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:

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

Approvals:

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

FDA Adverse Event Reporting System (Female)

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
Blood sodium decreased	170.27	23.22	81	9950	24171	63454820
Blood urea increased	157.87	23.22	79	9952	26300	63452691
Polydipsia	152.81	23.22	45	9986	3519	63475472
Underdose	132.03	23.22	71	9960	27385	63451606
Glomerular filtration rate decreased	119.76	23.22	53	9978	13388	63465603
Blood sodium increased	110.59	23.22	33	9998	2699	63476292
Wrong technique in product usage process	110.50	23.22	86	9945	62254	63416737
Alanine aminotransferase increased	99.39	23.22	101	9930	103669	63375322
Aspartate aminotransferase increased	95.94	23.22	93	9938	90184	63388807
Liver disorder	94.99	23.22	74	9957	53613	63425378
Brain natriuretic peptide increased	93.37	23.22	34	9997	5179	63473812
Death	89.38	23.22	188	9843	374193	63104798
Platelet count decreased	83.19	23.22	97	9934	116025	63362966
Blood pressure decreased	78.66	23.22	72	9959	64950	63414041
Blood creatinine increased	74.23	23.22	80	9951	87764	63391227
Cardiac failure chronic	72.43	23.22	27	10004	4391	63474600
Dehydration	69.27	23.22	109	9922	173245	63305746
Pulmonary arterial hypertension	67.69	23.22	43	9988	22534	63456457
Off label use	66.50	23.22	245	9786	674217	62804774
Product use in unapproved indication	59.96	23.22	104	9927	178976	63300015
Concomitant disease aggravated	56.57	23.22	28	10003	9084	63469907
Drug titration error	56.36	23.22	15	10016	808	63478183
Hepatic encephalopathy	53.71	23.22	29	10002	11253	63467738
Renal cyst haemorrhage	52.57	23.22	9	10022	52	63478939
Gallbladder polyp	52.27	23.22	14	10017	773	63478218
Blood uric acid increased	50.50	23.22	22	10009	5345	63473646
Urine output increased	48.56	23.22	15	10016	1378	63477613
Hyponatraemia	48.35	23.22	73	9958	111827	63367164
Pain	47.95	23.22	29	10002	740599	62738392
Therapy cessation	47.48	23.22	39	9992	30418	63448573
Hyperuricaemia	47.26	23.22	21	10010	5349	63473642
Pulmonary congestion	46.86	23.22	31	10000	17387	63461604
Nephrogenic anaemia	45.90	23.22	16	10015	2146	63476845
Drug ineffective	43.89	23.22	61	9970	1044704	62434287
Hospitalisation	43.31	23.22	60	9971	85021	63393970
Ascites	41.42	23.22	41	9990	40687	63438304
Inability to afford medication	40.88	23.22	15	10016	2332	63476659
Incorrect drug administration rate	39.77	23.22	17	10014	3945	63475046
Incorrect dose administered	39.43	23.22	48	9983	59920	63419071
Pleural effusion	39.11	23.22	60	9971	93150	63385841
Cerebral infarction	38.09	23.22	31	10000	23862	63455129
Pollakiuria	37.84	23.22	33	9998	27904	63451087
Joint swelling	37.64	23.22	4	10027	327662	63151329
Drug hypersensitivity	35.16	23.22	4	10027	310683	63168308
Renal cyst infection	33.84	23.22	7	10024	123	63478868
Swelling	32.57	23.22	3	10028	275375	63203616
Abdominal discomfort	31.99	23.22	6	10025	320879	63158112
Fatigue	31.41	23.22	58	9973	887970	62591021
Concomitant disease progression	31.21	23.22	12	10019	2122	63476869
Osmotic demyelination syndrome	31.19	23.22	9	10022	654	63478337
Blood alkaline phosphatase increased	29.23	23.22	35	9996	42932	63436059
Right ventricular failure	28.88	23.22	23	10008	17165	63461826
Hyperkalaemia	28.74	23.22	39	9992	54164	63424827
Rash	28.54	23.22	28	10003	560843	62918148
Renal cyst ruptured	28.38	23.22	5	10026	35	63478956
Urine output decreased	27.63	23.22	19	10012	11351	63467640
Arthralgia	27.23	23.22	30	10001	569680	62909311
Hepatic cirrhosis	27.21	23.22	26	10005	24708	63454283
Gamma-glutamyltransferase increased	26.98	23.22	30	10001	34001	63444990
Transfusion	26.94	23.22	21	10010	15196	63463795
Altered state of consciousness	26.77	23.22	26	10005	25204	63453787
Hepatic cyst	26.65	23.22	14	10017	5140	63473851
Pulmonary hypertension	26.51	23.22	31	10000	37092	63441899
Blood bilirubin increased	26.50	23.22	31	10000	37109	63441882
Polycystic liver disease	26.30	23.22	4	10027	9	63478982
Upper respiratory tract inflammation	25.90	23.22	11	10020	2512	63476479
Iron deficiency anaemia	25.86	23.22	23	10008	19946	63459045
Hepatic failure	25.84	23.22	30	10001	35626	63443365
No adverse event	25.38	23.22	32	9999	41373	63437618
Drug monitoring procedure incorrectly performed	25.28	23.22	6	10025	202	63478789
Hepatotoxicity	24.91	23.22	30	10001	37011	63441980
Drug intolerance	24.64	23.22	9	10022	308652	63170339
Uraemic encephalopathy	23.57	23.22	6	10025	271	63478720
Liver transplant	23.55	23.22	10	10021	2281	63476710
Alopecia	23.52	23.22	12	10019	337524	63141467

FDA Adverse Event Reporting System (Male)

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
Inappropriate schedule of product administration	123.53	20.84	117	9681	62179	34884954
Underdose	122.56	20.84	65	9733	13715	34933418
Nocturia	119.54	20.84	58	9740	10152	34936981
Blood creatinine increased	116.35	20.84	138	9660	94838	34852295
Glomerular filtration rate decreased	103.70	20.84	57	9741	12904	34934229
Cardiac failure chronic	95.98	20.84	46	9752	7833	34939300
Hepatic encephalopathy	94.44	20.84	56	9742	14629	34932504
Dehydration	82.76	20.84	138	9660	129831	34817302
Osmotic demyelination syndrome	77.70	20.84	22	9776	833	34946300
Hyperuricaemia	77.37	20.84	40	9758	8003	34939130
Wrong technique in product usage process	75.88	20.84	70	9728	35916	34911217
Low cardiac output syndrome	75.50	20.84	20	9778	588	34946545
Blood sodium decreased	72.06	20.84	49	9749	16202	34930931
Altered state of consciousness	67.56	20.84	54	9744	22839	34924294
Alanine aminotransferase increased	62.68	20.84	94	9704	80721	34866412
Death	62.63	20.84	248	9550	397801	34549332
Aspartate aminotransferase increased	60.08	20.84	84	9714	67699	34879434
Polydipsia	51.17	20.84	24	9774	3891	34943242
Liver disorder	50.63	20.84	54	9744	32943	34914190
Pulmonary arterial hypertension	50.17	20.84	31	9767	8708	34938425
Product use in unapproved indication	47.63	20.84	103	9695	117396	34829737
Blood pressure decreased	47.36	20.84	65	9733	51450	34895683
Hyperkalaemia	47.20	20.84	76	9722	69313	34877820
Urine output increased	41.29	20.84	15	9783	1272	34945861
Cerebral infarction	40.48	20.84	44	9754	27411	34919722
Right ventricular failure	40.15	20.84	27	9771	8757	34938376
Toxicity to various agents	39.20	20.84	5	9793	200357	34746776
Blood potassium increased	38.51	20.84	34	9764	16461	34930672
Concomitant disease aggravated	37.31	20.84	22	9776	5679	34941454
Off label use	37.23	20.84	222	9576	419302	34527831
Drug titration error	37.01	20.84	11	9787	495	34946638
Renal cyst haemorrhage	34.48	20.84	11	9787	628	34946505
Incorrect drug administration rate	33.77	20.84	14	9784	1691	34945442
Urine output decreased	32.43	20.84	25	9773	10024	34937109
Pain	31.82	20.84	9	9789	204666	34742467
Urine osmolarity decreased	30.25	20.84	6	9792	45	34947088
Renal cyst infection	29.28	20.84	6	9792	54	34947079
Product use issue	28.58	20.84	58	9740	63158	34883975
Procedural failure	28.11	20.84	6	9792	67	34947066
Prescribed underdose	26.18	20.84	21	9777	8912	34938221
Congestive hepatopathy	26.03	20.84	12	9786	1869	34945264
Inability to afford medication	25.55	20.84	11	9787	1459	34945674
Disseminated intravascular coagulation	25.47	20.84	31	9767	21785	34925348
Arthralgia	25.46	20.84	8	9790	170033	34777100
Hepatic failure	25.08	20.84	39	9759	34492	34912641
Fatigue	24.97	20.84	41	9757	370612	34576521
Hospitalisation	24.30	20.84	51	9747	56851	34890282
Hyponatraemia	23.26	20.84	63	9735	82628	34864505
Therapy cessation	22.94	20.84	26	9772	16947	34930186
Gamma-glutamyltransferase increased	22.61	20.84	34	9764	29197	34917936
Oedema	21.90	20.84	43	9755	45698	34901435
Renal cyst ruptured	21.56	20.84	4	9794	20	34947113
Hepatic enzyme increased	21.52	20.84	39	9759	39041	34908092
Nephrogenic anaemia	21.27	20.84	11	9787	2200	34944933

FDA Adverse Event Reporting System (Geriatric)

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
Nocturia	241.45	19.47	97	17762	13584	79712945
Inappropriate schedule of product administration	201.17	19.47	195	17664	133433	79593096
Blood creatinine increased	187.43	19.47	201	17658	154856	79571673
Glomerular filtration rate decreased	185.52	19.47	94	17765	22608	79703921
Underdose	178.21	19.47	104	17755	33047	79693482
Polydipsia	167.46	19.47	61	17798	6544	79719985
Hepatic encephalopathy	149.19	19.47	83	17776	24083	79702446
Cardiac failure chronic	146.29	19.47	64	17795	11071	79715458
Aspartate aminotransferase increased	143.85	19.47	166	17693	138475	79588054
Alanine aminotransferase increased	143.06	19.47	179	17680	162391	79564138
Liver disorder	142.74	19.47	123	17736	72294	79654235
Death	138.62	19.47	355	17504	566159	79160370
Dehydration	136.25	19.47	218	17641	247969	79478560
Hyperuricaemia	133.23	19.47	61	17798	11738	79714791
Blood pressure decreased	114.91	19.47	126	17733	99340	79627189
Pulmonary arterial hypertension	111.71	19.47	73	17786	28293	79698236
Blood sodium decreased	108.12	19.47	76	17783	33179	79693350
Low cardiac output syndrome	92.03	19.47	25	17834	1020	79725509
Off label use	91.74	19.47	423	17436	906792	78819737
Brain natriuretic peptide increased	91.11	19.47	43	17816	8857	79717672
Drug titration error	89.40	19.47	25	17834	1137	79725392
Concomitant disease aggravated	88.92	19.47	48	17811	13119	79713410
Altered state of consciousness	87.46	19.47	75	17784	43747	79682782
Urine output increased	84.94	19.47	28	17831	2228	79724301
Cerebral infarction	84.76	19.47	75	17784	45601	79680928
Osmotic demyelination syndrome	82.88	19.47	25	17834	1488	79725041
Product use in unapproved indication	79.51	19.47	174	17685	250185	79476344
Renal cyst haemorrhage	77.37	19.47	20	17839	672	79725857
Toxicity to various agents	74.94	19.47	5	17854	421535	79304994
Pain	73.46	19.47	33	17826	703769	79022760
Hyperkalaemia	67.50	19.47	104	17755	114294	79612235
Nephrogenic anaemia	66.52	19.47	27	17832	3875	79722654
Platelet count decreased	63.71	19.47	137	17722	194527	79532002
Right ventricular failure	63.42	19.47	48	17811	23449	79703080
Urine output decreased	60.46	19.47	42	17817	17980	79708549
Wrong technique in product usage process	59.60	19.47	78	17781	73797	79652732
Blood potassium increased	58.19	19.47	50	17809	29225	79697304
Renal cyst infection	54.38	19.47	12	17847	201	79726328
Blood uric acid increased	54.10	19.47	35	17824	13325	79713204
Pulmonary congestion	53.28	19.47	46	17813	27054	79699475
Pollakiuria	51.47	19.47	52	17807	37265	79689264
Arthralgia	50.56	19.47	33	17826	571770	79154759
Hepatic failure	48.39	19.47	64	17795	61148	79665381
Therapy cessation	47.58	19.47	50	17809	37512	79689017
Blood bilirubin increased	47.43	19.47	66	17793	66166	79660363
Ascites	46.39	19.47	70	17789	75492	79651037
Gamma-glutamyltransferase increased	46.08	19.47	59	17800	54621	79671908
Pleural effusion	43.83	19.47	99	17760	145163	79581366
Completed suicide	43.39	19.47	3	17856	245764	79480765
Fatigue	43.12	19.47	90	17769	929637	78796892
Drug ineffective	42.69	19.47	114	17745	1080799	78645730
Transfusion	41.51	19.47	36	17823	21294	79705235
Pulmonary hypertension	40.70	19.47	52	17807	48028	79678501
Gallbladder polyp	40.15	19.47	13	17846	977	79725552
Joint swelling	40.02	19.47	8	17851	288638	79437891
Hyponatraemia	39.69	19.47	108	17751	177740	79548789
Drug hypersensitivity	38.02	19.47	10	17849	298906	79427623
Swelling	37.24	19.47	3	17856	216708	79509821
Cardiac failure acute	36.94	19.47	32	17827	18897	79707632
Concomitant disease progression	36.22	19.47	17	17842	3456	79723073
Rash	36.10	19.47	46	17813	578312	79148217
Renal cyst ruptured	35.43	19.47	7	17852	66	79726463
Disseminated intravascular coagulation	33.92	19.47	41	17818	35801	79690728
Urine osmolarity decreased	33.03	19.47	7	17852	96	79726433
Sinusitis	32.79	19.47	3	17856	195498	79531031
Cardiac failure congestive	32.29	19.47	87	17772	142315	79584214
Blood alkaline phosphatase increased	32.21	19.47	54	17805	63610	79662919
Hepatotoxicity	32.12	19.47	48	17811	51304	79675225
Marasmus	31.77	19.47	11	17848	1017	79725512
Pneumonia aspiration	31.51	19.47	55	17804	66912	79659617
Incorrect dose administered	31.07	19.47	59	17800	76571	79649958
Neutropenia	29.13	19.47	14	17845	287696	79438833
Oedema	29.08	19.47	75	17784	119505	79607024
Hepatic cirrhosis	28.36	19.47	37	17822	34869	79691660
Procedural failure	28.20	19.47	6	17853	84	79726445
Drug intolerance	28.07	19.47	12	17847	264107	79462422
Hepatocellular carcinoma	27.88	19.47	20	17839	9001	79717528
Oesophageal varices haemorrhage	27.37	19.47	15	17844	4221	79722308
Pain in extremity	27.14	19.47	25	17834	364513	79362016
Anxiety	26.88	19.47	11	17848	248501	79478028
Hypersensitivity	26.18	19.47	13	17846	262226	79464303
N-terminal prohormone brain natriuretic peptide increased	25.75	19.47	15	17844	4740	79721789
Abdominal discomfort	25.69	19.47	12	17847	250715	79475814
Treatment failure	25.19	19.47	4	17855	170482	79556047
Atrial tachycardia	24.81	19.47	17	17842	7116	79719413
Ventricular tachycardia	24.53	19.47	38	17821	41897	79684632
Paraesthesia	24.19	19.47	5	17854	176318	79550211
Product use issue	24.13	19.47	102	17757	209720	79516809
Congestive hepatopathy	23.72	19.47	14	17845	4533	79721996
Iron deficiency anaemia	23.69	19.47	29	17830	25643	79700886
Hyperhidrosis	23.68	19.47	3	17856	151489	79575040
Prerenal failure	23.63	19.47	13	17846	3685	79722844
Prescribed underdose	23.54	19.47	31	17828	29483	79697046
Colon cancer	23.32	19.47	22	17837	14501	79712028
Upper respiratory tract inflammation	22.57	19.47	13	17846	4022	79722507
Renal pain	22.50	19.47	17	17842	8279	79718250
Drug dose titration not performed	22.48	19.47	8	17851	802	79725727
Hepatic cyst	22.34	19.47	15	17844	6074	79720455
Alopecia	22.30	19.47	12	17847	231343	79495186
Drug monitoring procedure incorrectly performed	22.30	19.47	7	17852	476	79726053
Infected cyst	22.24	19.47	9	17850	1281	79725248
Hyperammonaemia	22.15	19.47	19	17840	11074	79715455
Drug-induced liver injury	22.12	19.47	47	17812	66070	79660459
Hepatorenal syndrome	21.95	19.47	13	17846	4236	79722293
Inability to afford medication	21.24	19.47	11	17848	2762	79723767
Urine osmolarity increased	21.04	19.47	6	17853	293	79726236
Febrile neutropenia	20.82	19.47	13	17846	230986	79495543
Human chorionic gonadotropin positive	20.32	19.47	4	17855	37	79726492
Pulmonary vein occlusion	20.08	19.47	5	17854	144	79726385
Hypoalbuminaemia	19.56	19.47	24	17835	21273	79705256

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

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
Dehydration	contraindication	34095006
Hepatic failure	contraindication	59927004
Gastrointestinal hemorrhage	contraindication	74474003

🐶 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)

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)

Bioactivity Summary:

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

External reference:

ID	Source
4028789	VUID
N0000178481	NUI
D01213	KEGG_DRUG
4028789	VANDF
C1176308	UMLSCUI
CHEBI:32246	CHEBI
CHEMBL344159	ChEMBL_ID
D000077602	MESH_DESCRIPTOR_UI
DB06212	DRUGBANK_ID
2226	IUPHAR_LIGAND_ID
7969	INN_ID
21G72T1950	UNII
216237	PUBCHEM_CID
358257	RXNORM
165174	MMSL
26477	MMSL
334368	MMSL
d07447	MMSL
013121	NDDF
442901006	SNOMEDCT_US
443058000	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
Tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	31722-869	TABLET	30 mg	ORAL	ANDA	28 sections
Tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	49884-768	TABLET	15 mg	ORAL	ANDA	28 sections
Tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	49884-770	TABLET	30 mg	ORAL	ANDA	28 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
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
tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4317	TABLET	15 mg	ORAL	ANDA	30 sections
tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4318	TABLET	30 mg	ORAL	ANDA	30 sections
tolvaptan	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4318	TABLET	30 mg	ORAL	ANDA	30 sections
TOLVAPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4704	TABLET	15 mg	ORAL	NDA	33 sections
TOLVAPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4704	TABLET	15 mg	ORAL	NDA	33 sections
TOLVAPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4705	TABLET	30 mg	ORAL	NDA	33 sections
TOLVAPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4705	TABLET	30 mg	ORAL	NDA	33 sections
Tolvaptan	Human Prescription Drug Label	1	67877-635	TABLET	15 mg	ORAL	ANDA	28 sections
Tolvaptan	Human Prescription Drug Label	1	67877-636	TABLET	30 mg	ORAL	ANDA	28 sections
Tolvaptan	Human Prescription Drug Label	1	67877-636	TABLET	30 mg	ORAL	ANDA	28 sections
Tolvaptan	Human Prescription Drug Label	1	67877-636	TABLET	30 mg	ORAL	ANDA	28 sections
Tolvaptan	Human Prescription Drug Label	1	67877-637	TABLET	60 mg	ORAL	ANDA	28 sections
Tolvaptan	Human Prescription Drug Label	1	67877-637	TABLET	60 mg	ORAL	ANDA	28 sections
Tolvaptan	Human Prescription Drug Label	1	67877-637	TABLET	60 mg	ORAL	ANDA	28 sections