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 cat.
C
Legal status
Unlicensed
Routes
Oral
Pharmacokinetic data
Bioavailability
87%
Metabolism
Hepatic
Half-life
1.6 - 1.9 hours
Excretion
Renal
Identifiers
CAS number
120635-74-7 Y
ATC code
A03 AE03
PubChem
CID 6918107
ChemSpider
5293321 Y
UNII
2J6DQ1U5B5 Y
KEGG
D03495 Y
Chemical data
Formula
C 20 H 21 N 3 O
Mol. mass
319.4 g/mol
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 Y
Key:NCNFDKWULDWJDS-OAHLLOKOSA-N Y
Y (what is this?) (verify)
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 At time of writing; Solvay had recently withdrawn its application to the U.S. Food and Drug Administration (FDA) but was continuing its talks with the MHRA in the UK and EU regulators.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 [ edit ]
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)
Agonists : Azapirones : Alnespirone
Binospirone
Buspirone
Enilospirone
Eptapirone
Gepirone
Ipsapirone
Perospirone
Revospirone
Tandospirone
Tiospirone
Umespirone
Zalospirone ; Antidepressants : Etoperidone
Nefazodone
Trazodone
Vortioxetine ; Antipsychotics : Aripiprazole
Asenapine
Clozapine
Quetiapine
Ziprasidone ; Ergolines : Dihydroergotamine
Bromocriptine
Ergotamine
Lisuride
Methysergide
LSD ; Tryptamines : 5-CT
5-MeO-DMT
5-MT
Bufotenin
DMT
Indorenate
Psilocin
Psilocybin ; Others : 8-OH-DPAT
Adatanserin
Bay R 1531
Befiradol
BMY-14802
Cannabidiol
Dimemebfe
Ebalzotan
Eltoprazine
F-11,461
F-12,826
F-13,714
F-14,679
F-15,063
F-15,599
Flesinoxan
Flibanserin
Lesopitron
LY-293,284
LY-301,317
MKC-242
Naluzotan
NBUMP
Osemozotan
Oxaflozane
Pardoprunox
Piclozotan
Rauwolscine
Repinotan
Roxindole
RU-24,969
S 14,506
S-14,671
S-15,535
Sarizotan
SSR-181,507
Sunepitron
U-92,016-A
Urapidil
Vilazodone
Xaliproden
Yohimbine
Antagonists : Antipsychotics : Iloperidone
Risperidone
Sertindole ; Beta blockers : Alprenolol
Cyanopindolol
Iodocyanopindolol
Oxprenolol
Pindobind
Pindolol
Propranolol
Tertatolol ; Others : AV965
BMY-7,378
CSP-2503
Dotarizine
Flopropione
GR-46611
Isamoltane
Lecozotan
Mefway
Metitepine/Methiothepin
MPPF
NAN-190
Robalzotan
S-15535
SB-649,915
SDZ 216-525
Spiperone
Spiramide
Spiroxatrine
UH-301
WAY-100,135
WAY-100,635
Xylamidine
Agonists : Lysergamides : Dihydroergotamine
Methysergide ; Triptans : Almotriptan
Avitriptan
Eletriptan
Frovatriptan
Naratriptan
Rizatriptan
Sumatriptan
Zolmitriptan ; Tryptamines : 5-CT
5-Ethyl-DMT
5-MT
5-(Nonyloxy)tryptamine ; Others : CP-135,807
Bromocriptine
CP-286,601
GR-46611
L-694,247
L-772,405
PNU-109,291
PNU-142633
Antagonists : Lysergamides : Metergoline ; Others : Alniditan
BRL-15,572
Elzasonan
GR-127,935
Ketanserin
LY-310,762
LY-367,642
LY-456,219
LY-456,220
Metitepine/Methiothepin
Ritanserin
Yohimbine
Ziprasidone
Agonists : Phenethylamines : 2C-B
2C-E
2C-I
2C-T-2
2C-T-7
2C-T-21
DOB
DOC
DOI
DOM
MDA
MDMA
Mescaline ; Piperazines : Aripiprazole
mCPP
TFMPP ; Tryptamines : 5-CT
5-MeO-α-ET
5-MeO-α-MT
5-MeO-DET
5-MeO-DiPT
5-MeO-DMT
5-MeO-DPT
5-MT
α-ET
α-Methyl-5-HT
α-MT
Bufotenin
DET
DiPT
DMT
DPT
Psilocin
Psilocybin ; Others : A-372,159
AL-38022A
Alstonine
Bromocriptine
CP-809,101
Dimemebfe
Lorcaserin
Medifoxamine
MK-212
Org 12,962
ORG-37,684
Oxaflozane
PHA-57378
PNU-22394
PNU-181731
Ro60-0175
Ro60-0213
Vabicaserin
WAY-629
WAY-161,503
YM-348
Antagonists : Atypical antipsychotics : Clorotepine
Clozapine
Iloperidone
Melperone
Olanzapine
Paliperidone
Quetiapine
Risperidone
Sertindole
Ziprasidone
Zotepine ; Typical antipsychotics : Chlorpromazine
Loxapine
Pimozide
Pipamperone ; Antidepressants : Agomelatine
Amitriptyline
Amoxapine
Aptazapine
Etoperidone
Fluoxetine
Mianserin
Mirtazapine
Nefazodone
Nortriptyline
Tedatioxetine
Trazodone ; Others : Adatanserin
CEPC
Cinanserin
Cyproheptadine
Deramciclane
Dotarizine
Eltoprazine
Esmirtazapine
FR-260,010
Ketanserin
Ketotifen
Latrepirdine
Metitepine/Methiothepin
Methysergide
Pizotifen
Ritanserin
RS-102,221
S-14,671
SB-200,646
SB-206,553
SB-221,284
SB-228,357
SB-242,084
SB-243,213
SDZ SER-082
Xylamidine
Agonists : Lysergamides : Dihydroergotamine
Ergotamine
Lisuride
LSD
Mesulergine
Metergoline
Methysergide ; Tryptamines : 2-Methyl-5-HT
5-BT
5-CT
5-MT
Bufotenin
E-6801
E-6837
EMD-386,088
EMDT
LY-586,713
N -Methyl-5-HT
Tryptamine ; Others : WAY-181,187
WAY-208,466
Antagonists : Antidepressants : Amitriptyline
Amoxapine
Clomipramine
Doxepin
Mianserin
Nortriptyline ; Atypical antipsychotics : Aripiprazole
Asenapine
Clorotepine
Clozapine
Fluperlapine
Iloperidone
Olanzapine
Tiospirone ; Typical antipsychotics : Chlorpromazine
Loxapine ; Others : BGC20-760
BVT-5182
BVT-74316
Cerlapirdine
EGIS-12,233
GW-742,457
Ketanserin
Latrepirdine
Lu AE58054
Metitepine/Methiothepin
MS-245
PRX-07034
Ritanserin
Ro04-6790
Ro 63-0563
SB-258,585
SB-271,046
SB-357,134
SB-399,885
SB-742,457
Agonists : Lysergamides : LSD ; Tryptamines : 5-CT
5-MT
Bufotenin ; Others : 8-OH-DPAT
AS-19
Bifeprunox
E-55888
LP-12
LP-44
RU-24,969
Sarizotan
Antagonists : Lysergamides : 2-Bromo-LSD
Bromocriptine
Dihydroergotamine
Ergotamine
Mesulergine
Metergoline
Methysergide ; Antidepressants : Amitriptyline
Amoxapine
Clomipramine
Imipramine
Maprotiline
Mianserin ; Atypical antipsychotics : Amisulpride
Aripiprazole
Asenapine
Clorotepine
Clozapine
Olanzapine
Risperidone
Sertindole
Tiospirone
Ziprasidone
Zotepine ; Typical antipsychotics : Chlorpromazine
Loxapine ;
Pimozide ; Others : Butaclamol
EGIS-12,233
Ketanserin
LY-215,840
Metitepine/Methiothepin
Ritanserin
SB-258,719
SB-258,741
SB-269,970
SB-656,104
SB-656,104-A
SB-691,673
SLV-313
SLV-314
Spiperone
SSR-181,507
Vortioxetine