Last update 21 Jun 2024
Epaminurad
Last update 21 Jun 2024
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms SIM-0295, SIM-1909-13, SIM-295 + [3] |
Target |
Mechanism URAT1 inhibitors(Uric acid transporter 1 inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Inactive Organization- |
Drug Highest PhasePhase 3 |
First Approval Date- |
Regulation- |
Related
10
Clinical Trials associated with EpaminuradA 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
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
An Open, Single Dose Designed Clinical Study to Evaluate Safety and Pharmacokinetic/Pharmacodynamic Characteristics After Oral Administration of URC102 in Patients With Renal Impairment Under Fasted Conditions and Healthy Adult Volunteers Under Fasted and Fed Conditions
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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9
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 ; Hou, Zihan ; Ma, Aijinxiu ; 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.
02 Jan 2021Xenobiotica; the fate of foreign compounds in biological systemsQ4 · MEDICINE
Main contribution of UGT1A1 and CYP2C9 in the metabolism of UR-1102, a novel agent for the treatment of gout
Q4 · MEDICINE
Article
Author: Yamauchi, Tsuyoshi ; Nakagawa, Toshito ; Yamane, Mizuki ; Igarashi, Fumihiko
UR-1102, a novel uricosuric agent for treating gout, has been confirmed to exhibit a pharmacological effect in patients. We clarified its metabolic pathway, estimated the contribution of each metabolic enzyme, and assessed the impact of genetic polymorphisms using human in vitro materials. Glucuronide, sulfate and oxidative metabolites of UR-1102 were detected in human hepatocytes. The intrinsic clearance by glucuronidation or oxidation in human liver microsomes was comparable, but sulfation in the cytosol was much lower, indicating that the rank order of contribution was glucuronidation ≥ oxidation > sulfation. Recombinant UGT1A1 and UGT1A3 showed high glucuronidation of UR-1102. We took advantage of a difference in the inhibitory sensitivity of atazanavir to the UGT isoforms and estimated the fraction metabolised (fm) with UGT1A1 to be 70%. Studies using recombinant CYPs and CYP isoform-specific inhibitors showed that oxidation was mediated exclusively by CYP2C9. The effect of UGT1A1 and CYP2C9 inhibitors on UR-1102 metabolism in hepatocytes did not differ markedly between the wild type and variants.
2
News (Medical) associated with Epaminurad100 Deals associated with Epaminurad
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R&D Status
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Gout | Phase 3 | KR | 14 Mar 2023 | |
| Hyperuricemia | Phase 2 | KR | 24 Jul 2014 |
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Clinical Result
Clinical Result
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Phase 2 | Gout serum uric acid (sUA) levels | - | Placebo | tijlrrdbcb(ghjoklshzd) = reported as a serious AE, but unrelated to the study drug aymwviizzq (vuvhqkztyh ) View more | Positive | 07 Nov 2017 | |
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