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Drug ReportsVELUSETRAG
VELUSETRAG
Velusetrag is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against 5-hydroxytryptamine receptor 4.
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Commercial
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Drug
General
Drug common nameVELUSETRAG
INNvelusetrag
Description
Velusetrag (INN, USAN; previously known as TD-5108) is an experimental drug candidate for the treatment of gastric neuromuscular disorders including gastroparesis, and lower gastrointestinal motility disorders including chronic idiopathic constipation and irritable bowel syndrome. It is a potent, selective, high efficacy 5-HT4 receptor serotonin agonist being developed by Theravance Biopharma and Alfa Wassermann. Velusetrag demonstrates less selectivity for other serotonin receptors, such as 5-HT2 and 5-HT3, to earlier generation 5-HT agonists like cisapride and tegaserod.
Classification
Small molecule
Drug classserotonin 5-HT receptor agonists, not principally 5-HT2
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
CC(C)n1c(=O)c(C(=O)N[C@@H]2C[C@@H]3CC[C@H](C2)N3C[C@@H](O)CN(C)S(C)(=O)=O)cc2ccccc21
Identifiers
PDB
CAS-ID866933-46-2
RxCUI
ChEMBL IDCHEMBL2087337
ChEBI ID
PubChem CID53297466
DrugBank
UNII IDJ4VNV64ARB (ChemIDplus, GSRS)
Target
Agency Approved
HTR4
HTR4
Organism
Homo sapiens
Gene name
HTR4
Gene synonyms
NCBI Gene ID
Protein name
5-hydroxytryptamine receptor 4
Protein synonyms
5-hydroxytryptamine (serotonin) receptor 4, G protein-coupled, cardiac 5-HT4 receptor, Serotonin receptor 4
Uniprot ID
Mouse ortholog
Htr4 (15562)
5-hydroxytryptamine receptor 4 (Q9R2A4)
Alternate
No data
Variants
No data
Financial
No data
Trends
No data
Safety
Black-box Warning
No Black-box warning
Adverse Events
0 adverse events reported
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