Drug intelligence / Profile preview

dexfenfluramine

Development stage
Approved
Lead developer
Endo International
Modality
Small Molecules
Administration
Oral
01

Overview

Dexfenfluramine is the S-enantiomer of fenfluramine and a serotonergic anorectic drug that was formerly used as an appetite suppressant for weight loss in obesity. It acts primarily by increasing serotonin levels in the brain through two main mechanisms: inhibition of serotonin reuptake via blockade of the sodium-dependent serotonin transporter, and stimulation of serotonin release from synaptosomes. This leads to enhanced activation of serotonin receptors, particularly in hypothalamic centers regulating feeding behavior, resulting in appetite suppression. Dexfenfluramine does not possess catecholaminergic agonist activity and lacks amphetamine-like stimulant effects. The drug was approved by the US FDA under the brand name Redux but was withdrawn worldwide due to concerns over serious cardiovascular side effects, including valvular heart disease and primary pulmonary hypertension[1][2][3][4].

Brand names
Redux
Other names
dexfenfluramine hydrochloride
02

Targets

HTR2B (5-Hydroxytryptamine Receptor 2B)HTR2C (5-hydroxytryptamine 2C receptor)SERT (Sodium-dependent serotonin transporter)

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