APD125, our lead drug candidate for insomnia, is being evaluated in a Phase 2b clinical trial. In the Phase 2a clinical trial, which evaluated the safety and efficacy of nighttime dosing in patients with chronic insomnia, APD125 significantly improved endpoints measuring improvements in sleep maintenance, including Wake After Sleep Onset and Wake Time During Sleep. Significant improvements also were seen in other important measurements of sleep maintenance, including a decrease in the number of awakenings and arousals. In addition, APD125 significantly increased time spent in deep (stage 3 and 4) sleep and at the same time decreased the amount of time spent in light (stage 1) sleep. Treatment with APD125 was well tolerated in the trial, with no reports of serious adverse events and no emerging safety findings as compared to placebo. No next day impairment of cognitive function was observed.
Most currently approved therapies for insomnia work by activating 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 GABAergic drugs include the risk of developing tolerance and drug dependency in at-risk populations. In addition, GABAergic drugs are DEA-scheduled, controlled substances due to their potential for abuse.
APD125 acts through a different mechanism than currently marketed insomnia drugs. Based on our preclinical data, we believe that by selectively targeting the 5-HT2A receptor, APD125 blocks one of several CNS-activating pathways, rather than initiating a general CNS-suppressive effect. Because of the different mechanism of action, APD125 may not have the side effects generally associated with currently approved GABAergic drugs. Through this novel mechanism, APD125 has the potential to reduce insomnia symptoms and improve sleep maintenance.
The National Institutes of Health estimated in 2003 that between 30 to 40% of United States adults report some level of insomnia and that insomnia is a chronic problem for about 10% of the United States population. In these cases, the lack of restful sleep impairs the person's ability to carry out their daily responsibilities because they are too tired or have trouble concentrating. Despite the limitations of currently approved therapies, worldwide sales estimates for insomnia medications were over $3.5 billion in 2006.
Our product candidates have not been approved by the U.S. Food and Drug Administration or any international regulatory agency.
(NOTE: This page was last updated: June 5, 2008.)
