Drug intelligence / Profile preview

cutamesine

Development stage
Phase 2
Lead developer
M's Science
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Cutamesine (SA4503) is a potent and selective small molecule agonist of the sigma-1 receptor, an endoplasmic reticulum-resident chaperone protein. By activating sigma-1 receptors, cutamesine modulates intracellular calcium signaling, reduces oxidative stress, and promotes the expression of neurotrophic factors, thereby enhancing neuroplasticity and neurite outgrowth. It was primarily investigated for its potential to improve functional recovery following ischemic stroke and for the treatment of major depressive disorder. Additionally, it has been explored in neurodegenerative conditions such as Amyotrophic Lateral Sclerosis (ALS) and Parkinson's disease due to its neuroprotective properties. Development was largely led by M's Science Corporation, a subsidiary of Mitsubishi Tanabe Pharma, though clinical progress has largely stalled.

Brand names
Cutamesine
Other names
1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazinecutamesine dihydrochloride
02

Targets

DRD (Dopamine receptors)HRH1 (Histamine H1 Receptor)M1R (Monkeypox virus membrane protein M1)TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))AR (Adrenergic receptors)EBP (Sterol isomerase (emopamil-binding protein))SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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