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Effect on the Gastrointestinal Absorption of Drugs from Different Classes in the Biopharmaceutics Classification System, When Treating with Liraglutide
Novo Nordisk AS, DK-2860 Soborg, Denmark..
Novo Nordisk AS, DK-2860 Soborg, Denmark..
Quintiles AB, Phase Serv 1, SE-75323 Uppsala, Sweden..
Novo Nordisk AS, DK-2860 Soborg, Denmark..
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2015 (English)In: Molecular Pharmaceutics, ISSN 1543-8384, E-ISSN 1543-8392, Vol. 12, no 11, 4166-4173 p.Article in journal (Refereed) PublishedText
Abstract [en]

Like other GLP-1 receptor agonists used for treatment of type 2 diabetes, liraglutide delays gastric emptying. In this clinical absorption study, the primary objective was to investigate the effect of liraglutide (at steady state) on the rate and/or extent of gastrointestinal (GI) absorption of concomitantly orally taken drugs from three classes of the Biopharmaceutics Classification System (BCS). To provide a general prediction on liraglutide drugdrug absorption interaction, single-dose pharmacokinetics of drugs representing BCS classes II (low solubility-high permeability; atorvastatin 40 mg and griseofulvin 500 mg), III (high solubilitylow permeability; lisinopril 20 mg), and IV (low solubility-low permeability; digoxin 1 mg) were studied in healthy subjects at steady state of liraglutide 1.8 mg, or placebo, in a two-period crossover design. With liraglutide, the oral drugs atorvastatin, lisinopril, and digoxin showed delayed t(max) (by <= 2 h) and did not meet the criterion for bioequivalence for C-max (reduced C-max by 27-38%); griseofulvin had similar tmax and 37% increased C-max. Although the prespecified bioequivalence criterion was not met by all drugs, the overall plasma exposure (AUC) of griseofulvin, atorvastatin, lisinopril, and digoxin only exhibited minor changes and was not considered to be of clinical relevance.

Place, publisher, year, edition, pages
2015. Vol. 12, no 11, 4166-4173 p.
Keyword [en]
liraglutide, GLP-1 receptor agonist, gastrointestinal absorption, drug interaction, biopharmaceutical classification systems
National Category
Pharmaceutical Sciences
URN: urn:nbn:se:uu:diva-269985DOI: 10.1021/acs.molpharmaceut.5b00278ISI: 000364174800036PubMedID: 26426736OAI: oai:DiVA.org:uu-269985DiVA: diva2:885587
Novo Nordisk
Available from: 2015-12-19 Created: 2015-12-19 Last updated: 2015-12-19Bibliographically approved

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