End-to-end application of model-informed drug development for ertugliflozin, a novel sodium-glucose cotransporter 2 inhibitor.


Journal

CPT: pharmacometrics & systems pharmacology
ISSN: 2163-8306
Titre abrégé: CPT Pharmacometrics Syst Pharmacol
Pays: United States
ID NLM: 101580011

Informations de publication

Date de publication:
06 2021
Historique:
revised: 02 03 2021
received: 18 12 2020
accepted: 11 03 2021
pubmed: 2 5 2021
medline: 22 1 2022
entrez: 1 5 2021
Statut: ppublish

Résumé

Model-informed drug development (MIDD) is critical in all stages of the drug-development process and almost all regulatory submissions for new agents incorporate some form of modeling and simulation. This review describes the MIDD approaches used in the end-to-end development of ertugliflozin, a sodium-glucose cotransporter 2 inhibitor approved for the treatment of adults with type 2 diabetes mellitus. Approaches included (1) quantitative systems pharmacology modeling to predict dose-response relationships, (2) dose-response modeling and model-based meta-analysis for dose selection and efficacy comparisons, (3) population pharmacokinetics (PKs) modeling to characterize PKs and quantify population variability in PK parameters, (4) regression modeling to evaluate ertugliflozin dose-proportionality and the impact of uridine 5'-diphospho-glucuronosyltransferase (UGT) 1A9 genotype on ertugliflozin PKs, and (5) physiologically-based PK modeling to assess the risk of UGT-mediated drug-drug interactions. These end-to-end MIDD approaches for ertugliflozin facilitated decision making, resulted in time/cost savings, and supported registration and labeling.

Identifiants

pubmed: 33932126
doi: 10.1002/psp4.12633
pmc: PMC8213419
doi:

Substances chimiques

Bridged Bicyclo Compounds, Heterocyclic 0
Sodium-Glucose Transporter 2 Inhibitors 0
ertugliflozin 6C282481IP

Types de publication

Journal Article Research Support, Non-U.S. Gov't Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

529-542

Informations de copyright

© 2021 The Authors. CPT: Pharmacometrics & Systems Pharmacology published by Wiley Periodicals LLC on behalf of American Society for Clinical Pharmacology and Therapeutics.

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Auteurs

Daryl J Fediuk (DJ)

Pfizer Inc., Groton, Connecticut, USA.

Gianluca Nucci (G)

Pfizer Inc., Cambridge, Massachusetts, USA.

Vikas K Dawra (VK)

Pfizer Inc., New York, New York, USA.

Ernesto Callegari (E)

Pfizer Inc., Groton, Connecticut, USA.

Susan Zhou (S)

Merck & Co., Inc., Kenilworth, New Jersey, USA.

Cynthia J Musante (CJ)

Pfizer Inc., Cambridge, Massachusetts, USA.

Yali Liang (Y)

Pfizer Inc., Groton, Connecticut, USA.

Kevin Sweeney (K)

Pfizer Inc., Groton, Connecticut, USA.

Vaishali Sahasrabudhe (V)

Pfizer Inc., Groton, Connecticut, USA.

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Classifications MeSH