دورية أكاديمية
أعرض في EDS

Population Pharmacokinetic and Exposure-dizziness Modeling for a Metabotropic Glutamate Receptor Subtype 5 Negative Allosteric Modulator in Major Depressive Disorder Patients.

التفاصيل البيبلوغرافية
العنوان: Population Pharmacokinetic and Exposure-dizziness Modeling for a Metabotropic Glutamate Receptor Subtype 5 Negative Allosteric Modulator in Major Depressive Disorder Patients.
المؤلفون: Cosson V; Pharmaceutical Sciences Clinical Pharmacology, Roche Innovation Center Basel, F. Hoffmann-La Roche, Basel, Switzerland., Schaedeli-Stark F; Pharmaceutical Sciences Clinical Pharmacology, Roche Innovation Center Basel, F. Hoffmann-La Roche, Basel, Switzerland., Arab-Alameddine M; Pharmaceutical Sciences Clinical Pharmacology, Roche Innovation Center Basel, F. Hoffmann-La Roche, Basel, Switzerland., Chavanne C; Pharmaceutical Sciences Clinical Pharmacology, Roche Innovation Center Basel, F. Hoffmann-La Roche, Basel, Switzerland., Guerini E; Pharmaceutical Sciences Clinical Pharmacology, Roche Innovation Center Basel, F. Hoffmann-La Roche, Basel, Switzerland., Derks M; Pharmaceutical Sciences Clinical Pharmacology, Roche Innovation Center Welwyn, Roche Products, Welwyn, UK., Mallalieu NL; Pharmaceutical Sciences Clinical Pharmacology, Roche Innovation Center New York, F. Hoffmann-La Roche, New York, New York, USA.
المصدر: Clinical and translational science [Clin Transl Sci] 2018 Sep; Vol. 11 (5), pp. 523-531. Date of Electronic Publication: 2018 Jun 27.
نوع المنشور: Clinical Trial, Phase I; Clinical Trial, Phase II; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: WileyBlackwell Pub Country of Publication: United States NLM ID: 101474067 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1752-8062 (Electronic) Linking ISSN: 17528054 NLM ISO Abbreviation: Clin Transl Sci
أسماء مطبوعة: Original Publication: Malden, MA : WileyBlackwell Pub., 2008-
مواضيع طبية MeSH: Models, Biological*, Depressive Disorder, Major/*drug therapy , Dizziness/*chemically induced , Imidazoles/*adverse effects , Imidazoles/*pharmacokinetics , Pyridines/*adverse effects , Pyridines/*pharmacokinetics , Receptor, Metabotropic Glutamate 5/*metabolism, Allosteric Regulation ; Humans ; Imidazoles/therapeutic use ; Pyridines/therapeutic use
مستخلص: Dizziness, the most frequently observed adverse event in patients with major depressive disorder, was observed with basimglurant, a selective, orally active metabotropic glutamate receptor subtype 5 negative allosteric modulator. The potential relationship between dizziness and basimglurant exposure was explored. The pharmacokinetics of basimglurant was characterized with nonlinear mixed effects modeling using data from 288 trial participants enrolled in five clinical trials. The pharmacokinetics of basimglurant after daily oral administration of a modified release formulation was best described by a two-compartment disposition model with a transit compartment, lag time for the absorption, and first-order elimination. The largest covariate effects were the effect of smoking and male gender on apparent clearance followed by the effect of body weight on distribution volumes. Clearance was twofold higher in smokers and 40% higher in males. A logistic regression model showed a statistically significant correlation between basimglurant C max and incidence of dizziness. An increased risk of dizziness is predicted with increasing doses.
(© 2018 The Authors. Clinical and Translational Science published by Wiley Periodicals, Inc. on behalf of American Society for Clinical Pharmacology and Therapeutics.)
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المشرفين على المادة: 0 (2-chloro-4-(1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl)pyridine)
0 (Imidazoles)
0 (Pyridines)
0 (Receptor, Metabotropic Glutamate 5)
تواريخ الأحداث: Date Created: 20180608 Date Completed: 20190812 Latest Revision: 20190812
رمز التحديث: 20221213
مُعرف محوري في PubMed: PMC6132363
DOI: 10.1111/cts.12566
PMID: 29877614
قاعدة البيانات: MEDLINE
الوصف
تدمد:1752-8062
DOI:10.1111/cts.12566