Drug intelligence / Profile preview

betahistine + dexamethasone + lidocaine

Development stage
Unknown
Lead developer
Leading Edge Clinic
Modality
Small Molecules
Administration
Otic
01

Overview

This compounded therapeutic combination consists of betahistine, dexamethasone, and lidocaine, formulated in a dimethyl sulfoxide (DMSO) vehicle for otic administration. Developed by the Leading Edge Clinic, it is currently being evaluated in a pilot clinical trial for the treatment of refractory subjective tinnitus associated with post-acute sequelae of SARS-CoV-2 (PASC) and post-COVID-19 vaccine injury. Betahistine is a histamine H1 receptor agonist and H3 receptor antagonist that promotes microcirculation in the inner ear. Dexamethasone is a synthetic glucocorticoid that provides anti-inflammatory and immunosuppressive effects. Lidocaine is a local anesthetic that acts as a voltage-gated sodium channel blocker, potentially stabilizing aberrant neural signaling in the auditory system. The DMSO component serves as a penetration enhancer to facilitate the delivery of these active ingredients across the tympanic membrane or into the local tissues.

Other names
DMSO-based otic solution with betahistine, dexamethasone, and lidocaine
02

Targets

HRH3 (Histamine Receptor H3)HRH1 (Histamine H1 Receptor)GR (Glucocorticoid receptor)PXR (Pregnane X receptor)NaV (Voltage-gated sodium channels)

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