Advisor(s)

Eyob Adane, PhD, RPh, BCPS

Confirmation

1

Document Type

Poster

Location

McIntosh Activities Room

Start Date

19-4-2024 10:00 AM

End Date

19-4-2024 10:50 AM

Abstract

Background: Cangrelor (Kengreal(R) is a non-thienopyridine parenteral antiplatelet drug approved as an adjunct for the reduction of periprocedural myocardial infarction and stent thrombosis risk in patients undergoing percutaneous coronary intervention (PCI). It is also used off-label for bridging in patients who are off their antiplatelet agents prior to surgery. Cangrelor blocks the binding of adenosine diphosphate (ADP) by reversibly binding to P2Y12 receptors on platelet surfaces. In comparison to other P2Y12 antagonists, cangrelor has a rapidly reversible platelet inhibition effect with a short half-life of approximately 3-5 minutes. Data on simultaneous PK/PD modeling of cangrelor are, however, lacking. The aims of this study are, therefore, to propose a method for simultaneous PK/PD modeling and to simulate the PK/PD of alternative bolus and infusion doses of cangrelor. Methods: Plasma concentration versus time and pharmacodynamic response versus time data were extracted with PlotDigitizer from the publications of Akers et. al. (J Clin Pharmacol. 2010 Jan;50(1):27-35.) and Gelbenegger et. al. (Thromb J. 2022; 20: 19.), respectively. These data were used to generate 100 random samples at each time point from a log-normal distribution using R 4.2.3. These data would be simultaneously fit into a one-compartment pharmacokinetic model with linear elimination and a direct effect sigmoidal Imax model. Modeling and simulation would be performed to determine exposure and effect at various bolus and infusion doses of cangrelor using Monolix and Simulx (Lixoft, France). Results, Discussion & Conclusion: Pending

Keywords: Cangrelor, P2Y12 antagonist, non-thienopyridine, platelet inhibition, pharmacokinetics, pharmacodynamics, simulation

Level of Access

Open Access

Open Access

Available to all.

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Apr 19th, 10:00 AM Apr 19th, 10:50 AM

Pharmacokinetic/Pharmacodynamic Modeling and Simulation of Various Bolus and Infusion Doses of Cangrelor

McIntosh Activities Room

Background: Cangrelor (Kengreal(R) is a non-thienopyridine parenteral antiplatelet drug approved as an adjunct for the reduction of periprocedural myocardial infarction and stent thrombosis risk in patients undergoing percutaneous coronary intervention (PCI). It is also used off-label for bridging in patients who are off their antiplatelet agents prior to surgery. Cangrelor blocks the binding of adenosine diphosphate (ADP) by reversibly binding to P2Y12 receptors on platelet surfaces. In comparison to other P2Y12 antagonists, cangrelor has a rapidly reversible platelet inhibition effect with a short half-life of approximately 3-5 minutes. Data on simultaneous PK/PD modeling of cangrelor are, however, lacking. The aims of this study are, therefore, to propose a method for simultaneous PK/PD modeling and to simulate the PK/PD of alternative bolus and infusion doses of cangrelor. Methods: Plasma concentration versus time and pharmacodynamic response versus time data were extracted with PlotDigitizer from the publications of Akers et. al. (J Clin Pharmacol. 2010 Jan;50(1):27-35.) and Gelbenegger et. al. (Thromb J. 2022; 20: 19.), respectively. These data were used to generate 100 random samples at each time point from a log-normal distribution using R 4.2.3. These data would be simultaneously fit into a one-compartment pharmacokinetic model with linear elimination and a direct effect sigmoidal Imax model. Modeling and simulation would be performed to determine exposure and effect at various bolus and infusion doses of cangrelor using Monolix and Simulx (Lixoft, France). Results, Discussion & Conclusion: Pending

Keywords: Cangrelor, P2Y12 antagonist, non-thienopyridine, platelet inhibition, pharmacokinetics, pharmacodynamics, simulation