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tolvaptan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
vasopressin receptor antagonists	4110	150683-30-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: OPC 41061 jinarc tolvaptan samsca OPC-41061 tolvaptan sodium phosphate	A benzazepine derivative and selective VASOPRESSIN V2 RECEPTOR antagonist that is 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. Molecular weight: 448.95 Formula: C26H25ClN2O3 CLOGP: 3.91 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 69.64 ALOGS: -5.56 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

OPC 41061
jinarc
tolvaptan
samsca
OPC-41061
tolvaptan sodium phosphate

A benzazepine derivative and selective VASOPRESSIN V2 RECEPTOR antagonist that is 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.

Molecular weight: 448.95
Formula: C26H25ClN2O3
CLOGP: 3.91
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 69.64
ALOGS: -5.56
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
30	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	2.90 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.91 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	0.56 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
Vd (Volume of distribution)	0.50 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

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Date	Agency	Company
Feb. 26, 2015	EMA
May 19, 2009	FDA	OTSUKA AMERICA PHARM
Oct. 27, 2010	PMDA	Otsuka Pharmaceutical Co., Ltd

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Rapid correction of hyponatraemia	398.34	23.22	58	9973	83	63478908
Hypernatraemia	352.68	23.22	102	9929	7507	63471484
Incorrect product administration duration	335.13	23.22	108	9923	11438	63467553
Hepatic function abnormal	301.34	23.22	137	9894	37005	63441986
Thirst	291.19	23.22	102	9929	13939	63465052
Renal impairment	270.12	23.22	170	9861	88185	63390806
Cardiac failure	258.76	23.22	166	9865	88976	63390015
Polyuria	207.99	23.22	70	9961	8472	63470519
Nocturia	203.32	23.22	68	9963	8073	63470918
Inappropriate schedule of product administration	196.86	23.22	149	9882	103816	63375175

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypernatraemia	550.97	20.84	168	9630	8322	34938811
Thirst	402.57	20.84	130	9668	7765	34939368
Rapid correction of hyponatraemia	361.47	20.84	56	9742	60	34947073
Incorrect product administration duration	289.83	20.84	90	9708	4721	34942412
Renal impairment	246.74	20.84	207	9591	94306	34852827
Cardiac failure	228.17	20.84	195	9603	91053	34856080
Hepatic function abnormal	219.57	20.84	143	9655	44220	34902913
Blood sodium increased	178.74	20.84	55	9743	2793	34944340
Blood urea increased	167.82	20.84	105	9693	30259	34916874
Polyuria	161.93	20.84	68	9730	8506	34938627

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypernatraemia	863.56	19.47	255	17604	14196	79712333
Thirst	602.72	19.47	206	17653	18413	79708116
Hepatic function abnormal	504.94	19.47	270	17589	72837	79653692
Rapid correction of hyponatraemia	494.57	19.47	75	17784	94	79726435
Renal impairment	479.17	19.47	345	17514	157438	79569091
Cardiac failure	459.73	19.47	334	17525	154508	79572021
Incorrect product administration duration	338.73	19.47	120	17739	11902	79714627
Blood urea increased	322.06	19.47	175	17684	48615	79677914
Polyuria	305.58	19.47	118	17741	14896	79711633
Blood sodium increased	253.17	19.47	77	17782	4721	79721808

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C03XA01	CARDIOVASCULAR SYSTEM DIURETICS OTHER DIURETICS Vasopressin antagonists
CHEBI has role	CHEBI:59680	vasopressin receptor antagonists
CHEBI has role	CHEBI:194423	aquaretic agent
FDA EPC	N0000193181	Vasopressin V2 Receptor Antagonist
FDA MoA	N0000193178	Vasopressin V2 Receptor Antagonists
MeSH PA	D065092	Antidiuretic Hormone Receptor Antagonists
MeSH PA	D045283	Natriuretic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Polycystic kidney disease, adult type	indication	28728008
Syndrome of inappropriate vasopressin secretion	indication	55004003	DOID:3401
Hyponatremia	indication	89627008
Fluid retention in heart failure	indication
Nutritional disorder	contraindication	2492009	DOID:374
Alcoholism	contraindication	7200002
Hyperkalemia	contraindication	14140009
Cirrhosis of liver	contraindication	19943007	DOID:5082
Hypovolemia	contraindication	28560003
Demyelination	contraindication	32693004

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.1	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
15MG	JYNARQUE	OTSUKA	N204441	April 23, 2018	RX	TABLET	ORAL	April 23, 2025	INDICATED TO SLOW KIDNEY FUNCTION DECLINE IN ADULTS AT RISK OF RAPIDLY PROGRESSING AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE (ADPKD)
30MG	JYNARQUE	OTSUKA	N204441	April 23, 2018	RX	TABLET	ORAL	April 23, 2025	INDICATED TO SLOW KIDNEY FUNCTION DECLINE IN ADULTS AT RISK OF RAPIDLY PROGRESSING AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE (ADPKD)
45MG	JYNARQUE	OTSUKA	N204441	April 23, 2018	RX	TABLET	ORAL	April 23, 2025	INDICATED TO SLOW KIDNEY FUNCTION DECLINE IN ADULTS AT RISK OF RAPIDLY PROGRESSING AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE (ADPKD)
60MG	JYNARQUE	OTSUKA	N204441	April 23, 2018	RX	TABLET	ORAL	April 23, 2025	INDICATED TO SLOW KIDNEY FUNCTION DECLINE IN ADULTS AT RISK OF RAPIDLY PROGRESSING AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE (ADPKD)
90MG	JYNARQUE	OTSUKA	N204441	April 23, 2018	RX	TABLET	ORAL	April 23, 2025	INDICATED TO SLOW KIDNEY FUNCTION DECLINE IN ADULTS AT RISK OF RAPIDLY PROGRESSING AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE (ADPKD)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Vasopressin V2 receptor	GPCR	P30518	V2R_HUMAN	ANTAGONIST	Ki	9	WOMBAT-PK	DRUG LABEL
Vasopressin V1a receptor	GPCR	P37288	V1AR_HUMAN	ANTAGONIST	Ki	7.90	IUPHAR
Vasopressin V2 receptor	GPCR		V2R_RAT	ANTAGONIST	Ki	8.90	IUPHAR
Vasopressin V1a receptor	GPCR		V1AR_RAT	ANTAGONIST	Ki	6.50	IUPHAR

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External reference:

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ID	Source
013121	NDDF
165174	MMSL
216237	PUBCHEM_CID
21G72T1950	UNII
2226	IUPHAR_LIGAND_ID
26477	MMSL
334368	MMSL
358257	RXNORM
4028789	VUID
4028789	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
JYNARQUE	HUMAN PRESCRIPTION DRUG LABEL	1	59148-082	TABLET	15 mg	ORAL	NDA	32 sections
JYNARQUE	HUMAN PRESCRIPTION DRUG LABEL	1	59148-082	TABLET	15 mg	ORAL	NDA	32 sections
JYNARQUE	HUMAN PRESCRIPTION DRUG LABEL	1	59148-083	TABLET	30 mg	ORAL	NDA	32 sections
JYNARQUE	HUMAN PRESCRIPTION DRUG LABEL	1	59148-083	TABLET	30 mg	ORAL	NDA	32 sections
SAMSCA	HUMAN PRESCRIPTION DRUG LABEL	1	59148-020	TABLET	15 mg	ORAL	NDA	33 sections
SAMSCA	HUMAN PRESCRIPTION DRUG LABEL	1	59148-020	TABLET	15 mg	ORAL	NDA	33 sections
SAMSCA	HUMAN PRESCRIPTION DRUG LABEL	1	59148-021	TABLET	30 mg	ORAL	NDA	33 sections
SAMSCA	HUMAN PRESCRIPTION DRUG LABEL	1	59148-021	TABLET	30 mg	ORAL	NDA	33 sections
Tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	31722-868	TABLET	15 mg	ORAL	ANDA	28 sections
Tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	31722-869	TABLET	30 mg	ORAL	ANDA	28 sections

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