1. Bioavailability and pharmacokinetic profile of balovaptan, a selective, brain-penetrant vasopressin 1a receptor antagonist, in healthy volunteers
- Author
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Michael Derks, Christoph Wandel, Sian Lennon-Chrimes, Axel Paehler, Piotr Szczesny, Heidemarie Kletzl, Lisa Squassante, and Andreas Guenther
- Subjects
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 - Abstract
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.
- Published
- 2021
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