Delving into the Latest Updates on URAT1/Xanthine oxidase inhibitors(HEC Pharm) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

URAT1 x Xanthine oxidase

Action

inhibitors

Mechanism

URAT1 inhibitors(Uric acid transporter 1 inhibitors), Xanthine dehydrogenase inhibitors

Therapeutic Areas

Immune System DiseasesCongenital DisordersEndocrinology and Metabolic Disease+ [2]

Active Indication

Gout

Inactive Indication-

Originator Organization

HEC Pharm Co., Ltd.

Active Organization

HEC Pharm Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC16H8FNO4

InChIKeyVBWLCOGQAODFLX-UHFFFAOYSA-N

CAS Registry2089040-93-5

The main uric acid-lowering agents in clinical use for hyperuricemia and gout are xanthine oxidase (XO) inhibitors or urate transporter 1 (URAT1) inhibitors. While these therapies can partially control the disease, they have various limitations. The development of XO/URAT1 dual inhibitors offers the potential to enhance therapeutic potency and reduce toxicity compared with single-target inhibitors. Through scaffold hopping from the XO inhibitor febuxostat (2) and the URAT1 inhibitor probenecid (3), followed by structure-activity relationship (SAR) studies, we identified compound 27 as a potent dual inhibitor of XO and URAT1. Compound 27 demonstrated significant dual inhibition in vitro (XO IC₅₀ = 35 nM; URAT1 IC₅₀ = 31 nM) and exhibited favorable pharmacology and pharmacokinetic (PK) profiles in multiple species including monkeys. Furthermore, toxicity studies in rats and monkeys revealed general safety profiles, supporting that compound 27 emerges as a promising novel drug candidate with potent XO/URAT1 dual inhibition for the treatment of gout.

100 Deals associated with URAT1/Xanthine oxidase inhibitors(HEC Pharm)

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