betahistine + selegiline

This combination therapy, consisting of betahistine and selegiline, is being investigated by Ludwig-Maximilians University of Munich (LMU Munich) for the treatment of Ménière's disease and other vestibular disorders. Betahistine is a histamine analog that acts as a weak H1 receptor agonist and a potent H3 receptor antagonist, but it typically exhibits very poor bioavailability (approximately 1%) due to extensive first-pass metabolism by monoamine oxidases. Selegiline, a selective monoamine oxidase B (MAO-B) inhibitor, is included in the formulation to inhibit this metabolic pathway, thereby increasing betahistine's bioavailability by an estimated 80 to 100-fold. The combination has been evaluated in the Phase 1 PK-BeST trial, which demonstrated a significant increase in betahistine serum concentrations without safety concerns in healthy volunteers. This approach aims to enhance the clinical efficacy of betahistine in conditions such as Ménière's disease, acute vestibular syndrome, and post-BPPV residual dizziness.

Other names

betahistine and selegiline combinationbetahistine dihydrochloride + selegiline hydrochloride