# Gout management: Patent analytics and computational drug design explores URAT1 inhibitors landscape

**Authors:** Jiaxin Zhang, Liang Hong, Wenfei Xu, Xin Zhang, Huina Fu, Xinan Song, Jing Zhao

PMC · DOI: 10.1371/journal.pone.0328559 · PLOS One · 2025-08-13

## TL;DR

This paper explores the development of URAT1 inhibitors for gout treatment by analyzing patents and using computational methods to identify promising drug candidates.

## Contribution

The study combines patent analytics with computational drug design to identify novel URAT1 inhibitors and their scaffold diversity.

## Key findings

- Global research on URAT1 inhibitors is highly active, with China, the US, Japan, and Europe leading.
- Most patents focus on new compounds, suggesting significant potential for novel drug development.
- Molecular docking showed ideal binding affinities for most compounds, identifying top BM scaffolds.

## Abstract

Gout, caused by hyperuricemia, has a detrimental impact on patients’quality of life. The urate transporter 1 (URAT1) stands out as a key therapeutic target. However, its clinical development remains uncertain. This study aims to explore the landscape of URAT1 inhibitors by combining global patent analytics with computational drug design. We utilized the Derwent Innovation platform to analyze patents (from 2005 to 2024). Molecular docking was performed on 73.96% of novel compounds using AutoDock Vina. Additionally, scaffold diversity was analyzed using the Bemis-Murcko (BM) scaffold approach. A total of 2,195 entries were screened and eventually narrowed down to 1,056 high-value entries. The global research on URAT1 inhibitors is highly active, with China, the US, Japan, and Europe leading. Most patents are new compounds, indicating significant potential for novel drug development. Molecular docking showed ideal binding affinities for most compounds. The top five BM scaffolds were identified and compared with marketed drugs. This study highlights the potential for developing new URAT1 inhibitors. The identified compounds and scaffolds offer promising starting points for further drug development. Future work should focus on experimental validation and exploring clinical potential.

## Linked entities

- **Proteins:** SLC22A12 (solute carrier family 22 member 12)
- **Diseases:** gout (MONDO:0005393)

## Full-text entities

- **Genes:** OAT (ornithine aminotransferase) [NCBI Gene 4942] {aka GACR, HOGA, OATASE, OKT}, CASP1 (caspase 1) [NCBI Gene 834] {aka ICE, IL1BC, P45}, PPIG (peptidylprolyl isomerase G) [NCBI Gene 9360] {aka CARS-Cyp, CYP, SCAF10, SRCyp}, SLC22A12 (solute carrier family 22 member 12) [NCBI Gene 116085] {aka OAT4L, RST, UAT, URAT1, hURAT1}, UOX (urate oxidase (pseudogene)) [NCBI Gene 391051] {aka UOXP, URICASE}, PPARG (peroxisome proliferator activated receptor gamma) [NCBI Gene 5468] {aka CIMT1, FPLD3, GLM1, NR1C3, PPARG1, PPARG2}, SLC22A11 (solute carrier family 22 member 11) [NCBI Gene 55867] {aka OAT4, hOAT4}, CTBS (chitobiase) [NCBI Gene 1486] {aka CTB}
- **Diseases:** chronic kidney disease (MESH:D051436), insulin resistance (MESH:D007333), inflammatory arthritis (MESH:D001168), renal (MESH:D006030), toxicity (MESH:D064420), metabolic syndrome (MESH:D024821), Gout (MESH:D006073), hypertriglyceridemia (MESH:D015228), nausea (MESH:D009325), non-alcoholic fatty liver disease (MESH:D065626), hypercholesterolemia (MESH:D006937), hyperuricemia (MESH:D033461), gastrointestinal intolerance (MESH:D005767), metabolic disorder (MESH:D008659), abnormal liver function (MESH:D056486), inflammation (MESH:D007249)
- **Chemicals:** monosodium urate (MESH:D014527), WO2007138998A1 (-), Probenecid (MESH:D011339), febuxostat (MESH:D000069465), Verinurad (MESH:C000628929), sulfinpyrazone (MESH:D013442), Arhalofenate (MESH:C000593473), O (MESH:D010100), Purine (MESH:C030985), Hydrogen (MESH:D006859), guanine (MESH:D006147), digallic acid (MESH:C067648), glucose (MESH:D005947), adenine (MESH:D000225), inosine (MESH:D007288), Benzbromarone (MESH:D001553), water (MESH:D014867), salinomycin (MESH:C010327), Dotinurad (MESH:C000706811), Allopurinol (MESH:D000493), xanthine (MESH:D019820), S (MESH:D013455), Lesinurad (MESH:C000593471)
- **Species:** Homo sapiens (human, species) [taxon 9606]

## Full text

_Full body text omitted from this summary view._ Fetch the complete paper as Markdown: https://tomesphere.com/paper/PMC12349300/full.md

## Figures

10 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12349300/full.md

## References

58 references — full list in the complete paper: https://tomesphere.com/paper/PMC12349300/full.md

---
Source: https://tomesphere.com/paper/PMC12349300