Cilansetron

Cilansetron

Systematic (IUPAC) name
(10R)-10-[(2-methyl-1H-imidazol-1-yl)methyl]-5,6,9,10 -tetrahydro-4H-pyrido(3,2,1-jk)carbazol-11-one
Clinical data
Pregnancy category	C
Legal status	Unlicensed
Routes of administration	Oral
Pharmacokinetic data
Bioavailability	87%
Metabolism	Hepatic
Biological half-life	1.6 - 1.9 hours
Excretion	Renal
Identifiers
CAS Number	120635-74-7 Y
ATC code	A03AE03 (WHO)
PubChem	CID: 6918107
IUPHAR/BPS	2297
ChemSpider	5293321 Y
UNII	2J6DQ1U5B5 Y
KEGG	D03495 Y
ChEMBL	CHEMBL2103778
Chemical data
Formula	C20H21N3O
Molecular mass	319.4 g/mol
SMILES O=C3c2c1cccc5c1n(c2CC[C@@H]3Cn4ccnc4C)CCC5
InChI 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 Y Key:NCNFDKWULDWJDS-OAHLLOKOSA-N Y
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Cilansetron is a drug that is a 5HT-3 antagonist currently under trial phase in the EU and US it is manufactured by Solvay Pharmaceuticals INC.

5HT-3 receptors are responsible for causing many things from nausea to excess bowel movements. It is thought in conditions like irritable bowel syndrome (IBS) the receptors have become faulty or oversensitive. 5HT-3 antagonists work by blocking the nervous and chemical signals from reaching these receptors.

Studies have shown that the drug can greatly improve quality of life in men and women with diahorrea predominant IBS (1) Cilansetron is the first 5HT antagonist specifically designed for IBS that is effective in men as well as women.(1)

Solvay has had considerable difficulty with the medicines regulators in the UK, EU and USA with regards to licensing the drug. This could possibly be due to the problems discovered after licensing with the drug Lotronex. At time of writing; Solvay had recently withdrawn its application to the U.S. Food and Drug Administration (FDA) but was continuing its talks with the MHRA in the UK and EU regulators. (2)

It is not currently known what sort of timeframe the public are looking at to be able to obtain the drug. This matter is not helped by the lack of information about cilansetron and its trials in the public domain. The regulators have also stated this in their responses.

There is no information about future trials currently available.

Some people have tried the Anti-emetic ondansetron HCl (Zofran) as a substitute for the time being, results are mixed but noted effect has been shown in some males and females (3) However; due to its license in the UK it is usually only prescribable at consultant level. Since the licensing of a generic version it is more likely an NHS prescription will be accepted as the branded version is very expensive (Official NHS pricing.) In the USA and Canada: availability often depends on insurance and the doctors personal opinion on off-label prescribing.

References

1. http://www.drugdevelopment-technology.com/projects/cilanserton (General info on Cilansetron.)
2. http://www.solvaypress.com/pressreleases/0,,36423-2-0,00.htm#contact (Sovay press relaase 19 November 2005.)
3. http://www.blackwell-synergy.com/doi/abs/10.1046/j.1365-2036.1996.30172000.x (Clinical trial for 5-HT3 antagonists use in Diarrhoea-predominant IBS)