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Physiologically-based pharmacokinetics modelling of Semaglutide in children and adolescents with healthy and obese body weights
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  • Thayná Machado,
  • Thiago Honorio,
  • Thaisa Domingos,
  • Dailane Candido de Paula,
  • Lúcio Cabral,
  • Carlos Rodrigues,
  • Alessandra Souza,
  • Bárbara Abrahim-Vieira
Thayná Machado
Universidade Federal do Rio de Janeiro
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Thiago Honorio
Universidade Federal do Rio de Janeiro
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Thaisa Domingos
BIODATA Computing Services & Consulting
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Dailane Candido de Paula
Universidade Federal do Rio de Janeiro
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Lúcio Cabral
Universidade Federal do Rio de Janeiro
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Carlos Rodrigues
Universidade Federal do Rio de Janeiro
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Alessandra Souza
Universidade Federal do Rio de Janeiro

Corresponding Author:[email protected]

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Bárbara Abrahim-Vieira
Universidade Federal do Rio de Janeiro
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Abstract

Aim: Develop PBPK models of semaglutide to estimate the pharmacokinetic profile for subcutaneous (SC) injections in children and adolescents with healthy and obese body weights. Methods: Pharmacokinetic modeling and simulations of semaglutide SC injections were performed using the Transdermal Compartmental Absorption & Transit (TCAT™) model implemented in GastroPlus™ v.9.5 modules. A PBPK model of semaglutide was developed and verified in the adult population, by comparing the simulated plasma exposure with the observed data, and further scaled to the pediatric populations with normal and obese body weight. Results: The Semaglutide PBPK model was successfully developed in adults and scaled to the pediatric population. Our P-PBPK simulations indicated a significant increase in Cmax values for the 10-14 years pediatric population with healthy body weights, which was higher than the observed values in adults at the reference dose. Since gastrointestinal adverse events are related to increased semaglutide exposure, peak concentrations outside the target range may represent a safety risk for this pediatric age group. Besides, PBPK models indicated that body weight was inversely related to semaglutide exposure in children and adolescents, which is in line with the results observed in population pharmacokinetic studies in adults. Conclusion: Due to the absence of semaglutide pharmacokinetic data for the pediatric population, these PBPK models will aid in the development of dosing regimens and sampling times. Thus, increasing the efficiency of future pediatric clinical trial studies which can be replaced or improved by PBPK models.
14 Dec 2022Submitted to British Journal of Clinical Pharmacology
15 Dec 2022Submission Checks Completed
15 Dec 2022Assigned to Editor
15 Dec 2022Review(s) Completed, Editorial Evaluation Pending
25 Jan 2023Reviewer(s) Assigned
24 Feb 2023Editorial Decision: Revise Major
23 Apr 20231st Revision Received
24 Apr 2023Submission Checks Completed
24 Apr 2023Assigned to Editor
24 Apr 2023Review(s) Completed, Editorial Evaluation Pending
24 Apr 2023Reviewer(s) Assigned
31 May 2023Editorial Decision: Accept