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Development Strategy and Relative Bioavailability of a Pediatric Tablet Formulation of Ticagrelor

Mohammad Niazi1, Jenny Wissmar2, Anders R Berggren2

  • 1Quantitative Clinical Pharmacology, Early Clinical Development, AstraZeneca Gothenburg, Mölndal, Sweden. mohammad.niazi@astrazeneca.com.

Clinical Drug Investigation
|May 30, 2019
PubMed

Insights

This study shows that new pediatric ticagrelor formulations, including dispersible tablets, have similar bioavailability to adult versions. These findings support the use of ticagrelor in pediatric patients for conditions like sickle cell disease.

Area of Science:

  • Pharmacology
  • Clinical Pharmacy
  • Pediatric Medicine

Background:

  • Ticagrelor, a P2Y12 inhibitor, is approved for acute coronary syndrome and myocardial infarction.
  • Investigational use of ticagrelor includes reducing vaso-occlusive crises in pediatric sickle cell disease patients.
  • A new pediatric formulation was developed to facilitate administration in this age group.

Purpose of the Study:

  • To determine the relative bioavailability of pediatric ticagrelor formulations compared to adult immediate-release tablets.
  • To assess bioequivalence between pediatric tablets (whole and dispersed) and granules for oral suspension.
  • To evaluate the safety and tolerability of the new pediatric formulations.

Main Methods:

  • A randomized, four-period, cross-over, single-dose study design was employed.
  • Pharmacokinetic parameters for ticagrelor and its active metabolite (AR-C124910XX) were assessed.
  • Bioequivalence was established based on 90% confidence intervals for Cmax and AUC ratios within 80.00-125.00%.

Main Results:

  • Forty-four healthy adults participated in the study.
  • All tested comparisons demonstrated similar bioavailability for ticagrelor and its active metabolite.
  • Ticagrelor pediatric tablets, whether taken whole or dispersed, were bioequivalent to each other and well-tolerated.

Conclusions:

  • The new pediatric dispersible tablet formulation of ticagrelor exhibits similar bioavailability across various oral administration methods.
  • This pediatric formulation is suitable for use in a wide age range of pediatric patients.
  • The study supports the expanded use of ticagrelor in pediatric populations, particularly for sickle cell disease management.
Abstract

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