Drug intelligence / Profile preview

Adrafinil

Development stage
Discontinued
Lead developer
Teva Pharmaceutical Industries
Modality
Small Molecules
Administration
Oral
01

Overview

Adrafinil is a synthetic central nervous system stimulant and prodrug that is metabolized in the body to modafinil. It was formerly marketed in France under the brand name Olmifon for promoting wakefulness, alertness, and attention, particularly in elderly patients with excessive sleepiness or inattention[1][3][4]. Adrafinil has been used off-label as a nootropic to prevent fatigue and improve mental alertness but lacks FDA approval and is unregulated in the United States[1][2]. The drug was withdrawn from the market in France due to regulatory reassessment[1][3]. Its mechanism of action is not fully understood; however, it acts primarily through its active metabolite modafinil. Modafinil’s effects are believed to be mediated by weak inhibition of dopamine reuptake via binding at the sodium-dependent dopamine transporter (DAT), leading to increased extracellular dopamine levels. Additional mechanisms may include modulation of glutamate and GABA transmission, increased serotonin release, and activation of orexin neurotransmission[3][6][7]. Adrafinil itself does not appear to directly bind adrenergic receptors or cause peripheral sympathomimetic effects[3].

Brand names
Olmifon
Other names
adrafinil2-(diphenylmethyl)sulfinyl-N-hydroxyacetamide
02

Targets

SERT (Sodium-dependent serotonin transporter)DAT (Dopamine plasma membrane transport protein)

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