Intravenous Clopidogrel (MDCO-157) Compared with Oral Clopidogrel: The Randomized Cross-Over AMPHORE Study

摘要: Background The extent of P2Y12 inhibition during coronary intervention is an important determinant ischemic complications. currently available oral inhibitors are limited by a relatively slow onset action and variable on-treatment response. Objective Our objective was to determine the pharmacodynamic (PD) dose-antiplatelet response relationship pharmacokinetics MDCO-157, intravenous formulation clopidogrel complexed with sulphobutylether betacyclodextrin, identify dose level MDCO-157 that matches PD effect 300 mg. Methodology A randomized open-label crossover study performed in 33 healthy adult volunteers pharmacokinetic (clopidogrel H4 thiol active metabolite) (vasodilator-stimulated phosphoprotein [VASP]) effects at doses 75, 150, mg Results Data presented as %, mean (standard deviation). maximum receptor assessed flow cytometry using VASP 70.42 (6.7), 69.45 (7.1), 65.58 (12.6) for mg, respectively, compared 56.6 (17.5) administration (p Conclusions did not show significant platelet when administered up Higher longer infusion may be needed reach sufficient threshold metabolite generation. Trial registration ClinicalTrials.gov identifier: NCT01860105.