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CNS & Neurological Disorders - Drug Targets

Editor-in-Chief

ISSN (Print): 1871-5273
ISSN (Online): 1996-3181

Perspective

Lorcaserin: Worthy of Further Insights? Results from Recent Research

Author(s): Marianna Mazza*, Georgios D. Kotzalidis, Giuseppe Marano, Domenico De Berardis, Giovanni Martinotti, Enrico Romagnoli, Giuseppe Biondi-Zoccai, Antonio Abbate and Gabriele Sani

Volume 23, Issue 3, 2024

Published on: 28 April, 2023

Page: [278 - 283] Pages: 6

DOI: 10.2174/1871527322666230330124137

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Abstract

Lorcaserin is a 3-benzazepine that binds 5-HT2C serotonin receptors in the hypothalamus, where it mediates lack of hunger and/or satiety, and in the ventral tegmental area, the site of origin of the mesolimbic and mesocortical dopaminergic projections, which mediate pleasure and reward. The drug has been first developed for the treatment of obesity, where it has shown efficacy, and subsequently trialed to counter substance use (mostly cocaine, cannabis, opioids, and nicotine) and craving, but showed inconsistent effects. Since 2020, the US Food and Drug Administration obtained that the drug was voluntarily withdrawn from the US market on the grounds that its long-term use was found to be associated with a greater incidence of some types of cancer. Provided it can show to be free from cancerogenic effects, ongoing research suggests that lorcaserin may have therapeutic potential for a variety of disorders and conditions beyond obesity. Since 5-HT2C receptors are involved in many diversified physiological functions (mood, feeding, reproductive behavior, neuronal processes related to impulsiveness, and modulating reward-related mechanisms) this drug has the potential to treat different central nervous system conditions, such as depression and schizophrenia.

Keywords: Lorcaserin, 5-HT2C serotonin receptors, obesity, cocaine use disorder, nicotine use disorder, cancer risk.

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