keyword
MENU ▼
Read by QxMD icon Read
search

Lesinurad

keyword
https://www.readbyqxmd.com/read/29671542/lesinurad-zurampic-for-gout
#1
Phung C On
No abstract text is available yet for this article.
March 15, 2018: American Family Physician
https://www.readbyqxmd.com/read/29557073/cost-effectiveness-analysis-of-lesinurad-allopurinol-versus-febuxostat-for-the-management-of-gout-hyperuricemia-in-italy
#2
M Ruggeri, M Basile, C Drago, F R Rolli, A Cicchetti
BACKGROUND: Until very recently the only therapeutic alternative for the management of patients affected by gout/hyperuricemia that did not respond to a first-line treatment based on allopurinol alone or who cannot tolerate allopurinol was febuxostat, a xanthine oxidase non-purine-selective inhibitor. Lately, however, a new therapeutic alternative has become available for the management of this pathology: lesinurad, a urate transporter inhibitor. OBJECTIVE: To objective of this study was to evaluate the cost effectiveness of lesinurad/allopurinol in comparison with febuxostat as a second-line therapeutic strategy for the management of patients affected by gout and hyperuricemia that did not respond to a first-line therapy based on allopurinol alone...
March 19, 2018: PharmacoEconomics
https://www.readbyqxmd.com/read/29553292/change-gout-how-to-deal-with-this-silently-developing-killer-in-everyday-clinical-practice
#3
Carlo Alberto Scirè, Cristina Rossi, Leonardo Punzi, Augusto Genderini, Claudio Borghi, Walter Grassi
Despite being regarded as an easily-treatable disease, gout diagnosis and management can be challenging. We discuss here current issues in gout management and propose some potential solutions. Gout diagnosis should be reached as early as possible and often requires specific tests, such as synovial fluid analysis or imaging techniques that are not available in most centers, leaving health care professionals to rely only on clinical presentations and their experience. In addition, gout management requires the evaluation of multiple aspects, such as monitoring of serum uric acid (sUA) level (which should be reduced to <6 mg/dL) to ensure adherence and efficacy of treatment, evaluation of patient's risk profile and comorbidities, and continuous assessments to manage clinical manifestations...
March 19, 2018: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/29488355/individualized-treatment-strategies-for-hyperuricemia-informed-by-a-semi-mechanistic-exposure-response-model-of-uric-acid-dynamics
#4
Sergey Aksenov, Carl C Peck, Ulf G Eriksson, Donald R Stanski
To provide insight into pharmacological treatment of hyperuricemia we developed a semi-mechanistic, dynamical model of uric acid (UA) disposition in human. Our model represents the hyperuricemic state in terms of production of UA (rate, PUA), its renal filtration (glomerular filtration rate, GFR) and proximal tubular reabsorption (fractional excretion coefficient, FE). Model parameters were estimated using data from 9 Phase I studies of xanthine oxidase inhibitors (XOI) allopurinol and febuxostat and a novel uricosuric, the selective UA reabsorption inhibitor lesinurad, approved for use in combination with a XOI...
March 2018: Physiological Reports
https://www.readbyqxmd.com/read/29482353/lesinurad-a-novel-agent-for-management-of-chronic-gout
#5
Stacy L Haber, Gelila Fente, Skylar N Fenton, Elise P Walker, Brianne M Weaver, Alexander J Cano, Katherine Vu
OBJECTIVE: To review the pharmacology, efficacy, and safety of lesinurad and determine its role relative to other agents in the management of chronic gout. DATA SOURCES: A PubMed search (1946 to February 2018) using the terms lesinurad and RDEA594 was conducted to identify relevant articles. STUDY SELECTION AND DATA EXTRACTION: In vitro or in vivo evaluations of lesinurad published in the English language were eligible for inclusion. Phase II and III trials were selected for review of efficacy and safety...
February 1, 2018: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29474515/validated-stability-indicating-high-performance-liquid-chromatographic-determination-of-lesinurad
#6
Khalid A M Attia, Nasr M El-Abasawi, Ahmed El-Olemy, Ahmed H Abdelazim
Lesinurad is a novel selective uric acid reabsorption inhibitor which has been newly approved for the treatment of the chronic gout. The behavior of lesinurad under various stress conditions (hydrolysis, oxidation, thermal and photolysis) has been investigated as per ICH guidelines. The drug has been found to be labile to acidic hydrolysis, basic hydrolysis and oxidation but stable in neutral, thermal and photolytic conditions. A high performance liquid chromatographic method has been developed for selective determination of the studied drug in the presence of its related degradation products...
February 21, 2018: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29386212/effective-uric-acid-reduction-with-probenecid-and-febuxostat-in-a-patient-with-chronic-kidney-disease
#7
Robert Case, Brian Wentworth, Grant Jester
A 33-year-old male with poorly controlled chronic tophaceous gout and chronic kidney disease (CKD) with estimated glomerular filtration rate (GFR) of 37 cc/min. His uric acid was 11 mg/dL despite maximal dosing of febuxostat. He had previously failed pegloticase infusions as well. This patient had a reduction in his uric acid level to less than 6 mg/dL following addition of probenecid to his febuxostat regimen. Most guidelines recommend against utilisation of probenecid therapy in patients with GFR <50, but there is no obvious contraindication to its use, provided renal calculi do not develop...
January 31, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29382075/systematic-structure-activity-relationship-sar-exploration-of-diarylmethane-backbone-and-discovery-of-a-highly-potent-novel-uric-acid-transporter-1-urat1-inhibitor
#8
Wenqing Cai, Jingwei Wu, Wei Liu, Yafei Xie, Yuqiang Liu, Shuo Zhang, Weiren Xu, Lida Tang, Jianwu Wang, Guilong Zhao
In order to systematically explore and better understand the structure-activity relationship (SAR) of a diarylmethane backbone in the design of potent uric acid transporter 1 (URAT1) inhibitors, 33 compounds (1a-1x and 1ha-1hi) were designed and synthesized, and their in vitro URAT1 inhibitory activities (IC50) were determined. The three-round systematic SAR exploration led to the discovery of a highly potent novel URAT1 inhibitor, 1h, which was 200- and 8-fold more potent than parent lesinurad and benzbromarone, respectively (IC50 = 0...
January 27, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29318274/lesinurad-allopurinol-duzallo-for-gout-associated-hyperuricemia
#9
(no author information available yet)
No abstract text is available yet for this article.
January 9, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29251661/new-urate-lowing-therapies
#10
Abhishek Abhishek
PURPOSE OF REVIEW: To discuss recent studies of lesinurad and arhalofenate. RECENT FINDINGS: Lesinurad acts by blocking urate reabsorption channels URAT-1 and OAT-4. It has urate-lowering effect when used alone and in combination with xanthine oxidase inhibitors (XOIs). Its uricosuric activity depends on glomerular filtration, and its' efficacy is impaired at eGFR less than 30 ml/min. Lesinurad monotherapy (400 mg/day) associates with serum creatinine elevations...
March 2018: Current Opinion in Rheumatology
https://www.readbyqxmd.com/read/29181594/determination-of-lesinurad-in-rat-plasma-by-a-uhplc-ms-ms-assay
#11
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
#12
(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
#13
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
#14
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...
December 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
#15
RANDOMIZED CONTROLLED TRIAL
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...
December 1, 2017: Rheumatology
https://www.readbyqxmd.com/read/28988709/identification-and-characterization-of-a-potent-and-selective-inhibitor-of-human-urate-transporter-1
#16
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
#17
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
#18
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
#19
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
#20
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
keyword
keyword
30881
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"