tolvaptan ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasopressin receptor antagonists 4110 150683-30-0

Description:

MoleculeDescription

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:

DoseUnitRoute
30 mg O

ADMET properties:

PropertyValueReference
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 ยตM/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:

DateAgencyCompanyOrphan
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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.1 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Vasopressin V2 receptor GPCR ANTAGONIST Ki 9 WOMBAT-PK DRUG LABEL
Vasopressin V1a receptor GPCR ANTAGONIST Ki 7.90 IUPHAR
Vasopressin V2 receptor GPCR ANTAGONIST Ki 8.90 IUPHAR
Vasopressin V1a receptor GPCR ANTAGONIST Ki 6.50 IUPHAR

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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