Pruvanserin


Pruvanserin is a selective serotonin 5-HT2A receptor antagonist which was under development by Eli Lilly and Company for the treatment of insomnia. It was in phase II clinical trials in 2008 but appears to have been discontinued as it is no longer in the company's development pipeline.

Pharmacology

Pharmacodynamics

Pruvanserin acts as a selective serotonin 5-HT2A receptor antagonist. In addition to its sleep-improving properties, pruvanserin has also been shown to have antidepressant, anxiolytic, and working memory-enhancing effects in animal studies.

Pharmacodynamics

The time to peak levels of pruvanserin is 2 to 3hours, with a range of 2 to 6hours. The mean elimination half-life of pruvanserin is 8.6 to 9.5hours, with a range of 3.9 to 12.4hours. However, its brain serotonin 5-HT2A receptor occupancy lasts much longer, with a half-life of approximately 24hours.