Velusetrag

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Velusetrag
Velusetrag structure.svg
Velusetrag2.png
Systematic (IUPAC) name
N-{(1R,3r,5S)-8-[(2R)-2-Hydroxy-3-(N-methylmethanesulfonamido)propyl]-8-azabicyclo[3.2.1]octan-3-yl}-2-oxo-1-(propan-2-yl)-1,2-dihydroquinoline-3-carboxamide
Clinical data
Legal status
  • Investigational drug
Routes of
administration
Oral
Identifiers
CAS Number 866933-46-2
866933-51-9 (hydrochloride)
ATC code None
PubChem CID: 53297466
IUPHAR/BPS 8425
ChemSpider 28527582
UNII J4VNV64ARB
KEGG D09693
ChEMBL CHEMBL2087337
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
Chemical data
Formula C25H36N4O5S
Molecular mass 504.65 g·mol−1
  • CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)N[C@H]3C[C@H]4CC[C@@H](C3)N4C[C@H](CN(C)S(=O)(=O)C)O
  • InChI=1S/C25H36N4O5S/c1-16(2)29-23-8-6-5-7-17(23)11-22(25(29)32)24(31)26-18-12-19-9-10-20(13-18)28(19)15-21(30)14-27(3)35(4,33)34/h5-8,11,16,18-21,30H,9-10,12-15H2,1-4H3,(H,26,31)/t18-,19+,20-,21-/m0/s1
  • Key:HXLOHDZQBKCUCR-WOZUAGRISA-N

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

References

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