Drug intelligence / Profile preview

dimemorfan

Development stage
Phase 3
Lead developer
Astellas Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Dimemorfan is a nonnarcotic antitussive (cough suppressant) of the morphinan family, structurally related to dextromethorphan and dextrorphan. It is widely used in Japan and also marketed in Spain and Italy. Dimemorfan acts primarily as a potent agonist of the sigma-1 receptor, with little to no activity at NMDA receptors, which distinguishes it from dextromethorphan by reducing dissociative side effects and abuse potential. Its antitussive effect appears to be mediated by direct action on the cough center in the medulla rather than through opioid receptors. Clinical studies indicate that it is as effective or more effective than codeine or dextromethorphan for suppressing cough, with a low incidence of adverse events such as nausea, somnolence, dry mouth, and decreased appetite. Dimemorfan has also demonstrated anti-inflammatory properties via sigma-1 receptor-independent mechanisms involving inhibition of NADPH oxidase activity and NF-kappaB signaling pathways[1][3][4][6].

Brand names
AstominDastosirrTusben
Other names
dimemorphandimemorfan phosphate
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))

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