Drug intelligence / Profile preview

fenfluramine + mazindol

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

Overview

Fenfluramine + mazindol is a combination of two small-molecule drugs, both previously used as appetite suppressants in the treatment of obesity. Fenfluramine acts primarily as a serotonin releasing agent and agonist at several serotonin receptors (notably 5-HT2C), while also antagonizing sigma-1 receptors. Mazindol is a tricyclic anorectic agent that inhibits the reuptake of norepinephrine, dopamine, and to a lesser extent serotonin, thereby reducing appetite. The combination was studied for short-term weight loss efficacy and was found to be more effective than placebo with no evidence of addiction or severe adverse effects in short-term trials. However, both agents have been associated with cardiovascular risks; fenfluramine in particular has been linked to valvular heart disease and pulmonary hypertension when used chronically or at higher doses[3][1][4]. This specific combination does not have an established unique brand name or widespread regulatory approval.

02

Targets

SERT (Sodium-dependent serotonin transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)HTR2C (5-hydroxytryptamine 2C receptor)NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)HTR2B (5-Hydroxytryptamine Receptor 2B)

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