Prasugrel Intermediate Metabolite Modulates Platelet Inhibition by Negatively Interfering With an Active Metabolite: An Ex Vivo, In Vitro, and In Silico Study

Prasugrel is converted into prasugrel active metabolite (PAM; R-138727) through the cytochrome P450-mediated conversion of an intermediate metabolite (PIM; R-95913). It is unknown whether PIM exerts any biological function. The FABOLUS-FASTER trial (Facilitation Through Aggrastat or Cangrelor Bolus...

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Veröffentlicht in:	Arteriosclerosis, thrombosis, and vascular biology Jg. 45; H. 5; S. 792
Hauptverfasser:	Minuz, Pietro, Giorgetti, Alejandro, Meneguzzi, Alessandra, Taus, Francesco, Ribeiro, Rui P, Baldessari, Filippo, Gargiulo, Giuseppe, Gragnano, Felice, Landi, Antonio, Castelli, Marco, Gottardo, Rossella, Bortolotti, Federica, Verlato, Giuseppe, Fava, Cristiano, Cattaneo, Marco, Tagliaro, Franco, Valgimigli, Marco
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 01.05.2025
Schlagworte:	Administration, Oral Aged Binding Sites Blood Platelets - drug effects Blood Platelets - metabolism Cell Adhesion Molecules - blood Female Humans Male Microfilament Proteins - blood Middle Aged Molecular Docking Simulation Molecular Dynamics Simulation P-Selectin Phosphoproteins - blood Phosphorylation Piperazines Platelet Activation - drug effects Platelet Aggregation - drug effects Platelet Aggregation Inhibitors - administration & dosage Platelet Aggregation Inhibitors - blood Platelet Aggregation Inhibitors - pharmacokinetics Prasugrel Hydrochloride - administration & dosage Prasugrel Hydrochloride - blood Prasugrel Hydrochloride - metabolism Prasugrel Hydrochloride - pharmacokinetics Purinergic P2Y Receptor Antagonists - administration & dosage Purinergic P2Y Receptor Antagonists - blood Purinergic P2Y Receptor Antagonists - pharmacokinetics Receptors, Purinergic P2Y12 - blood Receptors, Purinergic P2Y12 - drug effects ST Elevation Myocardial Infarction - blood ST Elevation Myocardial Infarction - diagnosis ST Elevation Myocardial Infarction - drug therapy ST Elevation Myocardial Infarction - therapy Vasodilator-Stimulated Phosphoprotein pharmacokinetics drug interactions prasugrel hydrochloride myocardial infarction platelet aggregation
ISSN:	1524-4636, 1524-4636
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