Drug intelligence / Profile preview

Mazindol ER

Development stage
Phase 3
Lead developer
NLS Pharmaceutics
Modality
Small Molecules
Administration
Oral
01

Overview

Mazindol ER is an **extended-release oral formulation** of mazindol, a small-molecule **central nervous system (CNS) stimulant** that acts as a **triple monoamine reuptake inhibitor** (dopamine, norepinephrine, and serotonin transporters) and a **partial agonist at the orexin-2 (OX2R)** receptor[1][4][5][9]. It is being developed primarily for the treatment of **narcolepsy with cataplexy**, but studies and preclinical programs are also exploring its use in **idiopathic hypersomnia, ADHD, and opioid dependence** (notably fentanyl dependence)[2][5][6]. Mazindol ER has demonstrated significant improvements in cataplexy severity and excessive daytime sleepiness in adults with narcolepsy, showing sustained benefits in open-label extension studies[1][2]. The drug displays a **well-tolerated safety profile**, low risk of drug-drug interactions, fast onset of action, and pharmacological differentiation from other treatments for narcolepsy[4][8]. Mechanistically, in addition to monoamine reuptake inhibition, mazindol ER is believed to modulate the **5-HT1A receptor** and exhibit **partial mu-opioid receptor (MOP) agonist activity**, supporting its exploration for substance-use disorders[6][7]. It is **commercially developed by NLS Pharmaceutics**.

Brand names
Quilience
Other names
Mazindol Extended Release
02

Targets

SERT (Sodium-dependent serotonin transporter)HCRTR2 (Orexin/hypocretin receptor type 2)DAT (Dopamine plasma membrane transport protein)MOR (Mu opioid receptor)NET (Norepinephrine Transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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