January 22, 2007

A developing insomnia medication is one step closer to hitting the market as phase II clinical trials of HY10275 demonstrated significant improvements in wake after sleep onset (WASO).

HY10275 is specifically designed to modulate two key neurobiological mechanisms that interfere with the sleeping process, a press release from HY10275 maker, Hypnion Inc, Lexington, Mass, said. The drug is highly selective for histamine H1 and serotonin 5HT2a, two chemical receptors that are known to impact the ability to fall asleep and stay asleep. Born from translational sleep research pioneered by Hypnion cofounder and chief scientific officer, Dale M. Edgar, PhD, HY10275 was rationally designed to “let you sleep” rather than depress the entire brain to “make you sleep.” This dual-acting receptor activity and the lack of affinity for undesired off-target receptors are thought to account for the compounds excellent efficacy and tolerability profile.

According to the company, the results of the recent clinical trial demonstrated that WASO decreased in a dose dependent manner by 62 minutes for 3 mg (p<0.001) and 35 minutes for 1 mg (p<0.002) compared to placebo for the primary efficacy analysis. Subjects with moderate to severe transient insomnia responded as well as or better than subjects with mild to moderate transient insomnia. HY10275 also met secondary efficacy endpoints including latency to persistent sleep (LPS). There were no adverse events attributed to treatment, and there were no reports of next day impairment or residual fatigue.

A Non-scheduled Medication?

Given its mechanism of action, HY10275 may have the opportunity to be classified as a non-scheduled medication. Currently used medications that act via the GABA neurotransmitter system have been associated with physical dependence and drug-seeking behavior, and are therefore classified as controlled substances.

“We are very encouraged by the outcome of this initial Phase II trial, which demonstrates proof of concept for both efficacy and safety of HY10275,” said John F. Dee, president and CEO of Hypnion. “The pharmacodymamic and pharmacokinetic profile of the drug coupled with its unique mechanism of action offers strong promise as a highly differentiated therapeutic. HY10275 could represent a major improvement in the treatment of insomnia as a safe, non-scheduled and well tolerated medication with superior sleep maintenance efficacy and comparable sleep onset efficacy to currently used medications.”