Tolvaptan

Vasopressin V2 Receptor Antagonist — CARDIOVASCULAR SYSTEM

Key facts

Tolvaptan is an ofp drug in the Vasopressin V2 Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2009. Its mechanism of action is classified as Vasopressin V2 Receptor Antagonists. DrugCentral lists 8 molecular targets, including AVPR2, Avpr2 and AVPR1A. Recorded indications include Fluid retention in heart failure, Hyponatremia, Polycystic kidney disease, adult type and Syndrome of inappropriate vasopressin secretion.

• Approval status: ofp (first approved 2009 by the FDA).
• Drug class: Vasopressin V2 Receptor Antagonist.
• Mechanism of action: Vasopressin V2 Receptor Antagonists.
• Molecular targets: AVPR2, Avpr2, AVPR1A and Avpr1a (8 listed in DrugCentral).
• Indications: Fluid retention in heart failure, Hyponatremia, Polycystic kidney disease, adult type and Syndrome of inappropriate vasopressin secretion.
• ATC code: C03XA01 (Vasopressin antagonists).
• Molecular formula: C26H25ClN2O3; molecular weight 448.95 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (4)

• Fluid retention in heart failure
• Hyponatremia
• Polycystic kidney disease, adult type
• Syndrome of inappropriate vasopressin secretion

Contraindications (9)

• Alcoholism
• Cirrhosis of liver
• Dehydration
• Demyelination
• Gastrointestinal hemorrhage
• Hepatic failure
• Hyperkalemia
• Hypovolemia
• Nutritional disorder

Mechanism & targets

• Mechanism of action (MoA): Vasopressin V2 Receptor Antagonists
• Established pharmacologic class: Vasopressin V2 Receptor Antagonist

Molecular targets (8)

Target	Gene	Action	Activity
Vasopressin V2 receptor	AVPR2	antagonist	Ki 9.00
Vasopressin V2 receptor	Avpr2	antagonist	Ki 8.90
Vasopressin V1a receptor	AVPR1A	antagonist	Ki 7.90
Vasopressin V1a receptor	Avpr1a	antagonist	Ki 6.50
Mu-type opioid receptor	OPRM1	unknown	Ki 6.39
Transmembrane protein 97	TMEM97	unknown	Ki 5.99
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 5.31
Histamine H1 receptor	HRH1	unknown	Ki 5.17

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2015-02-26	EMA	—	—
2010-10-27	PMDA	—	Otsuka Pharmaceutical Co., Ltd	Yes
2009-05-19	FDA	—	OTSUKA AMERICA PHARM

ATC classification

ATC code	Therapeutic hierarchy
C03XA01	CARDIOVASCULAR SYSTEM › DIURETICS › OTHER DIURETICS › Vasopressin antagonists

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Thirst	1433.5
Hypernatraemia	1176.6
Renal impairment	1104.3
Rapid correction of hyponatraemia	1054.6
Polyuria	803.1
Cardiac failure	718.6
Incorrect product administration duration	581.7
Blood urea increased	572.2
Hepatic function abnormal	568.5
Glomerular filtration rate decreased	510.1
Nocturia	490.6
Blood sodium increased	463.0

Chemical structure

• Molecular formula: C₂₆H₂₅ClN₂O₃
• Molecular weight: 448.95 g/mol
• CAS number: 150683-30-0
• InChIKey: GYHCTFXIZSNGJT-UHFFFAOYSA-N
• PubChem CID: 216237

CC1=C(C=CC=C1)C(=O)NC1=CC(C)=C(C=C1)C(=O)N1CCCC(O)C2=CC(Cl)=CC=C12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Tolvaptan used for?

DrugCentral lists the following indications for Tolvaptan: Fluid retention in heart failure, Hyponatremia, Polycystic kidney disease, adult type and Syndrome of inappropriate vasopressin secretion.

How does Tolvaptan work?

Tolvaptan is classified as Vasopressin V2 Receptor Antagonists; its molecular targets in DrugCentral include AVPR2 (antagonist), Avpr2 (antagonist), AVPR1A (antagonist) and Avpr1a (antagonist).

When was Tolvaptan first approved?

Tolvaptan was first approved by the FDA in 2009.

What drug class does Tolvaptan belong to?

Tolvaptan is in the Vasopressin V2 Receptor Antagonist class.

What is the chemical formula of Tolvaptan?

Tolvaptan has the molecular formula C26H25ClN2O3 and a molecular weight of 448.95 g/mol.

Sources

• DrugCentral drug card 4110 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL344159 — compound record and bioactivity
• PubChem CID 216237 — chemical identifiers
• DrugBank DB06212 — drug record
• FDA UNII 21G72T1950 — substance identity
• DailyMed: FDA labels for Tolvaptan — current prescribing information (label search)
• UniProt P30518 (AVPR2) — target protein
• UniProt P37288 (AVPR1A) — target protein
• UniProt P35372 (OPRM1) — target protein
• UniProt Q5BJF2 (TMEM97) — target protein
• UniProt P28335 (HTR2C) — target protein
• UniProt P35367 (HRH1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.