cinacalcet Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 647 | 226256-56-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 60 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 22, 2004 | EMA | ||
| March 8, 2004 | FDA | AMGEN |
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 |
|---|---|---|---|---|---|---|
| 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 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 |
|---|---|---|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| 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)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.69 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |