Lorcaserin: Difference between revisions

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{{SI}}
#REDIRECT [[Lorcaserin Hydrochloride Hemihydrate]]
{{CMG}}; '''Associate Editor(s)-In-Chief:'''  {{UJ}}
==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 [[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]]".
==Mechanism of action==
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.
 
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]].
 
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.
==Side effects==
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.
 
The drug side effects compared with the placebo are listed in the following table:
{| class=wikitable border=1
!Side effects
!Placebo (%)
!Drug arm (%)
|-
|[[Headache]] (most common)
|11
|18
|-
|[[Upper respiratory tract infection]]
|11.9
|14.8
|-
|[[Nasopharyngitis]]
|12.0
|13.4
|-
|[[Nausea]]
|5.4
|7.5
|-
|}
 
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>
==Supportive trial data==
 
===BLOOM===
[http://clinicaltrials.gov/ct2/show/NCT00395135?term=Bloom+lorcaserin&rank=1]
 
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.
 
==References==
{{Reflist|2}}
 
[[Category:Antiobesity drugs]]
[[Category:Serotonin receptor agonists]]
[[Category:Organochlorides]]
[[Category:Benzazepines]]
 
{{WH}}
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Latest revision as of 21:29, 14 January 2015