Pharmacokinetic Profile of Betahistine With and Without Selegiline in Healthy Volunteers

Summary

The goal of this pharmakokinetic trial is to demonstrate that Betahistine serum concentration is higher after combination treatment with Betahistine and Selegiline compared to Betahistine alone. The main questions it aims to answer are: Is the plasma concentration of betahistine higher due to combination treatment with selegiline compared to betahistine monotherapy? How is the safety of the combination treatment with betahistine and selegiline, the pharmacokinetics of betahistine in different dosages in blood, and the inter-individual differences in the metabolism? Subjects satisfying all selection criteria will receive three different dosages of Betahistine alone orally in ascending order (24 mg, 48 mg, 96 mg) in the first period. In the second period, subjects received Betahistine treatment as described for first period but after pre- and continuous treatment with 5 mg/ml Selegiline orally. Plasma concentration (namely the AUC0-240min) of betahistine will be measured before and 10, 30, 60, 90, 120, 180, 240 minutes after treatment with blood examinations. Safety parameters include assessment of adverse events, ECG, vital signs, laboratory measurements including kidney and liver function, full blood count and pregnancy and drug screening test.

Timeline

Start

2021-06-02

Primary completion

2021-10-14

Completion

2021-10-14

Publications

• Strupp M, Churchill GC, Naumann I, Mansmann U, Al Tawil A, Golentsova A, Goldschagg N. Examination of betahistine bioavailability in combination with the monoamine oxidase B inhibitor, selegiline, in humans-a non-randomized, single-sequence, two-period titration, open label single-center phase 1 study (PK-BeST). Front Neurol. 2023 Oct 18;14:1271640. doi: 10.3389/fneur.2023.1271640. eCollection 2023.

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Indications