Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H34N4O3 |
Molecular Weight | 462.5839 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C(=O)[C@@H]1CCCN1C(=O)NCC2=C(C)C=C(C=C2)C(=O)N3CCCCC4=C3C=CC=C4
InChI
InChIKey=RUOLFWZIFNQQGH-DEOSSOPVSA-N
InChI=1S/C27H34N4O3/c1-19-17-21(25(32)30-15-7-6-10-20-9-4-5-11-23(20)30)13-14-22(19)18-28-27(34)31-16-8-12-24(31)26(33)29(2)3/h4-5,9,11,13-14,17,24H,6-8,10,12,15-16,18H2,1-3H3,(H,28,34)/t24-/m0/s1
Molecular Formula | C27H34N4O3 |
Molecular Weight | 462.5839 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.vantia.com/fedovapagon.htmlCurator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800028886
Sources: https://www.vantia.com/fedovapagon.html
Curator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800028886
Fedovapagon, also known as VA106483 and VT483, is a potent, nonpeptidic vasopressin V2 receptor agonist. Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. Fedovapagon (VA106483) was discovered by Vantia and currently in Phase II trials for the treatment of nocturia, a common condition that causes sufferers to wake frequently during the night in order to urinate. Fedovapagon has been extensively studied in clinical trials and data, presented at the American Urological Association meeting in 2010, demonstrated a dose-dependent reduction in nocturnal urine volumes and a reliable pharmacodynamic effect on repeated dosing. More recently, data presented in San Diego at the 2012 American Urological Association meeting, showed that fedovapagon was effective from the first night of dosing and that there was no effect following cessation of dosing. Further presentations are planned for the International Continence Society meeting being held in Barcelona in August 2013. These data suggest that fedovapagon has the potential to be an effective and well tolerated antidiuretic for the treatment of nocturia. Fedovapagon is currently being investigated as a new treatment for nocturia in a Phase-II/III clinical trials in USA (PO)(NCT02637960).
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1790 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19053774 |
24.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02637960
One daily dose of 2 mg fedovapagon for 12 weeks
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19053774
Fedovapagon revealed agonist activity (EC=24nM) at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 22:07:12 GMT 2023
by
admin
on
Fri Dec 15 22:07:12 GMT 2023
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Record UNII |
VX2GBO4I0V
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Record Status |
Validated (UNII)
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Record Version |
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DB11734
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300000036981
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DTXSID40188331
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TARGET -> AGONIST |
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ACTIVE MOIETY |