Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics

Abstract This study employed physiologically based pharmacokinetic (PBPK) modelling to compare the extent of foetal exposure between oral and long-acting injectable (LAI) aripiprazole and olanzapine. Adult and pregnancy PBPK models were developed and validated with relevant clinical data. Relevant i...

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Main Authors: Philip Bediako-Kakari, Mariella Monyo, Shakir Atoyebi, Adeniyi Olagunju
Format: Article
Language:English
Published: Nature Portfolio 2025-05-01
Series:npj Women's Health
Online Access:https://doi.org/10.1038/s44294-025-00077-9
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author Philip Bediako-Kakari
Mariella Monyo
Shakir Atoyebi
Adeniyi Olagunju
author_facet Philip Bediako-Kakari
Mariella Monyo
Shakir Atoyebi
Adeniyi Olagunju
author_sort Philip Bediako-Kakari
collection DOAJ
description Abstract This study employed physiologically based pharmacokinetic (PBPK) modelling to compare the extent of foetal exposure between oral and long-acting injectable (LAI) aripiprazole and olanzapine. Adult and pregnancy PBPK models were developed and validated with relevant clinical data. Relevant indices of foetal exposure during pregnancy were predicted from concentration-time data at steady-state dosing for both oral and LAI formulations. Foetal Cmax for aripiprazole was 59–78% higher with LAI than oral, and 68–181% higher with LAI olanzapine than the oral formulation. Predicted cord:maternal ratios (range) were 0.59–0.69 for oral aripiprazole and 0.61–0.66 for LAI aripiprazole, 0.34–0.64 for oral olanzapine and 0.89–0.96 for LAI olanzapine. Also, cumulative foetal exposure over 28 days from oral formulations were generally predicted to be lower compared with their therapeutic-equivalent LAI. As in utero foetal exposure to maternal drugs does not necessarily translate to risk, these data should be interpreted in a broader context that includes benefit-risk assessments.
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spelling doaj-art-7f25704a7e76439fbe809bbf830021f82025-08-20T02:25:09ZengNature Portfolionpj Women's Health2948-17162025-05-013111010.1038/s44294-025-00077-9Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychoticsPhilip Bediako-Kakari0Mariella Monyo1Shakir Atoyebi2Adeniyi Olagunju3School of Biosciences, University of LiverpoolSchool of Biosciences, University of LiverpoolCentre of Excellence for Long-acting Therapeutics, University of LiverpoolCentre of Excellence for Long-acting Therapeutics, University of LiverpoolAbstract This study employed physiologically based pharmacokinetic (PBPK) modelling to compare the extent of foetal exposure between oral and long-acting injectable (LAI) aripiprazole and olanzapine. Adult and pregnancy PBPK models were developed and validated with relevant clinical data. Relevant indices of foetal exposure during pregnancy were predicted from concentration-time data at steady-state dosing for both oral and LAI formulations. Foetal Cmax for aripiprazole was 59–78% higher with LAI than oral, and 68–181% higher with LAI olanzapine than the oral formulation. Predicted cord:maternal ratios (range) were 0.59–0.69 for oral aripiprazole and 0.61–0.66 for LAI aripiprazole, 0.34–0.64 for oral olanzapine and 0.89–0.96 for LAI olanzapine. Also, cumulative foetal exposure over 28 days from oral formulations were generally predicted to be lower compared with their therapeutic-equivalent LAI. As in utero foetal exposure to maternal drugs does not necessarily translate to risk, these data should be interpreted in a broader context that includes benefit-risk assessments.https://doi.org/10.1038/s44294-025-00077-9
spellingShingle Philip Bediako-Kakari
Mariella Monyo
Shakir Atoyebi
Adeniyi Olagunju
Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics
npj Women's Health
title Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics
title_full Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics
title_fullStr Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics
title_full_unstemmed Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics
title_short Comparative modelling of foetal exposure to maternal long-acting injectable versus oral daily antipsychotics
title_sort comparative modelling of foetal exposure to maternal long acting injectable versus oral daily antipsychotics
url https://doi.org/10.1038/s44294-025-00077-9
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AT mariellamonyo comparativemodellingoffoetalexposuretomaternallongactinginjectableversusoraldailyantipsychotics
AT shakiratoyebi comparativemodellingoffoetalexposuretomaternallongactinginjectableversusoraldailyantipsychotics
AT adeniyiolagunju comparativemodellingoffoetalexposuretomaternallongactinginjectableversusoraldailyantipsychotics