Velusetrag

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Velusetrag
Velusetrag.svg
Velusetrag2.png
Systematic (IUPAC) name
N-[8-[(2R)-2-hydroxy-3-[methyl(methylsulfonyl)amino]propyl]-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-1-propan-2-ylquinoline-3-carboxamide
Clinical data
Legal status ?
Identifiers
CAS number 866933-46-2
866933-51-9 (hydrochloride)
ATC code None
PubChem CID 53297466
Chemical data
Formula C25H36N4O5S 
Mol. mass 504.642 g/mol

Velusetrag (USAN; TD-5108) is an experimental drug candidate for the treatment of chronic constipation and irritable bowel syndrome.[1] It is a potent, selective, high efficacy 5-HT4 receptor agonist.[2]

In clinical trials, velusetrag was efficacious and well tolerated in patients with chronic constipation,[3] and showed accelerated intestinal and colonic transit after single dosing and accelerated gastric emptying after multiple dosing.[4]

See also[edit]

References[edit]

  1. ^ M. Vazquez-Roque, and M. Camilleri (2011). "Velusetrag". Drugs of the Future 36 (6): 447–454. doi:10.1358/dof.2011.36.6.1594078 (inactive 2014-03-23). 
  2. ^ Smith, JA; Beattie, DT; Marquess, D; Shaw, JP; Vickery, RG; Humphrey, PP (2008). "The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity". Naunyn-Schmiedeberg's archives of pharmacology 378 (1): 125–37. doi:10.1007/s00210-008-0282-y. PMID 18415081. 
  3. ^ Goldberg, M; Li, YP; Johanson, JF; Mangel, AW; Kitt, M; Beattie, DT; Kersey, K; Daniels, O (2010). "Clinical trial: The efficacy and tolerability of velusetrag, a selective 5-HT4 agonist with high intrinsic activity, in chronic idiopathic constipation - a 4-week, randomized, double-blind, placebo-controlled, dose-response study". Alimentary pharmacology & therapeutics 32 (9): 1102–12. doi:10.1111/j.1365-2036.2010.04456.x. PMID 21039672. 
  4. ^ Manini, ML; Camilleri, M; Goldberg, M; Sweetser, S; McKinzie, S; Burton, D; Wong, S; Kitt, MM et al. (2010). "Effects of Velusetrag (TD-5108) on gastrointestinal transit and bowel function in health and pharmacokinetics in health and constipation". Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society 22 (1): 42–9, e7–8. doi:10.1111/j.1365-2982.2009.01378.x. PMC 2905526. PMID 19691492.