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dc.contributor.authorStorey, Robert F.
dc.contributor.authorGurbel, Paul A.
dc.contributor.authorBerg, Jurrien ten
dc.contributor.authorBernaud, Corine
dc.contributor.authorDangas, George D.
dc.contributor.authorFrenoux, Jean Marie
dc.contributor.authorGorog, Diana A.
dc.contributor.authorHmissi, Abdel
dc.contributor.authorKunadian, Vijay
dc.contributor.authorJames, Stefan K.
dc.contributor.authorTanguay, Jean Francois
dc.contributor.authorTran, Henry
dc.contributor.authorTrenk, Dietmar
dc.contributor.authorUfer, Mike
dc.contributor.authorvan der Harst, Pim
dc.contributor.authorVan't Hof, Arnoud W.J.
dc.contributor.authorAngiolillo, Dominick J.
dc.date.accessioned2020-11-11T00:15:13Z
dc.date.available2020-11-11T00:15:13Z
dc.date.issued2020-09-01
dc.identifier.citationStorey , R F , Gurbel , P A , Berg , J T , Bernaud , C , Dangas , G D , Frenoux , J M , Gorog , D A , Hmissi , A , Kunadian , V , James , S K , Tanguay , J F , Tran , H , Trenk , D , Ufer , M , van der Harst , P , Van't Hof , A W J & Angiolillo , D J 2020 , ' Pharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y 12 receptor antagonist, in patients with chronic coronary syndromes ' , European Heart Journal , vol. 41 , no. 33 , pp. 3132-3140 . https://doi.org/10.1093/eurheartj/ehz807
dc.identifier.issn0195-668X
dc.identifier.otherPURE: 22963233
dc.identifier.otherPURE UUID: 5b0efd67-c91e-46b9-b096-0e478b044c23
dc.identifier.otherScopus: 85091127173
dc.identifier.otherPubMed: 31994703
dc.identifier.urihttp://hdl.handle.net/2299/23434
dc.description.abstractAims To study the pharmacodynamics and pharmacokinetics of selatogrel, a novel P2Y12 receptor antagonist for subcutaneous administration, in patients with chronic coronary syndromes (CCS). Methods In this double-blind, randomized study of 345 patients with CCS on background oral antiplatelet therapy, subcuta- and results neous selatogrel (8 mg, n = 114; or 16 mg, n = 115) was compared with placebo (n = 116) (ClinicalTrials.gov: NCT03384966). Platelet aggregation was assessed over 24 h (VerifyNow assay) and 8 h (light transmittance aggregometry; LTA). Pharmacodynamic responders were defined as patients having P2Y12 reaction units (PRU) <100 at 30 min post-dose and lasting >_3 h. At 30 min post-dose, 89% of patients were responders to selatogrel 8 mg, 90% to selatogrel 16 mg, and 16% to placebo (P < 0.0001). PRU values (mean ± standard deviation) were 10 ± 25 (8 mg), 4 ± 10 (16 mg), and 163 ± 73 (placebo) at 15 min and remained <100 up to 8 h for both doses, returning to pre-dose or near pre-dose levels by 24 h post-dose. LTA data showed similarly rapid and potent inhibition of platelet aggregation. Selatogrel plasma concentrations peaked 30 min post-dose. Selatogrel was safe and well-tolerated with transient dyspnoea occurring overall in 7% (16/229) of patients (95% confidence interval: 4-11%). Conclusions Selatogrel was rapidly absorbed following subcutaneous administration in CCS patients, providing prompt, potent, and consistent platelet P2Y12 inhibition sustained for >_8 h and reversible within 24 h. Further studies of subcutaneous selatogrel are warranted in clinical scenarios where rapid platelet inhibition is desirable.en
dc.format.extent9
dc.language.isoeng
dc.relation.ispartofEuropean Heart Journal
dc.rightsOpen
dc.subjectCoronary artery disease
dc.subjectP2Y receptor antagonist
dc.subjectPharmacodynamics
dc.subjectPharmacokinetics
dc.subjectPlatelet aggregation
dc.subjectSelatogrel
dc.subjectCardiology and Cardiovascular Medicine
dc.titlePharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y12 receptor antagonist, in patients with chronic coronary syndromesen
dc.contributor.institutionDepartment of Pharmacy, Pharmacology and Postgraduate Medicine
dc.contributor.institutionDepartment of Clinical, Pharmaceutical and Biological Science
dc.description.statusPeer reviewed
dc.identifier.urlhttp://www.scopus.com/inward/record.url?scp=85091127173&partnerID=8YFLogxK
dc.description.versiontypeFinal Published version
dcterms.dateAccepted2020-09-01
rioxxterms.versionVoR
rioxxterms.versionofrecordhttps://doi.org/10.1093/eurheartj/ehz807
rioxxterms.licenseref.urihttp://creativecommons.org/licenses/by/4.0/
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue
herts.rights.accesstypeOpen


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