Scroll

cinacalcet 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
calcium-sensing receptors (CaSR) agonists	647	226256-56-0

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
60	mg	O

ADMET properties:

Show entries

Search:

Property	Value	Reference
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
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	19.90 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	18.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	17.60 L/kg	Lombardo F, Berellini G, Obach RS
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
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS

Showing 1 to 9 of 9 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
March 8, 2004	FDA	AMGEN
Oct. 22, 2004	EMA

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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	8449.97	21.13	2562	25060	82519	63378881
Product dose omission issue	6762.93	21.13	2814	24808	231499	63229901
Laboratory test abnormal	6192.07	21.13	1573	26049	25339	63436061
Adverse drug reaction	1182.65	21.13	611	27011	79103	63382297
Blood parathyroid hormone increased	886.97	21.13	216	27406	2822	63458578
Intentional product misuse	862.72	21.13	453	27169	60464	63400936
Blood parathyroid hormone abnormal	487.79	21.13	85	27537	147	63461253
Arteriovenous fistula site complication	332.69	21.13	70	27552	443	63460957
Hospice care	323.84	21.13	124	27498	7808	63453592
Hypocalcaemia	273.69	21.13	171	27451	31542	63429858

Showing 1 to 10 of 132 entries

Previous1 2 3 4 5…14Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

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 issue	7274.77	21.73	2732	19631	116979	34817589
Hospitalisation	6662.80	21.73	2127	20236	54775	34879793
Laboratory test abnormal	5869.17	21.73	1539	20824	18852	34915716
Adverse drug reaction	1025.01	21.73	457	21906	28885	34905683
Intentional product misuse	676.85	21.73	399	21964	45212	34889356
Blood parathyroid hormone increased	658.68	21.73	160	22203	1354	34933214
Blood parathyroid hormone abnormal	485.57	21.73	85	22278	77	34934491
Arteriovenous fistula site complication	378.87	21.73	82	22281	385	34934183
Hypocalcaemia	217.49	21.73	155	22208	24134	34910434
Adverse event	210.60	21.73	138	22225	18739	34915829

Showing 1 to 10 of 94 entries

Previous1 2 3 4 5…10Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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
Laboratory test abnormal	9734.53	16.78	2293	33407	25755	79682933
Hospitalisation	5877.21	16.78	2016	33684	92220	79616468
Product dose omission issue	3036.05	16.78	1681	34019	245856	79462832
Blood parathyroid hormone increased	1060.23	16.78	257	35443	3188	79705500
Blood parathyroid hormone abnormal	761.85	16.78	134	35566	241	79708447
Arteriovenous fistula site complication	730.40	16.78	151	35549	838	79707850
Adverse drug reaction	483.32	16.78	325	35375	66067	79642621
Nausea	475.87	16.78	1203	34497	955993	78752695
Vomiting	376.65	16.78	881	34819	664947	79043741
Decreased appetite	349.00	16.78	581	35119	341837	79366851

Showing 1 to 10 of 183 entries

Previous1 2 3 4 5…19Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	H05BX01	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS CALCIUM HOMEOSTASIS ANTI-PARATHYROID AGENTS Other anti-parathyroid agents
CHEBI has role	CHEBI:48525	calcimimetics
CHEBI has role	CHEBI:50183	P450 inhibitors
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

Showing 1 to 8 of 8 entries

Previous1Next

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

Show entries

Search:

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

Showing 1 to 10 of 10 entries

Previous1Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Show entries

Search:

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

Showing 1 to 3 of 3 entries

Previous1Next

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Extracellular calcium-sensing receptor	GPCR	P41180	CASR_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	7.70	CHEMBL	CHEMBL
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	7.30	CHEMBL
Glycine receptor subunit alpha-1	Ion channel	P23415	GLRA1_HUMAN		EC50	6.49	CHEMBL
Metabotropic glutamate receptor 5	GPCR		GRM5_RAT	ALLOSTERIC MODULATOR	Ki	4.35	IUPHAR

Showing 1 to 4 of 4 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
008595	NDDF
008596	NDDF
156419	PUBCHEM_CID
18133	MMSL
303128	MMSL
3308	IUPHAR_LIGAND_ID
364782-34-3	SECONDARY_CAS_RN
384379	RXNORM
4021430	VUID
4021430	VANDF

Showing 1 to 10 of 26 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cinacalcet	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7067	TABLET, FILM COATED	30 mg	ORAL	ANDA	25 sections
Cinacalcet	Human Prescription Drug Label	1	16714-078	TABLET, FILM COATED	30 mg	ORAL	ANDA	27 sections
Cinacalcet	Human Prescription Drug Label	1	16714-078	TABLET, FILM COATED	30 mg	ORAL	ANDA	27 sections
Cinacalcet	Human Prescription Drug Label	1	16714-079	TABLET, FILM COATED	60 mg	ORAL	ANDA	27 sections
Cinacalcet	Human Prescription Drug Label	1	16714-079	TABLET, FILM COATED	60 mg	ORAL	ANDA	27 sections
Cinacalcet	Human Prescription Drug Label	1	16714-080	TABLET, FILM COATED	90 mg	ORAL	ANDA	27 sections
Cinacalcet	Human Prescription Drug Label	1	16714-080	TABLET, FILM COATED	90 mg	ORAL	ANDA	27 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	16729-442	TABLET, FILM COATED	90 mg	ORAL	ANDA	25 sections

Showing 1 to 10 of 30 entries

Previous1 2 3Next