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
ATC code	A03AE03
PubChem	CID 6918107
IUPHAR/BPS	2297
ChemSpider	5293321
UNII	2J6DQ1U5B5
KEGG	D03495
ChEMBL	CHEMBL2103778
Chemical data
Formula	C20H21N3O
Molar 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 ; Key:NCNFDKWULDWJDS-OAHLLOKOSA-N ;
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シランセトロン

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/12 18:04:24」(JST)

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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 At time of writing; Solvay had recently withdrawn its application to the U.S. Food and Drug Administration (FDA) but was continuing its talks with the MHRA in the UK and EU regulators.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.^{[citation needed]}

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

http://www.drugdevelopment-technology.com/projects/cilanserton (General info on Cilansetron.)
http://www.solvaypress.com/pressreleases/0,,36423-2-0,00.htm#contact (Sovay press relaase 19 November 2005.)
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)

UpToDate Contents

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1. 過敏性腸症候群に対するアロセトロン塩酸塩（Lotronex） alosetron hydrochloride lotronex for irritable bowel syndrome
2. 過敏性腸症候群の治療 treatment of irritable bowel syndrome

English Journal

The clinical potential of ramosetron in the treatment of irritable bowel syndrome with diarrhea (IBS-D).

Min YW1, Rhee PL2.
Therapeutic advances in gastroenterology.Therap Adv Gastroenterol.2015 May;8(3):136-42. doi: 10.1177/1756283X15572580.
Irritable bowel syndrome (IBS) is a highly prevalent functional bowel disorder. Serotonin (5-HT) is known to play a physiological and pathophysiological role in the regulation of gastrointestinal function. In experimental studies, 5-HT3 receptor antagonists have been reported to slow colon transit,
PMID 25949526

The risk of ischaemic colitis in irritable bowel syndrome patients treated with serotonergic therapies.

Lewis JH1.
Drug safety.Drug Saf.2011 Jul 1;34(7):545-65. doi: 10.2165/11590690-000000000-00000.
Ischaemic colitis (IC) is the most common form of ischaemic injury to the gastrointestinal (GI) tract. IC typically presents with the sudden onset of lower abdominal pain, cramping and rectal bleeding, and is usually self-limited with low morbidity, although it may cause gangrenous or fulminant coli
PMID 21663331

Alosetron, cilansetron and tegaserod modify mesenteric but not colonic blood flow in rats.

Painsipp E1, Shahbazian A, Holzer P.
British journal of pharmacology.Br J Pharmacol.2009 Nov;158(5):1210-26. doi: 10.1111/j.1476-5381.2009.00392.x. Epub 2009 Sep 25.
BACKGROUND AND PURPOSE: As the use of the 5-HT(3) receptor antagonist alosetron (GlaxoSmithKline) and the 5-HT(4) receptor agonist tegaserod (Novartis) in patients with irritable bowel syndrome has been associated with cases of ischaemic colitis, the effects of alosetron, cilansetron (Solvay) and te
PMID 19785647

Japanese Journal

Evaluation of the Pharmacological Profile of Ramosetron, a Novel Therapeutic Agent for Irritable Bowel Syndrome

HIRATA Takuya,KETO Yoshihiro,FUNATSU Toshiyuki,AKUZAWA Shinobu,SASAMATA Masao
Journal of pharmacological sciences 104(3), 263-273, 2007-07-20
… We examined the pharmacological profile of ramosetron, a 5-HTsub3/sub-receptor antagonist for irritable bowel syndrome with diarrhea, comparing it with those of other 5-HTsub3/sub-receptor antagonists, alosetron and cilansetron, and the anti-diarrheal agent loperamide. … Dissociation of ramosetron from the human 5-HTsub3/sub receptor was extremely slow (tsub1/2/sub = 560 min), while alosetron (tsub1/2/sub = 180 min) and cilansetron (tsub1/2/sub = 88 min) dissociated relatively rapidly. …
NAID 10024314859

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