Drug intelligence / Profile preview

fenfluramine + naloxone

Development stage
Unknown
Lead developer
UCB
Modality
Small Molecules
01

Overview

Fenfluramine + naloxone is a combination of two pharmaceutical agents, each with distinct mechanisms of action. Fenfluramine is a serotonergic agent that acts primarily as a serotonin (5-HT) releaser and reuptake inhibitor, leading to increased extracellular serotonin levels in the brain. This results in appetite suppression and, at higher doses or specific indications, anti-epileptic effects through agonism at 5-HT2C receptors and antagonism at sigma-1 receptors[2][8][10]. Naloxone is an opioid receptor antagonist that blocks the effects of opioids by competitively binding to opioid receptors without activating them[6]. It is primarily used for reversing opioid overdose but also appears in combination products to deter misuse of other drugs. There are no known approved or marketed products combining fenfluramine and naloxone as a fixed-dose formulation; however, both drugs have been studied individually and together for their pharmacological interactions on neuroendocrine axes[2], appetite regulation[7], and potential drug-drug interactions[1][3].

02

Targets

FLNA (Filamin A)MOR (Mu opioid receptor)HTR1D (5-hydroxytryptamine receptor 1D)HTR2C (5-hydroxytryptamine 2C receptor)SIGMAR1 (Sigma non-opioid intracellular receptor 1)SERT (Sodium-dependent serotonin transporter)

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