ABOUT
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Lorcaserin, marketed under the brand name Belviq[4][5] is a weight-loss drug developed by Arena Pharmaceuticals. It reduces appetite by activating a type of serotonin receptor known as the 5-HT2C receptor in a region of the brain called the hypothalamus, which is known to control appetite.[6] It was removed from the market in the United States in 2020 due to an increased risk of cancer detected in users of Belviq.
Lorcaserin is used long term for weight loss in those who are obese.[8]
Side effects
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In December 2012, the US Drug Enforcement Administration proposed classifying lorcaserin as a Schedule IV drug because it has hallucinogenic properties at higher than approved doses and users could develop psychiatric dependencies on the drug.[9][10] On 7 May 2013, the US Drug Enforcement Administration classified lorcaserin as a Schedule IV drug[11] under the Controlled Substances Act.[9]
There has been concern that lorcaserin can cause cardiac valvulopathy based upon the reports of subjects taking the drug in Phase 2 trials. However, a Phase 3 clinical trial of the drug was conducted and the results published in the October 2014 Postgraduate Medicine journal, a peer-reviewed medical journal for physicians. These results found no statistically significant differences in valvulopathy rates compared to control, being 2.4% for the drug subjects and 2.0% for controls, and concluded that the drug is safe for the target population[12][13] although more long-term data is needed.[14]
A drug safety communication from the US Food and Drug Administration (FDA), in January 2020, stated that a clinical trial demonstrated a possible increased risk of cancer for those taking lorcaserin.[15] The FDA approval of lorcaserin required the manufacturer to conduct a randomized, double-blind, placebo-controlled clinical trial to evaluate the risk of heart-related problems.[15] The trial was conducted in approximately 12,000 participants over five years and more patients taking lorcaserin were diagnosed with cancer compared to patients taking placebo.[15]
In February 2020, the FDA requested that the manufacturer lorcaserin voluntarily withdraw the drug from the US market because a safety clinical trial showed an increased occurrence of cancer. The drug manufacturer, Eisai, has submitted a request to voluntarily withdraw the drug.[16]
Mechanism of action
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Lorcaserin is a selective 5-HT2C receptor agonist,[17][18] and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets.[19][20][21] 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The activation of 5-HT2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety.[22] This hypothesis is supported by clinical trials and other studies. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, and endocrine secretion,[23] the exact mechanism of appetite regulation is not yet known. Lorcaserin has shown 100x selectivity for 5-HT2C versus the closely related 5-HT2B receptor, and 17x selectivity over the 5-HT2A receptor ongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
