stimulus for FMD and used in covariate analysis as described. All measurements will be performed, under co-I supervision by the same blinded technician. (NCT03648996)
Timeframe: Baseline and 6 months (final). The goal is to assess changes from baseline when compared to final time point.

InterventionPercentage (%) (Mean)
Allopurinol5.03
Placebo4.4
Low-fructose Diet, Hypocaloric7.10

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Insulin-stimulated Leg Blood Flow

We will perform a hyperinsulinemic euglycemic clamp to evaluate insulin-stimulated leg blood flow (to be assessed via Doppler ultrasound). Insulin will be infused at a constant rate to mimic postprandial insulin concentrations and glucose maintained at fasting values via a variable 20% dextrose infusion. Femoral artery blood flow will be assessed at the beginning and at end of the 60-minute insulin infusion, and data are presented as percent of change from pre-insulin infusion values. (NCT03648996)
Timeframe: The goal is to assess insulin stimulated responses in blood flow after 6 mo of intervention.

InterventionPercetage (%) change (Mean)
Allopurinol-7.68
Placebo68.18
Low-fructose Diet, Hypocaloric42.65

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Carotid Femoral Pulse Wave Velocity (cfPWV)

It is the gold standard non-invasive index of arterial stiffness. Transit time between carotid and femoral pressure waves is calculated using the foot-to-foot method. cfPWV is calculated as distance traveled by the pulse wave (i.e., femoral location-sternal notch minus sternal notch-carotid location) divided by pulse transit time. All the measurements will be done by the same blinded technician (NCT03648996)
Timeframe: This will be assessed at baseline and 6 months (final). The goal is to assess changes from baseline when compared to final time point.

Interventionm/s (Mean)
Allopurinol8.71
Placebo7.8
Low-fructose Diet, Hypocaloric8.28

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Serum Uric Acid Change

Change in Serum Uric Acid (NCT03865407)
Timeframe: The difference in Serum Uric Acid between baseline and 6 months will be measured

Interventionmg/dl (Mean)
Allopurinol-3.33
Standard of Care Control-0.46

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Systolic Blood Pressure

Change in systolic blood pressure (NCT03865407)
Timeframe: The difference in clinic systolic blood pressure between baseline and 6 months will be measured

InterventionmmHg (Mean)
Allopurinol-6.5
Standard of Care Control2.29

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Diastolic Blood Pressure

Change in diastolic blood pressure (NCT03865407)
Timeframe: The difference in clinic diastolic blood pressure between baseline and 6 months will be measured

InterventionmmHg (Mean)
Allopurinol-7.33
Standard of Care Control3.983

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eGFR Change

Change in Creatinine eGFR over time (NCT03865407)
Timeframe: The difference in Creatinine eGFR between baseline and 6 months will be measured

Interventionml/min/1.73m^2 (Mean)
Allopurinol3.86
Standard of Care Control0

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eGFR Change

Change in Cys-C eGFR over time (NCT03865407)
Timeframe: The difference in Cystatin C eGFR between baseline and 6 months will be measured

Interventionml/min/1.73m^2 (Mean)
Allopurinol3.14
Standard of Care Control-0.29

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Serum High Sensitivity C-reactive Protein (Hs-CRP)

Compare the mean difference of serum hs-CRP from baseline to 6 months between groups (NCT03865407)
Timeframe: Serum hs-CRP will be measured at baseline and 6 months

Interventionmg/dL (Mean)
Allopurinol1.66
Standard of Care Control-7.64

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P-cystatin C (mg/L) Change From Baseline at 6 Months (V8), Repeated Measures Mixed Model (MMRM)

"Change from baseline in P-cystatin C at 6 months (Visit 8), there were 7 comparisons requested for this endpoint, namely:~High dose vs Placebo~Inter. dose vs Placebo~Low dose vs Placebo~High dose vs Allopurinol~Inter. dose vs Allopurinol~Low dose vs Allopurinol~Allopurinol vs Placebo." (NCT03990363)
Timeframe: Baseline to 9 months (Visit 9); analysis at 6 months (Visit 8)

InterventionGeometric Mean Ratio (Geometric Mean)
High Dose Versus Placebo1.009
Intermediate Dose Versus Placebo1.038
Low Dose Versus Placebo1.018
High Dose Versus Allopurinol0.9849
Interemdiate Dose Versus Allopurinol1.014
Low Dose Versus Allopurinol0.9946
Allopurinol Versus Placebo1.024

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P-cystatin C (mg/L) Change From Baseline at 12 Months (Visit 10)

"Change from baseline in S-creatinine at 12 months (Visit 10) for the following treatments:~High Dose~Inter. Dose~Low Dose (a)~Switch Dose protocol version 5.0 (PA5) (b)~Allopurinol~Placebo~Subjects that switched from Verinurad 3 mg to Verinurad 24 mg at Visit 9 are not included in this group for Visit 10.~Contains all subjects randomized to the low dose group that later switched to Verinurad 24 mg plus Allopurinol 300 mg." (NCT03990363)
Timeframe: Change from baseline to 12 months (Visit 10)

Interventionmg/L (Geometric Mean)
High Dose1.070
Intermediate Dose1.079
Low Dose1.065
Switch Dose PA51.018
Allopurinol1.083
Placebo1.048

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Estimated Glomerular Filtration Rate (eGFR) (mL/Min/1.73 m²) Change From Baseline at 6 Months (V8), Repeated Measures Mixed Model (MMRM)

"Change from baseline in eGFR at 6 months (Visit 8), there were 7 comparisons requested for this endpoint, namely:~High dose vs Placebo~Inter. dose vs Placebo~Low dose vs Placebo~High dose vs Allopurinol~Inter. dose vs Allopurinol~Low dose vs Allopurinol~Allopurinol vs Placebo." (NCT03990363)
Timeframe: Baseline to 9 months (Visit 9); analysis at 6 months (Visit 8)

InterventionmL/min/1.73 m² (Geometric Mean)
High Dose Versus Placebo1.009
Intermediate Dose Versus Placebo0.9730
Low Dose Versus Placebo1.010
High Dose Versus Allopurinol1.023
Interemdiate Dose Versus Allopurinol0.9859
Low Dose Versus Allopurinol1.024
Allopurinol Versus Placebo0.9868

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Estimated Glomerular Filtration Rate (eGFR) (mL/Min/1.73 m²) Change From Baseline at 12 Months (Visit 10)

"Change from baseline in eGFR at 12 months (Visit 10) for the following treatments:~High Dose~Inter. Dose~Low Dose (a)~Switch Dose protocol version 5.0 (PA5) (b)~Allopurinol~Placebo~Subjects that switched from Verinurad 3 mg to Verinurad 24 mg at Visit 9 are not included in this group for Visit 10.~Contains all subjects randomized to the low dose group that later switched to Verinurad 24 mg plus Allopurinol 300 mg." (NCT03990363)
Timeframe: Change from baseline to 12 months (Visit 10)

InterventionmL/min/1.73 m² (Geometric Mean)
High Dose0.9809
Intermediate Dose0.9454
Low Dose0.9613
Switch Dose PA51.101
Allopurinol0.9593
Placebo0.9469

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Serum Uric Acid (sUA) Change From Baseline at 12 Months (Visit 10), Repeated Measures Mixed Model (MMRM)

Change from baseline in sUA at 12 months (Visit 10) for comparison of Switch dose protocol version 5.0 (PA5) versus double-capsule Placebo. (NCT03990363)
Timeframe: Baseline to 12 months (Visit 10); analysis at 12 months (Visit 10)

Interventionmg/dL (Geometric Mean)
Switch Dose PA5 Versus Placebo0.5540

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Urinary Albumin to Creatinine Ratio (uACR) (mg/g) Change From Baseline at 6 Months (Visit 8), Repeated Measures Mixed Model (MMRM)

"Analyses of change from baseline in uACR at 6 months (Visit 8) focused on:~High dose vs Placebo~High dose and Inter. dose combined vs Allopurinol alone~Inter. dose vs Placebo~Low dose vs Placebo~High dose vs Allopurinol~Inter. dose vs Allopurinol~Low dose vs Allopurinol~Allopurinol vs Placebo~For High dose and Inter. dose combined the 2 categories merged forming 1 new temporary category." (NCT03990363)
Timeframe: Baseline to 9 months (Visit 9); analysis at 6 months (Visit 8)

Interventionmg/g (Geometric Mean)
High Dose Versus Placebo0.8300
High Dose and Intermediate Dose Combined Versus Allopurinol1.043
Intermediate Dose Versus Placebo0.8369
Low Dose Versus Placebo0.8499
High Dose Versus Allopurinol1.037
Intermediate Dose Versus Allopurinol1.046
Low Dose Versus Allopurinol1.062
Allopurinol Versus Placebo0.8001

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Urinary Albumin to Creatinine Ratio (uACR) (mg/g) Change From Baseline at 12 Months (Visit 10), Repeated Measures Mixed Model (MMRM)

"Change from baseline in uACR at 12 months (Visit 10) for comparison of Switch dose protocol version 5.0 (PA5) versus double-capsule Placebo.~The statistical model applied was an MMRM, which was basically the same as the one applied in the primary analysis but adjusted for a 12 month horizon and adapted to the double-capsule regimen from Visit 9 on." (NCT03990363)
Timeframe: Baseline to 12 months (Visit 10); analysis at 12 months (Visit 10)

Interventionmg/g (Geometric Mean)
Switch Dose PA5 Versus Placebo1.016

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Serum Uric Acid (sUA) (mg/dL) Change From Baseline at 6 Months (Visit 8), Repeated Measures Mixed Model (MMRM)

"Change from baseline in sUA at 6 months (Visit 8), there were 7 comparisons requested for each endpoint, namely:~High dose vs Placebo~Inter. dose vs Placebo~Low dose vs Placebo~High dose vs Allopurinol~Inter. dose vs Allopurinol~Low dose vs Allopurinol~Allopurinol vs Placebo." (NCT03990363)
Timeframe: Baseline to 9 months (Visit 9); analysis at 6 months (Visit 8)

Interventionmg/dL (Geometric Mean)
High Dose Versus Placebo0.5098
Intermediate Dose Versus Placebo0.5810
Low Dose Versus Placebo0.6096
High Dose Versus Allopurinol0.8184
Interemdiate Dose Versus Allopurinol0.9327
Low Dose Versus Allopurinol0.9786
Allopurinol Versus Placebo0.6229

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S-creatinine (mg/dL) Change From Baseline at 6 Months (V8), Repeated Measures Mixed Model (MMRM)

"Change from baseline in S-creatinine at 6 months (Visit 8), there were 7 comparisons requested for this endpoint, namely:~High dose vs Placebo~Inter. dose vs Placebo~Low dose vs Placebo~High dose vs Allopurinol~Inter. dose vs Allopurinol~Low dose vs Allopurinol~Allopurinol vs Placebo." (NCT03990363)
Timeframe: Baseline to 9 months (Visit 9); analysis at 6 months (Visit 8)

InterventionGeometric Mean Ratio (Geometric Mean)
High Dose Versus Placebo0.9888
Intermediate Dose Versus Placebo1.023
Low Dose Versus Placebo0.9901
High Dose Versus Allopurinol0.9801
Interemdiate Dose Versus Allopurinol1.014
Low Dose Versus Allopurinol0.9814
Allopurinol Versus Placebo1.009

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S-creatinine (mg/dL) Change From Baseline at 12 Months (Visit 10)

"Change from baseline in S-creatinine at 12 months (Visit 10) for the following treatments:~High Dose~Inter. Dose~Low Dose (a)~Switch Dose protocol version 5.0 (PA5) (b)~Allopurinol~Placebo~Subjects that switched from Verinurad 3 mg to Verinurad 24 mg at Visit 9 are not included in this group for Visit 10.~Contains all subjects randomized to the low dose group that later switched to Verinurad 24 mg plus Allopurinol 300 mg." (NCT03990363)
Timeframe: Change from baseline to 12 months (Visit 10)

Interventionmg/dL (Geometric Mean)
High Dose1.011
Intermediate Dose1.038
Low Dose1.026
Switch Dose PA50.9078
Allopurinol1.028
Placebo1.043

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Model Predicted Baseline-corrected and Placebo-corrected QT Interval Corrected for Heart Rate (HR) Using Fridericia's Formula (QTcF)(ΔΔQTcF) (Derived From Concentration-QTcF Analysis) at Geometric Mean of Cmax of Verinurad

"Assessment of the effect of a single dose of verinurad given as either a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of International Council for Harmonisation Guideline E14 and associated Questions and Answers [ICH E14 Q&A]), both in combination with allopurinol 300 mg, on the QTcF interval compared to placebo using a concentration-QTcF analysis.~A linear mixed-effect concentration-QTcF model was used as the primary analysis. This is a result of the statistical model so it does not have values for every timepoint, it is just one set of numbers - summarizes data across all timepoints. No non-placebo-corrected QTcF data values were collected or could be obtained for each Arm/Group at Cmax of Verinurad." (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

Interventionmsec (Geometric Mean)
Treatment A-2.8
Treatment B-0.3

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Apparent Total Body Clearance of Drug From Plasma After Extravascular Administration (Parent Drug Only) (CL/F) for Verinurad and Allopurinol

Assessment of the PK of verinurad and allopurinol in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionLiter/Hour (Mean)
VerinuradAllopurinol
Treatment A64.0771.03
Treatment B45.0968.08

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Apparent Volume of Distribution at Steady State Following Extravascular Administration (Parent Drug Only) (Vss/F) for Verinurad and Allopurinol

Assessment of the PK of verinurad and allopurinol in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionLiter (Mean)
VerinuradAllopurinol
Treatment A1060182.9
Treatment B448.6165.3

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Apparent Volume of Distribution During the Terminal Phase After Extravascular Administration (Parent Drug Only) (Vz/F) for Verinurad and Allopurinol

Assessment of the PK of verinurad and allopurinol in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionLiter (Mean)
VerinuradAllopurinol
Treatment A1342103.6
Treatment B856.197.96

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Time to Reach Maximum Plasma Concentration (Tmax) for Verinurad, M1, M8, Allopurinol, and Oxypurinol

Assessment of the PK of verinurad and its metabolites (M1 and M8) and allopurinol and its metabolite (oxypurinol) in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionHour (Median)
VerinuradM1M8AllopurinolOxypurinol
Treatment A5.005.005.001.505.00
Treatment B1.021.501.501.503.00

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Number of Participants With Adverse Events (AEs)

Examination of the safety and tolerability of verinurad and allopurinol. (NCT04256629)
Timeframe: From Screening (Day -28 to Day -2) until the Follow-up visit (7 to 10 Days After the Last Dose)

,,
InterventionParticipants (Number)
Any AEAny AE with outcome = deathAny Serious adverse events (including events with outcome = death)Any AE leading to discontinuation of study drugAny AE leading to withdrawal from study
Treatment A80000
Treatment B40011
Treatment C50000

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Terminal Half-life (t½λz) for Verinurad, M1, M8, Allopurinol, and Oxypurinol

Assessment of the PK of verinurad and its metabolites (M1 and M8) and allopurinol and its metabolite (oxypurinol) in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionHour (Mean)
VerinuradM1M8AllopurinolOxypurinol
Treatment A14.9214.3016.891.02014.27
Treatment B13.3312.6513.961.01213.41

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Time Delay Between Drug Administration and the First Observed Concentration in Plasma (Tlag) for Verinurad, M1, M8, Allopurinol, and Oxypurinol

Assessment of the PK of verinurad and its metabolites (M1 and M8) and allopurinol and its metabolite (oxypurinol) in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionHour (Median)
VerinuradM1M8AllopurinolOxypurinol
Treatment A0.500.500.500.000.00
Treatment B0.000.000.000.000.00

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Baseline-corrected and Placebo-corrected QTcF Interval (ΔΔQTcF Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (QTcF). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-1.2-3.4-3.7-4.1-2.8-3.6-3.7-6.1-5.4-5.2-4.8-4.4-6.4
Treatment B-0.0-0.9-0.1-2.1-2.2-0.9-0.3-1.3-3.0-3.40.3-2.2-2.1

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Time of Last Quantifiable Plasma Concentration (Tlast) for Verinurad, M1, M8, Allopurinol, and Oxypurinol

Assessment of the PK of verinurad and its metabolites (M1 and M8) and allopurinol and its metabolite (oxypurinol) in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionHour (Median)
VerinuradM1M8AllopurinolOxypurinol
Treatment A48.0548.0548.058.0048.05
Treatment B48.0748.0748.077.0348.07

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Baseline-corrected QTcF Interval (ΔQTcF Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (QTcF). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-1.7-0.4-1.00.50.7-0.6-6.3-10.0-12.10.2-4.8-7.6-5.8
Treatment B-0.32.32.72.51.22.3-2.5-5.7-10.02.20.2-6.1-2.0
Treatment C-0.53.12.94.63.32.7-2.5-4.0-7.05.30.0-3.70.3

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Area Under Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC) for Verinurad, M1, M8, Allopurinol, and Oxypurinol

Assessment of the pharmacokinetic (PK) of verinurad and its metabolites (M1 and M8) and allopurinol and its metabolite (oxypurinol) in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
Interventionh*ng/mL (Geometric Mean)
VerinuradM1M8AllopurinolOxypurinol
Treatment A393.8413.7447.24501151100
Treatment B918.7904.8895.04617145000

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Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC[0-t]) for Verinurad, M1, M8, Allopurinol, and Oxypurinol

Assessment of the PK of verinurad and its metabolites (M1 and M8) and allopurinol and its metabolite (oxypurinol) in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
Interventionh*ng/mL (Geometric Mean)
VerinuradM1M8AllopurinolOxypurinol
Treatment A360.2383.2394.54408136000
Treatment B880.4865.4847.84524131400

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Baseline-corrected and Placebo-adjusted Heart Rate (ΔΔHR)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on HR. (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,
Interventionbpm (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-0.4-0.9-1.6-1.3-1.50.50.1-1.21.0-2.1-0.9-0.5-0.4
Treatment B-1.4-1.1-0.7-1.8-2.2-1.4-0.3-1.6-2.0-1.40.70.5-1.1

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Baseline-corrected and Placebo-adjusted PR Interval (ΔΔPR Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (PR). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-0.50.3-0.7-1.31.7-0.30.1-1.7-0.1-0.0-0.03.10.2
Treatment B0.0-0.30.5-1.70.40.2-0.30.40.20.30.52.80.9

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Baseline-corrected and Placebo-adjusted RR Interval (ΔΔRR Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (RR). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A6.722.238.926.925.1-3.44.621.0-12.836.515.15.76.5
Treatment B20.723.313.026.935.118.817.819.725.922.1-6.8-7.114.8

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Baseline-corrected and Placebo-corrected QRS Interval (ΔΔQRS Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (QRS). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-0.4-0.9-0.8-0.4-0.2-0.4-0.4-0.5-1.00.0-0.10.1-0.2
Treatment B-0.7-1.1-0.8-1.2-0.4-0.7-0.8-0.6-0.9-0.6-0.3-0.00.0

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Baseline-corrected and Placebo-corrected QT Interval (ΔΔQT Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (QT). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-0.3-0.71.0-0.70.3-4.3-3.4-3.6-7.2-0.8-2.5-3.3-5.7
Treatment B3.02.11.71.72.32.11.41.70.8-0.4-0.5-3.00.3

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Baseline-corrected Heart Rate (ΔHR)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on heart rate (HR). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 hour (h) post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,,
InterventionBeats per minute (bpm) (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-0.8-0.9-2.3-1.9-0.89.36.42.89.60.30.09.14.9
Treatment B-2.0-1.0-1.3-2.5-1.77.25.82.36.50.81.49.63.9
Treatment C-0.50.1-0.6-0.50.68.76.24.18.52.30.99.55.3

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Baseline-corrected PR Interval (ΔPR Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (PR). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-1.3-0.4-1.8-1.20.1-3.5-4.0-4.6-6.1-1.0-1.00.5-0.7
Treatment B-0.9-1.3-0.6-1.7-1.3-3.2-4.5-2.2-5.8-0.9-0.50.80.4
Treatment C-0.8-0.7-0.80.2-1.6-2.7-3.6-2.6-5.6-1.0-1.0-2.4-0.7

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Baseline-corrected QRS Interval (ΔQRS Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (QRS). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A-0.5-0.7-0.50.0-0.61.3-0.3-1.2-2.6-0.5-1.1-0.6-1.0
Treatment B-0.6-0.9-0.5-0.8-0.81.2-0.6-1.3-2.5-0.9-1.3-0.8-0.7
Treatment C0.00.10.30.3-0.41.70.1-0.7-1.7-0.4-0.9-0.7-0.7

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Baseline-corrected QT Interval (ΔQT Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (QT). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,,
Interventionmsec (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A0.21.54.85.02.1-19.9-19.5-16.0-31.1-0.7-4.9-24.8-16.0
Treatment B3.84.55.47.34.5-12.7-14.1-11.0-22.90.3-2.7-24.1-10.0
Treatment C0.42.13.75.31.8-15.6-15.9-12.7-23.90.3-2.5-21.6-10.7

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Baseline-corrected RR Interval (ΔRR Interval)

Investigation of the effect of verinurad given either as a 24 mg ER8 formulation (clinical exposure) or a 40 mg IR formulation (exposure needed to waive positive control as per question 5.1 of ICH E14 Q&A), both in combination with allopurinol 300 mg, on additional dECG variable (RR). (NCT04256629)
Timeframe: Baseline; Day 1: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8 and 12 h post-dose; Day 2: 24 and 36 h post-dose; Day 3: 48 h post-dose

,,
InterventionMilli second (msec) (Mean)
Day 1/ 0.5 hDay 1/ 1 hDay 1/ 1.5 hDay 1/ 2 hDay 1/ 3 hDay 1/ 4 hDay 1/ 5 hDay 1/ 6 hDay 1/ 8 hDay 1/ 12 hDay 2/ 24 hDay 2/ 36 hDay 3/ 48 h
Treatment A13.614.847.135.611.3-139.7-98.8-45.4-143.9-5.0-1.8-129.2-76.0
Treatment B28.215.820.336.524.4-111.7-82.6-44.6-100.6-16.3-20.9-134.1-63.2
Treatment C6.7-8.36.46.9-12.2-133.8-101.9-66.7-128.7-39.9-17.4-132.0-81.3

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Maximum Observed Plasma Concentration (Cmax) for Verinurad, M1, M8, Allopurinol, and Oxypurinol

Assessment of the PK of verinurad and its metabolites (M1 and M8) and allopurinol and its metabolite (oxypurinol) in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
Interventionng/mL (Geometric Mean)
VerinuradM1M8AllopurinolOxypurinol
Treatment A56.5754.9254.8016107591
Treatment B459.7364.4297.817807528

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Mean Residence Time of the Unchanged Drug in the Systemic Circulation From Zero to Infinity (MRT) for Verinurad and Oxypurinol

Assessment of the PK of verinurad and allopurinol in healthy participants. (NCT04256629)
Timeframe: Day 1: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, and 12 hours post-dose; Day 2: 24 and 36 hours post-dose; Day 3: 48 hours post-dose

,
InterventionHour (Geometric Mean)
VerinuradAllopurinol
Treatment A16.472.517
Treatment B9.3202.383

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Change From Baseline at Week 32 in Peak V02 Consumption in Verinurad + Allopurinol Compared to Placebo (ANCOVA Model)

"Mean change from baseline in peak VO2 at Week 32 between the treatment groups was compared using change from baseline (i.e., week 32 value - baseline value) as the dependent variable, treatment as the independent variable and baseline peak VO2 included as covariate.~H0: Difference in mean change from baseline in peak VO2 (verinurad + allopurinol vs placebo) = 0 Ha: Difference in mean change from baseline in peak VO2 (verinurad + allopurinol vs placebo) ≠ 0~A hierarchical test sequence was used for the confirmatory analysis of the primary and secondary objectives in order to address the issue of multiple testing and control the Type I error rate at an overall two-sided 0.05 level.~Since this was the first test in the hierarchical test sequence and endpoint was not rejected at a two-sided 0.05 level, the testing sequence did not continue." (NCT04327024)
Timeframe: From baseline to Week 32

InterventionmL/kg/min (Least Squares Mean)
Verinurad + Allopurinol0.27
Placebo0.37

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Change From Baseline at Week 32 in KCCQ-TSS in Verinurad+ Allopurinol Compared to Placebo (MMRM)

"The Kansas City Cardiomyopathy Questionnaire (KCCQ) is a 23-item assessment that measures the patient's perception of their health status, which includes heart failure-related symptoms (frequency, burden, recent change), impact on physical and social function, self-efficacy and knowledge, and how the patient's heart failure affects their quality of life. The Total Symptom Score (TSS) averages the frequency domain and the symptom burden domain subscales, which each range from 0 to 100. The TSS ranges from 0-100 (higher scores = better health status).~Mean change from baseline in KCCQ-TSS at Week 32 between the treatment groups was compared using MMRM analysis, with change from baseline (i.e., week 32 value - baseline value) as the dependent variable, treatment as the independent variable and visit, visit by treatment, and baseline KCCQ-TSS included as covariates.~The number analyzed at each timepoint represents the number of subjects with data at each visit." (NCT04327024)
Timeframe: From baseline to Week 22 and Week 32

,
InterventionScores on a scale (Least Squares Mean)
Week 22Week 32
Placebo3.551.16
Verinurad + Allopurinol0.504.31

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Change From Baseline at Week 32 in KCCQ-TSS in Verinurad+ Allopurinol Compared to Allopurinol Monotherapy (MMRM)

"The Kansas City Cardiomyopathy Questionnaire (KCCQ) is a 23-item assessment that measures the patient's perception of their health status, which includes heart failure-related symptoms (frequency, burden, recent change), impact on physical and social function, self-efficacy and knowledge, and how the patient's heart failure affects their quality of life. The Total Symptom Score (TSS) averages the frequency domain and the symptom burden domain subscales, which each range from 0 to 100. The TSS ranges from 0-100 (higher scores = better health status).~Mean change from baseline in KCCQ-TSS at Week 32 between the treatment groups was compared using MMRM analysis, with change from baseline (i.e., week 32 value - baseline value) as the dependent variable, treatment as the independent variable and visit, visit by treatment, and baseline KCCQ-TSS included as covariates.~The number analyzed at each timepoint represents the number of subjects with data at each visit." (NCT04327024)
Timeframe: From baseline to Week 22 and Week 32

,
InterventionScores on a scale (Least Squares Mean)
Week 22Week 32
Allopurinol Monotherapy2.854.45
Verinurad + Allopurinol0.504.31

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Change From Baseline at Week 32 in Peak V02 Consumption in Verinurad+ Allopurinol Compared to Allopurinol Monotherapy (ANCOVA Model)

"Mean change from baseline in peak VO2 at Week 32 between the treatment groups was compared using change from baseline (i.e., week 32 value - baseline value) as the dependent variable, treatment as the independent variable and baseline peak VO2 included as covariate.~H0: Difference in mean change from baseline in peak VO2 (verinurad + allopurinol vs allopurinol) = 0 Ha: Difference in mean change from baseline in peak VO2 (verinurad + allopurinol vs allopurinol) ≠ 0~A hierarchical test sequence was used for the confirmatory analysis of the primary and secondary objectives in order to address the issue of multiple testing and control the Type I error rate at an overall two-sided 0.05 level." (NCT04327024)
Timeframe: From baseline to Week 32

InterventionmL/Kg/min (Least Squares Mean)
Verinurad + Allopurinol0.27
Allopurinol Monotherapy-0.17

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Area Under Plasma Concentration-time Curve From Zero to 24 Hours Post-dose AUC(0-24) of Verinurad, M1, M8, Allopurinol and Oxypurinol

AUC(0-24) of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol62.0286.2379.803982100700
Period 2: Verinurad + Allopurinol + Cyclosporine192.2314.438.02391495080
Period 3: Verinurad + Allopurinol + Rifampicin118.4242.948.81416398460

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Geometric Mean Ratio of Area Under Plasma Concentration-time Curve From Time Zero to Infinity (AUCinf) for Verinurad

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad. Verinurad AUCinf ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

Interventionh*ng/mL (Geometric Mean)
Period 1: Verinurad + Allopurinol90.25
Period 2: Verinurad + Allopurinol + Cyclosporine215.1
Period 3: Verinurad + Allopurinol + Rifampicin138.0

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Geometric Mean Ratio of Area Under the Plasma Concentration-time Curve From Zero to Time of Last Quantifiable Concentration (AUClast) for Verinurad

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad. Verinurad AUClast ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

Interventionh*ng/mL (Geometric Mean)
Period 1: Verinurad + Allopurinol79.67
Period 2: Verinurad + Allopurinol + Cyclosporine208.6
Period 3: Verinurad + Allopurinol + Rifampicin133.4

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Geometric Mean Ratio of AUClast for Allopurinol and Oxypurinol

Evaluation of a single dose of cyclosporine or rifampicin on the PK of allopurinol and oxypurinol. AUClast ratio of geometric means of test geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol3889183600
Period 2: Verinurad + Allopurinol + Cyclosporine3821170600
Period 3: Verinurad + Allopurinol + Rifampicin4080182100

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Geometric Mean Ratio of AUCinf for Verinurad Metabolites: M1 and M8

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad metabolites M1 and M8. AUCinf ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
M1M8
Period 1: Verinurad + Allopurinol119.5110.3
Period 2: Verinurad + Allopurinol + Cyclosporine348.760.98
Period 3: Verinurad + Allopurinol + Rifampicin264.977.35

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Geometric Mean Ratio of AUCinf for Allopurinol and Oxypurinol

Evaluation of a single dose of cyclosporine or rifampicin on the PK of allopurinol and oxypurinol. AUCinf ratio of geometric means of test geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol3982196500
Period 2: Verinurad + Allopurinol + Cyclosporine3914181900
Period 3: Verinurad + Allopurinol + Rifampicin4163195500

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Number of Participants With Adverse Events (AEs) and Serious AEs (SAEs)

Assessment the safety and tolerability of verinurad and allopurinol in combination with cyclosporine or rifampicin (NCT04532918)
Timeframe: From screening (Day -28 to -2) until Follow-up or Early Termination (7-14 days after last verinurad dose)

,,
InterventionParticipants (Count of Participants)
Any AEAny AE with outcome = deathAny SAEAny AE leading to discontinuation of study drugAny AE leading to withdrawal from study
Period 1: Verinurad + Allopurinol20000
Period 2: Verinurad + Allopurinol + Cyclosporine100011
Period 3: Verinurad + Allopurinol + Rifampicin30100

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Metabolite:Parent (MP) AUClast Ratios for M1 and M8: Verinurad

Metabolite:parent (MP) AUClast ratios for M1 and M8: verinurad when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionRatio (Geometric Mean)
M1:verinuradM8:verinurad
Period 1: Verinurad + Allopurinol1.4001.278
Period 2: Verinurad + Allopurinol + Cyclosporine1.6390.2491
Period 3: Verinurad + Allopurinol + Rifampicin1.9550.5491

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Metabolite:Parent (MP) AUCinf Ratios for M1 and M8: Verinurad

Metabolite:parent (MP) AUCinf ratios for M1 and M8: verinurad when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionRatio (Geometric Mean)
M1:verinuradM8:verinurad
Period 1: Verinurad + Allopurinol1.3241.222
Period 2: Verinurad + Allopurinol + Cyclosporine1.6210.2834
Period 3: Verinurad + Allopurinol + Rifampicin1.9190.5604

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Metabolite:Parent (MP) Cmax Ratios for M1 and M8: Verinurad

Metabolite:parent (MP) Cmax ratios for M1 and M8: verinurad when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionRatio (Geometric Mean)
M1: verinuradM8: verinurad
Period 1: Verinurad + Allopurinol1.2961.171
Period 2: Verinurad + Allopurinol + Cyclosporine1.3880.1130
Period 3: Verinurad + Allopurinol + Rifampicin1.8660.2300

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Mean Residence Time of the Unchanged Drug in the Systemic Circulation (MRTinf) for Verinurad and Allopurinol

MRTinf for verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionHours (Geometric Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol21.282.316
Period 2: Verinurad + Allopurinol + Cyclosporine11.052.713
Period 3: Verinurad + Allopurinol + Rifampicin12.602.496

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Time to Reach Peak or Maximum Plasma Concentration (Tmax) for Verinurad, M1, M8, Allopurinol and Oxypurinol

tmax of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionHours (Median)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol4.034.024.520.504.00
Period 2: Verinurad + Allopurinol + Cyclosporine5.005.988.001.004.00
Period 3: Verinurad + Allopurinol + Rifampicin4.004.005.001.003.00

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Apparent Total Body Clearance of Drug From Plasma After Extravascular Administration (CL/F) for Verinurad and Allopurinol

CL/F for verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionLiter/Hours (Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol92.3077.12
Period 2: Verinurad + Allopurinol + Cyclosporine36.3278.09
Period 3: Verinurad + Allopurinol + Rifampicin55.9973.29

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Geometric Mean Ratio of Maximum Observed Plasma Peak Concentration (Cmax) for Verinurad

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad. Verinurad Cmax ratio of geometric mean of test treatment (verinurad+allopurinol with [cyclosporine or rifampicin], relative to reference treatment (verinurad+allopurinol alone) in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

Interventionng/mL (Geometric Mean)
Period 1: Verinurad + Allopurinol13.30
Period 2: Verinurad + Allopurinol + Cyclosporine33.96
Period 3: Verinurad + Allopurinol + Rifampicin26.09

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Geometric Mean Ratio of AUClast for Verinurad Metabolites: M1 and M8

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad metabolites M1 and M8. AUClast ratio of geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
M1M8
Period 1: Verinurad + Allopurinol111.6101.8
Period 2: Verinurad + Allopurinol + Cyclosporine341.951.95
Period 3: Verinurad + Allopurinol + Rifampicin260.673.23

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Geometric Mean Ratio of Cmax for Verinurad Metabolites: M1 and M8

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad metabolites M1 and M8. Cmax ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionng/mL (Geometric Mean)
M1M8
Period 1: Verinurad + Allopurinol17.2415.57
Period 2: Verinurad + Allopurinol + Cyclosporine47.143.839
Period 3: Verinurad + Allopurinol + Rifampicin48.706.002

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Geometric Mean Ratio of Cmax for Allopurinol and Oxypurinol

Evaluation of a single dose of cyclosporine or rifampicin on the PK of allopurinol and oxypurinol. Cmax ratio of geometric means of test geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionng/mL (Geometric Mean)
AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol19476064
Period 2: Verinurad + Allopurinol + Cyclosporine14575876
Period 3: Verinurad + Allopurinol + Rifampicin15976051

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Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration Time Curve (t½λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol

t½λz of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionHours (Mean)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol20.3118.0418.251.21023.19
Period 2: Verinurad + Allopurinol + Cyclosporine14.7313.0521.901.26122.36
Period 3: Verinurad + Allopurinol + Rifampicin15.0312.5214.891.17023.76

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Terminal Elimination Rate Constant (λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol

λz of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Intervention1/Hours (Geometric Mean)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol0.038420.042930.041630.57700.03086
Period 2: Verinurad + Allopurinol + Cyclosporine0.061010.065180.044970.56160.03169
Period 3: Verinurad + Allopurinol + Rifampicin0.055570.064170.051330.59500.02990

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Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Based on the Terminal Phase) (Vz/F) of Verinurad and Allopurinol

Vz/F of verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionLiters (Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol2455133.5
Period 2: Verinurad + Allopurinol + Cyclosporine721.8137.9
Period 3: Verinurad + Allopurinol + Rifampicin1153122.6

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Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Vss/F) of Verinurad and Allopurinol

Vss/F of verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionLiters (Geometric Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol1768174.5
Period 2: Verinurad + Allopurinol + Cyclosporine385.2208.0
Period 3: Verinurad + Allopurinol + Rifampicin685.0179.9

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Vz/F: Apparent Volume of Distribution During Terminal Phase After Extravascular Administration

The Vz/F of verinurad and allopurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
InterventionLiter (Geometric Mean)
VerinuradAllopurinol
Treatment 11495112.4
Treatment 21256114.2
Treatment 31184206.7
Treatment 41723114.1
Treatment 51356NA

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Vss/F: Apparent Volume of Distribution at Steady State Following Extravascular Administration

The Vss/F of verinurad and allopurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
InterventionLiter (Geometric Mean)
VerinuradAllopurinol
Treatment 11264175.8
Treatment 2939.3204.3
Treatment 31134390.7
Treatment 41578206.1
Treatment 51018NA

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MRTinf: Mean Residence Time of the Unchanged Drug in the Systemic Circulation From Zero to Infinity

The MRTinf of verinurad and allopurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionhour (Geometric Mean)
VerinuradAllopurinol
Treatment 118.992.629
Treatment 215.282.950
Treatment 318.914.626
Treatment 418.192.827
Treatment 515.94NA

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Cmax: Maximum Observed Plasma Drug Concentration

The Cmax of verinurad, allopurinol and oxypurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionnanogram/millilitre (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 126.6215266376
Treatment 234.9514716066
Treatment 320.1810795269
Treatment 413.8616275709
Treatment 535.35NANA

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Tmax: Time to Reach Maximum Observed Plasma Concentration Following Drug Administration

The tmax of verinurad, allopurinol and oxypurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionhour (Median)
VerinuradAllopurinolOxypurinol
Treatment 15.001.504.00
Treatment 24.001.504.00
Treatment 39.983.006.02
Treatment 45.031.504.00
Treatment 54.00NANA

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Number of Subjects With Adverse Events (AEs) and Serious Adverse Events

The safety of single doses of verinurad and allopurinol were assessed (NCT04550234)
Timeframe: From screening (Day -28 to -3) until follow-up visit (7 to 14 days post final dose) (approximately 52 to 59 days)

,,,,
InterventionParticipants (Count of Participants)
Any AEAny SAEAny SAE with outcome of deathAny AE leading to discontinuation of IPAny possibly related AEAny possibly related SAE
Treatment 1800030
Treatment 2200010
Treatment 3200010
Treatment 4600030
Treatment 5200010

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Tlag: Time Delay Between Drug Administration and First Observed Concentration in Plasma

The tlag of verinurad, allopurinol and oxypurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionhour (Median)
VerinuradAllopurinolOxypurinol
Treatment 10.000.000.00
Treatment 20.000.000.00
Treatment 31.001.020.00
Treatment 41.020.000.00
Treatment 50.00NANA

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CL/F: Apparent Total Body Clearance of Drug Clearance of Drug From Plasma After Extravascular Administration

The CL/F of verinurad and allopurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
InterventionLiter/hour (Geometric Mean)
VerinuradAllopurinol
Treatment 166.5466.88
Treatment 261.4669.25
Treatment 359.9784.47
Treatment 486.7372.93
Treatment 563.90NA

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AUClast: Area Under Plasma Concentration-time Curve From Zero to the Last Quantifiable Concentration in Fasted Condition

The AUClast of verinurad, allopurinol and oxypurinol were assessed in fasted condition as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,
Interventionhour*nanogram/milliliter (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 1169.34407157100
Treatment 2185.04251153100

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AUCinf: Area Under Plasma Concentration-time Curve From 0 to Infinity in Fasted Condition

The AUCinf of verinurad, allopurinol and oxypurinol were assessed in fasted state as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,
Interventionhour*nanogram/millilitre (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 1180.44486170100
Treatment 2195.24332167900

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AUClast: Area Under Plasma Concentration-time Curve From Zero to the Last Quantifiable Concentration

The AUClast of verinurad, allopurinol and oxypurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionhour*nanogram/milliliter (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 1169.34407157100
Treatment 2185.04251153100
Treatment 3190.33512139200
Treatment 4129.94030140100
Treatment 5176.4NANA

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tEmax, CB: Time of Maximum Percentage CB Change From Baseline (CB)

The tEmax, CB in serum uric acid (sUA) concentration (time-matched, Day -1) was assessed as PD parameter. (NCT04550234)
Timeframe: Day -1, Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

Interventionhour (Median)
Treatment 18.00
Treatment 26.00
Treatment 312.00
Treatment 412.00
Treatment 512.00

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λz: Terminal Elimination Rate Constant

The λz of verinurad, allopurinol and oxypurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionper hour (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 10.044370.59510.03653
Treatment 20.048760.60650.03309
Treatment 30.049570.40750.03512
Treatment 40.050630.63840.03425
Treatment 50.04651NANA

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t½λz: Half-life Associated With Terminal Slope (λz) of Semi-logarithmic Concentration-time Curve

The t½λz of verinurad, allopurinol and oxypurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionhour (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 115.571.16419.06
Treatment 214.171.14220.45
Treatment 313.691.69620.14
Treatment 413.771.08520.21
Treatment 514.71NANA

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Cmax: Maximum Observed Plasma Drug Concentration in Fasted State

The Cmax of verinurad, allopurinol and oxypurinol were assessed in fasted state as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,
Interventionnanogram/millilitre (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 126.6215266376
Treatment 234.9514716066

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Emax, CB: Maximum Percentage Change From Baseline (CB)

The Emax, CB in serum uric acid (sUA) concentration (time-matched, Day -1) was assessed as PD parameter. (NCT04550234)
Timeframe: Day -1, Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

Interventionpercentage (%) (Mean)
Treatment 1-50.44
Treatment 2-53.84
Treatment 3-56.63
Treatment 4-54.43
Treatment 5-38.15

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AUCinf: Area Under Plasma Concentration-time Curve From 0 to Infinity

The AUCinf of verinurad, allopurinol and oxypurinol were assessed as PK parameters (NCT04550234)
Timeframe: Day 1, Day 2, Day 3 and Day 4 of each Treatment Period

,,,,
Interventionhour*nanogram/millilitre (Geometric Mean)
VerinuradAllopurinolOxypurinol
Treatment 1180.44486170100
Treatment 2195.24332167900
Treatment 3200.13551153200
Treatment 4138.44114153300
Treatment 5187.8NANA

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