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Lesinurad

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https://www.readbyqxmd.com/read/29181594/determination-of-lesinurad-in-rat-plasma-by-a-uhplc-ms-ms-assay
#1
Xiao-Yang Zhou, Ling-Jing Yuan, Zhe Chen, Peng-Fei Tang, Xiang-Yu Li, Guo-Xin Hu, Jian-Ping Cai
Lesinurad is an oral inhibitor of urate-anion exchanger transporter 1 and has been approved by the US Food and Drug Administration for combination therapy with a xanthine oxidase inhibitor for the treatment of hyperuricemia associated with refractory gout. In the present study, a sensitive and specific ultra high-performance liquid chromatography with tandem mass spectrometry assay was established and verified for the determination of lesinurad in rat plasma and was described in details for the first time. Chromatographic separation of lesinurad and diazepam (internal standard, IS) was performed on a Rapid Resolution HT C18 column (3...
November 28, 2017: Chemistry Central Journal
https://www.readbyqxmd.com/read/29125593/lesinurad-allopurinol-duzallo-for-gout-associated-hyperuricemia
#2
(no author information available yet)
No abstract text is available yet for this article.
November 6, 2017: Medical Letter on Drugs and Therapeutics
https://www.readbyqxmd.com/read/29123379/guideline-development-for-the-management-of-gout-role-of-combination-therapy-with-a-focus-on-lesinurad
#3
REVIEW
Graeme Jones, Elena Panova, Richard Day
The aim of this review was to summarize the evidence for combination therapy to achieve serum urate (SUA) target levels in gout. Within this overarching aim, a second aim was to evaluate the evidence for a new uricosuric agent lesinurad, which inhibits urate transport in the kidney. In summary, this review indicates that there are a number of ways to approach patients who do not achieve a target serum urate with allopurinol (APL) monotherapy. These include higher doses of APL up to 600-800 mg/d, switching to febuxostat, or adding in a uricosuric...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29103339/lesinurad-for-the-treatment-of-hyperuricaemia-in-people-with-gout
#4
Philip C Robinson, Nicola Dalbeth
Gout is a common form of inflammatory arthritis caused by deposition of monosodium urate crystals. The central strategy for effective long-term management of gout is serum urate lowering. Current urate-lowering drugs include both xanthine oxidase inhibitors and uricosuric agents. Lesinurad is a URAT1 inhibitor that selectively inhibits urate rebsorption at the proximal renal tubule. Lesinurad 200mg daily in combination with a xanthine oxidase is approved for urate-lowering therapy in patients with gout. Areas covered: The published literature was searched using Pubmed and additional information was obtained from publically available regulatory documents...
November 13, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29029210/lesinurad-monotherapy-in-gout-patients-intolerant-to-a-xanthine-oxidase-inhibitor-a-6-month-phase-3-clinical-trial-and-extension-study
#5
Anne-Kathrin Tausche, Rieke Alten, Nicola Dalbeth, Jeff Kopicko, Maple Fung, Scott Adler, Nihar Bhakta, Chris Storgard, Scott Baumgartner, Kenneth Saag
Objective: To investigate the efficacy and safety of lesinurad, a selective uric acid reabsorption inhibitor, in a 6 month, phase 3 clinical trial and extension study. Methods: Patients with gout who cannot take a xanthine oxidase inhibitor (XOI) and have serum uric acid (sUA) ⩾6.5 mg/dl were randomized to receive oral lesinurad (400 mg daily) or placebo. The primary endpoint was the proportion of patients with sUA <6.0 mg/dl at month 6. Safety assessments included treatment-emergent adverse events (TEAEs) and laboratory data...
September 23, 2017: Rheumatology
https://www.readbyqxmd.com/read/28988709/identification-and-characterization-of-a-potent-and-selective-inhibitor-of-human-urate-transporter-1
#6
Ting Wu, Jiasheng Chen, Shuai Dong, Haixin Li, Ying Cao, Yuanxin Tian, Weimin Fu, Pingzheng Zhou, Baomin Xi, Jianxin Pang
BACKGROUND: Selective inhibitors of human urate transporter 1 (hURAT1) are considered to be effective treatment for hyperuricemia and gout, which can reduce the reabsorption of more than 90% of uric acid in the proximal tubule of the kidney. We aimed to design and synthesize a more potent hURAT1 based on the structure of Lesinurad (LU), which was reported to lower uric acid levels with IC50 value of hURAT1 (about 60μM). METHODS: A cell model was conducted and characterized via Real-time qRCR and Western blot...
May 6, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28980503/lesinurad-a-selective-urat-1-inhibitor-with-a-novel-mechanism-in-combination-with-a-xanthine-oxidase-inhibitor-for-hyperuricemia-associated-with-gout
#7
Emily Huneycutt, Chase Board, Jennifer N Clements
OBJECTIVE: To review the pharmacokinetics, clinical efficacy, safety, and role of lesinurad for the management of hyperuricemia associated with gout. DATA SELECTION: A MEDLINE search (2000 to April 2017) was conducted using the terms hyperuricemia, gout, URAT-1, URAT-1 transporter, and lesinurad. Published articles and scientific posters relevant to the efficacy and safety of lesinurad were reviewed and summarized. DATA SYNTHESIS: Lesinurad was evaluated in 3 randomized, phase 3 clinical trials (CRYSTAL, CLEAR 1 and 2)...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/28979780/lesinurad-what-the-nephrologist-should-know
#8
Maria Dolores Sanchez-Niño, Binbin Zheng-Lin, Lara Valiño-Rivas, Ana Belen Sanz, Adrian Mario Ramos, Jose Luño, Marian Goicoechea, Alberto Ortiz
Lesinurad is an oral inhibitor of the monocarboxylic/urate transporter URAT1 encoded by the SLC22A12 gene. Market authorization was granted in February 2016 in Europe and December 2015 in the USA. As a potentially nephrotoxic uricosuric drug acting on the kidney, nephrologists should become familiar with its indications and safety profile. The approved indication is treatment of gout in combination with a xanthine oxidase (XO) inhibitor in adult patients who have not achieved target serum uric acid levels with an XO inhibitor alone...
October 2017: Clinical Kidney Journal
https://www.readbyqxmd.com/read/28970208/response-to-a-response-to-singh-lesinurad-combination-therapy-with-allopurinol-in-gout-do-clear-studies-make-the-treatment-of-gout-clearer-by-valiyil-and-schechter
#9
Jasvinder A Singh
No abstract text is available yet for this article.
September 28, 2017: Annals of the Rheumatic Diseases
https://www.readbyqxmd.com/read/28942107/the-market-of-chiral-drugs-chiral-switches-versus-de-novo-enantiomerically-pure-compounds
#10
REVIEW
Andrea Calcaterra, Ilaria D'Acquarica
This review article is aimed at providing an overview of the current market of chiral drugs by exploring which is the nowadays tendency, for the pharmaceutical industry, either to exploit the chiral switching practice from already marketed racemates or to develop de novo enantiomerically pure compounds. A concise illustration of the main techniques developed to assess the absolute configuration (AC) and enantiomeric purity of chiral drugs has been given, where greater emphasis was placed on the contribution of enantioselective chromatography (HPLC, SFC and UHPC)...
July 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28888218/impact-of-non-adherence-on-the-safety-and-efficacy-of-uric-acid-lowering-therapies-in-the-treatment-of-gout
#11
Daniel Hill-McManus, Elena Soto, Scott Marshall, Steven Lane, Dyfrig Hughes
AIMS: Dual-urate lowering therapy (ULT) with xanthine oxidase inhibitor and uricosuric medications is a treatment option for severe gout. Uricosurics can cause hyperuricosuria, a risk factor for nephrolithiasis and acute uric acid nephropathy. The aims of this study were to simulate the relation between suboptimal drug adherence and efficacy, and to quantify the risk of hyperuricosuria in gout patients receiving mono and dual-ULTs. METHODS: The impact of poor medication adherence was studied using 2-compartment PK models based on published evidence and a semi-mechanistic, 4-compartment pharmacodynamic (PD) model...
September 9, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28689430/current-and-future-therapies-for-gout
#12
REVIEW
Tristan Pascart, Pascal Richette
Gout is a common disease responsible for recurrent flares triggered by the deposition of monosodium urate crystals secondary to longstanding hyperuricaemia. The management of gout implies both the treatment of flares and the treatment of hyperuricaemia itself. Recent improvement in the understanding of the disease led to the development of new drugs. Areas covered: This review covers data related to 'old' treatments of flares and hyperuricaemia, evidence on the recently approved drugs and emerging therapies in development...
August 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28658988/updates-on-the-treatment-of-gout-including-a-review-of-updated-treatment-guidelines-and-use-of-small-molecule-therapies-for-difficult-to-treat-gout-and-gout-flares
#13
REVIEW
Rose Soskind, Daniel T Abazia, Mary Barna Bridgeman
Gout is a rheumatologic condition associated with elevated serum uric acid levels and deposition of monosodium urate crystals in joints and soft tissues. Areas covered: In this article, we describe the role of currently available drug therapies for managing acute gout flares and used in reducing serum urate levels. Further, we explore the role of novel small molecular therapies and biologic agents in the treatment of refractory or severe gout symptoms. A literature search of MEDLINE and MEDLINE In-Process & Other Non-Indexed Citations Databases (1996-June 2017) was conducted utilizing the key words 'gout', 'interleukin-1 inhibitors', 'acute gout', 'gout treatment', 'urate lowering therapies', 'hyperuricemia', 'colchicine', 'pegloticase', 'lesinurad', 'xanthine oxidase', 'xanthine oxidase inhibitors', 'allopurinol', 'febuxostat', 'uricosurics', 'probenecid', and 'benzbromarone'...
August 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28597604/lesinurad-a-selective-uric-acid-reabsorption-inhibitor-in-combination-with-febuxostat-in-patients-with-tophaceous-gout-findings-of-a-phase-iii-clinical-trial
#14
RANDOMIZED CONTROLLED TRIAL
Nicola Dalbeth, Graeme Jones, Robert Terkeltaub, Dinesh Khanna, Jeff Kopicko, Nihar Bhakta, Scott Adler, Maple Fung, Chris Storgard, Scott Baumgartner, Fernando Perez-Ruiz
OBJECTIVE: To investigate the efficacy and safety of lesinurad in combination with febuxostat in a 12-month phase III trial in patients with tophaceous gout. METHODS: Patients with serum urate (UA) ≥8.0 mg/dl (≥6.0 mg/dl with urate-lowering therapy) and ≥1 measurable target tophus were given febuxostat 80 mg/day for 3 weeks before randomization to receive lesinurad (200 or 400 mg daily) or placebo in addition to the febuxostat. The primary end point was the proportion of patients achieving a serum UA level of <5...
September 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/28434436/treatment-options-for-gout
#15
Bettina Engel, Johannes Just, Markus Bleckwenn, Klaus Weckbecker
BACKGROUND: 1-2% of adults in Germany suffer from gout. Gout is one of the few rheumatological diseases that can be cured. It arises through the deposition of uric acid crystals in joints as a result of hyperuricemia. Painful redness and swelling of the affected joints are typical findings. Multiple pertinent guidelines and treatment recommendations have been published, but there is reason to believe that patients with gout are not always treated accordingly. METHODS: This review is based on relevant publications from the years 2000-2016 that were retrieved by a selective search in the Cochrane and PubMed databases...
March 31, 2017: Deutsches Ärzteblatt International
https://www.readbyqxmd.com/read/28425024/lesinurad-a-review-in-hyperuricaemia-of-gout
#16
REVIEW
Emma D Deeks
Lesinurad (Zurampic(®)) is an oral selective inhibitor of the URAT1 and OAT4 uric acid (UA) transporters of the kidney, via which it inhibits UA reabsorption and thus increases renal UA excretion and lowers serum UA (sUA) levels. Lesinurad 200 mg once daily is indicated for use in combination with a xanthine oxidase inhibitor (XOI) to treat hyperuricaemia in adults with gout who have not achieved target sUA levels with an XOI alone. Approval was based on three 12-month phase 3 trials that evaluated lesinurad in combination with allopurinol in adults with gout inadequately responsive to allopurinol (CLEAR 1 and 2) and in combination with febuxostat in adults with tophaceous gout (CRYSTAL)...
May 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28337320/discovery-and-assessment-of-atropisomers-of-%C3%A2-lesinurad
#17
Jianfei Wang, Wenqin Zeng, Shaohua Li, Liang Shen, Zhengxian Gu, Yang Zhang, Jian Li, Shuhui Chen, Xiangbo Jia
(+)- and (-)-Lesinurad were isolated as atropisomers from racemic lesinurad for the first time. No interconversion was observed between the two atropisomers under various conditions tested. The two atropisomers showed significant differences in hURAT1 highly expressed HEK293 cell-based inhibition assays, monkey pharmacokinetic studies, and in vitro human recombinant CYP2C9 stability studies. It was speculated that (+)-lesinurad might offer a better hyperuricemia/gout therapy than (-)-lesinurad or the racemate...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28246893/crystal-arthritides-gout-and-calcium-pyrophosphate-arthritis-part%C3%A2-3-treatment
#18
REVIEW
S Schlee, L C Bollheimer, T Bertsch, C C Sieber, P Härle
The treatment of gout is based on several principles. Symptom control and termination of the inflammatory process are important early goals, whereas the urate level should be lowered in the long term to prevent further gout attacks and complications. The non-pharmacological approach is based on individually informing the patient on dietary measures and changes of life style. Besides physical measures, such as cold applications on the affected joint, various medications are available for treatment of an acute gout attack...
February 28, 2017: Zeitschrift Für Gerontologie und Geriatrie
https://www.readbyqxmd.com/read/28163535/lesinurad-a-significant-advancement-or-just-another-addition-to-existing-therapies-of-gout
#19
REVIEW
Ajay Gupta, Pramod Kumar Sharma, Arup Kumar Misra, Surjit Singh
Gout is a metabolic disorder that usually presents as recurrent episodes of acute arthritis due to deposition of crystals in joints and cartilages. Despite the availability of several drugs for gout, its management is still less than adequate. There is always a search for newer, safer, and more potent urate-lowering therapies for treating patients inadequately controlled with available drugs. Lesinurad in combination with a xanthine oxidase inhibitor provides an effective mode of therapy in the management of hyperuricemia associated with gout...
October 2016: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/28074640/evaluation-of-pharmacokinetic-interactions-between-lesinurad-a-new-selective-urate-reabsorption-inhibitor-and-commonly-used-drugs-for-gout-treatment
#20
Zancong Shen, Kathy Tieu, David Wilson, Gail Bucci, Michael Gillen, Caroline Lee, Bradley Kerr
Lesinurad is a novel selective uric acid reabsorption inhibitor approved for treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors (XOIs). 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. Colchicine studies included consecutive 7-day treatment periods of (1) allopurinol 300 mg, allopurinol 300 mg plus lesinurad 400 or 600 mg, and continued lesinurad 400 or 600 mg; or (2) febuxostat 40 or 80 mg, febuxostat 40 or 80 mg plus lesinurad 400 mg, and continued febuxostat 40 or 80 mg plus lesinurad 600 mg...
January 11, 2017: Clinical Pharmacology in Drug Development
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