Drug intelligence / Profile preview

levocloperastine

Development stage
Phase 4
Lead developer
Pharmbio Korea
Modality
Small Molecules
Administration
Oral
01

Overview

Levocloperastine is a non-opioid antitussive agent that functions through a dual mechanism of action, affecting both the central nervous system and peripheral receptors. It acts centrally on the bulbar cough center, primarily by exhibiting high-affinity binding as an agonist to sigma-1 (σ1) receptors and by potently inhibiting G-protein-coupled inwardly-rectifying potassium (GIRK) channels within key nuclei of the medulla oblongata, such as the nucleus tractus solitarius (NTS). Additionally, it exerts peripheral effects on the tracheobronchial tree. This combined action suppresses the cough reflex, making it effective for the symptomatic relief of dry cough. Levocloperastine is the levorotatory isomer of cloperastine and is administered orally.

Brand names
Privituss
Other names
levocloperastinelevocloperastine fendizoate saltL-cloperastine fendizoate
02

Targets

GIRK (G protein-coupled inward-rectifier potassium channel)SIGMAR1 (Sigma non-opioid intracellular receptor 1)KACh (G protein–activated inwardly rectifying potassium channel)

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