cinacalcet Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
647 226256-56-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cinacalcet
  • mimpara
  • cinacalcet hydrochloride
  • sensipar
  • AMG 073
  • AMG-073
  • KRN1493
  • cinacalcet HCl
A naphthalene derivative and CALCIMIMETIC AGENT that increases the sensitivity of PARATHYROID GLAND calcium-sensing receptors to serum calcium. This action reduces parathyroid hormone secretion and decreases serum calcium in the treatment of PARATHYROID DISEASES.
  • Molecular weight: 357.42
  • Formula: C22H22F3N
  • CLOGP: 6.35
  • LIPINSKI: 1
  • HAC: 1
  • HDO: 1
  • TPSA: 12.03
  • ALOGS: -6.81
  • ROTB: 7

Drug dosage:

DoseUnitRoute
60 mg O

Approvals:

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

FDA Adverse Event Reporting System

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 22328.12 62.62 4674 13639 16051 3351495
Drug dose omission 5100.07 62.62 1671 16642 36761 3330785
Laboratory test abnormal 4920.49 62.62 1097 17216 4747 3362799
Nausea 1604.91 62.62 1093 17220 128552 3238994
Blood parathyroid hormone increased 1524.52 62.62 299 18014 543 3367003
Vomiting 1172.62 62.62 784 17529 88747 3278799
Death 992.15 62.62 880 17433 151444 3216102
Unevaluable event 903.88 62.62 354 17959 12722 3354824
Malaise 897.66 62.62 590 17723 64587 3302959
Blood parathyroid hormone abnormal 892.96 62.62 153 18160 52 3367494
Decreased appetite 848.53 62.62 484 17829 41006 3326540
Abdominal discomfort 826.17 62.62 369 17944 18515 3349031
Muscle spasms 797.54 62.62 402 17911 26501 3341045
Adverse drug reaction 710.43 62.62 271 18042 9040 3358506
Blood calcium decreased 694.35 62.62 199 18114 2621 3364925
Diarrhoea 582.57 62.62 555 17758 103793 3263753
Blood parathyroid hormone decreased 526.20 62.62 102 18211 167 3367379
Abdominal pain upper 485.09 62.62 282 18031 24634 3342912
Blood calcium increased 452.88 62.62 127 18186 1535 3366011
Transplant 445.82 62.62 104 18209 554 3366992
Hypocalcaemia 406.55 62.62 159 18154 5662 3361884
Rehabilitation therapy 375.77 62.62 80 18233 255 3367291
Intentional product misuse 358.66 62.62 184 18129 12517 3355029
Gastrointestinal tube insertion 350.64 62.62 89 18224 709 3366837
Blood calcium abnormal 347.78 62.62 74 18239 235 3367311
Living in residential institution 327.39 62.62 68 18245 185 3367361
Parathyroidectomy 321.51 62.62 62 18251 97 3367449
Paraesthesia 273.82 62.62 205 18108 27343 3340203
Hypotension 264.79 62.62 258 18055 49256 3318290
Hypercalcaemia 236.13 62.62 95 18218 3642 3363904
Unevaluable investigation 232.30 62.62 40 18273 15 3367531
Blood phosphorus increased 223.20 62.62 59 18254 560 3366986
Surgery 200.01 62.62 102 18211 6838 3360708
Wrong technique in product usage process 199.06 62.62 139 18174 16612 3350934
Gastrointestinal disorder 187.96 62.62 113 18200 10456 3357090
Gastrostomy 178.95 62.62 47 18266 434 3367112
Constipation 174.77 62.62 166 18147 30646 3336900
Enteral nutrition 171.45 62.62 32 18281 37 3367509
Dizziness 169.71 62.62 255 18058 76257 3291289
Renal transplant 168.79 62.62 48 18265 611 3366935
Hospice care 161.42 62.62 47 18266 654 3366892
Arteriovenous fistula site complication 160.75 62.62 36 18277 154 3367392
Gastric disorder 145.36 62.62 68 18245 3770 3363776
Hypoaesthesia 138.79 62.62 133 18180 24806 3342740
Hypophagia 134.88 62.62 75 18238 5986 3361560
Off label use 134.21 62.62 190 18123 53787 3313759
Dysphagia 133.11 62.62 117 18196 19534 3348012
Seizure 127.76 62.62 160 18153 40240 3327306
Pruritus 116.60 62.62 165 18148 46668 3320878
Blood phosphorus abnormal 109.55 62.62 23 18290 67 3367479
Cerebrovascular accident 107.17 62.62 137 18176 35151 3332395
Arrhythmia 106.78 62.62 79 18234 10318 3357228
Adverse event 105.83 62.62 82 18231 11475 3356071
Dialysis 101.69 62.62 55 18258 4154 3363392
Calciphylaxis 94.82 62.62 29 18284 482 3367064
Pneumonia 93.73 62.62 187 18126 69956 3297590
Parathyroid tumour benign 89.10 62.62 23 18290 197 3367349
Hypertension 87.64 62.62 130 18183 38336 3329210
Drug intolerance 87.47 62.62 74 18239 11724 3355822
Appetite disorder 80.54 62.62 28 18285 708 3366838
Parathyroid disorder 72.67 62.62 18 18295 128 3367418
Cardiac disorder 64.86 62.62 67 18246 13652 3353894
Adjusted calcium decreased 63.78 62.62 12 18301 15 3367531

Pharmacologic Action:

SourceCodeDescription
ATC H05BX01 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CALCIUM HOMEOSTASIS
ANTI-PARATHYROID AGENTS
Other anti-parathyroid agents
MeSH PA D057966 Calcimimetic Agents
MeSH PA D006727 Hormone Antagonists
MeSH PA D006730 Hormones, Hormone Substitutes, and Hormone Antagonists
CHEBI has role CHEBI:48525 calcimimetic
FDA EPC N0000175902 Calcium-sensing Receptor Agonist
FDA MoA N0000020081 Increased Calcium-sensing Receptor Sensitivity

Drug Use (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 DOID:1826
Disease of liver contraindication 235856003 DOID:409
Adynamic bone disease contraindication 236552002

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 RX TABLET ORAL 7829595 Sept. 22, 2026 METHOD OF TREATING HYPERPARATHYROIDISM; METHOD OF TREATING HYPERCALCEMIA
EQ 60MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL 7829595 Sept. 22, 2026 METHOD OF TREATING HYPERPARATHYROIDISM; METHOD OF TREATING HYPERCALCEMIA
EQ 90MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL 7829595 Sept. 22, 2026 METHOD OF TREATING HYPERPARATHYROIDISM; METHOD OF TREATING HYPERCALCEMIA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 30MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL Feb. 25, 2018 TREATMENT OF SEVERE HYPERCALCEMIA IN PATIENTS WITH PRIMARYHYPERPARATHYROIDISM WHO ARE UNABLE TO UNDERGO PARATHYROIDECTOMY
EQ 60MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL Feb. 25, 2018 TREATMENT OF SEVERE HYPERCALCEMIA IN PATIENTS WITH PRIMARYHYPERPARATHYROIDISM WHO ARE UNABLE TO UNDERGO PARATHYROIDECTOMY
EQ 90MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL Feb. 25, 2018 TREATMENT OF SEVERE HYPERCALCEMIA IN PATIENTS WITH PRIMARYHYPERPARATHYROIDISM WHO ARE UNABLE TO UNDERGO PARATHYROIDECTOMY
EQ 30MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL May 23, 2020 CLINICAL INFORMATION ADDED TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE LABELING.
EQ 60MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL May 23, 2020 CLINICAL INFORMATION ADDED TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE LABELING.
EQ 90MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL May 23, 2020 CLINICAL INFORMATION ADDED TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE LABELING.
EQ 30MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL Nov. 21, 2021 TREATMENT OF HYPERCALCEMIA IN ADULT PATIENTS WITH PRIMARY HYPERPARATHYROIDISM FOR WHOM PARATHYROIDECTOMY WOULD BE INDICATED ON THE BASIS OF SERUM CALCIUM LEVELS, BUT WHO ARE UNABLE TO UNDERGO PARATHYROIDECTOMY.
EQ 60MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL Nov. 21, 2021 TREATMENT OF HYPERCALCEMIA IN ADULT PATIENTS WITH PRIMARY HYPERPARATHYROIDISM FOR WHOM PARATHYROIDECTOMY WOULD BE INDICATED ON THE BASIS OF SERUM CALCIUM LEVELS, BUT WHO ARE UNABLE TO UNDERGO PARATHYROIDECTOMY.
EQ 90MG BASE SENSIPAR AMGEN N021688 March 8, 2004 RX TABLET ORAL Nov. 21, 2021 TREATMENT OF HYPERCALCEMIA IN ADULT PATIENTS WITH PRIMARY HYPERPARATHYROIDISM FOR WHOM PARATHYROIDECTOMY WOULD BE INDICATED ON THE BASIS OF SERUM CALCIUM LEVELS, BUT WHO ARE UNABLE TO UNDERGO PARATHYROIDECTOMY.

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Extracellular calcium-sensing receptor GPCR POSITIVE ALLOSTERIC MODULATOR EC50 7.70 CHEMBL CHEMBL
Glycine receptor subunit alpha-1 Ion channel EC50 6.49 CHEMBL

External reference:

IDSource
3308 IUPHAR_LIGAND_ID
4021430 VUID
N0000148841 NUI
C1337242 UMLSCUI
D03504 KEGG_DRUG
1K860WSG25 UNII
364782-34-3 SECONDARY_CAS_RN
DB01012 DRUGBANK_ID
409391006 SNOMEDCT_US
409392004 SNOMEDCT_US
407990 RXNORM
4021430 VANDF
d05218 MMSL
N0000148841 NDFRT
008595 NDDF
156419 PUBCHEM_CID
CHEMBL1200776 ChEMBL_ID
CHEMBL1201284 ChEMBL_ID
8287 INN_ID
D000069449 MESH_DESCRIPTOR_UI
CHEBI:48390 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 53808-0577 TABLET, COATED 30 mg ORAL NDA 14 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 53808-0578 TABLET, COATED 60 mg ORAL NDA 14 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 54868-5616 TABLET, COATED 30 mg ORAL NDA 18 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55154-4875 TABLET, COATED 30 mg ORAL NDA 18 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55154-4876 TABLET, COATED 60 mg ORAL NDA 18 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-073 TABLET, COATED 30 mg ORAL NDA 18 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-074 TABLET, COATED 60 mg ORAL NDA 18 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-075 TABLET, COATED 90 mg ORAL NDA 18 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 68151-4740 TABLET, COATED 30 mg ORAL NDA 18 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 69189-0730 TABLET, COATED 30 mg ORAL NDA 18 sections