5-HT3 antagonists under development
- 5-HT3 antagonists under development
- 정유훈; 추현아
- 5-HT3 antagonist; anti-emesis; chemotherapy; IBS; irritable bowel syndrome
- Issue Date
- Expert opinion on investigational drugs
- VOL 19, NO 11, 1309-1319
- Importance of the field: The main therapeutic area of 5-HT3 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-HT3 receptor antagonists is
in the treatment of irritable bowel syndrome (IBS). 5-HT3 antagonists have
been widely used and found to decrease gut transit, increase fluid absorption
and reduce pain. The uses of 5-HT3 antagonists are expending to treatment of
CNS diseases such as anxiety and sleep disorders as antipsychotics and so on.
Areas covered in this review: The structures, in vitro activities, in vivo effects
and some clinical data on 5-HT3 receptor antagonists under development.
What the reader will gain: Future research directions in 5-HT3 antagonists
based on the clinical trial data of the pipeline molecules.
Take home message: Most drug candidates in clinical trials were discovered in
the early 1990s and their patent expiry is imminent. Acquiring intellectual
properties of novel 5-HT3 receptor antagonists with improved efficacies
would provide a bright future. Particularly, as the current 5-HT3 receptor
antagonists are classified into only three representative structural families
(one third are zacopride-like benzamides and the others are ondansteronlike
tricyclic compounds and dolansetron-like bicyclic compounds), structurally
diverse compound libraries need to be extensively investigated for
identification of novel 5-HT3 receptor antagonists.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.