Velusetrag
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| Synonyms | N-[(3-endo)-8-{(2R)-2-Hydroxy-3-[methyl(methylsulfonyl)amino]propyl}-8-azabicyclo[3.2.1]oct-3-yl]-1-isopropyl-2-oxo-1,2-dihydro-3-quinolinecarboxamide |
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| Formula | C25H36N4O5S |
| Molar mass | 504.65 g·mol−1 |
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Velusetrag (INN,[1] USAN; previously known as TD-5108) is an experimental drug candidate for the treatment of gastroparesis, chronic constipation and irritable bowel syndrome.[2] It is a potent, selective, high efficacy 5-HT4 receptor agonist.[3] In clinical trials, velusetrag was efficacious and well tolerated in patients with chronic constipation,[4] and showed accelerated intestinal and colonic transit after single dosing and accelerated gastric emptying after multiple dosing.[5]
As of August 31, 2015, clinical trials for chronic constipation and Alzheimer's disease seem to be terminated.[6] One study exploring the efficacy and safety of velusetrag in idiopathic or diabetic gastroparesis is recruiting participants.[7]
See also[edit]
References[edit]
- ^ "WHO Drug Information, Vol. 24, No. 1, 2010. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 63" (PDF). World Health Organization. p. 79. Retrieved 26 April 2016.
- ^ 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 2017-01-15).
- ^ 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.
- ^ 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.
- ^ 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. - ^ "Velusetrag — AdisInsight". Springer International Publishing AG. Retrieved 26 April 2016.
- ^ "The Diabetic and Idiopathic Gastroparesis Efficacy, Safety, and Tolerability (DIGEST) Study". ClinicalTrials.gov. Retrieved 26 April 2016.
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