Drug intelligence / Profile preview

trebenzomine

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Trebenzomine (CI-686) is a chromanamine derivative developed in the late 1970s as a psychotropic agent with potential applications in psychiatry. Initially characterized in animal models as an atypical antipsychotic due to its ability to antagonize certain dopaminergic effects without inducing catalepsy or elevating serum prolactin, it failed to demonstrate clinical efficacy in double-blind trials for schizophrenia when compared to standard neuroleptics like thioridazine. However, trebenzomine showed significant therapeutic promise as an antidepressant and anxiolytic, demonstrating efficacy comparable to doxepin in patients with anxious depression. Its pharmacological profile is primarily associated with the inhibition of norepinephrine reuptake, distinguishing it from classical antipsychotics. Development of the compound was ultimately discontinued following its failure in schizophrenia trials.

Other names
trebenzomine hydrochlorideN,N,2-trimethyl-3-chromanamine
02

Targets

NET (Norepinephrine Transporter)DRD2 (Dopamine D2 Receptor)

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