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Cilansetron

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Cilansetron
Clinical data
Other namesCalmactin; KC 9946
Pregnancy
category
  • C
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • Unlicensed
Pharmacokinetic data
Bioavailability87%
MetabolismHepatic
Eliminationhalf-life1.6 - 1.9 hours
ExcretionRenal
Identifiers
  • (10R)-10-[(2-Methyl-1H-imidazol-1-yl)methyl]-5,6,9,10-tetrahydro-4H-pyrido(3,2,1-jk)carbazol-11-one
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC20H21N3O
Molar mass319.408 g·mol−1
3D model (JSmol)
  • O=C3c2c1cccc5c1n(c2CC[C@@H]3Cn4ccnc4C)CCC5
  • InChI=1S/C20H21N3O/c1-13-21-9-11-22(13)12-15-7-8-17-18(20(15)24)16-6-2-4-14-5-3-10-23(17)19(14)16/h2,4,6,9,11,15H,3,5,7-8,10,12H2,1H3/t15-/m1/s1 checkY
  • Key:NCNFDKWULDWJDS-OAHLLOKOSA-N checkY
  (verify)

Cilansetron is an experimental drug that is a5-HT3 antagonist underdevelopment bySolvay Pharmaceuticals.[1][2][3]

5-HT3 receptors are responsible for causing many things from nausea to excessbowel movements. In conditions such asirritable bowel syndrome (IBS), the receptors have become faulty or oversensitive. 5-HT3 antagonists work by blocking the nervous and chemical signals from reaching these receptors.

Studies have shown that the drug can improve quality of life in men and women with diarrhea-predominant IBS.[4] Cilansetron is the first 5-HT antagonist specifically designed for IBS that is effective in men as well as women.[4]

In 2005, Solvay received response from the U.S. Food and Drug Administration that cilansertron is not approvable without additional clinical trials;[5][6] further development has been discontinued.[7]

References

[edit]
  1. ^Chey WD, Cash BD (February 2005). "Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea".Expert Opinion on Investigational Drugs.14 (2):185–93.doi:10.1517/13543784.14.2.185.PMID 15757394.S2CID 8606399.
  2. ^Olden KW, Crowell MD (October 2005). "Cilansetron".Drugs of Today.41 (10). Barcelona, Spain:661–6.doi:10.1358/dot.2005.41.10.920427.PMID 16389408.
  3. ^Stacher G (October 2007). "Cilansetron in the treatment of diarrhea-predominant irritable bowel syndrome?".Expert Review of Gastroenterology & Hepatology.1 (1):15–27.doi:10.1586/17474124.1.1.15.PMID 19072430.S2CID 24301639.
  4. ^abGeneral info on Cilansetron
  5. ^"Solvay's cilansetron "not approvable"". PharmaTimes. April 4, 2005. RetrievedAugust 14, 2019.
  6. ^"Calmactin Approval Status".Drugs.com. RetrievedAugust 14, 2019.
  7. ^"Cilansetron". RetrievedAugust 14, 2019.
Drugs for
functional
bowel
disorders
Antimuscarinics
Tertiary
amino group
Quaternary
ammonium

compounds
Phosphodiesterase
inhibitors
Acting on
serotonin receptors
Other
Belladonna
and derivatives
(antimuscarinics)
Propulsives
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Retrieved from "https://en.wikipedia.org/w/index.php?title=Cilansetron&oldid=1330780244"
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