5-HT₃ antagonists under development.
BACKGROUND
The main therapeutic area of 5-HT(3) receptor antagonists is the treatment of chemotherapy-induced nausea and vomiting (CINV), which is the most common and distressing side effects of anticancer treatment. The second major clinical application of 5-HT(3) receptor antagonists is in the treatment of irritable bowel syndrome (IBS). 5-HT(3) antagonists have been widely used and found to decrease gut transit, increase fluid absorption and reduce pain. The uses of 5-HT(3) antagonists are expending to treatment of CNS diseases such as anxiety and sleep disorders as antipsychotics and so on.


METHODS
The structures, in vitro activities, in vivo effects and some clinical data on 5-HT(3) receptor antagonists under development.


RESULTS
Future research directions in 5-HT(3) antagonists based on the clinical trial data of the pipeline molecules.


CONCLUSIONS
Most drug candidates in clinical trials were discovered in the early 1990s and their patent expiry is imminent. Acquiring intellectual properties of novel 5-HT(3) receptor antagonists with improved efficacies would provide a bright future. Particularly, as the current 5-HT(3) receptor antagonists are classified into only three representative structural families (one third are zacopride-like benzamides and the others are ondansteron-like tricyclic compounds and dolansetron-like bicyclic compounds), structurally diverse compound libraries need to be extensively investigated for identification of novel 5-HT(3) receptor antagonists.
Konkuk University, Bio/Molecular Informatics Center, Department of Bioscience and Biotechnology, 1 Hwayang-dong, Gwangjin-gu, Seoul 143-701, Republic of Korea.
Youhoon
Y
Chong
Hyunah
H
Choo
D000818:Animals; D002986:Clinical Trials as Topic; D055808:Drug Discovery; D006801:Humans; D058831:Serotonin 5-HT3 Receptor Antagonists / Q000737:chemistry* / Q000494:pharmacology*
D058831:Serotonin 5-HT3 Receptor Antagonists