主要目的：评价硫酸舒欣啶片 1200mg BID治疗伴或不伴非持续性室性心动过速的室性早搏患者 4 周结束时早搏次数减少的有效率是否非劣于盐酸美西律片 150mg TID。次要目的：评价硫酸舒欣啶片 1200 mg BID 治疗伴或不伴非持续性室性心动过速的室性早搏患者 24 周的安全性，描述硫酸舒欣啶片群体药代动力学特性。

开始日期2021-05-31

申办/合作机构

中国科学院上海药物研究所

NCT04650542 / Completed临床1期

Open-Label, Two-Period Phase 1 Study in Healthy Subjects to Evaluate the Potential Effect of Multiple Doses of Paroxetine on the Pharmacokinetics and Safety of HBI-3000

Drug-Drug Interaction Study of HBI-3000 and Paroxetine in Healthy Adult Male and Female Subjects

开始日期2021-02-21

申办/合作机构

HUYA Bioscience International LLC

100 项与硫酸舒欣啶相关的临床结果

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100 项与硫酸舒欣啶相关的转化医学

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100 项与硫酸舒欣啶相关的专利（医药）

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项与硫酸舒欣啶相关的文献（医药）

2023-05-01·Pharmaceutical research

Retraction Note: Characterization of Preclinical Pharmacokinetic Properties and Prediction of Human PK Using a Physiologically Based Pharmacokinetic Model for a Novel Anti-Arrhythmic Agent Sulcardine Sulfate.

作者: Sun, Mengqi ; Ning, Chen ; Zhao, Di ; Lu, Yang ; Li, Ning ; Zhang, Mei ; Wang, Yao ; Zhang, Yongjie ; Su, Shengdi ; Kong, Dexuan ; Bian, Yueying ; Chen, Xijing ; Ren, Chang ; Wang, Yucong ; Cheng, Yujie

2021-11-01·Pharmaceutical research3区 · 医学

RETRACTED ARTICLE: Characterization of Preclinical Pharmacokinetic Properties and Prediction of Human PK Using a Physiologically Based Pharmacokinetic Model for a Novel Anti-Arrhythmic Agent Sulcardine Sulfate

3区 · 医学

Article

作者: Sun, Mengqi ; Ning, Chen ; Zhao, Di ; Lu, Yang ; Li, Ning ; Zhang, Mei ; Wang, Yao ; Zhang, Yongjie ; Su, Shengdi ; Chen, Xijing ; Kong, Dexuan ; Bian, Yueying ; Ren, Chang ; Wang, Yucong ; Cheng, Yujie

PURPOSE:

Sulcardine sulfate (Sul) is a novel antiarrhythmic agent with promising pharmacological properties, which is currently being evaluated in several clinical trials as an oral formulation. To meet the medication needs of patients with acute conditions, the injection formulation of Sul has been developed. The objective of this study was to systemically investigate the pharmacokinetic profiles of Sul after intravenous infusion.

METHODS:

This research included the plasma protein binding and metabolic stability studies in vitro, plasma pharmacokinetics, biodistribution, excretion studies in animals, and the prediction of the clinical PK of Sul injection using a physiologically based pharmacokinetics (PBPK) model.

RESULTS:

The metabolic stability was similarly in dogs and humans but lower in rats. The plasma protein binding rates showed a concentration-dependent manner and species differences. The pharmacokinetic behavior after intravenous administration was linear in rats within the dose range of 30-90 mg/kg, but nonlinear in dogs within 30-60 mg/kg. Sul could be rapidly and widely distributed in multiple tissues after intravenous administration. About 12% of the parent compound were excreted via the urine and only a small fraction via bile and feces,and eight metabolites were found and identified in the rat excretion. The PBPK models were developed and simulated the observed PK date well in both rats and dogs. The PBPK model refined with human data predicted the PK characteristics of the first intravenous infusion of Sul in human.

CONCLUSIONS:

Our study systematically explored the pharmacokinetic characteristics of Sul and successfully developed the PBPK model to predict of its clinical PK.

2019-02-01·European journal of pharmacology3区 · 医学

Characteristics of hERG and hNav1.5 channel blockade by sulcardine sulfate, a novel anti-arrhythmic compound

3区 · 医学

Article

作者: Lu Gan ; Weihai Chen ; Yiping Wang

Sulcardine sulfate (sulcardine) is a novel anti-arrhythmic compound, which blocks multiple channels and was shown to be safe and tolerated in clinical trials. The aim of the present study was to investigate the electrophysiological characteristics of sulcardine on the hERG and hNav1.5 channels. The hERG and hNav1.5 channels were heterologously stably expressed in human embryonic kidney 293 cells, and the effects of sulcardine on the hERG and hNav1.5 channels were recorded using the standard whole-cell patch-clamp technique. Sulcardine inhibited hERG channels in a concentration-dependent and reversible manner (IC₅₀ = 94.3 μM). In addition, sulcardine shifted the activation curve of hERG channels to more negative potentials. The relative block of sulcardine on hERG channels was close to zero at the time point corresponding to channel opening, which was achieved by applying a depolarizing voltage, and quickly increased afterward. Sulcardine inhibited hNav1.5 channels in a concentration-dependent and reversible manner (IC₅₀ = 15.0 μM) and shifted the inactivation curve of hNav1.5 channels to more negative potentials. The blockade of sulcardine on hNav1.5 channels was use-dependent. In conclusion, sulcardine is a potent hNav1.5 channel blocker with a mild inhibitory effect on hERG channels and preferentially binds to both hERG and hNav1.5 channels in the open and inactivated states rather than in the resting state.

项与硫酸舒欣啶相关的新闻（医药）

2022-06-14

·PRNewswire

HUYABIO INTERNATIONAL ANNOUNCES INITIATION OF HBI-3000 PHASE 2 TRIAL

SAN DIEGO, June 14, 2022 /PRNewswire/ -- HUYABIO International today announced that the first three patients had been dosed in an ongoing Phase 2 study of HUYABIO's novel drug for pharmacological cardioversion of atrial fibrillation (AF). Dr. Mireille Gillings, President, CEO & Executive Chair, said, "We are excited to proceed with dosing AF patients in our Phase 2 trial of HBI-3000. AF is a growing global problem and HUYABIO's drug is well-positioned to provide a new pharmacological treatment for patients, many of whom would otherwise get electrically cardioverted which can be both stressful and painful." The study is evaluating pharmacological cardioversion of acute AF. Cardioversion aims to restore a normal heart rate and rhythm in AF patients and is often done by high energy electrical shock. The Phase 2 trial HBI-3000-402 is a two-stage, serial cohort dose escalation and expansion study of a single intravenous infusion of HBI-3000 in patients with AF between 2 and 72 hours. Denis Roy, MD, Montreal Heart Institute and Chief Investigator of the trial, said, "Demonstrating efficacy of HBI-3000 in this trial is an important step towards development of a new therapeutic option to AF patients." AF is a serious condition that affects more than 3.5 million patients in the US and 30 million worldwide. There is a significant need for safer and more effective pharmacological interventions to treat AF, as the current standard of care treatments have poor safety and efficacy profiles and the alternative, electrical cardioversion, requires fasting and sedation and can be anxiety provoking for patients. About HBI-3000 HBI-3000 is a multi-ion channel blocker with in vitro inhibitory effects on INa-Peak, INa-Late, ICa, L and IKr being developed by HUYABIO International for the conversion of recent onset atrial fibrillation. The drug's preclinical and clinical pharmacology supports the potential of HBI-3000 to restore sinus rhythm in Atrial Fibrillation. The drug has demonstrated a low risk for proarrhythmia in preclinical testing. Data from the first in human Phase 1 trial of the IV formulation were presented during a poster session at the American Heart Association 2019 annual meeting. . About HUYABIO International HUYABIO is the leader in accelerating the global development of novel biopharmaceutical product opportunities originating in China enabling faster, more cost-effective and lower-risk drug development in global markets. Through extensive collaboration with biopharmaceutical, academic and commercial organizations, it has built the largest China-sourced compound portfolio covering all therapeutic areas. With offices in the US, Japan, South Korea, Canada, Ireland and eight strategic locations across China, the company has become a partner of choice to accelerate product development and maximize value globally. For more information, please visit . Contact Details: Yiota Merianos Corporate Communications +1.858.353.1217 ymerian[email protected] SOURCE HUYABIO International

AHA会议

2021-04-27

·GlobeNewswire

Atrial Fibrillation Pipeline Drugs and Companies Insight Report

Los Angeles, USA, April 26, 2021 (GLOBE NEWSWIRE) -- Atrial Fibrillation Pipeline Drugs and Companies Insight Report: Analysis of Clinical Trials, Therapies, Mechanism of Action, Route of Administration, and Developments The global demand for Atrial Fibrillation treatment options is emerging swiftly, driven by consumption in major emerging markets. As more growth opportunities will surge, several companies such as ARCA biopharma, AbbVie, Hanmi Pharmaceutical, Espero BioPharma, Vivasc Therapeutics, HUYA Bioscience, Novartis, Acesion Pharma, and others are working on Atrial Fibrillation pipeline. DelveInsight’s “Atrial Fibrillation Pipeline Insight” report provides comprehensive insights about 17+ companies and 17+ pipeline drugs in the Atrial Fibrillation pipeline landscapes. It comprises Atrial Fibrillation pipeline drug profiles, including clinical and non-clinical stage products. It also includes the Atrial Fibrillation therapeutics assessment by product type, stage, route of administration, and molecule type and further highlights the inactive Atrial Fibrillation pipeline products. Some of the key takeaways of the Atrial Fibrillation Pipeline Report Get an overview of pipeline landscape @ Atrial Fibrillation Clinical Trials Analysis Atrial Fibrillation is an irregular heartbeat that can lead to blood clots, stroke, heart failure and other heart-related complications. The atria beat chaotically and irregularly out of coordination with the ventricles of the heart. Atrial Fibrillation Emerging Drugs Etripamil, the lead investigational product, is developed to be a rapid-response therapy for episodic cardiovascular conditions. The novel calcium channel blocker is self-administered through a nasal spray that may shift the current treatment paradigm for many patients with Paroxysmal supraventricular tachycardia (PSVT) in the emergency department to the at-home setting. Milestone is conducting a thorough development program for etripamil, with Phase 3 trials underway in PSVT, and intends to start a Phase 2 proof-of-concept trial in patients with atrial fibrillation with rapid ventricular rate, with subsequent studies anticipated in other conditions where calcium channel blockers are utilised. OMT-28 is a stable synthetic small molecule analogue of the natural omega-3 fatty acid metabolite 17, 18-EEQ, which has a structure optimised to confer efficacy, safety, and oral availability. The compound has shown its anti-arrhythmic, cardioprotective, and anti-fibrotic potential in different in vivo models. Presently, it is in phase 2 of clinical trials for the Atrial Fibrillation treatment. HBI-3000 is a multi-ion channel blocker with effects on INa-Peak, INa-Late, ICa, L, and IKr with similar in vitro potencies across these several ion channels in human atrial cardiomyocytes. It is being developed by HUYA Bioscience International® (HUYABIO™) for the conversion of recent-onset Atrial Fibrillation. It is currently undergoing phase 1 of clinical trials. It is based on the inhibition of SK channels - ion channels present in the atria that regulate the cardiac rhythm. Inhibiting these ion channels with a functionally atrial selective drug help avoid harmful effects on the ventricles. Targeting the SK channels thereby comprises a novel and promising approach for an effective treatment for Atrial Fibrillation with an anticipated higher safety and tolerability profile. For further information, refer to the detailed report @ Atrial Fibrillation Pipeline Therapeutics Scope of Atrial Fibrillation Pipeline Drug Insight Key Questions regarding Current Atrial Fibrillation Treatment Landscape and Emerging Therapies Answered in the Pipeline Report Table of Contents Get a customised pipeline report @ Atrial Fibrillation Drugs Pipeline Report Related Reports DelveInsight's Atrial Fibrillation - Market Insights, Epidemiology and Market Forecast - 2030 report provides a detailed overview of the disease and a depth understanding of historical and forecasted epidemiology. DelveInsight's Atrial Fibrillation - Epidemiology Forecast 2030 report delivers an in-depth understanding of the disease, historical, and forecasted epidemiology of Atrial Fibrillation in the United States, EU5 (Germany, France, Italy, Spain, and the United Kingdom), and Japan. DelveInsight’s Atrial Flutter Market Insights, Epidemiology and Market Forecast - 2030 report provides a detailed overview of the disease and a depth understanding of historical and forecasted epidemiology. DelveInsight's Cystic fibrosis - Market Insights, Epidemiology and Market Forecast - 2030 report provides a detailed overview of the disease and a depth understanding of historical and forecasted epidemiology. DelveInsight’s Fibrocystic Breast Condition Market Insights, Epidemiology and Market Forecast - 2030 report provides a detailed overview of the disease and a depth understanding of historical and forecasted epidemiology. About DelveInsightDelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports Pharma companies by providing comprehensive end-to-end solutions to improve their performance. It also proffers Healthcare Consulting Services, which benefits in market analysis to accelerate the business growth and overcome challenges with a practical approach.

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适应症	最高研发状态	国家/地区	公司	日期
室性早搏	临床3期	中国	中国科学院上海药物研究所	2021-05-31
心房颤动	临床2期	美国	HUYA Bioscience International LLC	2021-06-01
心房颤动	临床2期	波斯尼亚和黑塞哥维那	HUYA Bioscience International LLC	2021-06-01
心房颤动	临床2期	加拿大	HUYA Bioscience International LLC	2021-06-01
心房颤动	临床2期	新西兰	HUYA Bioscience International LLC	2021-06-01
心房颤动	临床2期	塞尔维亚	HUYA Bioscience International LLC	2021-06-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ESC2024	N/A	心房颤动	-	Sulcardine (HBI-3000)	鑰繭顧齋範鹹選獵夢願(構夢觸範憲醖顧襯鹽積) = nausea and headache (n=2 each [5.1%]) 夢簾鬱網鬱鏇願顧選蓋 (醖鏇衊獵糧蓋鏇鹹觸繭 ) 更多	-	2024-09-01