Identification

Name
Cinacalcet
Accession Number
DB01012  (APRD00872)
Type
Small Molecule
Groups
Approved
Description

Cinacalcet (INN) is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues) by allosteric activation of the calcium-sensing receptor that is expressed in various human organ tissues. It is sold by Amgen under the trade name Sensipar® in North America and Australia and as Mimpara® in Europe. Cinacalcet is used to treat hyperparathyroidism (elevated parathyroid hormone levels), a consequence of parathyroid tumors and chronic renal failure.

Structure
Thumb
Synonyms
  • (R)-alpha-Methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethane amine
  • CNC
  • Mimpara
  • N-((1R)-1-(Naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine
External IDs
AMG 073 / AMG-073 / AMG073 / KRN-1493 / KRN1493
Product Ingredients
IngredientUNIICASInChI Key
Cinacalcet hydrochloride1K860WSG25364782-34-3QANQWUQOEJZMLL-PKLMIRHRSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CinacalcetTablet90 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
CinacalcetTablet60 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
CinacalcetTablet30 mgOralJubilant Generics LimitedNot applicableNot applicableCanada
Sandoz CinacalcetTablet30 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz CinacalcetTablet90 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz CinacalcetTablet60 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
SensiparTablet, coated30 mg/1OralAvera McKennan Hospital2015-03-172018-06-08Us69189 073020180907 15195 1ow1d6z
SensiparTablet, coated60 mg/1OralCardinal Health2004-04-042018-05-25Us
SensiparTablet30 mgOralAmgen2004-09-16Not applicableCanada
SensiparTablet, coated30 mg/1OralPhysicians Total Care, Inc.2010-03-02Not applicableUs54868 561620180907 15195 1582sku
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-cinacalcetTablet30 mgOralApotex Corporation2016-05-20Not applicableCanada
Apo-cinacalcetTablet90 mgOralApotex Corporation2016-05-20Not applicableCanada
Apo-cinacalcetTablet60 mgOralApotex Corporation2016-05-20Not applicableCanada
CinacalcetTablet, film coated60 mg/1OralCadila Healthcare Limited2018-09-13Not applicableUs
CinacalcetTablet90 mg/1OralCipla Limited2018-03-08Not applicableUs
CinacalcetTablet, film coated30 mg/1OralZydus Pharmaceuticals (USA) Inc.2018-09-13Not applicableUs
CinacalcetTablet, film coated30 mg/1OralCadila Healthcare Limited2018-09-13Not applicableUs
CinacalcetTablet60 mg/1OralCipla Limited2018-03-08Not applicableUs
CinacalcetTablet, film coated90 mg/1OralZydus Pharmaceuticals (USA) Inc.2018-09-13Not applicableUs
CinacalcetTablet, film coated90 mg/1OralCadila Healthcare Limited2018-09-13Not applicableUs
Categories
UNII
UAZ6V7728S
CAS number
226256-56-0
Weight
Average: 357.412
Monoisotopic: 357.170434324
Chemical Formula
C22H22F3N
InChI Key
VDHAWDNDOKGFTD-MRXNPFEDSA-N
InChI
InChI=1S/C22H22F3N/c1-16(20-13-5-10-18-9-2-3-12-21(18)20)26-14-6-8-17-7-4-11-19(15-17)22(23,24)25/h2-5,7,9-13,15-16,26H,6,8,14H2,1H3/t16-/m1/s1
IUPAC Name
[(1R)-1-(naphthalen-1-yl)ethyl]({3-[3-(trifluoromethyl)phenyl]propyl})amine
SMILES
C[C@@H](NCCCC1=CC(=CC=C1)C(F)(F)F)C1=CC=CC2=CC=CC=C12

Pharmacology

Indication

For the treatment of secondary hyperparathyroidism in patients with Chronic Kidney Disease who are on hemodialysis or peritoneal dialysis. Also for the treatment of hypercalcemia in patients with parathyroid carcinoma.

Associated Conditions
Pharmacodynamics

Cinacalcet is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues). Secondary hyperparathyroidism (HPT) in patients with chronic kidney disease (CKD) is a progressive disease, associated with increases in parathyroid hormone (PTH) levels and derangements in calcium and phosphorus metabolism. Increased PTH stimulates osteoclastic activity resulting in cortical bone resorption and marrow fibrosis. The goals of treatment of secondary hyperparathyroidism are to lower levels of PTH, calcium, and phosphorus in the blood, in order to prevent progressive bone disease and the systemic consequences of disordered mineral metabolism. In CKD patients on dialysis with uncontrolled secondary HPT, reductions in PTH are associated with a favorable impact on bone-specific alkaline phosphatase (BALP), bone turnover and bone fibrosis. Cinacalcet reduces calcium levels by increasing the sensitivity of the calcium sensing receptor to extracellular calcium.

Mechanism of action

The calcium-sensing receptors on the surface of the chief cell of the parathyroid gland is the principal regulator of parathyroid hormone secretion (PTH). Cinacalcet directly lowers parathyroid hormone levels by increasing the sensitivity of the calcium sensing receptors to activation by extracellular calcium, resulting in the inhibition of PTH secretion. The reduction in PTH is associated with a concomitant decrease in serum calcium levels.

TargetActionsOrganism
AExtracellular calcium-sensing receptor
agonist
Human
Absorption

Rapidly absorbed following oral administration.

Volume of distribution
  • 1000 L
Protein binding

Approximately 93 to 97% bound to plasma proteins.

Metabolism

Metabolism is hepatic by multiple enzymes, primarily CYP3A4, CYP2D6, and CYP1A2. After administration of a 75 mg radiolabeled dose to healthy volunteers, cinacalcet was rapidly and extensively metabolized via: 1) oxidative N-dealkylation to hydrocinnamic acid and hydroxy-hydrocinnamic acid, which are further metabolized via ß-oxidation and glycine conjugation; the oxidative N-dealkylation process also generates metabolites that contain the naphthalene ring; and 2) oxidation of the naphthalene ring on the parent drug to form dihydrodiols, which are further conjugated with glucuronic acid.

Route of elimination

Cinacalcet is metabolized by multiple enzymes, primarily CYP3A4, CYP2D6 and CYP1A2. Renal excretion of metabolites was the primary route of elimination of radioactivity.

Half life

Terminal half-life is 30 to 40 hours. The mean half-life of cinacalcet is prolonged by 33% and 70% in patients with moderate and severe hepatic impairment, respectively.

Clearance
Not Available
Toxicity

Doses titrated up to 300 mg once daily have been safely administered to patients on dialysis. Overdosage of cinacalcet may lead to hypocalcemia.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Cinacalcet.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Cinacalcet.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Cinacalcet.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Cinacalcet.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Cinacalcet.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Cinacalcet.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Cinacalcet.
6-Deoxyerythronolide BThe metabolism of Cinacalcet can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe serum concentration of 6-O-benzylguanine can be increased when it is combined with Cinacalcet.
7-DeazaguanineThe serum concentration of 7-Deazaguanine can be increased when it is combined with Cinacalcet.
Food Interactions
  • Food markedly increases product bioavailability.
  • Peak levels and area under curve (drug exposure) are increased (82% and 68% respectively) when product is taken with a lipid-rich meal.
  • Take with food or soon after a meal.

References

Synthesis Reference

Revital Lifshitz-Liron, "Process for the preparation of cinacalcet base." U.S. Patent US20070259964, issued November 08, 2007.

US20070259964
General References
  1. Torres PU: Cinacalcet HCl: a novel treatment for secondary hyperparathyroidism caused by chronic kidney disease. J Ren Nutr. 2006 Jul;16(3):253-8. [PubMed:16825031]
  2. Padhi D, Harris R: Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride. Clin Pharmacokinet. 2009;48(5):303-11. doi: 10.2165/00003088-200948050-00002. [PubMed:19566113]
  3. Dong BJ: Cinacalcet: An oral calcimimetic agent for the management of hyperparathyroidism. Clin Ther. 2005 Nov;27(11):1725-51. [PubMed:16368445]
External Links
Human Metabolome Database
HMDB0015147
PubChem Compound
156419
PubChem Substance
46506315
ChemSpider
137743
BindingDB
50416875
ChEBI
48390
ChEMBL
CHEMBL1201284
Therapeutic Targets Database
DAP000256
PharmGKB
PA164776671
IUPHAR
3308
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cinacalcet
ATC Codes
H05BX01 — Cinacalcet
AHFS Codes
  • 92:92.00 — Other Miscellaneous Therapeutic Agents
FDA label
Download (278 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary1
1CompletedTreatmentHealthy Volunteers1
1Unknown StatusTreatmentHypophosphatemic Rickets, X-Linked Dominant1
2CompletedBasic ScienceMemory Functions1
2CompletedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer1
2CompletedTreatmentEnd Stage Renal Disease (ESRD)3
2CompletedTreatmentHyperparathyroidism, Secondary3
2CompletedTreatmentHyperparathyroidism, Secondary / Renal Insufficiency,Chronic1
2CompletedTreatmentPrimary Hyperparathyroidism2
2CompletedTreatmentRenal Osteodystrophy1
2TerminatedTreatmentChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary1
2, 3CompletedTreatmentHyperparathyroidism, Secondary1
2, 3RecruitingTreatmentPrimary Hyperparathyroidism1
2, 3Unknown StatusTreatmentHyperparathyroidism, Secondary1
3CompletedTreatmentChronic Allograft Nephropathy (CAN) / Chronic Kidney Disease (CKD) / Chronic Renal Failure (CRF) / Disordered Mineral Metabolism / End Stage Renal Disease (ESRD) / Hyperparathyroidism / Hypophosphatemia / Kidney Diseases / Post Renal Transplantation / Transplantation, Kidney1
3CompletedTreatmentChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary2
3CompletedTreatmentChronic Kidney Disease (CKD) / Kidney Diseases1
3CompletedTreatmentEnd Stage Renal Disease (ESRD) / Hyperparathyroidism, Secondary3
3CompletedTreatmentHypercalcemia / Parathyroid Carcinoma / Primary Hyperparathyroidism1
3CompletedTreatmentHypercalcemia / Primary Hyperparathyroidism1
3CompletedTreatmentHyperparathyroidism1
3CompletedTreatmentSecondary Hyperparathyroidism, Chronic Kidney Disease1
3Enrolling by InvitationTreatmentParathyroid Adenomas / Parathyroid Hyperplasia / Primary Hyperparathyroidism1
3RecruitingTreatmentChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary1
3TerminatedTreatmentChronic Kidney Disease (CKD) / Hyperparathyroidism / Hyperparathyroidism, Secondary / Kidney Diseases1
3TerminatedTreatmentChronic Kidney Disease, Secondary Hyperparathyroidism1
3TerminatedTreatmentChronic Renal Failure (CRF) / Hemodialysis Treatment1
4CompletedNot AvailableChronic Kidney Disease (CKD)1
4CompletedDiagnosticChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary / Kidney Diseases1
4CompletedDiagnosticParathyroid Hormone Suppression Test With Cinacalcet1
4CompletedTreatmentAnemias / Hyperparathyroidism, Secondary1
4CompletedTreatmentArterial Stiffness / Hyperparathyroidism1
4CompletedTreatmentCalcification / Calcifications, Vascular / Cardiovascular Disease (CVD) / Chronic Kidney Disease (CKD) / Chronic Renal Failure (CRF) / Coronary Artery Calcifications / End Stage Renal Disease (ESRD) / Hyperparathyroidism / Hyperparathyroidism, Secondary / Kidney Diseases / Nephrology1
4CompletedTreatmentChronic Kidney Disease (CKD) / Hemodialysis Treatment / Hyperparathyroidism, Secondary1
4CompletedTreatmentChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary1
4CompletedTreatmentEnd Stage Renal Disease (ESRD)1
4CompletedTreatmentHyperparathyroidism, Secondary4
4CompletedTreatmentHyperparathyroidism / Parathyroid Neoplasms1
4CompletedTreatmentOsteoporosis / Primary Hyperparathyroidism1
4RecruitingTreatmentHyperparathyroidism; Secondary, Renal1
4TerminatedTreatmentHyperparathyroidism, Secondary1
Not AvailableCompletedNot AvailableNephrology1
Not AvailableCompletedNot AvailablePrimary Hyperparathyroidism1
Not AvailableCompletedBasic ScienceRelationship Between Calcimimetic and the RAAS1
Not AvailableCompletedDiagnosticHealthy Volunteers1
Not AvailableRecruitingHealth Services ResearchPrimary Hyperparathyroidism1
Not AvailableRecruitingTreatmentChronic Renal Failure (CRF)1
Not AvailableRecruitingTreatmentHyperparathyroidism, Secondary / Renal Failure / Vascular Diseases1
Not AvailableUnknown StatusTreatmentFamilial Hypophosphatemic Rickets1
Not AvailableUnknown StatusTreatmentHypophosphatemia / Transplant, Kidney1
Not AvailableWithdrawnTreatmentHypercalcemia / Hyperparathyroidism, Secondary1

Pharmacoeconomics

Manufacturers
  • Amgen inc
Packagers
  • Amgen Inc.
  • Cardinal Health
  • Dept Health Central Pharmacy
  • Kaiser Foundation Hospital
  • Patheon Inc.
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
TabletOral30 mg/1
TabletOral60 mg/1
TabletOral90 mg/1
Tablet, film coatedOral30 mg/1
Tablet, film coatedOral60 mg/1
Tablet, film coatedOral90 mg/1
Tablet, film coatedOral30 mg
Tablet, film coatedOral60 mg
Tablet, film coatedOral90 mg
TabletOral30 mg
TabletOral60 mg
TabletOral90 mg
Tablet, coatedOral30 mg/1
Tablet, coatedOral60 mg/1
Tablet, coatedOral90 mg/1
Prices
Unit descriptionCostUnit
Sensipar 90 mg tablet44.03USD tablet
Sensipar 60 mg tablet29.35USD tablet
Sensipar 30 mg tablet14.69USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2202879No2005-08-302015-10-23Canada
US6031003No2000-02-292016-12-14Us
US6211244No2001-04-032015-10-23Us
US7829595No2010-11-092026-09-22Us
US6011068No2000-01-042018-03-08Us
US6313146No2001-11-062016-12-14Us
US9375405No2016-06-282026-09-22Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySlightly soluble (in HCl salt form)Not Available
logP6.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility5.59e-05 mg/mLALOGPS
logP5.57ALOGPS
logP6.27ChemAxon
logS-6.8ALOGPS
pKa (Strongest Basic)10.3ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area12.03 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity100.12 m3·mol-1ChemAxon
Polarizability37.9 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9927
Caco-2 permeable+0.7058
P-glycoprotein substrateSubstrate0.5309
P-glycoprotein inhibitor IInhibitor0.8512
P-glycoprotein inhibitor IIInhibitor0.6937
Renal organic cation transporterInhibitor0.5305
CYP450 2C9 substrateNon-substrate0.7761
CYP450 2D6 substrateSubstrate0.8293
CYP450 3A4 substrateNon-substrate0.5425
CYP450 1A2 substrateInhibitor0.9206
CYP450 2C9 inhibitorNon-inhibitor0.8572
CYP450 2D6 inhibitorInhibitor0.8188
CYP450 2C19 inhibitorInhibitor0.8795
CYP450 3A4 inhibitorInhibitor0.7166
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5904
Ames testNon AMES toxic0.5152
CarcinogenicityNon-carcinogens0.8785
BiodegradationNot ready biodegradable0.9932
Rat acute toxicity2.8511 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9175
hERG inhibition (predictor II)Inhibitor0.8494
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as naphthalenes. These are compounds containing a naphthalene moiety, which consists of two fused benzene rings.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Naphthalenes
Sub Class
Not Available
Direct Parent
Naphthalenes
Alternative Parents
Trifluoromethylbenzenes / Phenylpropylamines / Aralkylamines / Dialkylamines / Organopnictogen compounds / Organofluorides / Hydrocarbon derivatives / Alkyl fluorides
Substituents
Naphthalene / Phenylpropylamine / Trifluoromethylbenzene / Aralkylamine / Monocyclic benzene moiety / Secondary amine / Secondary aliphatic amine / Organopnictogen compound / Organonitrogen compound / Organofluoride
Molecular Framework
Aromatic homopolycyclic compounds
External Descriptors
secondary amino compound, naphthalenes, (trifluoromethyl)benzenes (CHEBI:48390)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
Senses changes in the extracellular concentration of calcium ions. The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system.
Gene Name
CASR
Uniprot ID
P41180
Uniprot Name
Extracellular calcium-sensing receptor
Molecular Weight
120672.385 Da
References
  1. de Francisco AL: Cinacalcet HCl: a novel therapeutic for hyperparathyroidism. Expert Opin Pharmacother. 2005 Mar;6(3):441-52. [PubMed:15794735]
  2. Rothe HM, Shapiro WB, Sun WY, Chou SY: Calcium-sensing receptor gene polymorphism Arg990Gly and its possible effect on response to cinacalcet HCl. Pharmacogenet Genomics. 2005 Jan;15(1):29-34. [PubMed:15864123]
  3. Tasic V: Management of renal osteodystrophy in children. Turk J Pediatr. 2005;47 Suppl:13-8. [PubMed:15884662]
  4. Moe SM, Cunningham J, Bommer J, Adler S, Rosansky SJ, Urena-Torres P, Albizem MB, Guo MD, Zani VJ, Goodman WG, Sprague SM: Long-term treatment of secondary hyperparathyroidism with the calcimimetic cinacalcet HCl. Nephrol Dial Transplant. 2005 Oct;20(10):2186-93. Epub 2005 Jul 19. [PubMed:16030053]
  5. Cunningham J: Management of secondary hyperparathyroidism. Ther Apher Dial. 2005 Aug;9 Suppl 1:S35-40. [PubMed:16109140]
  6. Eriguchi R, Umakoshi J, Tominaga Y, Sato Y: Successful treatment of inoperable recurrent secondary hyperparathyroidism with cinacalcet HCl. NDT Plus. 2008 Aug;1(4):218-220. Epub 2008 May 25. [PubMed:19461861]
  7. Belozeroff V, Goodman WG, Ren L, Kalantar-Zadeh K: Cinacalcet lowers serum alkaline phosphatase in maintenance hemodialysis patients. Clin J Am Soc Nephrol. 2009 Mar;4(3):673-9. doi: 10.2215/CJN.03790808. Epub 2009 Mar 4. [PubMed:19261825]
  8. Meola M, Petrucci I, Barsotti G: Long-term treatment with cinacalcet and conventional therapy reduces parathyroid hyperplasia in severe secondary hyperparathyroidism. Nephrol Dial Transplant. 2009 Mar;24(3):982-9. doi: 10.1093/ndt/gfn654. Epub 2009 Jan 30. [PubMed:19181759]
  9. Drueke TB, Ritz E: Treatment of secondary hyperparathyroidism in CKD patients with cinacalcet and/or vitamin D derivatives. Clin J Am Soc Nephrol. 2009 Jan;4(1):234-41. doi: 10.2215/CJN.04520908. Epub 2008 Dec 3. [PubMed:19056615]
  10. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Padhi D, Harris R: Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride. Clin Pharmacokinet. 2009;48(5):303-11. doi: 10.2165/00003088-200948050-00002. [PubMed:19566113]
  2. Dong BJ: Cinacalcet: An oral calcimimetic agent for the management of hyperparathyroidism. Clin Ther. 2005 Nov;27(11):1725-51. [PubMed:16368445]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Padhi D, Harris R: Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride. Clin Pharmacokinet. 2009;48(5):303-11. doi: 10.2165/00003088-200948050-00002. [PubMed:19566113]
  2. Dong BJ: Cinacalcet: An oral calcimimetic agent for the management of hyperparathyroidism. Clin Ther. 2005 Nov;27(11):1725-51. [PubMed:16368445]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Padhi D, Harris R: Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride. Clin Pharmacokinet. 2009;48(5):303-11. doi: 10.2165/00003088-200948050-00002. [PubMed:19566113]
  2. Dong BJ: Cinacalcet: An oral calcimimetic agent for the management of hyperparathyroidism. Clin Ther. 2005 Nov;27(11):1725-51. [PubMed:16368445]
  3. Poon G: Cinacalcet hydrochloride (Sensipar). Proc (Bayl Univ Med Cent). 2005 Apr;18(2):181-4. [PubMed:16200170]
  4. Cinacalcet FDA label [File]

Drug created on June 13, 2005 07:24 / Updated on November 17, 2018 07:15