Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe Asthma

ABSTRACT In this study, we investigated the pharmacokinetic/pharmacodynamic (PK/PD) relationship of dupilumab as an add‐on therapy in the intent‐to‐treat (ITT) uncontrolled moderate‐to‐severe asthma population and identified the factors significantly contributing to variability in forced expiratory...

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Main Authors: Li Zhang, John D. Davis, Vanaja Kanamaluru, Christine Xu
Format: Article
Language:English
Published: Wiley 2025-08-01
Series:CPT: Pharmacometrics & Systems Pharmacology
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Online Access:https://doi.org/10.1002/psp4.70057
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author Li Zhang
John D. Davis
Vanaja Kanamaluru
Christine Xu
author_facet Li Zhang
John D. Davis
Vanaja Kanamaluru
Christine Xu
author_sort Li Zhang
collection DOAJ
description ABSTRACT In this study, we investigated the pharmacokinetic/pharmacodynamic (PK/PD) relationship of dupilumab as an add‐on therapy in the intent‐to‐treat (ITT) uncontrolled moderate‐to‐severe asthma population and identified the factors significantly contributing to variability in forced expiratory volume in 1 second; (FEV1). A semi‐mechanistic population PK/PD model was developed using data from two placebo‐controlled pivotal studies in 2654 adult and adolescent patients (n = 794 treated with placebo; n = 1860 treated with dupilumab 200 mg [400‐mg loading dose] or 300 mg [600‐mg loading dose] administered subcutaneously every 2 [Q2W] or 4 weeks [Q4W]). Treatment effect was described using a dupilumab concentration‐dependent direct‐response Emax model, and placebo effect was described using an empirical time‐dependent function. Demographic variables, baseline disease characteristics, type‐2 inflammation biomarkers, and immunogenicity were tested as covariates using the stepwise forward selection and backward elimination method. Baseline type‐2 inflammation biomarkers (fractional exhaled nitric oxide [FeNO] level and blood eosinophil [EOS] count) were found to be significant covariates for FEV1, with greater efficacy in patients with elevated biomarker levels. None of the other tested covariates, including age (12–87 years), had a significant impact on FEV1. The PK/PD model predicted near‐maximum FEV1 response (0.1 L) over a dose of dupilumab. 200–300 mg Q2W in patients with moderate‐to‐severe asthma.
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spelling doaj-art-b12760a958ed4691bf79caec1d0fc93e2025-08-20T03:07:01ZengWileyCPT: Pharmacometrics & Systems Pharmacology2163-83062025-08-011481370138010.1002/psp4.70057Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe AsthmaLi Zhang0John D. Davis1Vanaja Kanamaluru2Christine Xu3Sanofi, Bridgewater New Jersey USARegeneron Pharmaceuticals, Inc. Tarrytown New York USASanofi, Bridgewater New Jersey USASanofi, Bridgewater New Jersey USAABSTRACT In this study, we investigated the pharmacokinetic/pharmacodynamic (PK/PD) relationship of dupilumab as an add‐on therapy in the intent‐to‐treat (ITT) uncontrolled moderate‐to‐severe asthma population and identified the factors significantly contributing to variability in forced expiratory volume in 1 second; (FEV1). A semi‐mechanistic population PK/PD model was developed using data from two placebo‐controlled pivotal studies in 2654 adult and adolescent patients (n = 794 treated with placebo; n = 1860 treated with dupilumab 200 mg [400‐mg loading dose] or 300 mg [600‐mg loading dose] administered subcutaneously every 2 [Q2W] or 4 weeks [Q4W]). Treatment effect was described using a dupilumab concentration‐dependent direct‐response Emax model, and placebo effect was described using an empirical time‐dependent function. Demographic variables, baseline disease characteristics, type‐2 inflammation biomarkers, and immunogenicity were tested as covariates using the stepwise forward selection and backward elimination method. Baseline type‐2 inflammation biomarkers (fractional exhaled nitric oxide [FeNO] level and blood eosinophil [EOS] count) were found to be significant covariates for FEV1, with greater efficacy in patients with elevated biomarker levels. None of the other tested covariates, including age (12–87 years), had a significant impact on FEV1. The PK/PD model predicted near‐maximum FEV1 response (0.1 L) over a dose of dupilumab. 200–300 mg Q2W in patients with moderate‐to‐severe asthma.https://doi.org/10.1002/psp4.70057asthmadupilumabforced expiratory volume in 1 smonoclonal antibodiespopulation pharmacokinetic/pharmacodynamic
spellingShingle Li Zhang
John D. Davis
Vanaja Kanamaluru
Christine Xu
Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe Asthma
CPT: Pharmacometrics & Systems Pharmacology
asthma
dupilumab
forced expiratory volume in 1 s
monoclonal antibodies
population pharmacokinetic/pharmacodynamic
title Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe Asthma
title_full Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe Asthma
title_fullStr Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe Asthma
title_full_unstemmed Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe Asthma
title_short Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV1) in Uncontrolled Moderate‐To‐Severe Asthma
title_sort semi mechanistic population pharmacokinetic pharmacodynamic pk pd modeling of dupilumab on pre bronchodilator forced expiratory volume in 1 second fev1 in uncontrolled moderate to severe asthma
topic asthma
dupilumab
forced expiratory volume in 1 s
monoclonal antibodies
population pharmacokinetic/pharmacodynamic
url https://doi.org/10.1002/psp4.70057
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