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Drug ReportsTolvaptan
Samsca(tolvaptan)
Jinarc, Jynarque, Samsca, Tolvaptan (tolvaptan) is a small molecule pharmaceutical. Tolvaptan was first approved as Tolvaptan accord on . It is used to treat hyponatremia in the USA. It has been approved in Europe to treat autosomal dominant polycystic kidney and inappropriate adh syndrome. The pharmaceutical is active against vasopressin V2 receptor. In addition, it is known to target vasopressin V1a receptor.
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Clinical
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5D
1M
3M
6M
YTD
1Y
2Y
5Y
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FDA approval date
EMA approval date
Patent expiration date
Study first post date
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
nervous system diseasesD009422
urogenital diseasesD000091642
hereditary congenital and neonatal diseases and abnormalitiesD009358
nutritional and metabolic diseasesD009750
endocrine system diseasesD004700
Trade Name
FDA
EMA
Jynarque, Samsca, Tolvaptan (discontinued: Samsca)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Tolvaptan
Tradename
Company
Number
Date
Products
JYNARQUEOtsukaN-204441 RX2018-04-23
5 products, RLD
SAMSCAOtsukaN-022275 RX2009-05-19
2 products, RLD, RS
Show 1 discontinued
Labels
FDA
EMA
Brand Name
Status
Last Update
jynarqueNew Drug Application2022-11-08
samscaNew Drug Application2022-11-09
tolvaptanANDA2024-10-01
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
hyponatremiaHP_0002902D007010E87.1
Agency Specific
FDA
EMA
Expiration
Code
TOLVAPTAN, JYNARQUE, OTSUKA
2025-04-23ODE-178
Patent Expiration
Patent
Expires
Flag
FDA Information
Tolvaptan, Jynarque, Otsuka
109056942030-04-07DP
85017302026-09-01DP
ATC Codes
C: Cardiovascular system drugs
— C03: Diuretics
— C03X: Other diuretics in atc
— C03XA: Vasopressin antagonists, diuretics
— C03XA01: Tolvaptan
HCPCS
No data
Clinical
Clinical Trials
117 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Heart failureD006333HP_0001635I50241011532
HyponatremiaD007010HP_0002902E87.1—31161332
Polycystic kidney diseasesD007690HP_0000113Q61.3—8132629
Autosomal dominant polycystic kidneyD016891EFO_1001496Q61.2—8112627
Kidney diseasesD007674EFO_0003086N08—9122427
ArthrogryposisD001176EFO_0003857——472114
Liver cirrhosisD008103EFO_0001422K74.01361212
AscitesD001201HP_0001541R181223—7
Diabetes insipidusD003919—E23.2122217
Healthy volunteers/patients———31—116
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Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Inappropriate adh syndromeD007177EFO_1000982E22.2114—712
FibrosisD005355——136—110
EdemaD004487HP_0000969R60.9—25——7
Cardiac edemaD004489EFO_1001771———5——5
Chronic renal insufficiencyD051436—N18—31——4
Water-electrolyte imbalanceD014883————2—13
Autosomal recessive polycystic kidneyD017044—Q61.1——2——2
SyndromeD013577——111——2
Water intoxicationD014869————2——2
RecurrenceD012008———11——1
Show 4 more
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Chronic kidney failureD007676EFO_0003884N18.9—3———3
NephritisD009393—N05—2———2
HypovolemiaD020896HP_0011106E86—1———1
Diabetes mellitusD003920HP_0000819E08-E13—1———1
Nephrogenic diabetes insipidusD018500—N25.1—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NephrolithiasisD053040—N20.01————1
Kidney calculiD007669EFO_0004253N201————1
CardiomyopathiesD009202EFO_0000318I421————1
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Pituitary diseasesD010900—E23.7————11
Nervous system traumaD020196EFO_0009490—————11
UrolithiasisD052878—N20-N23————11
Urinary calculiD014545——————11
CystinuriaD003555—E72.01————11
Brain injuriesD001930—S06.9————11
HypernatremiaD006955HP_0003228E87.0————11
Wasting syndromeD019282——————11
CachexiaD002100HP_0004326R64————11
PolyuriaD011141HP_0000103R35————11
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameTolvaptan
INNtolvaptan
Description
Tolvaptan is a benzazepine derivative incorporating a benzenedicarboxamide function whch is a selective vasopressin V2 receptor antagonist used to treat euvolemic and hypervolemic hyponatremia. It is also used in the treatment of rapidly progressing autosomal dominant polycystic kidney disease to slow the rate of cyst development and renal insufficiency. Tolvaptan is a racemate consisting of a 1:1 mixture of 5R and 5S stereomers. It has a role as a vasopressin receptor antagonist and an aquaretic. It is a benzazepine and a benzenedicarboxamide.
Classification
Small molecule
Drug classaptamers, classical and mirror; vasopressin receptor antagonists
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cc(Cl)ccc32)c(C)c1
Identifiers
PDB—
CAS-ID150683-30-0
RxCUI—
ChEMBL IDCHEMBL344159
ChEBI ID32246
PubChem CID216237
DrugBankDB06212
UNII ID21G72T1950 (ChemIDplus, GSRS)
Target
Agency Approved
AVPR2
AVPR2
Organism
Homo sapiens
Gene name
AVPR2
Gene synonyms
ADHR, DIR, DIR3, V2R
NCBI Gene ID
Protein name
vasopressin V2 receptor
Protein synonyms
Antidiuretic hormone receptor, AVPR V2, Renal-type arginine vasopressin receptor
Uniprot ID
Mouse ortholog
Avpr2 (12000)
vasopressin V2 receptor (O88721)
Alternate
AVPR1A
AVPR1A
Organism
Homo sapiens
Gene name
AVPR1A
Gene synonyms
AVPR1
NCBI Gene ID
Protein name
vasopressin V1a receptor
Protein synonyms
Antidiuretic hormone receptor 1a, AVPR V1a, SCCL vasopressin subtype 1a receptor, V1-vascular vasopressin receptor AVPR1A, V1a vasopressin receptor, Vascular/hepatic-type arginine vasopressin receptor
Uniprot ID
Mouse ortholog
Avpr1a (54140)
vasopressin V1a receptor (Q9QYH2)
Variants
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 3,810 documents
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Safety
Black-box Warning
Black-box warning for: Jynarque, Samsca, Tolvaptan
Adverse Events
Top Adverse Reactions
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8,718 adverse events reported
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