Drug intelligence / Profile preview

CWHM-974

Development stage
Preclinical
Lead developer
Washington University in St. Louis
Modality
Small Molecules
Administration
Oral
01

Overview

CWHM-974 is a novel phenothiazine derivative and an N-benzyl-linked analog of fluphenazine. Originally designed to treat brain-resident fungal infections, it has been repurposed for the treatment of primary brain tumors and brain metastases, such as melanoma. Unlike traditional phenothiazines that act as potent dopamine and serotonin receptor antagonists (leading to sedation), CWHM-974 is 100-1000-fold less active at these receptors. Its anti-cancer efficacy is primarily attributed to its activity as a calmodulin (CaM) inhibitor. The compound demonstrates 2-10-fold higher potency than fluphenazine across various cancer cell lines and is designed to penetrate the blood-brain barrier.

Other names
N-benzyl-linked fluphenazine derivative
02

Targets

CaM (Calmodulin)

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