Cited by 1,218Gout, Hyperuricemia, Uric AcidBiochemical and Molecular ResearchAdenosine and Purinergic Signaling

Therapeutic Effects of Xanthine Oxidase Inhibitors: Renaissance Half a Century after the Discovery of Allopurinol

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Pacher, Pál, Nivorozhkin, Alex, Szabó, Csaba·2006·Pharmacological Reviews

Abstract

The prototypical xanthine oxidase (XO) inhibitor allopurinol, has been the cornerstone of the clinical management of gout and conditions associated with hyperuricemia for several decades. More recent data indicate that XO also plays an important role in various forms of ischemic and other types of tissue and vascular injuries, inflammatory diseases, and chronic heart failure. Allopurinol and its active metabolite oxypurinol showed considerable promise in the treatment of these conditions both in experimental animals and in small-scale human clinical trials. Although some of the beneficial effects of these compounds may be unrelated to the inhibition of the XO, the encouraging findings rekindled significant interest in the development of additional, novel series of XO inhibitors for various therapeutic indications. Here we present a critical overview of the effects of XO inhibitors in various pathophysiological conditions and also review the various emerging therapeutic strategies offered by this approach.

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  1. Giler S, Eshel Y, Pinkhas J, Ventura E, Levy E, Urea I, Sperling O, de Vries A. Elevation of serum xanthine oxidase activity following halothane anesthesia in man. Experientia. 1977;33:1356–1358. doi: 10.1007/BF01920178. [DOI] [PubMed] [Google Scholar] · DOI
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Authors
Pacher, P., Nivorozhkin, A., & Szabó, C.
Affiliations
  • National Institutes of Health (US)
  • Semmelweis University (HU)
Venue
Pharmacological Reviews
Publisher
Elsevier BV
Published
2006-03
Volume
58
Issue
1
Pages
87-114
ISSN
0031-6997 (ISSN-L)
OpenAlex
W2119515450
Cited by
1,218
References
451
Citations by year
2026: 34 · 2025: 51 · 2024: 60 · 2023: 56 · 2022: 83 · 2021: 75 · 2020: 85 · 2019: 84 · 2018: 72 · 2017: 71 · 2016: 67 · 2015: 76 · 2014: 75 · 2013: 67 · 2012: 72
FWCI
5.50
Type
journal article
Language
en
Open access
Locations
  • Pharmacological Reviews (publishedVersion)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
Funders
  • National Institutes of Health
  • National Institute on Alcohol Abuse and Alcoholism (Z01AA000375)
Topics
  • Health Sciences › Medicine › Nephrology › Gout, Hyperuricemia, Uric Acid
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Molecular Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Physiology › Adenosine and Purinergic Signaling
Keywords
xanthine oxidase inhibitors, allopurinol, oxypurinol, gout, hyperuricemia, ischemic injury, vascular injury, inflammation, chronic heart failure, drug repurposing
MeSH terms
Allopurinol, Animals, Cardiovascular Diseases, Enzyme Inhibitors, Humans, Superoxides, Xanthine Oxidase, Inflammatory Bowel Diseases, Reperfusion Injury

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