cinacalcet 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
calcium-sensing receptors (CaSR) agonists 647 226256-56-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cinacalcet
  • mimpara
  • cinacalcet hydrochloride
  • sensipar
  • AMG 073
  • AMG-073
  • KRN1493
  • cinacalcet HCl
Cinacalcet is a calcimimetic agent that increases the sensitivity of the calcium-sensing receptor to activation by extracellular calcium. It directly lowers PTH levels by increasing the sensitivity of the calcium sensing receptor to extracellular calcium. The reduction in PTH is associated with a concomitant decrease in serum calcium levels.
  • Molecular weight: 357.42
  • Formula: C22H22F3N
  • CLOGP: 6.35
  • LIPINSKI: 1
  • HAC: 1
  • HDO: 1
  • TPSA: 12.03
  • ALOGS: -6.81
  • ROTB: 7
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 7.19 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 20 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 17.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 18.30 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 19.90 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK 40
kinase-selectivity-class AKT3,AXL,BRAF,EIF2AK3,EPHB4,GRK2,PDK4,PRKCD 8
pfas-class PFAS structural alert (1 = True, 0 = False) 1

Approvals:

DateAgencyCompanyOrphan
Oct. 22, 2004 EMA
March 8, 2004 FDA AMGEN

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
Hospitalisation 8174.10 22.28 2570 26940 125530 90473407
Product dose omission issue 6984.93 22.28 2825 26685 288862 90310075
Laboratory test abnormal 5952.13 22.28 1573 27937 40281 90558656
Adverse drug reaction 1132.47 22.28 612 28898 116089 90482848
Blood parathyroid hormone increased 991.55 22.28 229 29281 3208 90595729
Intentional product misuse 821.60 22.28 453 29057 89151 90509786
Blood parathyroid hormone abnormal 518.59 22.28 87 29423 167 90598770
Parathyroid tumour benign 405.34 22.28 87 29423 849 90598088
Death 399.23 22.28 607 28903 455944 90142993
Hypocalcaemia 378.96 22.28 211 29299 42157 90556780
Calciphylaxis 365.90 22.28 103 29407 3273 90595664
Arteriovenous fistula site complication 359.51 22.28 71 29439 438 90598499
Hospice care 338.14 22.28 125 29385 9579 90589358
Living in residential institution 259.84 22.28 57 29453 621 90598316
Blood calcium increased 250.76 22.28 107 29403 11951 90586986
Nausea 239.69 22.28 847 28663 1109469 89489468
Hungry bone syndrome 219.92 22.28 39 29471 118 90598819
Hypophagia 214.49 22.28 138 29372 35799 90563138
Rehabilitation therapy 212.88 22.28 60 29450 1914 90597023
Renal transplant 198.92 22.28 55 29455 1633 90597304
Adverse event 176.28 22.28 204 29306 117214 90481723
Decreased appetite 173.59 22.28 380 29130 376160 90222777
Blood calcium decreased 170.53 22.28 112 29398 30070 90568867
Transplant 165.30 22.28 43 29467 1006 90597931
Malaise 160.68 22.28 486 29024 585500 90013437
Hypercalcaemia 157.72 22.28 112 29398 34128 90564809
Nephrogenic systemic fibrosis 150.79 22.28 55 29455 4053 90594884
Blood calcium abnormal 146.80 22.28 45 29465 1932 90597005
Blood parathyroid hormone decreased 146.39 22.28 74 29436 12142 90586795
Vomiting 145.55 22.28 573 28937 787720 89811217
Parathyroid tumour malignant 138.18 22.28 23 29487 41 90598896
Parathyroidectomy 131.93 22.28 29 29481 319 90598618
Peritonitis bacterial 124.68 22.28 51 29459 5120 90593817
Unevaluable investigation 124.58 22.28 21 29489 42 90598895
Brown tumour 118.99 22.28 20 29490 39 90598898
Hyperparathyroidism 116.28 22.28 43 29467 3294 90595643
Hepatic enzyme increased 103.68 22.28 3 29507 360733 90238204
Dialysis 102.79 22.28 57 29453 11272 90587665
Arthralgia 100.64 22.28 65 29445 778457 89820480
Rheumatoid arthritis 97.48 22.28 5 29505 362609 90236328
Fatigue 96.52 22.28 142 29368 1153881 89445056
Joint swelling 96.06 22.28 23 29487 503277 90095660
Systemic lupus erythematosus 94.19 22.28 6 29504 361890 90237047
Contraindicated product administered 90.77 22.28 3 29507 320136 90278801
Gastrointestinal tube insertion 88.97 22.28 28 29482 1312 90597625
Blood phosphorus increased 88.71 22.28 38 29472 4280 90594657
Arthropathy 87.20 22.28 9 29501 366233 90232704
Glossodynia 81.78 22.28 6 29504 321773 90277164
Skin induration 81.47 22.28 33 29477 3229 90595708
Mastication disorder 79.56 22.28 30 29480 2426 90596511
Sinusitis 77.76 22.28 10 29500 343078 90255859
Pyrexia 76.35 22.28 62 29448 660423 89938514
Product use issue 71.52 22.28 11 29499 329908 90269029
Blood phosphorus abnormal 67.99 22.28 15 29495 168 90598769
Stomatitis 67.35 22.28 6 29504 274692 90324245
Pain 66.51 22.28 141 29369 996200 89602737
Unevaluable event 65.55 22.28 85 29425 54763 90544174
Wheezing 64.86 22.28 3 29507 238077 90360860
Arteriovenous fistula occlusion 62.30 22.28 16 29494 355 90598582
Condition aggravated 61.52 22.28 62 29448 595483 90003454
Hypervolaemia 61.39 22.28 64 29446 32693 90566244
Product use in unapproved indication 60.97 22.28 17 29493 336219 90262718
Swelling 59.70 22.28 31 29479 419027 90179910
Wound 59.43 22.28 13 29497 302967 90295970
Skin hypertrophy 58.81 22.28 27 29483 3583 90595354
Parathyroid disorder 58.71 22.28 18 29492 773 90598164
Therapeutic product effect decreased 58.48 22.28 10 29500 277561 90321376
Peritonitis 57.06 22.28 49 29461 19656 90579281
Abdominal discomfort 56.42 22.28 305 29205 477023 90121914
Skin tightness 53.22 22.28 27 29483 4461 90594476
Skin fibrosis 52.55 22.28 17 29493 871 90598066
Intentional product use issue 52.46 22.28 5 29505 216887 90382050
End stage renal disease 51.32 22.28 33 29477 8538 90590399
Wrong technique in product usage process 50.98 22.28 87 29423 71484 90527453
Weight increased 49.77 22.28 38 29472 417889 90181048
Cerebrovascular accident 49.32 22.28 118 29392 123415 90475522
Parathyroid hyperplasia 49.16 22.28 11 29499 132 90598805
Hyperphosphataemia 48.95 22.28 24 29486 3687 90595250
Blue toe syndrome 48.92 22.28 14 29496 472 90598465
Gastrostomy 48.81 22.28 16 29494 855 90598082
Surgery 46.66 22.28 65 29445 44822 90554115
Blister 46.01 22.28 13 29497 254985 90343952
Rash 45.60 22.28 122 29388 795978 89802959
Neonatal hypocalcaemia 45.16 22.28 8 29502 24 90598913
Lower respiratory tract infection 44.82 22.28 13 29497 250646 90348291
Hyperparathyroidism tertiary 44.44 22.28 8 29502 27 90598910
Impaired healing 44.03 22.28 11 29499 234188 90364749
Liver injury 43.83 22.28 3 29507 170564 90428373
Chronic kidney disease-mineral and bone disorder 43.40 22.28 10 29500 138 90598799
Contusion 43.17 22.28 14 29496 251202 90347735
Alopecia 43.08 22.28 59 29451 495012 90103925
Treatment failure 42.50 22.28 23 29487 303905 90295032
Osteoarthritis 41.33 22.28 7 29503 195723 90403214
Musculoskeletal stiffness 40.65 22.28 23 29487 296509 90302428
Nephrocalcinosis 39.73 22.28 15 29495 1217 90597720
Pelvic deformity 38.76 22.28 10 29500 226 90598711
Joint contracture 38.18 22.28 16 29494 1706 90597231
Discomfort 38.00 22.28 21 29489 274314 90324623
Neutropenia 37.82 22.28 13 29497 224891 90374046
Febrile neutropenia 37.37 22.28 4 29506 158345 90440592
Foetal heart rate deceleration abnormality 36.15 22.28 12 29498 667 90598270
Hyperparathyroidism primary 36.13 22.28 11 29499 461 90598476
Sleep disorder 35.89 22.28 10 29500 198020 90400917
Migraine 35.67 22.28 9 29501 190383 90408554
Peritoneal dialysis complication 35.39 22.28 14 29496 1288 90597649
Hypoparathyroidism 35.25 22.28 13 29497 988 90597949
Injection site pain 34.98 22.28 7 29503 173692 90425245
Arteriovenous fistula site infection 34.93 22.28 7 29503 47 90598890
Thyroid operation 34.90 22.28 9 29501 203 90598734
Neonatal cholestasis 34.31 22.28 7 29503 52 90598885
Dysphagia 34.27 22.28 97 29413 112181 90486756
Enteral nutrition 33.76 22.28 9 29501 232 90598705
C-reactive protein increased 33.17 22.28 9 29501 181380 90417557
Arteriovenous fistula thrombosis 32.98 22.28 9 29501 254 90598683
Osteomalacia 32.91 22.28 12 29498 883 90598054
Gastric disorder 32.71 22.28 47 29463 33337 90565600
Hypersensitivity 32.21 22.28 62 29448 454615 90144322
Treatment noncompliance 31.84 22.28 59 29451 51668 90547269
Peripheral swelling 31.34 22.28 54 29456 413052 90185885
Adjusted calcium increased 30.96 22.28 6 29504 33 90598904
Toxicity to various agents 30.78 22.28 29 29481 287817 90311120
Drug hypersensitivity 29.65 22.28 67 29443 463542 90135395
Thrombosis in device 29.35 22.28 16 29494 3059 90595878
Arteriovenous fistula site haemorrhage 29.01 22.28 8 29502 235 90598702
Asthma 28.82 22.28 22 29488 242138 90356799
Night sweats 28.55 22.28 4 29506 128762 90470175
Urticaria 28.47 22.28 36 29474 312698 90286239
Cardiac operation 28.18 22.28 17 29493 3932 90595005
Abdominal pain upper 27.50 22.28 194 29316 332480 90266457
General physical health deterioration 27.31 22.28 46 29464 355069 90243868
Parathyroid tumour 27.23 22.28 7 29503 156 90598781
Shunt occlusion 27.05 22.28 10 29500 765 90598172
Liver disorder 26.35 22.28 4 29506 121265 90477672
Shunt stenosis 26.29 22.28 9 29501 550 90598387
Skin hyperpigmentation 26.10 22.28 20 29490 6831 90592106
Adjusted calcium decreased 24.90 22.28 7 29503 221 90598716
Hyperparathyroidism secondary 24.81 22.28 12 29498 1789 90597148
High turnover osteopathy 23.27 22.28 5 29505 49 90598888
Lung disorder 22.98 22.28 10 29500 149873 90449064
Confusional state 22.95 22.28 58 29452 386147 90212790
Neuropathy peripheral 22.88 22.28 8 29502 136962 90461975
White blood cell count decreased 22.83 22.28 13 29497 167096 90431841
Headache 22.81 22.28 176 29334 862570 89736367
Hypercholesterolaemia 22.69 22.28 3 29507 100889 90498048
Parathyroid hormone-related protein increased 22.58 22.28 4 29506 12 90598925
Road traffic accident 22.38 22.28 4 29506 107622 90491315
Pulmonary fibrosis 22.34 22.28 4 29506 107499 90491438

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
Product dose omission issue 6950.53 19.93 2737 21208 151628 42445762
Hospitalisation 6404.98 19.93 2136 21809 72194 42525196
Laboratory test abnormal 5881.51 19.93 1539 22406 21439 42575951
Adverse drug reaction 978.09 19.93 458 23487 36976 42560414
Blood parathyroid hormone increased 726.86 19.93 177 23768 1750 42595640
Intentional product misuse 612.14 19.93 399 23546 61501 42535889
Blood parathyroid hormone abnormal 499.23 19.93 87 23858 97 42597293
Arteriovenous fistula site complication 392.10 19.93 83 23862 402 42596988
Hypocalcaemia 303.84 19.93 197 23748 29976 42567414
Transplant 214.29 19.93 58 23887 896 42596494
Adverse event 201.00 19.93 139 23806 23501 42573889
Parathyroidectomy 191.00 19.93 35 23910 63 42597327
Parathyroid tumour benign 181.55 19.93 39 23906 205 42597185
Hospice care 173.21 19.93 88 23857 8425 42588965
Calciphylaxis 171.50 19.93 51 23894 1122 42596268
Blood parathyroid hormone decreased 162.65 19.93 53 23892 1590 42595800
Blood calcium increased 159.32 19.93 83 23862 8371 42589019
Nausea 150.42 19.93 526 23419 396273 42201117
Blood calcium abnormal 147.37 19.93 41 23904 705 42596685
Death 144.16 19.93 583 23362 470602 42126788
Hungry bone syndrome 143.66 19.93 31 23914 167 42597223
Blood calcium decreased 143.36 19.93 85 23860 11023 42586367
Abdominal discomfort 142.81 19.93 193 23752 75062 42522328
Living in residential institution 141.15 19.93 39 23906 653 42596737
Renal transplant 138.80 19.93 52 23893 2373 42595017
Hypophagia 135.53 19.93 116 23829 26840 42570550
Rehabilitation therapy 118.16 19.93 38 23907 1092 42596298
Hypercalcaemia 116.73 19.93 90 23855 17968 42579422
Vomiting 115.53 19.93 391 23554 289332 42308058
Unevaluable investigation 105.83 19.93 18 23927 15 42597375
Parathyroid tumour malignant 95.02 19.93 19 23926 65 42597325
Febrile neutropenia 84.35 19.93 5 23940 185698 42411692
Acute kidney injury 83.20 19.93 52 23893 367285 42230105
Neutropenia 80.57 19.93 9 23936 199422 42397968
Malaise 79.74 19.93 281 23664 211875 42385515
Toxicity to various agents 77.58 19.93 17 23928 229119 42368271
Abdominal pain upper 77.37 19.93 154 23791 82455 42514935
Parathyroid hyperplasia 76.90 19.93 13 23932 10 42597380
Peritonitis bacterial 76.60 19.93 48 23897 6867 42590523
Parathyroid disorder 66.82 19.93 13 23932 37 42597353
Blood phosphorus increased 63.13 19.93 54 23891 12471 42584919
Nephrogenic systemic fibrosis 62.05 19.93 33 23912 3468 42593922
Pyrexia 60.37 19.93 80 23865 393962 42203428
Dialysis 59.03 19.93 51 23894 11935 42585455
Product use in unapproved indication 54.27 19.93 18 23927 184438 42412952
Hyperparathyroidism tertiary 53.08 19.93 11 23934 47 42597343
Surgery 52.74 19.93 57 23888 17559 42579831
Unevaluable event 51.83 19.93 79 23866 34209 42563181
Decreased appetite 51.61 19.93 230 23715 192907 42404483
Leg amputation 50.12 19.93 26 23919 2597 42594793
Drug interaction 49.86 19.93 46 23899 266953 42330437
Gastrostomy 49.51 19.93 19 23926 926 42596464
Gastrointestinal disorder 47.33 19.93 90 23855 46563 42550827
Gastrointestinal tube insertion 47.25 19.93 21 23924 1489 42595901
Hyperparathyroidism 46.95 19.93 20 23925 1279 42596111
Condition aggravated 46.27 19.93 47 23898 260707 42336683
Disease progression 45.94 19.93 12 23933 143644 42453746
Adjusted calcium decreased 45.40 19.93 8 23937 10 42597380
Brown tumour 44.87 19.93 10 23935 64 42597326
Mastication disorder 43.99 19.93 21 23924 1755 42595635
Gastric disorder 41.83 19.93 42 23903 11880 42585510
Blood phosphorus abnormal 41.31 19.93 11 23934 159 42597231
Fatigue 40.27 19.93 119 23826 435522 42161868
Hyperparathyroidism secondary 37.34 19.93 19 23926 1823 42595567
Treatment noncompliance 36.15 19.93 71 23874 37601 42559789
Platelet count decreased 35.07 19.93 17 23928 138564 42458826
Skin induration 33.69 19.93 18 23927 1909 42595481
Overdose 33.25 19.93 9 23936 105255 42492135
Drug effective for unapproved indication 32.21 19.93 28 23917 6605 42590785
High turnover osteopathy 31.94 19.93 7 23938 41 42597349
Neuropathy peripheral 31.62 19.93 9 23936 101844 42495546
Shunt stenosis 31.56 19.93 13 23932 764 42596626
Hyponatraemia 31.44 19.93 9 23936 101453 42495937
Parathyroid gland enlargement 31.26 19.93 9 23936 176 42597214
Alanine aminotransferase increased 31.03 19.93 6 23939 88400 42508990
White blood cell count decreased 30.36 19.93 12 23933 110384 42487006
Peritonitis 29.67 19.93 44 23901 18589 42578801
Confusional state 28.80 19.93 31 23914 167566 42429824
Pulmonary embolism 28.29 19.93 16 23929 119596 42477794
Shunt occlusion 28.07 19.93 13 23932 1014 42596376
Dyspnoea 27.92 19.93 141 23804 442480 42154910
Nephrocalcinosis 27.83 19.93 12 23933 791 42596599
Anaemia 26.98 19.93 75 23870 280203 42317187
Wrong technique in product usage process 26.95 19.93 68 23877 42567 42554823
Calcinosis 26.94 19.93 12 23933 855 42596535
Thrombocytopenia 26.70 19.93 41 23904 190238 42407152
Appetite disorder 26.24 19.93 18 23927 2997 42594393
Thyroid operation 26.03 19.93 5 23940 13 42597377
Peritoneal dialysis complication 25.52 19.93 15 23930 1912 42595478
Angina pectoris 24.59 19.93 56 23889 32840 42564550
Weight decreased 23.65 19.93 51 23894 207897 42389493
Aspartate aminotransferase increased 23.62 19.93 7 23938 77156 42520234
Haemoglobin increased 23.33 19.93 21 23924 5185 42592205
COVID-19 22.78 19.93 19 23926 115929 42481461
Hypervolaemia 22.69 19.93 44 23901 23081 42574309
Vestibular neuronitis 22.52 19.93 8 23937 313 42597077
Rash 22.50 19.93 80 23865 276874 42320516
Injection site pain 22.34 19.93 3 23942 57795 42539595
Rhabdomyolysis 22.25 19.93 8 23937 78011 42519379
Arteriovenous fistula thrombosis 21.91 19.93 8 23937 339 42597051
Tachycardia 21.86 19.93 15 23930 101072 42496318

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
Laboratory test abnormal 9259.47 17.27 2293 36408 41786 110508812
Hospitalisation 5565.53 17.27 2022 36679 140471 110410127
Product dose omission issue 3032.78 17.27 1690 37011 320092 110230506
Blood parathyroid hormone increased 1194.46 17.27 281 38420 3967 110546631
Blood parathyroid hormone abnormal 801.28 17.27 136 38565 260 110550338
Arteriovenous fistula site complication 773.44 17.27 153 38548 877 110549721
Parathyroid tumour benign 538.98 17.27 114 38587 951 110549647
Death 534.72 17.27 909 37792 697960 109852638
Nausea 511.59 17.27 1244 37457 1234446 109316152
Calciphylaxis 486.40 17.27 137 38564 4050 110546548
Hypocalcaemia 467.81 17.27 289 38412 65077 110485521
Adverse drug reaction 421.92 17.27 326 38375 105233 110445365
Vomiting 366.99 17.27 909 37792 909766 109640832
Hungry bone syndrome 345.07 17.27 65 38636 274 110550324
Living in residential institution 337.91 17.27 77 38624 934 110549664
Decreased appetite 321.38 17.27 587 38114 475259 110075339
Rehabilitation therapy 303.10 17.27 82 38619 2079 110548519
Blood calcium increased 251.72 17.27 124 38577 17916 110532682
Renal transplant 249.06 17.27 77 38624 3161 110547437
Unevaluable investigation 239.66 17.27 39 38662 49 110550549
Hypercalcaemia 237.92 17.27 167 38534 46490 110504108
Parathyroid tumour malignant 220.51 17.27 40 38661 130 110550468
Blood calcium abnormal 215.10 17.27 60 38641 1709 110548889
Peritonitis bacterial 188.66 17.27 86 38615 10447 110540151
Malaise 184.06 17.27 584 38117 671235 109879363
Blood calcium decreased 179.71 17.27 127 38574 35718 110514880
Abdominal discomfort 179.05 17.27 413 38288 393445 110157153
Hyperparathyroidism 162.20 17.27 58 38643 3752 110546846
Unevaluable event 156.05 17.27 144 38557 59083 110491515
Nephrogenic systemic fibrosis 155.44 17.27 62 38639 5421 110545177
Blood parathyroid hormone decreased 153.47 17.27 80 38621 13009 110537589
Brown tumour 146.11 17.27 27 38674 100 110550498
Intentional product misuse 145.92 17.27 205 38496 132699 110417899
Parathyroidectomy 140.48 17.27 30 38671 263 110550335
Muscle spasms 127.71 17.27 293 38408 277864 110272734
Blood phosphorus increased 118.69 17.27 73 38628 16267 110534331
Dialysis 118.48 17.27 78 38623 19541 110531057
Abdominal pain upper 107.92 17.27 317 38384 348794 110201804
Surgery 100.34 17.27 96 38605 41187 110509411
Skin induration 95.16 17.27 41 38660 4354 110546244
Adjusted calcium decreased 93.61 17.27 21 38680 236 110550362
Gastric disorder 93.52 17.27 84 38617 33273 110517325
Hepatic enzyme increased 91.89 17.27 5 38696 320887 110229711
Parathyroid disorder 91.79 17.27 25 38676 650 110549948
Transplant 88.38 17.27 28 38673 1246 110549352
Rheumatoid arthritis 87.92 17.27 4 38697 299609 110250989
Hypophagia 87.69 17.27 100 38601 52526 110498072
Parathyroid hyperplasia 83.47 17.27 18 38683 166 110550432
Joint swelling 82.78 17.27 26 38675 442819 110107779
Pyrexia 82.22 17.27 117 38584 898148 109652450
Hyperparathyroidism tertiary 80.25 17.27 15 38686 60 110550538
Febrile neutropenia 79.39 17.27 9 38692 316758 110233840
Gastrointestinal tube insertion 78.32 17.27 29 38672 2072 110548526
Hypervolaemia 77.41 17.27 91 38610 49369 110501229
Shunt occlusion 76.05 17.27 27 38674 1710 110548888
Arthralgia 74.89 17.27 98 38603 779534 109771064
Neutropenia 73.66 17.27 20 38681 374600 110175998
Sinusitis 72.93 17.27 9 38692 296679 110253919
Contraindicated product administered 70.66 17.27 4 38697 248263 110302335
Condition aggravated 69.92 17.27 93 38608 734743 109815855
Product use in unapproved indication 69.32 17.27 35 38666 447342 110103256
Arteriovenous fistula occlusion 68.48 17.27 19 38682 530 110550068
Peritonitis 68.43 17.27 70 38631 32537 110518061
Leg amputation 67.93 17.27 32 38669 4186 110546412
Gastrostomy 67.50 17.27 24 38677 1526 110549072
Toxicity to various agents 66.73 17.27 43 38658 480512 110070086
Shunt stenosis 65.77 17.27 23 38678 1393 110549205
Skin hypertrophy 65.39 17.27 33 38668 5014 110545584
Diarrhoea 65.21 17.27 646 38055 1138859 109411739
Skin tightness 64.92 17.27 34 38667 5579 110545019
Stomatitis 64.50 17.27 9 38692 270233 110280365
Peritoneal dialysis complication 62.61 17.27 26 38675 2520 110548078
Wheezing 62.10 17.27 8 38693 255222 110295376
Blood phosphorus abnormal 61.99 17.27 16 38685 336 110550262
Systemic lupus erythematosus 61.82 17.27 8 38693 254330 110296268
Fatigue 61.61 17.27 219 38482 1215739 109334859
Pericarditis 60.93 17.27 4 38697 219110 110331488
Hyperparathyroidism secondary 59.23 17.27 27 38674 3277 110547321
Arthropathy 59.10 17.27 14 38687 287508 110263090
Glossodynia 59.04 17.27 5 38696 221999 110328599
High turnover osteopathy 57.97 17.27 12 38689 89 110550509
Lower respiratory tract infection 55.93 17.27 9 38692 243097 110307501
Product use issue 55.25 17.27 20 38681 311675 110238923
Skin fibrosis 54.68 17.27 20 38681 1380 110549218
Parathyroid gland enlargement 53.76 17.27 13 38688 207 110550391
Arteriovenous fistula thrombosis 53.47 17.27 16 38685 587 110550011
End stage renal disease 52.30 17.27 50 38651 21423 110529175
Cerebrovascular accident 51.57 17.27 160 38541 181124 110369474
Hyperparathyroidism primary 51.11 17.27 15 38686 514 110550084
Nephrocalcinosis 49.64 17.27 20 38681 1794 110548804
Blood cholesterol increased 49.58 17.27 4 38697 184781 110365817
Hyperphosphataemia 49.40 17.27 43 38658 16338 110534260
Drug effective for unapproved indication 48.49 17.27 40 38661 14127 110536471
Pelvic deformity 48.09 17.27 10 38691 76 110550522
Hypotension 47.59 17.27 330 38371 523519 110027079
Malignant neoplasm progression 46.23 17.27 4 38697 174563 110376035
Drug interaction 44.82 17.27 66 38635 500117 110050481
Wrong technique in product usage process 44.49 17.27 96 38605 87252 110463346
Therapeutic product effect decreased 44.46 17.27 15 38686 244301 110306297
Chronic kidney disease-mineral and bone disorder 44.16 17.27 14 38687 624 110549974
Intentional product use issue 43.77 17.27 16 38685 247890 110302708
Blue toe syndrome 43.13 17.27 14 38687 674 110549924
Appetite disorder 43.00 17.27 32 38669 9737 110540861
Weight increased 42.04 17.27 51 38650 419593 110131005
Wound 41.61 17.27 15 38686 234422 110316176
Cardiac operation 41.55 17.27 26 38675 5969 110544629
Swelling 41.54 17.27 37 38664 351004 110199594
Arrhythmia 40.75 17.27 81 38620 69494 110481104
Alopecia 40.18 17.27 41 38660 364712 110185886
Injection site pain 40.01 17.27 7 38694 177915 110372683
Arteriovenous fistula site infection 39.64 17.27 10 38691 191 110550407
Angina pectoris 39.50 17.27 75 38626 62220 110488378
Rash 39.41 17.27 151 38550 820813 109729785
Parathyroid haemorrhage 39.32 17.27 6 38695 3 110550595
Asthma 38.11 17.27 20 38681 250271 110300327
Treatment noncompliance 38.06 17.27 81 38620 72909 110477689
Type 2 diabetes mellitus 37.68 17.27 8 38693 177224 110373374
Parathyroid tumour 37.58 17.27 8 38693 69 110550529
Arteriovenous fistula site haemorrhage 37.56 17.27 11 38690 374 110550224
Therapeutic procedure 37.46 17.27 14 38687 1026 110549572
Joint contracture 37.37 17.27 18 38683 2473 110548125
Osteoarthritis 37.31 17.27 9 38692 182614 110367984
Liver injury 35.90 17.27 5 38696 150408 110400190
Calcinosis 35.06 17.27 18 38683 2834 110547764
Psoriasis 35.00 17.27 4 38697 139989 110410609
Blister 34.87 17.27 18 38683 227358 110323240
Bursitis 34.33 17.27 3 38698 129915 110420683
Impaired healing 34.21 17.27 13 38688 196704 110353894
Migraine 34.02 17.27 9 38692 171643 110378955
White blood cell count decreased 33.95 17.27 19 38682 229371 110321227
Alanine aminotransferase increased 33.92 17.27 11 38690 183762 110366836
Constipation 33.40 17.27 227 38474 357559 110193039
Confusional state 32.85 17.27 72 38629 468608 110081990
Urticaria 32.72 17.27 38 38663 318819 110231779
Phosphaturic mesenchymal tumour 32.44 17.27 5 38696 3 110550595
Osteomalacia 31.74 17.27 14 38687 1573 110549025
Thrombosis in device 31.72 17.27 21 38680 5306 110545292
Shunt infection 31.62 17.27 9 38692 276 110550322
Platelet count decreased 31.43 17.27 21 38680 230422 110320176
Adjusted calcium increased 31.42 17.27 7 38694 76 110550522
Neutrophil count decreased 31.40 17.27 3 38698 120938 110429660
Neuropathy peripheral 30.92 17.27 12 38689 179265 110371333
Fistula repair 30.63 17.27 7 38694 86 110550512
Toe amputation 30.54 17.27 19 38682 4319 110546279
Parathyroid hormone-related protein increased 29.30 17.27 5 38696 10 110550588
Thyroid operation 29.08 17.27 8 38693 216 110550382
Night sweats 28.57 17.27 6 38695 133977 110416621
Hospice care 28.41 17.27 28 38673 12445 110538153
Musculoskeletal stiffness 28.01 17.27 34 38667 279788 110270810
Neoplasm malignant 27.72 17.27 48 38653 37095 110513503
COVID-19 27.60 17.27 27 38674 245033 110305565
Treatment failure 27.42 17.27 34 38667 277200 110273398
Pain 27.29 17.27 209 38492 954746 109595852
Cardiac disorder 27.16 17.27 73 38628 76207 110474391
Parathyroid gland operation 26.95 17.27 5 38696 19 110550579
Aplasia pure red cell 26.60 17.27 24 38677 9554 110541044
Lung disorder 26.51 17.27 15 38686 180032 110370566
Sleep disorder due to general medical condition, insomnia type 26.45 17.27 3 38698 105640 110444958
Loss of personal independence in daily activities 25.94 17.27 10 38691 150010 110400588
Sleep disorder 25.90 17.27 19 38682 198625 110351973
Haemoglobin increased 25.56 17.27 23 38678 9124 110541474
Aspartate aminotransferase increased 25.52 17.27 12 38689 159924 110390674
Hypercalciuria 25.52 17.27 9 38692 559 110550039
Hepatic cyst infection 24.71 17.27 7 38694 211 110550387
General physical health deterioration 24.63 17.27 72 38629 425223 110125375
Skin hyperpigmentation 24.57 17.27 22 38679 8674 110541924
Hypocalciuria 24.41 17.27 5 38696 35 110550563
Hypersensitivity 23.68 17.27 68 38633 403930 110146668
Mucosal inflammation 23.41 17.27 3 38698 96138 110454460
Intermittent claudication 23.04 17.27 15 38686 3686 110546912
Renal cyst infection 23.03 17.27 7 38694 271 110550327
Fibrosis 22.92 17.27 20 38681 7622 110542976
Blood phosphorus decreased 22.87 17.27 20 38681 7645 110542953
Renal haemorrhage 22.84 17.27 13 38688 2512 110548086
Hypoparathyroidism 22.79 17.27 11 38690 1519 110549079
Medical procedure 22.33 17.27 8 38693 520 110550078
Blood pressure increased 22.24 17.27 35 38666 258338 110292260
Depression 22.01 17.27 49 38652 317286 110233312
Blood glucose decreased 21.87 17.27 38 38663 29450 110521148
Foetal heart rate deceleration abnormality 21.60 17.27 6 38695 168 110550430
Placental insufficiency 21.40 17.27 10 38691 1284 110549314
Extremity contracture 21.32 17.27 11 38690 1750 110548848
Pulmonary fibrosis 20.89 17.27 5 38696 102037 110448561
Pseudofracture 20.87 17.27 3 38698 0 110550598
Deltaretrovirus test positive 20.87 17.27 3 38698 0 110550598
Parathyroid cyst 20.87 17.27 3 38698 0 110550598
Blood pressure abnormal 20.83 17.27 32 38669 22392 110528206
Contusion 20.67 17.27 31 38670 233330 110317268
Acute kidney injury 20.60 17.27 134 38567 635296 109915302
Oncocytoma 20.51 17.27 4 38697 21 110550577
Haemodialysis 20.42 17.27 28 38673 17691 110532907
Dry mouth 20.32 17.27 24 38677 199924 110350674
Sciatica 19.99 17.27 4 38697 92395 110458203
Chronic kidney disease 19.55 17.27 65 38636 76226 110474372
Foot amputation 19.54 17.27 9 38692 1119 110549479
Hypercholesterolaemia 19.51 17.27 4 38697 90833 110459765
Poor peripheral circulation 19.04 17.27 14 38687 4183 110546415
Crystal deposit intestine 18.91 17.27 6 38695 268 110550330
Inflammation 18.79 17.27 24 38677 193214 110357384
Blood potassium increased 18.62 17.27 38 38663 33211 110517387
Myelosuppression 18.59 17.27 5 38696 94335 110456263
Discomfort 18.56 17.27 29 38672 214678 110335920
Pulmonary calcification 18.39 17.27 7 38694 540 110550058
Intracardiac mass 18.36 17.27 6 38695 295 110550303
Hypocalcaemic seizure 18.21 17.27 5 38696 134 110550464
Overdose 17.99 17.27 34 38667 233760 110316838
Dyspnoea 17.97 17.27 276 38425 1106596 109444002
Vestibular neuronitis 17.76 17.27 8 38693 945 110549653
Drug-induced liver injury 17.68 17.27 10 38691 120057 110430541
Cardiac valve disease 17.66 17.27 16 38685 6405 110544193
Peripheral swelling 17.65 17.27 77 38624 403957 110146641
Anaphylactic reaction 17.59 17.27 9 38692 114291 110436307
Oedema 17.55 17.27 29 38672 209947 110340651
Peripheral venous disease 17.46 17.27 4 38697 84113 110466485
Product quality issue 17.46 17.27 3 38698 77296 110473302
Hepatitis 17.32 17.27 5 38696 90049 110460549

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H05BX01 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CALCIUM HOMEOSTASIS
ANTI-PARATHYROID AGENTS
Other anti-parathyroid agents
FDA MoA N0000020081 Increased Calcium-sensing Receptor Sensitivity
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D006727 Hormone Antagonists
MeSH PA D057966 Calcimimetic Agents
FDA EPC N0000175902 Calcium-sensing Receptor Agonist
CHEBI has role CHEBI:48525 calcimimetic
CHEBI has role CHEBI:50183 P450 inhibitor
CHEBI has role CHEBI:231911 renoprotective agent
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

H05BX Other anti-parathyroid agents 5 drugs
calcifedioldoxercalciferoletelcalcetideevocalcetparicalcitol

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

DiseaseRelationSNOMED_IDDOID
Hypercalcemia due to Primary Hyperparathyroidism indication
Hyperparathyroidism Secondary to Chronic Renal Failure with Dialysis indication
Parathyroid Carcinoma with Hypercalcemia indication
Hypophosphatemia contraindication 4996001
Hypocalcemia contraindication 5291005
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Seizure disorder contraindication 128613002
Disease of liver contraindication 235856003 DOID:409
Adynamic bone disease contraindication 236552002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.69 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 30MG BASE SENSIPAR AMGEN N021688 March 8, 2004 DISCN TABLET ORAL 7829595 Sept. 22, 2026 METHOD OF TREATING HYPERPARATHYROIDISM; METHOD OF TREATING HYPERCALCEMIA
EQ 60MG BASE SENSIPAR AMGEN N021688 March 8, 2004 DISCN TABLET ORAL 7829595 Sept. 22, 2026 METHOD OF TREATING HYPERPARATHYROIDISM; METHOD OF TREATING HYPERCALCEMIA
EQ 90MG BASE SENSIPAR AMGEN N021688 March 8, 2004 DISCN TABLET ORAL 7829595 Sept. 22, 2026 METHOD OF TREATING HYPERPARATHYROIDISM; METHOD OF TREATING HYPERCALCEMIA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Extracellular calcium-sensing receptor GPCR POSITIVE ALLOSTERIC MODULATOR EC50 7.70 CHEMBL CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7.04 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 6.11 CHEMBL
Sodium-dependent noradrenaline transporter Transporter Ki 5.84 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.71 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 6.08 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 7.40 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 6.18 CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 5.74 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 6.24 CHEMBL
D(3) dopamine receptor GPCR Ki 6.41 CHEMBL
Histamine H2 receptor GPCR Ki 5.58 CHEMBL
5-hydroxytryptamine receptor 1D GPCR Ki 5.77 CHEMBL
Alpha-2C adrenergic receptor GPCR Ki 5.80 CHEMBL
Cytochrome P450 2D6 Enzyme IC50 7.30 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 5.54 CHEMBL
Kappa-type opioid receptor GPCR Ki 6.35 CHEMBL
Glycine receptor subunit alpha-1 Ion channel EC50 6.49 CHEMBL
5-hydroxytryptamine receptor 5A GPCR Ki 6.01 CHEMBL
Mu-type opioid receptor GPCR Ki 5.89 CHEMBL
Transmembrane protein 97 Enzyme Ki 6.41 CHEMBL
Metabotropic glutamate receptor 5 GPCR ALLOSTERIC MODULATOR Ki 4.35 IUPHAR
Replicase polyprotein 1ab Enzyme IC50 5.22 CHEMBL

External reference:

IDSource
4021430 VUID
N0000148841 NUI
D03504 KEGG_DRUG
364782-34-3 SECONDARY_CAS_RN
384379 RXNORM
C1337242 UMLSCUI
CHEBI:48390 CHEBI
CHEMBL1201284 ChEMBL_ID
CHEMBL1200776 ChEMBL_ID
DB01012 DRUGBANK_ID
D000069449 MESH_DESCRIPTOR_UI
156419 PUBCHEM_CID
3308 IUPHAR_LIGAND_ID
8287 INN_ID
UAZ6V7728S UNII
18133 MMSL
303128 MMSL
49840 MMSL
d05218 MMSL
008595 NDDF
008596 NDDF
409391006 SNOMEDCT_US
409392004 SNOMEDCT_US
426512007 SNOMEDCT_US
YP4 PDB_CHEM_ID
4021430 VANDF
UAZ6V7728S INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 0904-7502 TABLET, FILM COATED 30 mg ORAL ANDA 23 sections
CINACALCET HUMAN PRESCRIPTION DRUG LABEL 1 16729-440 TABLET, FILM COATED 30 mg ORAL ANDA 25 sections
CINACALCET HUMAN PRESCRIPTION DRUG LABEL 1 16729-440 TABLET, FILM COATED 30 mg ORAL ANDA 25 sections
CINACALCET HUMAN PRESCRIPTION DRUG LABEL 1 16729-441 TABLET, FILM COATED 60 mg ORAL ANDA 25 sections
CINACALCET HUMAN PRESCRIPTION DRUG LABEL 1 16729-441 TABLET, FILM COATED 60 mg ORAL ANDA 25 sections
CINACALCET HUMAN PRESCRIPTION DRUG LABEL 1 16729-442 TABLET, FILM COATED 90 mg ORAL ANDA 25 sections
CINACALCET HUMAN PRESCRIPTION DRUG LABEL 1 16729-442 TABLET, FILM COATED 90 mg ORAL ANDA 25 sections
Cinacalcet Human Prescription Drug Label 1 31722-103 TABLET, FILM COATED 30 mg ORAL ANDA 29 sections
Cinacalcet Human Prescription Drug Label 1 31722-104 TABLET, FILM COATED 60 mg ORAL ANDA 29 sections
Cinacalcet Human Prescription Drug Label 1 31722-105 TABLET, FILM COATED 90 mg ORAL ANDA 29 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 43598-367 TABLET 30 mg ORAL ANDA 24 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 43598-368 TABLET 60 mg ORAL ANDA 24 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 43598-369 TABLET 90 mg ORAL ANDA 24 sections
Cinacalcet Human Prescription Drug Label 1 47335-379 TABLET, FILM COATED 30 mg ORAL ANDA 27 sections
Cinacalcet Human Prescription Drug Label 1 47335-380 TABLET, FILM COATED 60 mg ORAL ANDA 27 sections
Cinacalcet Human Prescription Drug Label 1 47335-600 TABLET, FILM COATED 90 mg ORAL ANDA 27 sections
SENSIPAR HUMAN PRESCRIPTION DRUG LABEL 1 50090-7096 TABLET, COATED 90 mg ORAL NDA 27 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 50268-188 TABLET, FILM COATED 30 mg ORAL ANDA 23 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 53808-0577 TABLET, COATED 30 mg ORAL NDA 26 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 53808-0578 TABLET, COATED 60 mg ORAL NDA 26 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 54868-5616 TABLET, COATED 30 mg ORAL NDA 22 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-073 TABLET, COATED 30 mg ORAL NDA 27 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-074 TABLET, COATED 60 mg ORAL NDA 27 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-075 TABLET, COATED 90 mg ORAL NDA 27 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 60687-516 TABLET, FILM COATED 30 mg ORAL ANDA 23 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 63629-8763 TABLET, FILM COATED 30 mg ORAL ANDA 25 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 63629-8764 TABLET, FILM COATED 60 mg ORAL ANDA 25 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 63629-8765 TABLET, FILM COATED 90 mg ORAL ANDA 25 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 63629-9606 TABLET, FILM COATED 90 mg ORAL ANDA 25 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 63629-9607 TABLET, FILM COATED 60 mg ORAL ANDA 25 sections