Lorcaserin

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Lorcaserin is a weight-loss drug developed by Arena Pharmaceuticals. It has serotonergic properties and acts as an anorectic. On 27 June 2012, the FDA officially approved lorcaserin for use in the treatment of obesity for adults with a BMI equal to or greater than 30 or adults with a BMI of 27 or greater who "have at least one weight-related health condition, such as high blood pressure, type 2 diabetes, or high cholesterol".

Mechanism of action

Lorcaserin is a selective 5-HT_2C receptor agonist and in vitro testing of the drug showed reasonable selectivity for 5-HT_2C over other related targets.

5-HT_2C receptors are located almost exclusively in the brain, and can also be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus.

The activation of 5-HT_2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety. This hypothesis is supported by clinical trials and other studies.

Side effects

Lorcaserin was shown in phase III testing to be a mild and tolerable.

• Trial participants found lorcaserin about as tolerable as placebo, with 7% of participants in both the lorcaserin drug and placebo arms dropping out due to side effects.