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

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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

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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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Authors: Pacher, P., Nivorozhkin, A., & Szabó, C.
Affiliations: National Institutes of Health (US)
Semmelweis University (HU)
ORCID: Pacher, Pál
Nivorozhkin, Alex
Szabó, Csaba
Venue: Pharmacological Reviews
Publisher: Elsevier BV
Published: 2006-03
Volume: 58
Issue: 1
Pages: 87-114
ISSN: 0031-6997 (ISSN-L)
DOI: 10.1124/pr.58.1.6
PMC: PMC2233605
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: green
www.ncbi.nlm.nih.gov
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
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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Therapeutic Effects of Xanthine Oxidase Inhibitors: Renaissance Half a Century after the Discovery of Allopurinol

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