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Last update 29 May 2025
Epaminurad
Last update 29 May 2025
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms SIM-0295, SIM-1909-13, SIM-295 + [3] |
Target |
Action inhibitors |
Mechanism URAT1 inhibitors(Uric acid transporter 1 inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Inactive Organization- |
License Organization |
Drug Highest PhasePhase 3 |
First Approval Date- |
Regulation- |
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Structure/Sequence
Molecular FormulaC14H10Br2N2O3 |
InChIKeyZMVGQIIOXCGAFV-UHFFFAOYSA-N |
CAS Registry1198153-15-9 |
Related
11
Clinical Trials associated with EpaminuradNCT06665425
An Open-label, Crossover, Phase 1 Clinical Trial to Evaluate the Pharmacokinetic/pharmacodynamic Drug-drug Interactions and Safety/tolerability of Epaminurad and C2406 When Co-administered in Healthy Adults
NCT06435442
A Phase 1 Study to Evaluate the Safety and PK/PD Drug-drug Interaction Between Epaminurad and Naproxen or to Assess the Safety and Multiple-Dose PK/PD Characteristics of Epaminurad in Healthy Volunteers
NCT05815901
A Multi-center, Randomized, Double-blind, Active-controlled, Therapeutic Confirmatory, Phase III Study to Compare and Evaluate the Efficacy and Safety of Epaminurad With Febuxostat in Gout Patients
100 Clinical Results associated with Epaminurad
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100 Translational Medicine associated with Epaminurad
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100 Patents (Medical) associated with Epaminurad
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12
Literatures (Medical) associated with Epaminurad02 Dec 2023Expert opinion on drug metabolism & toxicology
Overview of the pharmacokinetics and pharmacodynamics of URAT1 inhibitors for the treatment of hyperuricemia and gout
Review
Author: Zhao, Xu ; Ma, Aijinxiu ; Hou, Zihan ; Mao, Jiale ; Song, Danni
INTRODUCTION:
Hyperuricemia is a common metabolic disease, which is a risk factor for gouty arthritis and ureteral stones and may also lead to cardiovascular and chronic kidney disease (CDK). Therefore, hyperuricemia should be treated early. Xanthine oxidase inhibitors (XOIs) and uricosuric agents (UAs), which target uric acid, are two types of medications that are used to treat gout and hyperuricemia. XOIs stop the body from producing excessive uric acid, while UAs eliminate it rapidly via the kidneys. Urate transporter 1 (URAT1) belongs to the organic anion transporter family (OAT) and is specifically localized to the apical membrane of the epithelial cells of proximal tubules. Unlike other organic anion transporter family members, URAT1 identifies and transports organic anions that are primarily responsible for urate transport.
AREAS COVERED:
This article reviews the pharmacokinetics and pharmacodynamics of the existing URAT1 inhibitors to serve as a reference for subsequent drug studies.
EXPERT OPINION:
The URAT1 inhibitors that are currently used as clinical drugs mainly include dotinurad, benzbromarone, and probenecid. Results indicate that RDEA3170 may be the most promising inhibitor, in addition to SHR4640, URC-102, and MBX-102, which are in the early stages of development.
01 May 2023Expert opinion on investigational drugs
Model Informed Development of SIM0295 in Patients with Gout and Hyperuricemia and Healthy Volunteers Using a Population Pharmacokinetics/ Pharmacodynamics Approach.
Article
Author: Huang, Qin ; Chen, Yueting ; Zhang, Xiaoyu ; Kim, Jin Sook ; Jiao, Zheng ; Yang, Yang ; Xu, Shansen ; Shu, Pan ; Wang, Chenyu
BACKGROUND:
SIM0295, a novel inhibitor of human uric acid transporter 1 (hURAT1), is used to treat patients with gout and hyperuricemia. This study aimed to develop population pharmacokinetics and pharmacodynamics (popPK/PD) models of SIM0295 and explore potential covariates to inform clinical drug development.
RESEARCH DESIGN AND METHODS:
Data were obtained from four phase I studies conducted in healthy Korean and Chinese subjects and two phase II studies conducted in Korean patients with gout and hyperuricemia. The popPK/PD model of SIM0295 was developed using nonlinear mixed effects modeling.
RESULTS:
SIM0295 pharmacokinetics was described using a two-compartment model with the absorption of four transit compartments and first-order elimination. PK parameters were normalized to weight via allometric scaling. Food was identified as a factor significantly affecting the absorption rate, with no clinical relevance. The sigmoid Emax model with a semi-mechanism of inhibition of serum uric acid (sUA) reabsorption was used to describe the exposure-response relationship. Additionally, Monte Carlo simulations demonstrated that approimately 9 mg/day of SIM0295 for 7 days could achieve the maximum decrease in sUA.
CONCLUSION:
The established popPK/PD model characterized the dose-exposure-response relationship for SIM0295 in healthy subjects and patients with gout and hyperuricemia and could be used to inform the drug development.
01 Dec 2021Bioorganic chemistryQ2 · CHEMISTRY
Novel natural scaffold as hURAT1 inhibitor identified by 3D-shape-based, docking-based virtual screening approach and biological evaluation
Q2 · CHEMISTRY
Article
Author: Chen, Xinhua ; Chang, Shan ; Tian, Yuanxin ; Li, Zhonghuang ; Zhao, Zean ; Wan, Shanhe ; Zhang, Jiajie ; Shen, Yudong ; Wu, Ting ; Pang, Jianxin ; Luo, Jiajun
As a promising therapeutic target for gout, hURAT1 has attracted increasing attention. In this work, we identified a novel scaffold of hURAT1 inhibitors from a personal natural product database of verified herb-treated gout. First, we constructed more than 800 natural compounds from Chinese medicine that were verified to treat gout. Following the application of both shape-based and docking-based virtual screening (VS) methods, taking into account the shape similarity and flexibility of the target, we identified isopentenyl dihydroflavones that might inhibit hURAT1. Specifically, 9 compounds with commercial availability were tested with biochemical assays for the inhibition of 14C-uric acid uptake in high-expression hURAT1 cells (HEK293-hURAT1), and their structure-activity relationship was evaluated. As a result, 8-isopentenyl dihydroflavone was identified as a novel scaffold of hURAT1 inhibitors since isobavachin (DHF3) inhibited hURAT1 with an IC50 value of 0.39 ± 0.17 μM, which was comparable to verinurad with an IC50 value of 0.32 ± 0.23 μM. Remarkably, isobavachin also displayed an eminent effect in the decline of serum uric acid in vivo experiments. Taken together, isobavachin is a promising candidate for the treatment of hyperuricemia and gout.
3
News (Medical) associated with Epaminurad23 Apr 2021
100 Deals associated with Epaminurad
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R&D Status
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Gout | Phase 3 | United States | 14 Mar 2023 | |
| Primary gout | Phase 2 | United States | 21 Jan 2019 | |
| Hyperuricemia | Phase 2 | United States | 24 Jul 2014 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
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Phase 2 | Gout serum uric acid (sUA) levels | - | Placebo | aapafhrikp(tjqeedxlqj) = reported as a serious AE, but unrelated to the study drug ilmlaujefs (iiuwspfkkp ) View more | Positive | 07 Nov 2017 | |
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