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Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor

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  • Source:
    Medicine 2020 99 4, e18683 (e18683) Published by: NLM (Medline) United States
  • Additional Information
    • Author(s):
      Li H, Chen H, Chen W, Xu H, Yuan F, Yang M, Sun H, Yang J, Liu Y, Lai X, Gong Y, Liu X, Li Y, Sheng L, Liu C, Li X
    • Language:
      English
    • Publication Type:
      Journal Article; Observational Study; Randomized Controlled Trial
    • Record Status:
      This record is this issue.
    • Abstract:
      Vicagrel is a new antiplatelet pro-drug based on clopidogrel sulfur lactone metabolites. The purpose of the study was to evaluate the safety, tolerability, and pharmacodynamics (PD) of vicagrel in healthy Chinese subjects.This study was designed as a single-center, randomized, double-blind, placebo-controlled, single oral ascending dose study. Fifty nine subjects were assigned to 6 vicagrel dose cohorts (5, 10, 20, 40, 60, and 75 mg), and 8 subjects were assigned to 75 mg clopidogrel. Within each vicagrel dose cohort, the 10 subjects (9 in the 75 mg cohort) were randomized 4:1 to receive vicagrel or placebo. Platelet function was assessed using VerifyNow P2Y12. ΔP2Y12 reaction units (ΔPRU) and percent inhibition platelet aggregation (%IPA) were used to evaluate the PD of vicagrel.Although the number of adverse events (AEs) increased with vicagrel dose, none were considered serious, suggesting that vicagrel is safe and well-tolerated. The ΔPRU and %IPA patterns suggest that inhibition of ADP-induced platelet aggregation increased in a dose-dependent manner across the 10 to 40 mg dose range. The inhibitory effect was nearly complete at 4 hours (mean %IPA 87.9%-93.0%, mean ΔPRU 206.6-240.0) for doses of 40 to 75 mg of vicagrel. In contrast, for 5 mg vicagrel and 75 mg clopidogrel, there were no measurable effects on platelet aggregation throughout the study.The results suggest that vicagrel at 40 to 75 mg inhibits ADP-induced platelet aggregation, with a fast onset of action and significantly greater potency than clopidogrel. These findings indicate that vicagrel may be a highly effective and well-tolerated antiplatelet agent.
    • EMBASE keywords:
      adult; adverse drug reaction; article; Chinese; clinical trial; cohort analysis; controlled study; double blind procedure; *drug safety; drug therapy; female; human; human cell; human experiment; major clinical study; male; pharmacodynamics; pharmacokinetics; randomized controlled trial; side effect; *thrombocyte aggregation; thrombocyte function analyzer
      Adult
      Female
      Humans
      Male
      Young Adult
      Clopidogrel/pharmacology
      Dose-Response Relationship, Drug
      Double-Blind Method
      Phenylacetates/administration & dosage
      Phenylacetates/adverse effects
      Platelet Activation/drug effects
      Platelet Aggregation Inhibitors/administration & dosage
      Platelet Aggregation Inhibitors/adverse effects
      Platelet Function Tests
      Thiophenes/administration & dosage
      Thiophenes/adverse effects
      Phenylacetates/*pharmacology
      Platelet Aggregation/*drug effects
      Platelet Aggregation Inhibitors/*pharmacology
      Thiophenes/*pharmacology
    • Accession Number:
      630716848
    • Source:
      This document should be cited as: Li H Chen H Chen W Xu H Yuan F Yang M Sun H Yang J Liu Y Lai X Gong Y Liu X Li Y Sheng L Liu C Li X. Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor 2020 (The Cochrane Controlled Trials Register (CCTR/CENTRAL). DOI: 10.1097/MD.0000000000018683. Oxford: Update Software. Updated quarterly.
    • Accession Number:
      CN-02076773
  • Citations
    • ABNT:
      LI H et al. Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor. Medicine, [s. l.], v. 99, n. 4, p. e18683, 2020. DOI 10.1097/MD.0000000000018683. Disponível em: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=cgh&AN=CN-02076773. Acesso em: 28 set. 2020.
    • AMA:
      Li H, Chen H, Chen W, et al. Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor. Medicine. 2020;99(4):e18683. doi:10.1097/MD.0000000000018683
    • APA:
      Li H, Chen H, Chen W, Xu H, Yuan F, Yang M, Sun H, Yang J, Liu Y, Lai X, Gong Y, Liu X, Li Y, Sheng L, Liu C, & Li X. (2020). Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor. Medicine, 99(4), e18683. https://doi.org/10.1097/MD.0000000000018683
    • Chicago/Turabian: Author-Date:
      Li H, Chen H, Chen W, Xu H, Yuan F, Yang M, Sun H, et al. 2020. “Platelet Inhibitory Activity, Tolerability, and Safety of Vicagrel, a Novel Thienopyridine P2Y12 Inhibitor.” Medicine 99 (4): e18683. doi:10.1097/MD.0000000000018683.
    • Harvard:
      Li H et al. (2020) ‘Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor’, Medicine, 99(4), p. e18683. doi: 10.1097/MD.0000000000018683.
    • Harvard: Australian:
      Li H, Chen H, Chen W, Xu H, Yuan F, Yang M, Sun H, Yang J, Liu Y, Lai X, Gong Y, Liu X, Li Y, Sheng L, Liu C & Li X 2020, ‘Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor’, Medicine, vol. 99, no. 4, p. e18683, viewed 28 September 2020, .
    • MLA:
      Li H, et al. “Platelet Inhibitory Activity, Tolerability, and Safety of Vicagrel, a Novel Thienopyridine P2Y12 Inhibitor.” Medicine, vol. 99, no. 4, Jan. 2020, p. e18683. EBSCOhost, doi:10.1097/MD.0000000000018683.
    • Chicago/Turabian: Humanities:
      Li H, Chen H, Chen W, Xu H, Yuan F, Yang M, Sun H, et al. “Platelet Inhibitory Activity, Tolerability, and Safety of Vicagrel, a Novel Thienopyridine P2Y12 Inhibitor.” Medicine 99, no. 4 (January 1, 2020): e18683. doi:10.1097/MD.0000000000018683.
    • Vancouver/ICMJE:
      Li H, Chen H, Chen W, Xu H, Yuan F, Yang M, et al. Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor. Medicine [Internet]. 2020 Jan 1 [cited 2020 Sep 28];99(4):e18683. Available from: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=cgh&AN=CN-02076773