Bioavailability and pharmacokinetic profile of balovaptan, a selective, brain-penetrant vasopressin 1a receptor antagonist, in healthy volunteers
| Autor: | Michael Derks, Christoph Wandel, Sian Lennon-Chrimes, Axel Paehler, Piotr Szczesny, Heidemarie Kletzl, Lisa Squassante, Andreas Guenther |
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| Rok vydání: | 2021 |
| Předmět: |
Adult
Male Vasopressin Time Factors Adolescent Pyridines medicine.drug_class Administration Oral Biological Availability Pharmacology Benzodiazepines Food-Drug Interactions Young Adult chemistry.chemical_compound Double-Blind Method Pharmacokinetics Healthy volunteers medicine Humans Tissue Distribution Pharmacology (medical) Cross-Over Studies Dose-Response Relationship Drug Chemistry General Medicine Middle Aged Triazoles Receptor antagonist Bioavailability Area Under Curve Female Penetrant (biochemical) Antidiuretic Hormone Receptor Antagonists Half-Life |
| Zdroj: | Expert Opinion on Investigational Drugs. 30:893-901 |
| ISSN: | 1744-7658 1354-3784 |
| Popis: | Balovaptan is a potent, selective vasopressin 1a receptor antagonist. The early-phase pharmacokinetics (PK) of balovaptan are reported.Two Phase 1 studies (overallAbsolute balovaptan bioavailability was high (103-116%). Steady-state (Day 14) balovaptan PK was approximately dose proportional with a half-life of 45-47 hours, but single-dose CBalovaptan was well tolerated at single (≤76 mg) and multiple (≤52 mg/day) doses, with a PK profile supportive of once-daily administration without food restrictions.ClinicalTrials.gov NCT03764449; NCT01418963. |
| Databáze: | OpenAIRE |
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