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| {{SI}}
| | #REDIRECT [[Lorcaserin Hydrochloride Hemihydrate]] |
| {{CMG}}; '''Associate Editor(s)-In-Chief:''' {{UJ}}
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| ==Overview==
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| Lorcaserin is a weight-loss drug developed by Arena Pharmaceuticals. It has [[serotonergic]] properties and acts as an [[anorectic]]. On 27 June 2012, the [[Food and Drug Administration|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]]".
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| ==Mechanism of action==
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| Lorcaserin is a selective [[5-HT2C receptor|5-HT<sub>2C</sub> receptor]] [[agonist]] and ''in vitro'' testing of the drug showed reasonable selectivity for 5-HT<sub>2C</sub> over other related targets. | |
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| 5-HT<sub>2C</sub> receptors are located almost exclusively in the brain, and can also be found in the [[choroid plexus]], [[Cerebral cortex|cortex]], [[hippocampus]], [[cerebellum]], [[amygdala]], [[thalamus]], and [[hypothalamus]].
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| The activation of 5-HT<sub>2C</sub> 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.
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| ==Side effects==
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| Lorcaserin was approximately as tolerable as placebo in Phase III, with 7% of participants in both the lorcaserin drug and placebo arms dropping out due to side effects.
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| The drug side effects compared with the placebo are listed in the following table:
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| {| class=wikitable border=1
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| !Side effects
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| !Placebo (%)
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| !Drug arm (%)
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| |-
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| |[[Headache]] (most common)
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| |11
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| |18
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| |-
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| |[[Upper respiratory tract infection]]
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| |11.9
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| |14.8
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| |-
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| |[[Nasopharyngitis]]
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| |12.0
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| |13.4
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| |-
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| |[[Nausea]]
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| |5.4
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| |7.5
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| |-
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| |}
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| It was reported by national news-media that lorcaserin was associated with the development of cancer in laboratory rats.<ref name="sfgate">{{cite news|url=http://www.sfgate.com/cgi-bin/article.cgi?f=/c/a/2010/09/15/BU521FDLBC.DTL|title=FDA staff says Arena diet pill linked to cancer|publisher=SFGate|date=15 September 2010 | first=Catherine | last=Larkin}}</ref>
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| ==Supportive trial data==
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| ===BLOOM===
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| [http://clinicaltrials.gov/ct2/show/NCT00395135?term=Bloom+lorcaserin&rank=1]
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| BLOOM top line results were released on 30 March 2009. Measurements of [[efficacy]] using an [[intention to treat]] – [[last observation carried forward]] (ITT-LOCF), analysis showed that 47.5% of lorcaserin patients lost at least 5% of their body weight, compared to 20.3% for placebo.
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| ===BLOSSOM===
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| [http://clinicaltrials.gov/ct2/show/NCT00603902]
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| BLOSSOM results were released on September 18, 2009. Measurements of efficacy using an intent-to-treat last observation carried forward, or ITT-LOCF, analysis showed that 47.2% of lorcaserin patients lost at least 5% of their body weight, compared to 25.0% for placebo. Lorcaserin patients achieved an average weight loss of 5.9%, or 12.7 pounds, compared to 2.8%, or 6.3 pounds, for placebo.
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| ==References==
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| {{Reflist|2}}
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| [[Category:Antiobesity drugs]]
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| [[Category:Serotonin receptor agonists]]
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| [[Category:Organochlorides]]
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| [[Category:Benzazepines]]
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| {{WH}}
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| {{WS}}
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