lesinurad profile

lesinurad: a uric acid reabsorption inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

lesinurad : A member of the class of triazoles that is [(3-bromo-1,2,4-triazol-5-yl)sulfanyl]acetic acid substituted at position 1 of the triazole ring by a 4-cyclopropylnaphthalen-1-yl group. Used for treatment of gout. [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]

ID Source	ID
PubMed CID	53465279
CHEMBL ID	2105720
CHEBI ID	90929
SCHEMBL ID	842962
MeSH ID	M000600400

Synonym
878672-00-5
zurampic (tn)
lesinurad (usan/inn)
D09921
rdea594
acetic acid, 2-((5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4h-1,2,4-triazol-3-yl)thio)-
zurampic
lesinurad [usan:inn]
unii-09erp08i3w
rdea 594
lesinurad
09erp08i3w ,
CHEMBL2105720
rdea-594
S4640 ,
HY-15258
CS-1389
duzallo component lesinurad
lesinurad [mi]
lesinurad [usan]
2-((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3- yl)sulfanyl)acetic acid
lesinurad [inn]
lesinurad [orange book]
lesinurad [who-dd]
2-[[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-1,2,4-triazol-3-yl]sulfanyl]acetic acid
gtpl7673
SCHEMBL842962
2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-ylthio)acetic acid
2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4h-1,2,4-triazol-3-ylthio)acetic acid
(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4h-1,2,4-triazol-3-ylthio)acetic acid
FGQFOYHRJSUHMR-UHFFFAOYSA-N
{[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-yl]sulfanyl}acetic acid
CHEBI:90929 ,
us10093631, compound lesinurad
bdbm37953
2-((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-yl)thio)acetic acid
AC-29310
2-[[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-yl]thio]acetic acid
EX-A1289
2-{[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-yl]sulfanyl}acetic acid
AKOS027327368
mfcd22572730
lesinurad, >=98% (hplc)
lesinurad (rdea594)
lesinurad (rdea594
DB11560
rdea 594;rdea-594;rdea594
BCP06435
Q21820633
2-[[5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4h-1,2,4-triazol-3-yl]thio]-acetic acid
unii-q59cat99rs
unii-73wy698hz7
SB16705
HMS3874M03
lesinurad free acid
878672-00-5 (free acid)
AMY27876
CCG-268685
FT-0776044
2-(((4s)-5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4h-1,2,4-triazol-3-yl)thio)acetic acid
Q59CAT99RS ,
acetic acid, 2-(((4r)-5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4h-1,2,4-triazol-3-yl)thio)-
lesinurad, (4s)-
lesinurad, (4r)-
(-)-lesinurad
1890222-25-9
lesinurad, (+)-
lesinurad, (-)-
2-(((4r)-5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4h-1,2,4-triazol-3-yl)thio)acetic acid
acetic acid, 2-(((4s)-5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4h-1,2,4-triazol-3-yl)thio)-
(+)-lesinurad
1890222-26-0
73WY698HZ7 ,
rdea 594;sodium 2-((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-yl)thio)acetate
A857828
AS-56014
DTXSID201026091
EN300-7399813
2-{[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-\\ 3-yl]sulfanyl}acetic acid
lesinuradum
((5-bromo-4-(4-cyclopropyl-1-naphthyl)-4h-1,2,4-triazol-3-yl)sulfanyl)acetic acid
m04ab05
2-((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-yl)sulfanyl)acetic acid
((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-yl)sulfanyl)acetic acid

Research Excerpts

Overview

Lesinurad is a novel selective uric acid reabsorption inhibitor prescribed for the treatment of chronic gout. It is approved at 200 mg daily for use with a xanthine oxidase inhibitor (XOI) to treat hyperuricaemia in gout patients failing to achieve target serum urate.

Excerpt	Reference	Relevance
"Lesinurad is a uricosuric agent for the treatment of hyperuricemia associated with gout, which was found lacking in efficacy and safety. "	( Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability. Ji, J; Liang, R; Liao, H; Liu, X; Pang, J; Shi, X; Tao, Y; Wu, T; Zhan, P; Zhang, J; Zhang, Z; Zhao, F; Zhao, T, 2022)	2.16
"Lesinurad is a novel selective uric acid reabsorption inhibitor prescribed for the treatment of chronic gout."	( Spectrophotometric quantitative analysis of lesinurad using extractive acid dye reaction based on greener selective computational approach. Abdelazim, AH; Ramzy, S, 2022)	1.7
"Lesinurad is a URAT1 inhibitor that selectively inhibits urate rebsorption at the proximal renal tubule."	( Lesinurad for the treatment of hyperuricaemia in people with gout. Dalbeth, N; Robinson, PC, 2017)	2.62
"Lesinurad is a novel selective uric acid reabsorption inhibitor which has been newly approved for the treatment of the chronic gout. "	( Validated Stability Indicating High Performance Liquid Chromatographic Determination of Lesinurad. Abdelazim, AH; Attia, KAM; El-Abasawi, NM; El-Olemy, A, 2018)	2.15
"Lesinurad (LESU) is a selective urate reabsorption inhibitor approved at 200 mg daily for use with a xanthine oxidase inhibitor (XOI) to treat hyperuricaemia in gout patients failing to achieve target serum urate on XOI. "	( 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)	2.2
"Lesinurad is a selective uric acid reabsorption inhibitor approved for use in combination with xanthine oxidase inhibitors for the treatment of hyperuricemia associated with gout. "	( Lesinurad: Evaluation of Pharmacokinetic and Pharmacodynamic Interactions With Warfarin in Healthy Volunteers. Gillen, M; Kerr, B; Lee, CA; Shen, Z; Valdez, S; Wallach, K; Wilson, DM, 2019)	3.4
"Lesinurad is a selective uric acid reabsorption inhibitor under investigation for the treatment of gout. "	( Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males. Hingorani, V; Kerr, B; Manhard, K; Quart, B; Rowlings, C; Shen, Z; Storgard, C; Yeh, LT, 2015)	2.11
"Lesinurad (ZURAMPIC(®)) is an oral urate-anion exchanger transporter 1 (URAT1) inhibitor developed by Ardea Biosciences (a subsidiary of AstraZeneca) for the treatment of hyperuricaemia associated with gout. "	( Lesinurad: First Global Approval. Hoy, SM, 2016)	3.32
"Lesinurad is a selective uric acid reabsorption inhibitor (SURI) under investigation for the treatment of gout. "	( In Vitro and In Vivo Interaction Studies Between Lesinurad, a Selective Urate Reabsorption Inhibitor, and Major Liver or Kidney Transporters. Gillen, M; Kerr, B; Shen, Z; Wallach, K; Yeh, LT; Zhu, N, 2016)	2.13
"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)	3.34
"Lesinurad is a selective uric acid reabsorption inhibitor approved in the United States and Europe for treatment of gout in combination with a xanthine oxidase inhibitor. "	( Supratherapeutic dose evaluation and effect of lesinurad on cardiac repolarization: a thorough QT/QTc study. Gillen, M; Harmon, E; Kerr, B; Lee, CA; Nguyen, M; Shen, Z; Tieu, K; Wilson, DM, 2016)	2.13
"Lesinurad is a selective uric acid reabsorption inhibitor approved for the treatment of gout in combination with a xanthine oxidase inhibitor (XOI) in patients who have not achieved target serum uric acid (sUA) levels with an XOI alone. "	( Effects of renal function on pharmacokinetics and pharmacodynamics of lesinurad in adult volunteers. Gillen, M; Kerr, B; Lee, CA; Shen, Z; Valdez, S; Zhou, D, 2016)	2.11
"Lesinurad is a selective uric acid reabsorption inhibitor approved for the treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors. "	( Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and CYP Enzyme Substrates Sildenafil, Amlodipine, Tolbutamide, and Repaglinide. Gillen, M; Kerr, B; Lee, C; Shen, Z; Valdez, S; Wilson, D; Yang, C, 2017)	2.15
"Lesinurad is a novel selective uric acid reabsorption inhibitor approved for treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors (XOIs). "	( Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and Commonly Used Drugs for Gout Treatment. Bucci, G; Gillen, M; Kerr, B; Lee, C; Shen, Z; Tieu, K; Wilson, D, 2017)	2.15

Effects

Lesinurad has a novel mechanism of action and is safe and effective. It also has a favorable selectivity and safety profile, consistent with an important role in sUA-lowering therapy for patients with gout.

Excerpt	Reference	Relevance
"Lesinurad has a novel mechanism of action and is safe and effective for the treatment of chronic gout. "	( Lesinurad: A Novel Agent for Management of Chronic Gout. Cano, AJ; Fente, G; Fenton, SN; Haber, SL; Vu, K; Walker, EP; Weaver, BM, 2018)	3.37
"Lesinurad also has a favorable selectivity and safety profile, consistent with an important role in sUA-lowering therapy for patients with gout."	( Lesinurad, a novel, oral compound for gout, acts to decrease serum uric acid through inhibition of urate transporters in the kidney. Girardet, JL; Hagerty, DT; Hyndman, D; Iverson, C; Liu, S; Manhard, K; Miner, JN; Nanavati, P; Quart, B; Shen, Z; Tan, PK; Terkeltaub, R; Yeh, LT, 2016)	2.6

Treatment

Treatment with lesinurad (200 mg and 400 mg) plus febuxostat reduced the total target tophi area as compared with feboxostat alone (50.1% and 52.9%) Study was terminated prematurely.

Excerpt	Reference	Relevance
"Treatment with lesinurad (200 mg and 400 mg) plus febuxostat reduced the total target tophi area as compared with febuxostat alone (50.1% and 52.9% versus 28.3%, respectively; P < 0.05)."	( Lesinurad, a Selective Uric Acid Reabsorption Inhibitor, in Combination With Febuxostat in Patients With Tophaceous Gout: Findings of a Phase III Clinical Trial. Adler, S; Baumgartner, S; Bhakta, N; Dalbeth, N; Fung, M; Jones, G; Khanna, D; Kopicko, J; Perez-Ruiz, F; Storgard, C; Terkeltaub, R, 2017)	2.24
"Treatment with lesinurad in combination with febuxostat demonstrated superior lowering of serum UA levels as compared with febuxostat alone, with clinically relevant added effects on tophi and an acceptable safety profile with lesinurad 200 mg in patients with tophaceous gout warranting additional therapy."	( Lesinurad, a Selective Uric Acid Reabsorption Inhibitor, in Combination With Febuxostat in Patients With Tophaceous Gout: Findings of a Phase III Clinical Trial. Adler, S; Baumgartner, S; Bhakta, N; Dalbeth, N; Fung, M; Jones, G; Khanna, D; Kopicko, J; Perez-Ruiz, F; Storgard, C; Terkeltaub, R, 2017)	2.25
"Treatment with lesinurad 400 mg resulted in rapid and sustained sUA lowering that persisted for up to 18 months before the study was terminated prematurely."	( Lesinurad monotherapy in gout patients intolerant to a xanthine oxidase inhibitor: a 6 month phase 3 clinical trial and extension study. Adler, S; Alten, R; Baumgartner, S; Bhakta, N; Dalbeth, N; Fung, M; Kopicko, J; Saag, K; Storgard, C; Tausche, AK, 2017)	2.24

Toxicity

The frequency of treatment-emergent adverse events (TEAEs) in the XOI group was significantly lower than that in the lesinurad 400 mg + XOi group (OR 0.01). Exposure-adjusted incidence rates of treatment and renal-related TEAEs in the core study were not increased with prolonged lesInurad exposure in the extension study.

Excerpt	Reference	Relevance
" Lesinurad was generally safe and well tolerated."	( Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males. Hingorani, V; Kerr, B; Manhard, K; Quart, B; Rowlings, C; Shen, Z; Storgard, C; Yeh, LT, 2015)	1.58
" 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)	0.75
" 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)	0.75
"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)	0.75
" The secondary outcome was the number of treatment-emergent adverse events (TEAEs)."	( Efficacy and Safety of Lesinurad in Patients with Hyperuricemia Associated with Gout: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Chang, YS; Chang, YT; Lee, CH; Lin, YC; Loh, EW; Tam, KW; Wu, JY; Wu, MY, 2018)	0.79
" However, no studies using combined xanthine oxidase inhibition and uricosuric ULT have focused on clinical outcomes or adverse events (AEs) beyond 12 months of therapy."	( Efficacy and safety during extended treatment of lesinurad in combination with febuxostat in patients with tophaceous gout: CRYSTAL extension study. Baumgartner, S; Dalbeth, N; Fung, M; Jones, G; Khanna, D; Perez-Ruiz, F; Terkeltaub, R, 2019)	0.77
" Exposure-adjusted incidence rates of treatment-emergent adverse events (TEAEs) and renal-related TEAEs in the core study were not increased with prolonged lesinurad exposure in the extension study."	( Efficacy and safety during extended treatment of lesinurad in combination with febuxostat in patients with tophaceous gout: CRYSTAL extension study. Baumgartner, S; Dalbeth, N; Fung, M; Jones, G; Khanna, D; Perez-Ruiz, F; Terkeltaub, R, 2019)	0.97

Pharmacokinetics

Open-label pharmacokinetic studies were performed in volunteers or subjects with hyperuricemia (serum uric acid ≥ 8 mg/dL) The validated lesinurad plasma quantification method was successfully applied for the pharmacokinetics evaluations.

Excerpt	Reference	Relevance
" A relative bioavailability study in healthy males (N=8) indicated a nearly identical pharmacokinetic profile following dosing of tablets or capsules."	( Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males. Hingorani, V; Kerr, B; Manhard, K; Quart, B; Rowlings, C; Shen, Z; Storgard, C; Yeh, LT, 2015)	0.67
" Open-label pharmacokinetic studies were performed in volunteers or subjects with hyperuricemia (serum uric acid ≥ 8 mg/dL) to investigate interactions of lesinurad (with and without concurrent XOIs) with colchicine and 2 nonsteroidal anti-inflammatory drugs: naproxen and indomethacin."	( Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and Commonly Used Drugs for Gout Treatment. Bucci, G; Gillen, M; Kerr, B; Lee, C; Shen, Z; Tieu, K; Wilson, D, 2017)	0.9
" 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)	0.92
" 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)	0.87
" 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)	0.51

Compound-Compound Interactions

Lesinurad is a selective uric acid reabsorption inhibitor used for the treatment of gout in combination with a xanthine oxidase inhibitor.

Excerpt	Reference	Relevance
"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)	2.14
"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)	2.06
" 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)	2.79
"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)	3.32
"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)	3.34
"To investigate the efficacy and safety of lesinurad in combination with febuxostat in a 12-month phase III trial in patients with tophaceous gout."	( Lesinurad, a Selective Uric Acid Reabsorption Inhibitor, in Combination With Febuxostat in Patients With Tophaceous Gout: Findings of a Phase III Clinical Trial. Adler, S; Baumgartner, S; Bhakta, N; Dalbeth, N; Fung, M; Jones, G; Khanna, D; Kopicko, J; Perez-Ruiz, F; Storgard, C; Terkeltaub, R, 2017)	2.16
"Treatment with lesinurad in combination with febuxostat demonstrated superior lowering of serum UA levels as compared with febuxostat alone, with clinically relevant added effects on tophi and an acceptable safety profile with lesinurad 200 mg in patients with tophaceous gout warranting additional therapy."	( Lesinurad, a Selective Uric Acid Reabsorption Inhibitor, in Combination With Febuxostat in Patients With Tophaceous Gout: Findings of a Phase III Clinical Trial. Adler, S; Baumgartner, S; Bhakta, N; Dalbeth, N; Fung, M; Jones, G; Khanna, D; Kopicko, J; Perez-Ruiz, F; Storgard, C; Terkeltaub, R, 2017)	2.25
"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)	1.09
" The aim of this Phase 2a, randomized, open-label study was to investigate the multiple-dose pharmacodynamics, pharmacokinetics and safety of oral verinurad combined with febuxostat vs febuxostat alone and verinurad alone."	( Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study. Gillen, M; Hall, J; Ito, Y; Liu, S; Shen, Z; Shiramoto, M; Yamamoto, A; Yan, X, 2018)	0.48
"Japanese male subjects aged 21-65 years with gout (n = 37) or asymptomatic hyperuricaemia (n = 35) and serum urate (sUA) ⩾8 mg/dl were randomized to febuxostat (10, 20, 40 mg) in combination with verinurad (2."	( Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study. Gillen, M; Hall, J; Ito, Y; Liu, S; Shen, Z; Shiramoto, M; Yamamoto, A; Yan, X, 2018)	0.48
"Verinurad combined with febuxostat decreased sUA dose-dependently while maintaining uric acid excretion similar to baseline."	( Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study. Gillen, M; Hall, J; Ito, Y; Liu, S; Shen, Z; Shiramoto, M; Yamamoto, A; Yan, X, 2018)	0.48
"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)	1.02

Bioavailability

Excerpt	Reference	Relevance
" A relative bioavailability study in healthy males (N=8) indicated a nearly identical pharmacokinetic profile following dosing of tablets or capsules."	( Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males. Hingorani, V; Kerr, B; Manhard, K; Quart, B; Rowlings, C; Shen, Z; Storgard, C; Yeh, LT, 2015)	0.67
"The objectives of this study were to determine the absolute bioavailability of lesinurad and to characterized its disposition in humans."	( Metabolism and disposition of lesinurad, a uric acid reabsorption inhibitor, in humans. Gillen, M; Hall, J; Kerr, BM; Lee, CA; Shah, V; Shen, Z; Tieu, K; Wilson, DM; Yang, C, 2019)	1.03

Dosage Studied

Lesinurad is an effective urate-lowering drug that has a generally acceptable safety profile when used at 200mg daily dosing in combination with a xanthine oxidase inhibitor.

Excerpt	Relevance	Reference
" A relative bioavailability study in healthy males (N=8) indicated a nearly identical pharmacokinetic profile following dosing of tablets or capsules."	( Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males. Hingorani, V; Kerr, B; Manhard, K; Quart, B; Rowlings, C; Shen, Z; Storgard, C; Yeh, LT, 2015)	0.67
"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)	1.9
"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)	0.48
" Expert opinion: Lesinurad is an effective urate-lowering drug that has a generally acceptable safety profile when used at 200mg daily dosing in combination with a xanthine oxidase inhibitor."	( Lesinurad for the treatment of hyperuricaemia in people with gout. Dalbeth, N; Robinson, PC, 2017)	2.24
" The developed method has been successfully applied for the estimation of lesinurad in its pharmaceutical dosage form and could be used for the routine analysis of the studied drug in the quality control laboratories."	( Validated Stability Indicating High Performance Liquid Chromatographic Determination of Lesinurad. Abdelazim, AH; Attia, KAM; El-Abasawi, NM; El-Olemy, A, 2018)	0.93
" 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)	0.48
" 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)	1.05
"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)	1.1
"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)	1.06
"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)	2.59

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Role	Description
uricosuric drug	A gout suppressant that acts directly on the renal tubule to increase the excretion of uric acid, thus reducing its concentrations in plasma.
[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]

Class	Description
triazoles	An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.
naphthalenes	Any benzenoid aromatic compound having a skeleton composed of two ortho-fused benzene rings.
cyclopropanes	Cyclopropane and its derivatives formed by substitution.
organobromine compound	A compound containing at least one carbon-bromine bond.
aryl sulfide	Any organic sulfide in which the sulfur is attached to at least one aromatic group.
monocarboxylic acid	An oxoacid containing a single carboxy group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 1A2	Homo sapiens (human)	IC50 (µMol)	26.1667	0.0001	1.7740	10.0000	AID1435227
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	45.9333	0.0001	1.7536	10.0000	AID1435225
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	74.9000	0.0000	2.0151	10.0000	AID1435223
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	46.1042	0.0000	2.8005	10.0000	AID1435224; AID1435226; AID1435227; AID1435236
Cytochrome P450 2C19	Homo sapiens (human)	IC50 (µMol)	27.7000	0.0000	2.3983	10.0000	AID1435226
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	30.0000	0.0009	1.9014	10.0000	AID1435222
Solute carrier family 22 member 12	Homo sapiens (human)	IC50 (µMol)	7.4756	0.0260	2.6152	7.3000	AID1435236; AID1559413; AID1575209; AID1575210; AID1649923; AID1676234; AID1901571
Solute carrier family 22 member 11	Homo sapiens (human)	IC50 (µMol)	4.6650	2.0300	4.6650	7.3000	AID1559411; AID1649922
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
steroid catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
porphyrin-containing compound metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
toxin biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
post-embryonic development	Cytochrome P450 1A2	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
regulation of gene expression	Cytochrome P450 1A2	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
dibenzo-p-dioxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lung development	Cytochrome P450 1A2	Homo sapiens (human)
methylation	Cytochrome P450 1A2	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
cellular respiration	Cytochrome P450 1A2	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 1A2	Homo sapiens (human)
cellular response to cadmium ion	Cytochrome P450 1A2	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C19	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
monoatomic ion transport	Solute carrier family 22 member 12	Homo sapiens (human)
response to xenobiotic stimulus	Solute carrier family 22 member 12	Homo sapiens (human)
urate transport	Solute carrier family 22 member 12	Homo sapiens (human)
cellular homeostasis	Solute carrier family 22 member 12	Homo sapiens (human)
cellular response to insulin stimulus	Solute carrier family 22 member 12	Homo sapiens (human)
urate metabolic process	Solute carrier family 22 member 12	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 12	Homo sapiens (human)
renal urate salt excretion	Solute carrier family 22 member 12	Homo sapiens (human)
organic anion transport	Solute carrier family 22 member 12	Homo sapiens (human)
monoatomic ion transport	Solute carrier family 22 member 11	Homo sapiens (human)
inorganic anion transport	Solute carrier family 22 member 11	Homo sapiens (human)
organic anion transport	Solute carrier family 22 member 11	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 11	Homo sapiens (human)
urate metabolic process	Solute carrier family 22 member 11	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
monooxygenase activity	Cytochrome P450 1A2	Homo sapiens (human)
iron ion binding	Cytochrome P450 1A2	Homo sapiens (human)
protein binding	Cytochrome P450 1A2	Homo sapiens (human)
electron transfer activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 1A2	Homo sapiens (human)
enzyme binding	Cytochrome P450 1A2	Homo sapiens (human)
heme binding	Cytochrome P450 1A2	Homo sapiens (human)
demethylase activity	Cytochrome P450 1A2	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 1A2	Homo sapiens (human)
aromatase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Cytochrome P450 1A2	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C19	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxygen binding	Cytochrome P450 2C19	Homo sapiens (human)
enzyme binding	Cytochrome P450 2C19	Homo sapiens (human)
heme binding	Cytochrome P450 2C19	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C19	Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C19	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
urate transmembrane transporter activity	Solute carrier family 22 member 12	Homo sapiens (human)
PDZ domain binding	Solute carrier family 22 member 12	Homo sapiens (human)
solute:inorganic anion antiporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
protein binding	Solute carrier family 22 member 11	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
endoplasmic reticulum membrane	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C19	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C19	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Solute carrier family 22 member 12	Homo sapiens (human)
membrane	Solute carrier family 22 member 12	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 12	Homo sapiens (human)
brush border membrane	Solute carrier family 22 member 12	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 12	Homo sapiens (human)
plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
external side of plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (121)

Assay ID	Title	Year	Journal	Article
AID1901591	Acute toxicity in Kunming mouse assessed as death at 250 mg/kg, IG measured up to 1 week	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435281	Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring parent compound remaining at 250 pmol/ml after 60 mins in presence of NADPH by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435229	Stability of the compound in solid state assessed as racemization after 80 days	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676190	Tmax in male Kunming mouse at 50 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435244	Drug metabolism in ethanol assessed as (+)-Lesinurad formation at 37 degC	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1649923	Inhibition of URAT1 (unknown origin)	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Pharmacological urate-lowering approaches in chronic kidney disease.
AID1676200	Sub-acute toxicity in female Kunming mouse assessed as increase in body weight at 50 mg/kg, po administered once every second day for 14 days	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1676188	Cmax in male Kunming mouse at 50 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435234	Stability in human plasma at 37 degC up to 2 hrs	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435251	Drug metabolism in Sprague-Dawley rat plasma assessed as (-)-Lesinurad formation at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435249	Drug metabolism in Sprague-Dawley rat plasma assessed as (+)-Lesinurad formation at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901599	Subacute toxicity in Kunming mouse assessed as clonic convulsion at 50 mg/kg, po treated every other day for 14 days	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435264	Drug metabolism in cynomolgus monkey assessed as (+)-Lesinurad level in urine at 2 mg/kg, iv administered as single bolus dose measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676199	AUC (0 to t) in male Kunming mouse at 2 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435235	Stability in Sprague-Dawley rat plasma at 37 degC up to 2 hrs	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435237	Metabolic stability in human microsomes	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676196	Half-life in male Kunming mouse at 2 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435240	Metabolic stability in dog microsomes	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435248	AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901562	Hypouricemic activity in Kunming mouse model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid ratio at 2 mg/kg,po and measured after 4 hrs	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1559413	Inhibition of human URAT1 expressed in HEK293T cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	The Druggability of Solute Carriers.
AID1435250	Drug metabolism in Sprague-Dawley rat plasma assessed as (+)-Lesinurad formation at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435269	Drug recovery in cynomolgus monkey urine at 10 mg/kg, po administered as single dose via gavage measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435253	AUC (0 to infinity) in Sprague-Dawley rat assessed as (-)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901570	Hypouricemic activity in rat model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid ratio at 2 mg/kg, po	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1918194	Lipophilicity, log D of the compound	2022	Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21	Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1435275	Drug level in cynomolgus monkey urine at 10 mg/kg, po administered as single dose via gavage measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435227	Inhibition of CYP1A2 (unknown origin)	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435245	AUC (0 to infinity) in Sprague-Dawley rat at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435276	Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring compound half life at 250 pmol/ml preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435242	Apparent permeability from apical to basolateral side in MDCK cells expressing MDR1	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1649926	Plasma protein binding in human	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Pharmacological urate-lowering approaches in chronic kidney disease.
AID1435243	Apparent permeability from basolateral to apical side in MDCK cells expressing MDR1	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435256	Apparent plasma clearance in Sprague-Dawley rat assessed as (+)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435236	Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435230	Stability of the compound in ethanol at 37 degC for 4 days	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901559	Hypouricemic activity in Kunming mouse model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid ratio at 2 mg/kg, po incubated for more than 4 hrs	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435224	Inhibition of CYP2C9 (unknown origin)	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676191	AUC (0 to infinity) in male Kunming mouse at 50 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1901607	Toxicity in Kunming mouse assessed as glomerular enlargement in kidney at 50 mg/kg, po treated every other day for 14 days by H and E staining analysis	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435282	Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring parent compound remaining at 250 pmol/ml after 60 mins in absence of NADPH by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676201	Sub-acute toxicity in male Kunming mouse assessed as increase in body weight at 50 mg/kg, po administered once every second day for 14 days	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435231	Stability of the compound in DMSO at 80 degC for 4 days	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435238	Metabolic stability in rat microsomes	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676198	AUC (0 to infinity) in male Kunming mouse at 2 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435241	Metabolic stability in monkey microsomes	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901608	Subacute toxicity in Kunming mouse assessed as death at 100 mg/kg, po for 15 days	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1649925	Half life in human	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Pharmacological urate-lowering approaches in chronic kidney disease.
AID1435267	Drug metabolism in cynomolgus monkey assessed as (-)-Lesinurad level in urine at 10 mg/kg, po administered as single dose via gavage measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435225	Inhibition of CYP3A4 (unknown origin)	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676194	Cmax in male Kunming mouse at 2 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435257	AUC (0 to infinity) in Sprague-Dawley rat assessed as (-)-Lesinurad level at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435252	Drug metabolism in Sprague-Dawley rat plasma assessed as (-)-Lesinurad formation at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676202	Acute toxicity in female Kunming mouse assessed as change in body weight at 500 mg/kg, ig measured for 1 week	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1676207	Acute toxicity in Kunming mouse assessed as death at 250 mg/kg, ig measured for 1 week relative to control	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435266	AUC (0 to infinity) in cynomolgus monkey assessed as (+)-Lesinurad level at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901600	Subacute toxicity in Kunming mouse assessed as anorexia at 50 mg/kg, po treated every other day for 14 days	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435274	AUC (0 to infinity) in cynomolgus monkey at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676177	Sub-acute toxicity in Kunming mouse assessed as hepatocellular condensation of liver at 50 mg/kg, po administered as single dose every other day for 14 days by H and E staining based assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1901606	Toxicity in Kunming mouse assessed as hydropic degeneration of hepatocyte at 50 mg/kg, po treated every other day for 14 days by H and E staining analysis	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435284	Drug metabolism in human liver microsomes assessed as CYP2C9-mediated mono-oxidative metabolite formation at 250 pmol/ml preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1649922	Inhibition of OAT4 (unknown origin)	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Pharmacological urate-lowering approaches in chronic kidney disease.
AID1435254	AUC (0 to infinity) in Sprague-Dawley rat assessed as (+)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435226	Inhibition of CYP2C19 (unknown origin)	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901598	Subacute toxicity in Kunming mouse assessed as lethargy at 50 mg/kg, po treated every other day for 14 days	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435262	Apparent plasma clearance in cynomolgus monkey assessed as (+)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435271	AUC (0 to infinity) in cynomolgus monkey at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901597	Subacute toxicity in Kunming mouse assessed as death at 50 mg/kg, po treated every other day for 14 days	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1901602	Subacute toxicity in Kunming mouse assessed as increase in body weight at 50 mg/kg, po measured treated every other day for 14 days	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435239	Metabolic stability in mouse microsomes	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435272	Apparent plasma clearance in cynomolgus monkey at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1575209	Inhibition of human URAT1 expressed in HEK293 cells assessed as reduction in [8-14C]uric acid uptake	2019	Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3	Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout.
AID1435273	Drug level in cynomolgus monkey urine at 2 mg/kg, iv administered as single bolus dose measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435268	Drug metabolism in cynomolgus monkey assessed as (+)-Lesinurad level in urine at 10 mg/kg, po administered as single dose via gavage measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1559411	Inhibition of human OAT4 expressed in HEK293 cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method	2020	Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8	The Druggability of Solute Carriers.
AID1435233	Drug metabolism in DMSO assessed as (-)-Lesinurad formation at 120 degC for 24 hrs	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676195	Tmax in male Kunming mouse at 2 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435261	Apparent plasma clearance in cynomolgus monkey assessed as (-)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1918193	Dissociation constant, pKa of the compound	2022	Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21	Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1435258	AUC (0 to infinity) in Sprague-Dawley rat assessed as (+)-Lesinurad level at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676193	AUC (0 to t) in male Kunming mouse at 50 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1676203	Acute toxicity in Kunming mouse assessed as induction of abnormal behaviors by measuring lethargy at 500 mg/kg, ig	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1901557	Acute toxicity in Kunming mouse assessed as death at 500 mg/kg, IG measured up to 1 week	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1901605	Toxicity in Kunming mouse assessed as hepatocellular condensation in liver at 50 mg/kg, po treated every other day for 14 days by H and E staining analysis	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1649924	Tmax in human	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Pharmacological urate-lowering approaches in chronic kidney disease.
AID1435247	Apparent clearance in Sprague-Dawley rat plasma at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676197	MRT (0 to infinity) in male Kunming mouse at 2 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1901558	Hypouricemic activity in Kunming mouse model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid concentration at 2 mg/kg, po incubated for more than 4 hrs	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1575210	Inhibition of human URAT1	2019	Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3	Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout.
AID1901561	Hypouricemic activity in Kunming mouse model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid concentration at 2 mg/kg, po and measured after 4 hrs	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435278	Drug metabolism in human liver microsomes assessed as CYP2C9-mediated metabolism by measuring compound intrinsic clearance at 250 pmol/ml preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676236	Hypouricemic activity in Kunming mouse model of xanthine/potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid level at 2 mg/kg administered 3 hrs prior to xanthine/potassium oxonate and measured after 6 hrs relative to con	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435259	AUC (0 to infinity) in cynomolgus monkey assessed as (-)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676189	Half-life in male Kunming mouse at 50 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1901564	Hypouricemic activity in Kunming mouse model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid ratio at 1 mg/kg, po and measured after 4 hrs	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1676179	Sub-acute toxicity in Kunming mouse assessed as ballooning degeneration of liver at 50 mg/kg, po administered as single dose every other day for 14 days by H and E staining based assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435223	Inhibition of CYP2D6 (unknown origin)	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676192	MRT (0 to infinity) in male Kunming mouse at 50 mg/kg, po by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435260	AUC (0 to infinity) in cynomolgus monkey assessed as (+)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435228	Stability of the compound in solid state assessed as compound purity after 80 days	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676180	Sub-acute toxicity in Kunming mouse assessed as congestion in hepatic central vein at 50 mg/kg, po administered as single dose every other day for 14 days by H and E staining based assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1676204	Acute toxicity in male Kunming mouse assessed as change in body weight at 500 mg/kg, ig measured for 1 week	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1676205	Acute toxicity in Kunming mouse assessed as induction of abnormal behaviors by measuring clonic convulsion at 500 mg/kg, ig	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435255	Apparent plasma clearance in Sprague-Dawley rat assessed as (-)-Lesinurad level at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901569	Hypouricemic activity in rat model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid concentration at 2 mg/kg, po	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1676206	Acute toxicity in Kunming mouse assessed as induction of abnormal behaviors by measuring anorexia at 500 mg/kg, ig	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1901601	Subacute toxicity in Kunming mouse assessed as ruffled fur at 50 mg/kg, po treated every other day for 14 days	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435265	AUC (0 to infinity) in cynomolgus monkey assessed as (-)-Lesinurad level at 10 mg/kg, po administered as single dose via gavage by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1918192	Inhibition of human OAT2 tv.1 variant expressed in HEK293 cells assessed as inhibition of [3H]cGMP uptake by scintillation analysis	2022	Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21	Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1901604	Toxicity in Kunming mouse assessed as ballooning degeneration of liver at 50 mg/kg, po treated every other day for 14 days by H and E staining analysis	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1901571	Inhibition of human URAT1 mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate incubated for 30 mins by liquid scintillation counter	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1676181	Sub-acute toxicity in Kunming mouse assessed as hydropic degeneration of hepatocytes at 50 mg/kg, po administered as single dose every other day for 14 days by H and E staining based assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435222	Inhibition of human ERG	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676234	Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition by liquid scintillation counting method	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1676178	Sub-acute toxicity in Kunming mouse assessed as edema in proximal tubule at 50 mg/kg, po administered as single dose every other day for 14 days by H and E staining based assay	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435246	Drug metabolism in DMSO assessed as (+)-Lesinurad formation at 120 degC for 24 hrs	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1676235	Hypouricemic activity in rat model of xanthine/potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid level relative to control	2020	Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19	Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
AID1435270	Drug recovery in cynomolgus monkey urine at 2 mg/kg, iv administered as single bolus dose measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1901563	Hypouricemic activity in Kunming mouse model of xanthine and potassium oxonate-induced acute hyperuricemia assessed as decrease in serum uric acid concentration at 1 mg/kg, po and measured after 4 hrs	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
AID1435232	Drug metabolism in ethanol assessed as (-)-Lesinurad formation at 37 degC	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
AID1435263	Drug metabolism in cynomolgus monkey assessed as (-)-Lesinurad level in urine at 2 mg/kg, iv administered as single bolus dose measured at 24 hrs post dose by LC-MS/MS analysis	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Discovery and Assessment of Atropisomers of (±)-Lesinurad.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	67 (80.72)	24.3611
2020's	16 (19.28)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	16 (19.05%)	5.53%
Reviews	23 (27.38%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	45 (53.57%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (22)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
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 2	227 participants (Actual)	Interventional	2009-10-31	Completed
Post-Authorisation Safety Study of Lesinurad [NCT04072471]		0 participants (Actual)	Observational	2021-01-29	Withdrawn(stopped due to The study was withdrawn as lesinurad was withdrawn from the market in Europe by the market authorization holder. Hence the commitment to do this PASS was removed by the European Medicines Agency.)
A Phase 1, Randomized, Open-Label, Crossover Study in Healthy Adult Male Subjects to Assess the Relative Bioavailability of Lesinurad Tablets Manufactured at Two Different Sites [NCT01986556]	Phase 1	36 participants (Actual)	Interventional	2013-11-30	Completed
Randomized, Double-Blind, Multicenter, Placebo-Controlled, Safety and Efficacy Study of RDEA594 Versus Placebo in the Treatment of Hyperuricemia in Patients With Gout [NCT00955981]	Phase 2	123 participants (Actual)	Interventional	2009-07-31	Completed
A Phase 1, Randomized, Open-Label, Crossover Study to Assess the Bioequivalence of Lesinurad Tablets From Two Manufacturing Sites in Healthy Adult Male Subjects [NCT02127775]	Phase 1	54 participants (Actual)	Interventional	2014-04-30	Completed
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 1	116 participants (Actual)	Interventional	2015-10-31	Completed
A Phase 1 Study to Evaluate the Potential Two-Way Pharmacokinetic Interaction Between Lesinurad and Naproxen and Between Lesinurad and Indomethacin in Healthy Adult Male Subjects [NCT01884272]	Phase 1	24 participants (Actual)	Interventional	2013-06-30	Completed
A Phase 1, Open-Label, Drug-Drug Interaction Study to Evaluate the Potential Effects of Ranitidine on the Pharmacokinetics of Lesinurad in Healthy Adult Male Subjects [NCT01908257]	Phase 1	16 participants (Actual)	Interventional	2013-07-31	Completed
A Phase 1, Randomized, Open-Label, Drug-Drug Interaction Study to Evaluate the Potential Pharmacokinetic and Pharmacodynamic Interaction Between Lesinurad and Calcium Carbonate and Aluminum/Magnesium Hydroxide-Containing Antacids in Healthy Adult Male Sub [NCT01982201]	Phase 1	24 participants (Actual)	Interventional	2013-11-30	Completed
A Phase 1, Randomized, Open-Label, Single-Dose Study to Evaluate Potential Pharmacokinetic Interaction Between Lesinurad and Metformin and Between Lesinurad and Furosemide in Health Adult Male Subjects [NCT02028689]	Phase 1	23 participants (Actual)	Interventional	2013-10-31	Completed
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 1	28 participants (Actual)	Interventional	2016-08-30	Completed
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 1	32 participants (Actual)	Interventional	2017-08-14	Completed
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 3	610 participants (Actual)	Interventional	2011-12-31	Completed
A Phase 1, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single and Multiple Doses of Lesinurad in Healthy Male Japanese Subjects [NCT01744379]	Phase 1	40 participants (Actual)	Interventional	2012-12-31	Completed
A Long-Term Extension Study of Lesinurad in Combination With Allopurinol for Subjects Completing an Efficacy and Safety Study of Lesinurad and Allopurinol [NCT01808131]	Phase 3	717 participants (Actual)	Interventional	2013-02-28	Completed
A Long-Term Open-Label Extension Study for Subjects Completing a Phase 3 Efficacy and Safety Study of Lesinurad Monotherapy in Subjects With Gout [NCT01650246]	Phase 3	143 participants (Actual)	Interventional	2012-08-31	Completed
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 4	242 participants (Actual)	Interventional	2017-07-19	Terminated(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 Febuxostat Compared to Febuxostat Alone at Lowering Serum Uric Acid and Resolving Tophi in Subjects With Tophaceou [NCT01510769]	Phase 3	330 participants (Actual)	Interventional	2012-01-31	Completed
A Phase 1, Open-Label Study to Assess the Absolute Bioavailability of a Single Oral Dose of Lesinurad With Respect to an Intravenous Micro Tracer Dose of [14C]Lesinurad in Healthy Adult Male Subjects [NCT02039700]	Phase 1	10 participants (Actual)	Interventional	2014-01-31	Completed
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 3	607 participants (Actual)	Interventional	2012-01-31	Completed
A Long-Term Extension Study of Lesinurad in Combination With Febuxostat for Subjects With Gout Completing an Efficacy and Safety Study of Lesinurad and Febuxostat [NCT01808144]	Phase 3	196 participants (Actual)	Interventional	2013-03-01	Completed
A Phase 3 Randomized, Double-Blind, Multicenter, Placebo- Controlled Study to Assess the Efficacy and Safety of Lesinurad Monotherapy Compared to Placebo in Subjects With Gout and an Intolerance or Contraindication to a Xanthine Oxidase Inhibitor [NCT01508702]	Phase 3	214 participants (Actual)	Interventional	2012-01-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
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.
NCT01508702 (1) [back to overview]	Number of Subjects With an sUA Level That is < 6.0 mg/dL
NCT01510158 (3) [back to overview]	Gout Flares
NCT01510158 (3) [back to overview]	Proportion of Subjects With an sUA Level That is < 6.0 mg/dL
NCT01510158 (3) [back to overview]	Tophus
NCT01510769 (4) [back to overview]	Complete or Partial Response of at Least One Tophus
NCT01510769 (4) [back to overview]	Complete Resolution of at Least One Target Tophus
NCT01510769 (4) [back to overview]	Quality of Life
NCT01510769 (4) [back to overview]	Subjects With a Serum Urate (sUA) Level That is < 5.0 mg/dL by Month 6
NCT01650246 (2) [back to overview]	Incidence of Treatment-emergent Adverse Events (TEAEs)
NCT01650246 (2) [back to overview]	Proportion of Subjects With a Serum Urate (sUA) Level That is < 6.0 mg/dL
NCT01808144 (2) [back to overview]	Percentage of Participants (With at Least One Target Tophus at Baseline) Who Experience Complete Resolution of at Least One Target Tophus
NCT01808144 (2) [back to overview]	Percentage of Participants With an sUA Level That is < 5.0 mg/dL
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]	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
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]	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]	Percentage of Participants Renal-Related and Kidney Stone Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
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

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

Intervention	Gout Flares (Mean)
Lesinurad 200 mg + Allopurinol	0.7
Lesinurad 400 mg + Allopurinol	0.8
Placebo + Allopurinol	0.9

Intervention	Proportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol	0.314
Lesinurad 400 mg + Allopurinol	0.276
Placebo + Allopurinol	0.333

Intervention	Proportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol	0.554
Lesinurad 400 mg + Allopurinol	0.665
Placebo + Allopurinol	0.233

Intervention	Proportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol	0.542
Lesinurad 400 mg + Allopurinol	0.592
Placebo + Allopurinol	0.279

Intervention	Proportion of Subjects (Number)
Lesinurad 200 mg + Allopurinol	0
Lesinurad 400 mg + Allopurinol	0.211
Placebo + Allopurinol	0.294

Intervention	Proportion of Subjects (Number)
Lesinurad 200 mg + Febuxostat 80 mg	0.566
Lesinurad 400 mg + Febuxostat 80 mg	0.587
Placebo + Febuxostat 80 mg	0.505

Intervention	Proportion of Subjects (Number)
Lesinurad 200 mg + Febuxostat 80 mg	0.255
Lesinurad 400 mg + Febuxostat 80 mg	0.303
Placebo + Febuxostat 80 mg	0.211

Intervention	Proportion of Subjects (Number)
Lesinurad 200 mg + Febuxostat 80 mg	0.442
Lesinurad 400 mg + Febuxostat 80 mg	0.333
Placebo + Febuxostat 80 mg	0.525

Intervention	Percentage of participants (Number)
Lesinurad 400 mg + Febuxostat 80 mg	61.0
Lesinurad 200 mg + Febuxostat 80 mg	54.3

Intervention	Percentage of participants (Number)
Lesinurad 400 mg + Febuxostat 80 mg	82.5
Lesinurad 200 mg + Febuxostat 80 mg	77.8

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

Intervention	percentage of participants (Number)
	Treatment-Emergent SAEs	Treatment-Emergent AEs
Lesinurad + XOI	0.8	5.6
Placebo + XOI	0.0	4.2

Intervention	percentage of participants (Number)
	Baseline	Month 1	Month 3	Month 6	Month 9	Month 12	Month 15
Lesinurad + XOI	10.6	58.8	52.5	58.8	42.9	56.5	62.5

Condition	Indicated	Relationship Strength	Studies	Trials
Gout Metabolic disorder characterized by recurrent acute arthritis, hyperuricemia and deposition of sodium urate in and around the joints, sometimes with formation of URIC ACID calculi.	1	16.86	50	12
Hyperuricemia Excessive URIC ACID or urate in blood as defined by its solubility in plasma at 37 degrees C; greater than 0.42mmol per liter (7.0mg/dL) in men or 0.36mmol per liter (6.0mg/dL) in women. This condition is caused by overproduction of uric acid or impaired renal clearance. Hyperuricemia can be acquired, drug-induced or genetically determined (LESCH-NYHAN SYNDROME). It is associated with HYPERTENSION and GOUT.	1	12.63	25	3
Chronic Kidney Diseases [description not available]	0	3.12	1	0
Renal Insufficiency, Chronic Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)	0	3.12	1	0
Diseases, Metabolic [description not available]	0	3.17	1	0
Nervous System Disorders [description not available]	0	3.17	1	0
Metabolic Diseases Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed)	0	3.17	1	0
Nervous System Diseases Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle.	0	3.17	1	0
Hepatic Insufficiency Conditions in which the LIVER functions fall below the normal ranges. Severe hepatic insufficiency may cause LIVER FAILURE or DEATH. Treatment may include LIVER TRANSPLANTATION.	0	2.21	1	0
Kidney Failure A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.	0	4.88	2	1
Renal Insufficiency Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.	0	4.88	2	1
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	6.99	5	1
Chronic Illness [description not available]	0	4.29	3	0
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	0	4.29	3	0
Dry Eye [description not available]	0	2.15	1	0
Dry Eye Syndromes Corneal and conjunctival dryness due to deficient tear production, predominantly in menopausal and post-menopausal women. Filamentary keratitis or erosion of the conjunctival and corneal epithelium may be caused by these disorders. Sensation of the presence of a foreign body in the eye and burning of the eyes may occur.	0	2.15	1	0
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	0	3.95	2	1
Gouty Arthritis [description not available]	0	3.04	1	0
Arthritis, Gouty Arthritis, especially of the great toe, as a result of gout. Acute gouty arthritis often is precipitated by trauma, infection, surgery, etc. The initial attacks are usually monoarticular but later attacks are often polyarticular. Acute and chronic gouty arthritis are associated with accumulation of MONOSODIUM URATE in and around affected joints.	0	3.04	1	0
Kahler Disease [description not available]	0	2.13	1	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	0	2.13	1	0
Acute Symptom Flare [description not available]	0	4.45	1	1

lesinurad

Description

Cross-References

Synonyms (84)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (1)

Drug Classes (6)

Protein Targets (8)

Inhibition Measurements

Biological Processes (75)

Molecular Functions (51)

Ceullar Components (16)

Bioassays (121)

Research

Studies (83)

Market Indicators

Research Demand Index: 50.96

Study Types

Clinical Trials (22)

Trial Overview

Trial Outcomes

Gout Flares

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

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

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

Gout Flares

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

Tophus

Complete or Partial Response of at Least One Tophus

Complete Resolution of at Least One Target Tophus

Quality of Life

Subjects With a Serum Urate (sUA) Level That is < 5.0 mg/dL by Month 6

Incidence of Treatment-emergent Adverse Events (TEAEs)

Proportion of Subjects With a Serum Urate (sUA) Level That is < 6.0 mg/dL

Percentage of Participants (With at Least One Target Tophus at Baseline) Who Experience Complete Resolution of at Least One Target Tophus

Percentage of Participants With an sUA Level That is < 5.0 mg/dL

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

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

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

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

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

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

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

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

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

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

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

Percentage of Participants Renal-Related and Kidney Stone Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)

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

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

Related Drugs (84)

Related Conditions (22)