Arena Pharmaceuticals Initiates Phase 2b Clinical Trial of APD125 for the Treatment o...(he improvementswere achieved without any...),Health

About APD125

Discovered by Arena, APD125 is a novel and oral selective inverse agonist of the 5-HT2A serotonin receptor. The vast majority of approved drugs for insomnia activate the GABA-A receptor complex in the brain, causing a general suppressive effect on the central nervous system, or CNS. These GABAergic drugs are generally associated with CNS side effects, including a sensation of dullness and lethargy upon awakening, often referred to as the "hangover effect." Other potential problems associated with the GABAergic drugs include the risk of developing tolerance and drug dependency in at-risk populations. In addition, GABAergic drugs are scheduled controlled substances by the Drug Enforcement Administration due to their potential for abuse.

By selectively targeting the 5-HT2A receptor, APD125 acts through a different mechanism than currently marketed insomnia drugs and blocks one of several CNS activating pathways. Because of the different mechanism of action, APD125 may not have the side effects or abuse potential generally associated with currently approved GABAergic drugs. Through its novel mechanism, APD125 has the potential to reduce insomnia symptoms by improving sleep maintenance.

About Insomnia

Insomnia is characterized by inadequate or poor sleep due to nonrefreshing sleep, frequent wakening with difficulty falling back to sleep, difficulty falling asleep or waking too early. Most insomnia complaints relate to sleep maintenance issues, such as waking frequently or awakening too early, as opposed to problems with sleep latency (i.e. falling asleep). About 30% of US adults report some level of insomnia in the course of a year, and about 10% of US adults indicate that their condition is chronic. In these cases, the lack of restful sleep i
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