cinacalcet Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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
  • 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

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 ┬ÁM/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

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 10992.72 64.80 2466 10940 12387 2332292
Product dose omission 10122.25 64.80 2775 10631 35482 2309197
Laboratory test abnormal 7843.69 64.80 1569 11837 3721 2340958
Adverse drug reaction 2172.21 64.80 608 12798 7675 2337004
Intentional product misuse 1394.48 64.80 446 12960 9043 2335636
Blood parathyroid hormone increased 929.13 64.80 188 13218 448 2344231
Nausea 756.30 64.80 653 12753 111536 2233143
Malaise 650.50 64.80 450 12956 55135 2289544
Decreased appetite 588.42 64.80 333 13073 28558 2316121
Abdominal discomfort 569.44 64.80 276 13130 17180 2327499
Hospice care 550.67 64.80 123 13283 539 2344140
Adverse event 484.09 64.80 193 13213 7466 2337213
Blood parathyroid hormone abnormal 463.88 64.80 82 13324 53 2344626
Vomiting 454.12 64.80 404 13002 71198 2273481
Death 378.07 64.80 387 13019 81081 2263598
Hypophagia 343.08 64.80 126 13280 3874 2340805
Blood calcium decreased 330.56 64.80 105 13301 2053 2342626
Blood parathyroid hormone decreased 320.32 64.80 65 13341 157 2344522
Hypocalcaemia 298.91 64.80 113 13293 3770 2340909
Living in residential institution 270.98 64.80 55 13351 133 2344546
Abdominal pain upper 266.76 64.80 183 13223 21917 2322762
Rehabilitation therapy 264.66 64.80 59 13347 255 2344424
Blood calcium increased 264.55 64.80 78 13328 1173 2343506
Diarrhoea 183.80 64.80 273 13133 83291 2261388
Blood calcium abnormal 177.85 64.80 41 13365 212 2344467
Transplant 170.73 64.80 42 13364 299 2344380
Gastrointestinal disorder 149.80 64.80 91 13315 8826 2335853
Parathyroidectomy 146.23 64.80 30 13376 78 2344601
Hypercalcaemia 145.28 64.80 60 13346 2532 2342147
Renal transplant 123.45 64.80 32 13374 288 2344391
Dysphagia 117.69 64.80 90 13316 12715 2331964
Unevaluable investigation 116.77 64.80 21 13385 17 2344662
Mastication disorder 104.21 64.80 30 13376 412 2344267
Unevaluable event 103.26 64.80 72 13334 8819 2335860
Surgery 99.44 64.80 59 13347 5476 2339203
Arteriovenous fistula site complication 98.18 64.80 23 13383 129 2344550
Off label use 91.23 64.80 187 13219 73411 2271268
Blood phosphorus increased 90.32 64.80 26 13380 357 2344322
Gastric disorder 86.76 64.80 47 13359 3663 2341016
Cerebrovascular accident 85.99 64.80 92 13314 20094 2324585
Gastrointestinal tube insertion 85.08 64.80 24 13382 305 2344374
Muscle spasms 77.60 64.80 90 13316 21476 2323203
Constipation 77.39 64.80 90 13316 21539 2323140
Blood phosphorus abnormal 73.96 64.80 15 13391 36 2344643
Calciphylaxis 68.96 64.80 22 13384 435 2344244
Dizziness 65.57 64.80 143 13263 58522 2286157
Parathyroid tumour benign 65.47 64.80 17 13389 154 2344525

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 10304.49 75.19 2707 8951 19733 1715390
Hospitalisation 8165.90 75.19 2018 9640 10682 1724441
Laboratory test abnormal 7398.64 75.19 1536 10122 2823 1732300
Adverse drug reaction 1554.77 75.19 449 11209 4289 1730834
Intentional product misuse 1149.75 75.19 396 11262 6962 1728161
Blood parathyroid hormone increased 684.44 75.19 141 11517 221 1734902
Nausea 487.22 75.19 425 11233 50771 1684352
Blood parathyroid hormone abnormal 442.24 75.19 79 11579 17 1735106
Vomiting 371.48 75.19 322 11336 37993 1697130
Hospice care 338.02 75.19 87 11571 503 1734620
Abdominal discomfort 330.38 75.19 174 11484 8907 1726216
Adverse event 302.55 75.19 133 11525 4535 1730588
Malaise 285.10 75.19 248 11410 29317 1705806
Hypophagia 260.61 75.19 110 11548 3387 1731736
Blood parathyroid hormone decreased 221.61 75.19 46 11612 76 1735047
Blood calcium increased 219.78 75.19 63 11595 574 1734549
Decreased appetite 217.37 75.19 194 11464 23677 1711446
Transplant 216.01 75.19 55 11603 302 1734821
Death 213.21 75.19 364 11294 87079 1648044
Blood calcium decreased 206.04 75.19 72 11586 1305 1733818
Abdominal pain upper 195.60 75.19 133 11525 10868 1724255
Hypocalcaemia 191.80 75.19 86 11572 3070 1732053
Living in residential institution 180.83 75.19 39 11619 85 1735038
Parathyroidectomy 168.26 75.19 33 11625 33 1735090
Blood calcium abnormal 163.09 75.19 37 11621 111 1735012
Rehabilitation therapy 155.48 75.19 37 11621 145 1734978
Blood phosphorus increased 153.84 75.19 43 11615 354 1734769
Arteriovenous fistula site complication 130.38 75.19 33 11625 176 1734947
Unevaluable event 106.90 75.19 73 11585 5993 1729130
Renal transplant 103.73 75.19 32 11626 383 1734740
Surgery 101.48 75.19 54 11604 2809 1732314
Gastrointestinal disorder 100.32 75.19 64 11594 4684 1730439
Hypercalcaemia 94.57 75.19 45 11613 1841 1733282
Unevaluable investigation 93.33 75.19 18 11640 15 1735108
Diarrhoea 90.55 75.19 192 11466 53660 1681463
Muscle spasms 81.71 75.19 82 11576 11539 1723584
Constipation 75.96 75.19 89 11569 14911 1720212

Pharmacologic Action:

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

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 0378-6195 TABLET, FILM COATED 90 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 0378-6196 TABLET, FILM COATED 60 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 0378-6197 TABLET, FILM COATED 30 mg ORAL ANDA 16 sections
Cinacalcet Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2416 TABLET, FILM COATED 30 mg ORAL ANDA 17 sections
Cinacalcet Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2417 TABLET, FILM COATED 60 mg ORAL ANDA 17 sections
Cinacalcet Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0591-2418 TABLET, FILM COATED 90 mg ORAL ANDA 17 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 16714-078 TABLET, FILM COATED 30 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 16714-079 TABLET, FILM COATED 60 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 16714-080 TABLET, FILM COATED 90 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 47335-379 TABLET, FILM COATED 30 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 47335-380 TABLET, FILM COATED 60 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 47335-600 TABLET, FILM COATED 90 mg ORAL ANDA 16 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 50090-3529 TABLET, COATED 30 mg ORAL NDA 17 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 50090-4470 TABLET, COATED 30 mg ORAL NDA 17 sections
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 55513-073 TABLET, COATED 30 mg ORAL NDA 16 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-074 TABLET, COATED 60 mg ORAL NDA 16 sections
Sensipar HUMAN PRESCRIPTION DRUG LABEL 1 55513-075 TABLET, COATED 90 mg ORAL NDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 60687-525 TABLET, FILM COATED 30 mg ORAL ANDA 17 sections
Cinacalcet Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 64380-883 TABLET, FILM COATED 30 mg ORAL ANDA 16 sections
Cinacalcet Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 64380-884 TABLET, FILM COATED 60 mg ORAL ANDA 16 sections
Cinacalcet Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 64380-885 TABLET, FILM COATED 90 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 65862-831 TABLET, FILM COATED 30 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 65862-832 TABLET, FILM COATED 60 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 65862-833 TABLET, FILM COATED 90 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 67877-503 TABLET, FILM COATED 30 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 67877-504 TABLET, FILM COATED 60 mg ORAL ANDA 16 sections
Cinacalcet HUMAN PRESCRIPTION DRUG LABEL 1 67877-505 TABLET, FILM COATED 90 mg ORAL ANDA 16 sections