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lixivaptan

Structure via PubChem · Public domain (PubChem)

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lixivaptan

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Also known as VPA-985, VPA985, WAY-VPA-985

Lixivaptan (VPA-985) is an orally-active, non-peptide, selective vasopressin V2 receptor antagonist being developed as an investigational drug by Palladio Biosciences, Inc. (Palladio), a subsidiary of Centessa Pharmaceuticals plc. , lixivaptan is in phase III clinical development for the treatment of autosomal dominant polycystic kidney disease (ADPKD), the most common form of polycystic kidney disease. The U.S. Food and Drug Administration (FDA) has granted orphan drug designation to lixivaptan for the treatment of ADPKD.

Chemical data

Formula
C27H21ClFN3O2
Molecular weight
473.9 g/mol
IUPAC name
N-[3-chloro-4-(6,11-dihydropyrrolo[2,1-c][1,4]benzodiazepine-5-carbonyl)phenyl]-5-fluoro-2-methylbenzamide
SMILES
CC1=C(C=C(C=C1)F)C(=O)NC2=CC(=C(C=C2)C(=O)N3CC4=CC=CN4CC5=CC=CC=C53)Cl
InChIKey
PPHTXRNHTVLQED-UHFFFAOYSA-N
XLogP
4.8
Polar surface area
54.3 Ų
H-bond donors
1
H-bond acceptors
3
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Phase 3
Molecule type
Small molecule
Indications
congestive heart failure, Hyponatremia, Autosomal dominant polycystic kidney disease, Polycystic Kidney Disease

via ChEMBL · EBI

Wikidata facts

Mass
473.130633
Show 3 more facts
chemical formula
C₂₇H₂₁ClFN₃O₂
canonical SMILES
CC1=C(C=C(C=C1)F)C(=O)NC2=CC(=C(C=C2)C(=O)N3CC4=CC=CN4CC5=CC=CC=C53)Cl
Commons category
Lixivaptan
Sources (2)

via Wikidata · CC0

~7 min read

Encyclopedic overview

12 sections
Contents
  • Mechanism of action
  • Hyponatremia
  • ADPKD
  • Research
  • V<sub>2</sub> receptor antagonists in ADPKD
  • Clinical studies
  • Hyponatremia
  • ADPKD
  • The ACTION study
  • The ALERT study
  • DILIsym simulations
  • References

Lixivaptan (VPA-985) is an orally-active, non-peptide, selective vasopressin V2 receptor antagonist being developed as an investigational drug by Palladio Biosciences, Inc. (Palladio), a subsidiary of Centessa Pharmaceuticals plc. , lixivaptan is in phase III clinical development for the treatment of autosomal dominant polycystic kidney disease (ADPKD), the most common form of polycystic kidney disease. The U.S. Food and Drug Administration (FDA) has granted orphan drug designation to lixivaptan for the treatment of ADPKD.

==Mechanism of action== Lixivaptan is a potent, non-peptide, selective vasopressin receptor antagonist. It is a member of the vaptan class of drugs.

Excerpted from Wikipedia’s “lixivaptan” article, available under the CC BY-SA 4.0 licence.

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