Efficacy and Safety of Vicagrel in Patients With With Acute Coronary Syndrome (ACS) Undergoing Percutaneous Coronary Intervention (PCI): a Multi-center, Randomized, Double-blind, Double-dummy , Parallel-controlled, Phase III Trial

This is a multi-center, randomized, double-blind, double-dummy, parallel-controled, phase III trial, aiming to evaluate the effectiveness and safety of long-term continuous administration of Vicagrel capsules in ACS patients undergoing PCI.

Start Date06 Sep 2024

Sponsor / Collaborator

Jiangsu Vcare PharmaTech Co., Ltd.

CTR20242930

/ RecruitingPhase 3

评价维卡格雷在拟行经皮冠状动脉介入术（PCI）的急性冠脉综合征（ACS）患者中有效性、安全性的多中心、随机、双盲、双模拟、平行对照的III期临床研究

[Translation] A multicenter, randomized, double-blind, double-dummy, parallel-controlled phase III clinical study to evaluate the efficacy and safety of vicagrelor in patients with acute coronary syndrome (ACS) who are scheduled to undergo percutaneous coronary intervention (PCI)

以氯吡格雷片为对照，评价维卡格雷胶囊在拟行经皮冠状动脉介入术（PCI）的急性冠脉综合征（ACS）患者中预防心血管事件发生的有效性和安全性。

[Translation]

To evaluate the efficacy and safety of vicagrelor capsules in preventing cardiovascular events in patients with acute coronary syndrome (ACS) who were scheduled to undergo percutaneous coronary intervention (PCI), using clopidogrel tablets as a control.

Start Date06 Sep 2024

Sponsor / Collaborator

Jiangsu Vcare PharmaTech Co., Ltd.

[+1]

CTR20222479

/ RecruitingPhase 1

一项在健康成年受试者中评估奥美拉唑对维卡格雷胶囊药代动力学及药效动力学影响的临床试验

[Translation] A clinical trial evaluating the effect of omeprazole on the pharmacokinetics and pharmacodynamics of vicagrelor capsules in healthy adult subjects

主要目的：评价奥美拉唑对健康受试者单次口服维卡格雷胶囊后的药代动力学及药效动力学影响。次要目的：评价健康受试者单次口服维卡格雷胶囊及与奥美拉唑联合用药的安全性。

[Translation]

Primary objective: To evaluate the effect of omeprazole on the pharmacokinetics and pharmacodynamics of Vicagrelor capsules after a single oral administration in healthy subjects. Secondary objective: To evaluate the safety of Vicagrelor capsules in combination with omeprazole after a single oral administration in healthy subjects.

Start Date14 Nov 2022

Sponsor / Collaborator

Jiangsu Vcare PharmaTech Co., Ltd.

[+1]

100 Clinical Results associated with Vicagrel

100 Translational Medicine associated with Vicagrel

100 Patents (Medical) associated with Vicagrel

Literatures (Medical) associated with Vicagrel

01 Dec 2024·BIOCHEMICAL PHARMACOLOGY

Sex differences in the metabolic activation of and platelet response to vicagrel in mice: Androgen as a key player

Article

Author: Zheng, Zhao-Dong ; Jia, Yu-Meng ; Tai, Ting ; Wang, Jin ; Jiang, Li-Ping ; Feng, Lei ; Li, Xue-Mei ; Ding, Pei-Jie ; Yin, Na ; Fu, Min ; Yang, Li ; Xie, Hong-Guang ; Sun, Ya-Lan ; Ji, Jin-Zi ; Zhu, Ting ; Mi, Qiong-Yu ; Han, Hao-Ru ; Duan, Fu-Yang

As a biological variable, sex influences the metabolism of and/or response to certain drugs. Vicagrel is being developed as an investigational new drug in China; however, it is unknown whether sex could affect its metabolic activation and platelet responsiveness. This study aimed to determine whether such differences could exist, and to elucidate the mechanisms involved. Orchiectomized (ORX) or ovariectomized (OVX) mouse models were used to investigate the effects of androgens or estrogens on the metabolic activation of and platelet response to vicagrel. Plasma vicagrel active metabolite H4 concentrations, platelet inhibition of vicagrel, and protein levels of intestinal hydrolases Aadac and Ces2 were measured, respectively. Further, p38-MAPK signaling pathway was enriched, whose role was determined using SB202190. Results showed that female mice exhibited significantly elevated systemic exposure of H4 and enhanced platelet responses to vicagrel than males, and that protein expression levels of Aadac and Ces2 differed by sex. OVX mice exhibited less changes than sham mice. ORX mice exhibited increases in protein levels of intestinal hydrolases, systemic exposure of H4, and platelet inhibition of vicagrel, but dihydrotestosterone (DHT) reversed these changes in ORX mice and suppressed these changes in OVX mice. Phosphorylated p38 levels were reduced in female or ORX mice but increased in ORX mice by DHT. SB202190 reversed DHT-induced changes observed in ORX mice. We concluded that sex differences exist in metabolic activation of and platelet response to vicagrel in mice through elevation of p38 phosphorylation by androgens, suggesting sex-based vicagrel dosage adjustments for patient care.

20 Oct 2024·XENOBIOTICA

The metabolic activation of and platelet response to vicagrel vary with P-glycoprotein deficiency, rather than P-glycoprotein inhibition, in mice

Article

Author: Wang, Jin ; Tai, Ting ; Li, Xue-Mei ; Shao, Yuan-Yuan ; Li, Hao-Dong ; Wu, Yu ; Jiang, Li-Ping ; Fu, Min ; Xie, Hong-Guang ; Zheng, Zhao-Dong ; Tang, Ke ; Ji, Jin-Zi ; Ding, Pei-Jie ; Mi, Qiong-Yu

This study aimed to determine changes in the hydrolysis of vicagrel, a substrate drug of arylacetamide deacetylase (Aadac) and carboxylesterase 2 (Ces2), in P-glycoprotein (P-gp)-deficient or P-gp-inhibited mice and to elucidate the mechanisms involved.Male wild-type (WT) and P-gp knock-out (KO) mice were used to investigate the systemic exposure of vicagrel thiol active metabolite H4 and platelet response to vicagrel, and the mRNA and protein expression levels of intestinal Aadac and Ces2. Moreover, WT mice were administered vicagrel alone or in combination with elacridar (a potent P-gp inhibitor) to determine drug-drug interactions.Compared with WT mice, P-gp KO mice exhibited significant increases in the systemic exposure of H4, the protein expression levels of intestinal Aadac and Ces2, and inhibition of ADP-induced platelet aggregation by vicagrel. Further, the H4 exposure was positively correlated with intestinal Aadac protein expression levels but did not vary with short-term inhibition of P-gp efflux activity by elacridar.P-gp-deficient mice, rather than elacridar-treated mice, exhibited significant upregulation of intestinal Aadac and Ces2 and thus, enhanced metabolic activation of and platelet response to vicagrel, suggesting that the metabolic activation of vicagrel may vary with P-gp deficiency, not P-gp inhibition, in mice.

01 Sep 2024·DRUG METABOLISM AND DISPOSITION

Effects of the Thiol Methyltransferase Inhibitor (±)-2,3-Dichloro-α-Methylbenzylamine (DCMB) on the Pharmacokinetics and Metabolism of Vicagrel in Rats

Article

Author: Huang, Wensi ; Wu, Yong ; Sun, Hongbin ; Zheng, Yuandong ; Xue, Mingzhen ; Chen, Chong ; Yuan, Yali ; Yang, Chen ; Lu, Huiping ; Gong, Jingru ; Liu, Yongqiang ; Diao, Xingxing ; Yang, Cheng ; He, Yifei ; Zhong, Dafang ; Gong, Yanchun ; Lai, Xiaojuan

P2Y₁₂ receptor inhibitors are commonly used in clinical antiplatelet therapy, typically alongside other medications. Vicagrel, a promising P2Y₁₂ receptor inhibitor, has submitted a new drug marketing application to the United States Food and Drug Administration. Its primary metabolites and some metabolic pathways are identical to those of clopidogrel. The aim of this study was to investigate the effects of the thiol methyltransferase inhibitor (±)-2,3-dichloro-α-methylbenzylamine (DCMB) on the metabolism and pharmacokinetics of vicagrel. In vitro incubation with human and rat liver microsomes revealed that DCMB significantly inhibited the methylation of vicagrel's thiol metabolite M15-1. Rats were orally administered 6 mg/kg [¹⁴C]vicagrel (100 μCi/kg) 1 hour after peritoneal injection with or without DCMB (80 mg/kg). Compared with the control group, the plasma of DCMB-pretreated rats exhibited maximum plasma concentration (C _max) decrease and time to reach C _max (T _max) delay for all vicagrel-related substances, the methylation product of the thiol metabolite (M9-2), and the derivatization product of the active thiol metabolite (MP-M15-2). However, no significant changes in area under the curve (AUC) or half-life (t _1/2) were observed. DCMB had negligible effect on the total radiological recovery of vicagrel within 72 hours, although the rate of vicagrel excretion slowed down within 48 hours. DCMB had a negligible impact on the metabolic pathway of vicagrel. Overall, the present study found that DCMB did not significantly affect the total exposure, metabolic pathways, metabolite profiles, or total excretion rates of vicagrel-related metabolites in rats, but led to C _max decrease, T _max delay, and slower excretion rate within 48 hours. SIGNIFICANCE STATEMENT: This study used liquid chromatography-tandem mass spectrometry combined with radiolabeling technology to investigate the effects of the thiol methyltransferase inhibitor (±)-2,3-dichloro-α-methylbenzylamine on the absorption, metabolism, and excretion of vicagrel in rats. This work helps to better understand the in vivo metabolism of active thiol metabolites of P2Y₁₂ inhibitors such as clopidogrel, vicagrel, etc.

News (Medical) associated with Vicagrel

04 Jan 2024

·www.biospace.com

Jiangsu Vcare Files NDA for Vicagrel Capsules with US FDA

NANJING, China, Jan. 4, 2024 /PRNewswire/ -- On December 28, 2023, Jiangsu Vcare PharmaTech Co., Ltd. (Jiangsu Vcare) successfully submitted a New Drug Application (NDA) to the U.S. Food and Drug Administration (FDA) for Vicagrel capsule, which is indicated to treat a range of thrombotic cardiovascular and cerebrovascular diseases, including acute coronary syndrome, ischaemic stroke, and peripheral arterial disease. This filing marks a significant milestone as Jiangsu Vcare's first NDA submission from its innovative drug pipeline. This NDA filing builds on continuous dialogues with the FDA and is supported by robust nonclinical data and clinical studies conducted in both China and US. Vicagrel, a novel oral P2Y12 receptor antagonist, represents Jiangsu Vcare's commitment to addressing unmet clinical needs with innovative approaches. Its mechanism of action involves the same active metabolite as clopidogrel that effectively inhibits platelet activation and aggregation, while addressing the issue of "clopidogrel resistance". This NDA filing reflects more than ten years of persistent innovation and dedication by Jiangsu Vcare. Once approved, Vicagrel promises to offer a new treatment option for the estimated 27.6 million US patients with coronary heart disease and stroke. About Vicagrel Vicagrel, a product of the collaboration between Jiangsu Vcare and China Pharmaceutical University, is under the exclusive ownership of Jiangsu Vcare. The early R&D breakthroughs were published in prestigious journals including the American Chemical Society's Journal of Medicinal Chemistry (2012) and Nature-affiliated SciBX (2012). Vicagrel stands out among antithrombotic treatments, offering key advantages in both pharmacogenomics and pharmacokinetics over clopidogrel due to its unique structural design. Recent Pharmacokinetics/Pharmacodynamics data positions vicagrel as a superior version of clopidogrel, eliminating the Black Box Warning associated with clopidogrel use and reducing drug interaction concerns, all achievable at a much lower daily dose. About Jiangsu Vcare Founded in 2010, Jiangsu Vcare PharmaTech Co., Ltd. is a high-tech enterprise specializing in innovative drug development, with over 700 employees, mostly technical staff, and operates a major R&D center in Nanjing Biomedical Valley. The company's research portfolio encompasses a range of clinical assets and preclinical projects, targeting key areas such as cardiovascular and cerebrovascular diseases, oncology, and autoimmune disorders. The company features a start-of-art drug discovery platform and partners with China Pharmaceutical University for postdoctoral and graduate research in Nanjing. Having raised nearly 1 billion yuan through three financing rounds between 2021 and 2023, the company aims to leverage its decade-long experience to develop innovative drugs addressing unmet medical needs. Jiangsu Vcare is seeking worldwide commercialization partner(s) for Vicagrel, and welcomes interested parties to contact us. Contact person: Eric Zhang, PhD AmberSight LLC Rockville, MD 20850 Cell: 01-301-518-5028 Yongheng.zhang@amber-sight.com Disclaimer: This news release was compiled and provided by Jiangsu Vcare, and any Commercial use is prohibited without permission. In any case, it is for non-commercial communication and reference purposes only and does not indicate any intention for cooperation or express any opinions. Please independently assess whether to use the content and information in this article at your own risk, Jiangsu Vcare does not assume any legal responsibility. While the company and the team strive for accuracy, they do not guarantee the full accuracy of the contents. If you have any questions about this information, please contact us. This statement will be governed by and interpreted under the laws of the People's Republic of China (PRC). As an essential component of this article, the above statement must be read and confirmed. Your use of this article implies your acceptance of this statement. View original content to download multimedia: SOURCE Jiangsu Vcare

NDA

100 Deals associated with Vicagrel

External Link

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Coronary Artery Disease	NDA/BLA	United States	Jiangsu Vcare PharmaTech Co., Ltd.	03 Jan 2024
Peripheral Arterial Disease	NDA/BLA	United States	Jiangsu Vcare PharmaTech Co., Ltd.	03 Jan 2024
Stroke	NDA/BLA	United States	Jiangsu Vcare PharmaTech Co., Ltd.	03 Jan 2024
Non ST segment elevation acute coronary syndrome	Phase 3	China	China Pharmaceutical University	06 Sep 2024
Non ST segment elevation acute coronary syndrome	Phase 3	China	Jiangsu Vcare PharmaTech Co., Ltd.	06 Sep 2024
Non-St Elevated Myocardial Infarction	Phase 3	China	Jiangsu Vcare PharmaTech Co., Ltd.	06 Sep 2024
Non-St Elevated Myocardial Infarction	Phase 3	China	China Pharmaceutical University	06 Sep 2024
ST Elevation Myocardial Infarction	Phase 3	China	Jiangsu Vcare PharmaTech Co., Ltd.	06 Sep 2024
ST Elevation Myocardial Infarction	Phase 3	China	China Pharmaceutical University	06 Sep 2024
Coronary Disease	Phase 3	China	China Pharmaceutical University	30 Jan 2022

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