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Identification
NameCinacalcet
Accession NumberDB01012  (APRD00872)
TypeSmall Molecule
GroupsApproved
DescriptionCinacalcet (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 Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mylan-cinacalcetTablet30 mgOralMylan Pharmaceuticals Ulc2016-06-29Not applicableCanada
Mylan-cinacalcetTablet60 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-cinacalcetTablet90 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Sandoz CinacalcetTablet30 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz CinacalcetTablet60 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz CinacalcetTablet90 mgOralSandoz Canada IncorporatedNot applicableNot applicableCanada
SensiparTablet, coated60 mg/1OralAmgen Inc2004-04-04Not applicableUs
SensiparTablet, coated30 mg/1OralREMEDYREPACK INC.2013-04-012016-10-13Us
SensiparTablet90 mgOralAmgen Canada Inc2004-09-16Not applicableCanada
SensiparTablet, coated30 mg/1OralCarilion Materials Management2004-04-04Not applicableUs
SensiparTablet, coated30 mg/1OralCardinal Health2004-04-04Not applicableUs
SensiparTablet, coated90 mg/1OralAmgen Inc2004-04-04Not applicableUs
SensiparTablet, coated30 mg/1OralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
SensiparTablet, coated60 mg/1OralCardinal Health2004-04-04Not applicableUs
SensiparTablet30 mgOralAmgen Canada Inc2004-09-16Not applicableCanada
SensiparTablet, coated60 mg/1OralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
SensiparTablet, coated30 mg/1OralAmgen Inc2004-04-04Not applicableUs
SensiparTablet60 mgOralAmgen Canada Inc2004-09-16Not applicableCanada
SensiparTablet, coated30 mg/1OralPhysicians Total Care, Inc.2010-03-02Not applicableUs
SensiparTablet, coated30 mg/1OralAvera Mc Kennan Hospital2015-03-17Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-cinacalcetTablet30 mgOralApotex Inc2016-05-20Not applicableCanada
Apo-cinacalcetTablet60 mgOralApotex Inc2016-05-20Not applicableCanada
Apo-cinacalcetTablet90 mgOralApotex Inc2016-05-20Not applicableCanada
Cinacalcet MylanTablet, film coated60 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated90 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated30 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated60 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated90 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated30 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated60 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated30 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated90 mgOralMylan S.A.S.2015-11-19Not applicableEu
Cinacalcet MylanTablet, film coated30 mgOralMylan S.A.S.2015-11-19Not applicableEu
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Cinacalcet hydrochloride
ThumbNot applicableDBSALT001463
Categories
UNIIUAZ6V7728S
CAS number226256-56-0
WeightAverage: 357.412
Monoisotopic: 357.170434324
Chemical FormulaC22H22F3N
InChI KeyVDHAWDNDOKGFTD-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
IndicationFor 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.
Structured Indications
PharmacodynamicsCinacalcet 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 actionThe 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Extracellular calcium-sensing receptorProteinyes
agonist
HumanP41180 details
Related Articles
AbsorptionRapidly absorbed following oral administration.
Volume of distribution
  • 1000 L
Protein bindingApproximately 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.

SubstrateEnzymesProduct
Cinacalcet
Not Available
Hydrocinnamic acidDetails
Cinacalcet
Not Available
hydroxy-hydrocinnamic acidDetails
Route of eliminationCinacalcet is metabolized by multiple enzymes, primarily CYP3A4, CYP2D6 and CYP1A2. Renal excretion of metabolites was the primary route of elimination of radioactivity.
Half lifeTerminal 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.
ClearanceNot Available
ToxicityDoses 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Cinacalcet.Experimental, Illicit
AbirateroneThe serum concentration of Cinacalcet can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Cinacalcet.Approved
AcetylcholineThe metabolism of Acetylcholine can be decreased when combined with Cinacalcet.Approved
AjmalineThe metabolism of Ajmaline can be decreased when combined with Cinacalcet.Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Cinacalcet.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Cinacalcet.Approved
AlprenololThe metabolism of Alprenolol can be decreased when combined with Cinacalcet.Approved, Withdrawn
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Cinacalcet.Illicit, Withdrawn
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Cinacalcet.Approved, Withdrawn
AmiodaroneThe metabolism of Cinacalcet can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Cinacalcet.Approved
AmoxapineThe metabolism of Amoxapine can be decreased when combined with Cinacalcet.Approved
AmphetamineThe metabolism of Amphetamine can be decreased when combined with Cinacalcet.Approved, Illicit
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Cinacalcet.Approved
AmsacrineThe metabolism of Amsacrine can be decreased when combined with Cinacalcet.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Cinacalcet.Approved
AprepitantThe serum concentration of Cinacalcet can be increased when it is combined with Aprepitant.Approved, Investigational
AprindineThe metabolism of Aprindine can be decreased when combined with Cinacalcet.Approved
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Cinacalcet.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Cinacalcet.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Cinacalcet.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Cinacalcet.Approved, Withdrawn
AtazanavirThe metabolism of Cinacalcet can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Atomoxetine can be increased when it is combined with Cinacalcet.Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Cinacalcet.Approved
AzithromycinThe metabolism of Cinacalcet can be decreased when combined with Azithromycin.Approved
BenzatropineThe metabolism of Benzatropine can be decreased when combined with Cinacalcet.Approved
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Cinacalcet.Approved
BepridilThe metabolism of Bepridil can be decreased when combined with Cinacalcet.Approved, Withdrawn
BetaxololThe metabolism of Betaxolol can be decreased when combined with Cinacalcet.Approved
BexaroteneThe serum concentration of Cinacalcet can be decreased when it is combined with Bexarotene.Approved, Investigational
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Cinacalcet.Approved
BoceprevirThe metabolism of Cinacalcet can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Bortezomib can be decreased when combined with Cinacalcet.Approved, Investigational
BosentanThe serum concentration of Cinacalcet can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Cinacalcet.Approved
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Cinacalcet.Approved
BufuralolThe metabolism of Bufuralol can be decreased when combined with Cinacalcet.Experimental, Investigational
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Cinacalcet.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Cinacalcet.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Cinacalcet.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Cinacalcet.Approved, Investigational
CaffeineThe metabolism of Caffeine can be decreased when combined with Cinacalcet.Approved
CaptoprilThe metabolism of Captopril can be decreased when combined with Cinacalcet.Approved
CarbamazepineThe metabolism of Cinacalcet can be increased when combined with Carbamazepine.Approved, Investigational
CariprazineThe metabolism of Cariprazine can be decreased when combined with Cinacalcet.Approved
CarteololThe metabolism of Carteolol can be decreased when combined with Cinacalcet.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Cinacalcet.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Cinacalcet.Approved, Vet Approved
CeritinibThe serum concentration of Cinacalcet can be increased when it is combined with Ceritinib.Approved
CevimelineThe metabolism of Cevimeline can be decreased when combined with Cinacalcet.Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Cinacalcet.Approved, Illicit
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Cinacalcet.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Cinacalcet.Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Cinacalcet.Approved, Vet Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Cinacalcet.Approved
CilostazolThe metabolism of Cilostazol can be decreased when combined with Cinacalcet.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Cinacalcet.Approved
CitalopramThe metabolism of Citalopram can be decreased when combined with Cinacalcet.Approved
ClarithromycinThe metabolism of Cinacalcet can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Cinacalcet can be decreased when combined with Clemastine.Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Cinacalcet.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Cinacalcet.Approved, Vet Approved
ClonidineThe metabolism of Clonidine can be decreased when combined with Cinacalcet.Approved
ClotrimazoleThe metabolism of Cinacalcet can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Cinacalcet.Approved
CobicistatThe metabolism of Cinacalcet can be decreased when combined with Cobicistat.Approved
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Cinacalcet.Approved, Illicit
ConivaptanThe serum concentration of Cinacalcet can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Cinacalcet can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Cinacalcet.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Cinacalcet.Approved, Investigational
CyclosporineThe metabolism of Cinacalcet can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Cinacalcet can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Cinacalcet can be decreased when it is combined with Dabrafenib.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Cinacalcet.Approved
DarifenacinThe metabolism of Darifenacin can be decreased when combined with Cinacalcet.Approved, Investigational
DarunavirThe metabolism of Cinacalcet can be decreased when combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Cinacalcet.Approved
DasatinibThe serum concentration of Cinacalcet can be increased when it is combined with Dasatinib.Approved, Investigational
DebrisoquinThe metabolism of Debrisoquin can be decreased when combined with Cinacalcet.Approved
DeferasiroxThe serum concentration of Cinacalcet can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Delavirdine can be decreased when combined with Cinacalcet.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Cinacalcet.Approved
DexamethasoneThe serum concentration of Cinacalcet can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Cinacalcet.Approved, Illicit, Withdrawn
DexmethylphenidateThe metabolism of Dexmethylphenidate can be decreased when combined with Cinacalcet.Approved
DextroamphetamineThe metabolism of Dextroamphetamine can be decreased when combined with Cinacalcet.Approved, Illicit
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Cinacalcet.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Cinacalcet.Approved, Illicit
DihydroergotamineThe metabolism of Cinacalcet can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Cinacalcet.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Cinacalcet.Approved
DolasetronThe metabolism of Dolasetron can be decreased when combined with Cinacalcet.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Cinacalcet.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Cinacalcet.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Cinacalcet.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Cinacalcet.Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Cinacalcet.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Cinacalcet.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Cinacalcet.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Cinacalcet.Approved, Investigational
DoxycyclineThe metabolism of Cinacalcet can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Dronedarone can be decreased when combined with Cinacalcet.Approved
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Cinacalcet.Approved
EfavirenzThe serum concentration of Cinacalcet can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe metabolism of Eletriptan can be decreased when combined with Cinacalcet.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Cinacalcet.Approved
EncainideThe metabolism of Encainide can be decreased when combined with Cinacalcet.Approved, Withdrawn
EnclomipheneThe metabolism of Enclomiphene can be decreased when combined with Cinacalcet.Investigational
EnzalutamideThe serum concentration of Cinacalcet can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Cinacalcet.Approved, Investigational
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Cinacalcet.Approved, Investigational
ErythromycinThe metabolism of Cinacalcet can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Cinacalcet.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Cinacalcet can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Cinacalcet.Investigational
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Cinacalcet.Approved, Illicit
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Cinacalcet.Approved, Investigational
EtravirineThe serum concentration of Cinacalcet can be decreased when it is combined with Etravirine.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cinacalcet.Approved
FingolimodThe metabolism of Fingolimod can be decreased when combined with Cinacalcet.Approved, Investigational
FlecainideThe metabolism of Flecainide can be decreased when combined with Cinacalcet.Approved, Withdrawn
FluconazoleThe metabolism of Cinacalcet can be decreased when combined with Fluconazole.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Cinacalcet.Approved
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Cinacalcet.Approved, Vet Approved
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Cinacalcet.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Cinacalcet.Approved
FluvoxamineThe metabolism of Cinacalcet can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Cinacalcet.Approved, Investigational
FosamprenavirThe metabolism of Cinacalcet can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Cinacalcet can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Cinacalcet can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Cinacalcet can be increased when it is combined with Fusidic Acid.Approved
GalantamineThe metabolism of Galantamine can be decreased when combined with Cinacalcet.Approved
GefitinibThe metabolism of Gefitinib can be decreased when combined with Cinacalcet.Approved, Investigational
GranisetronThe metabolism of Granisetron can be decreased when combined with Cinacalcet.Approved, Investigational
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Cinacalcet.Approved
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Cinacalcet.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Cinacalcet.Approved, Vet Approved
HydrocodoneThe serum concentration of the active metabolites of Hydrocodone can be reduced when Hydrocodone is used in combination with Cinacalcet resulting in a loss in efficacy.Approved, Illicit
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Cinacalcet.Approved, Illicit
IbrutinibThe metabolism of Ibrutinib can be decreased when combined with Cinacalcet.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Cinacalcet.Approved
IdelalisibThe serum concentration of Cinacalcet can be increased when it is combined with Idelalisib.Approved
IloperidoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Cinacalcet.Approved
ImatinibThe metabolism of Imatinib can be decreased when combined with Cinacalcet.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Cinacalcet.Approved
IndinavirThe metabolism of Cinacalcet can be decreased when combined with Indinavir.Approved
Ipratropium bromideThe metabolism of Ipratropium bromide can be decreased when combined with Cinacalcet.Approved
IsavuconazoniumThe metabolism of Cinacalcet can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Cinacalcet can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Cinacalcet can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Cinacalcet can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Cinacalcet.Approved
KetoconazoleThe metabolism of Cinacalcet can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe metabolism of Labetalol can be decreased when combined with Cinacalcet.Approved
LevodopaThe metabolism of Levodopa can be decreased when combined with Cinacalcet.Approved
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Cinacalcet.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Cinacalcet.Approved, Vet Approved
LisurideThe metabolism of Lisuride can be decreased when combined with Cinacalcet.Approved
LomustineThe metabolism of Lomustine can be decreased when combined with Cinacalcet.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Cinacalcet.Approved
LopinavirThe metabolism of Cinacalcet can be decreased when combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Cinacalcet.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Cinacalcet.Approved
LovastatinThe metabolism of Cinacalcet can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Cinacalcet can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Cinacalcet can be increased when combined with Lumacaftor.Approved
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Cinacalcet.Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Cinacalcet.Investigational, Withdrawn
MequitazineThe serum concentration of Mequitazine can be increased when it is combined with Cinacalcet.Approved
MesoridazineThe metabolism of Mesoridazine can be decreased when combined with Cinacalcet.Approved
MethadoneThe metabolism of Methadone can be decreased when combined with Cinacalcet.Approved
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Cinacalcet.Approved, Illicit
MethotrimeprazineThe metabolism of Methotrimeprazine can be decreased when combined with Cinacalcet.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Cinacalcet.Approved, Vet Approved
MethylphenidateThe metabolism of Methylphenidate can be decreased when combined with Cinacalcet.Approved, Investigational
MethyprylonThe metabolism of Methyprylon can be decreased when combined with Cinacalcet.Approved, Illicit, Withdrawn
MetoclopramideThe metabolism of Metoclopramide can be decreased when combined with Cinacalcet.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Cinacalcet.Approved, Investigational
MexiletineThe metabolism of Cinacalcet can be decreased when combined with Mexiletine.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Cinacalcet.Approved
MifepristoneThe serum concentration of Cinacalcet can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe metabolism of Minaprine can be decreased when combined with Cinacalcet.Approved
MirabegronThe metabolism of Mirabegron can be decreased when combined with Cinacalcet.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Cinacalcet.Approved
MitotaneThe serum concentration of Cinacalcet can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Cinacalcet.Approved
ModafinilThe serum concentration of Cinacalcet can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe metabolism of Morphine can be decreased when combined with Cinacalcet.Approved, Investigational
NafcillinThe serum concentration of Cinacalcet can be decreased when it is combined with Nafcillin.Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Cinacalcet.Approved, Investigational
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Cinacalcet.Approved, Investigational
NefazodoneThe metabolism of Cinacalcet can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Cinacalcet can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Cinacalcet can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Cinacalcet can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Nicardipine can be decreased when combined with Cinacalcet.Approved
NicergolineThe metabolism of Nicergoline can be decreased when combined with Cinacalcet.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Cinacalcet.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Cinacalcet.Approved
NilotinibThe metabolism of Cinacalcet can be decreased when combined with Nilotinib.Approved, Investigational
NitrofuralThe metabolism of Nitrofural can be decreased when combined with Cinacalcet.Approved, Vet Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Cinacalcet.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Cinacalcet.Approved, Investigational
OlaparibThe metabolism of Cinacalcet can be decreased when combined with Olaparib.Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Cinacalcet.Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Cinacalcet.Investigational
OsimertinibThe serum concentration of Cinacalcet can be increased when it is combined with Osimertinib.Approved
OxycodoneThe metabolism of Oxycodone can be decreased when combined with Cinacalcet.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Cinacalcet.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Cinacalcet can be increased when it is combined with Palbociclib.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Cinacalcet.Approved, Investigational
ParoxetineThe metabolism of Paroxetine can be decreased when combined with Cinacalcet.Approved, Investigational
PazopanibThe metabolism of Pazopanib can be decreased when combined with Cinacalcet.Approved
Peginterferon alfa-2bThe serum concentration of Cinacalcet can be increased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Cinacalcet.Approved
PentobarbitalThe metabolism of Cinacalcet can be increased when combined with Pentobarbital.Approved, Vet Approved
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Cinacalcet.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Cinacalcet.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Cinacalcet.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Cinacalcet.Withdrawn
PhenforminThe metabolism of Phenformin can be decreased when combined with Cinacalcet.Approved, Withdrawn
PhenobarbitalThe metabolism of Cinacalcet can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Cinacalcet can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Cinacalcet.Approved
PindololThe metabolism of Pindolol can be decreased when combined with Cinacalcet.Approved
PiperazineThe metabolism of Piperazine can be decreased when combined with Cinacalcet.Approved, Vet Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Cinacalcet.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Cinacalcet.Approved
PosaconazoleThe metabolism of Cinacalcet can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Cinacalcet can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideThe metabolism of Procainamide can be decreased when combined with Cinacalcet.Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Cinacalcet.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Cinacalcet.Approved, Vet Approved
PromethazineThe metabolism of Promethazine can be decreased when combined with Cinacalcet.Approved
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Cinacalcet.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Cinacalcet.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Cinacalcet.Approved, Investigational
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Cinacalcet.Approved
PseudoephedrineThe metabolism of Pseudoephedrine can be decreased when combined with Cinacalcet.Approved
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Cinacalcet.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Cinacalcet.Approved
RanitidineThe metabolism of Ranitidine can be decreased when combined with Cinacalcet.Approved
RanolazineThe metabolism of Cinacalcet can be decreased when combined with Ranolazine.Approved, Investigational
RemoxiprideThe metabolism of Remoxipride can be decreased when combined with Cinacalcet.Approved, Withdrawn
repinotanThe metabolism of repinotan can be decreased when combined with Cinacalcet.Investigational
RifabutinThe metabolism of Cinacalcet can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Cinacalcet can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Cinacalcet can be increased when combined with Rifapentine.Approved
RisperidoneThe metabolism of Risperidone can be decreased when combined with Cinacalcet.Approved, Investigational
RitonavirThe metabolism of Cinacalcet can be decreased when combined with Ritonavir.Approved, Investigational
RopiniroleThe metabolism of Cinacalcet can be decreased when combined with Ropinirole.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Cinacalcet.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Cinacalcet.Approved
SaquinavirThe metabolism of Cinacalcet can be decreased when combined with Saquinavir.Approved, Investigational
SertindoleThe metabolism of Sertindole can be decreased when combined with Cinacalcet.Approved, Withdrawn
SertralineThe metabolism of Sertraline can be decreased when combined with Cinacalcet.Approved
SildenafilThe metabolism of Sildenafil can be decreased when combined with Cinacalcet.Approved, Investigational
SiltuximabThe serum concentration of Cinacalcet can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Cinacalcet can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Cinacalcet.Approved
SparteineThe metabolism of Sparteine can be decreased when combined with Cinacalcet.Experimental
St. John's WortThe serum concentration of Cinacalcet can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Cinacalcet can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Cinacalcet can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be decreased when it is combined with Cinacalcet.Approved, Investigational
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Cinacalcet resulting in a loss in efficacy.Approved
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Cinacalcet.Approved, Investigational
TapentadolThe metabolism of Tapentadol can be decreased when combined with Cinacalcet.Approved
TegaserodThe metabolism of Tegaserod can be decreased when combined with Cinacalcet.Investigational, Withdrawn
TelaprevirThe metabolism of Cinacalcet can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Cinacalcet can be decreased when combined with Telithromycin.Approved
TenofovirThe metabolism of Cinacalcet can be decreased when combined with Tenofovir.Approved, Investigational
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Cinacalcet.Withdrawn
TeriflunomideThe serum concentration of Cinacalcet can be decreased when it is combined with Teriflunomide.Approved
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Cinacalcet.Investigational
TetrabenazineThe serum concentration of Tetrabenazine can be increased when it is combined with Cinacalcet.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Cinacalcet.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Cinacalcet.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Cinacalcet.Approved
TiclopidineThe metabolism of Ticlopidine can be decreased when combined with Cinacalcet.Approved
TimololThe metabolism of Timolol can be decreased when combined with Cinacalcet.Approved
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Cinacalcet.Approved
TipranavirThe metabolism of Tipranavir can be decreased when combined with Cinacalcet.Approved, Investigational
TocilizumabThe serum concentration of Cinacalcet can be decreased when it is combined with Tocilizumab.Approved
TolterodineThe metabolism of Tolterodine can be decreased when combined with Cinacalcet.Approved, Investigational
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Cinacalcet.Approved, Investigational
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Cinacalcet.Approved, Investigational
TrazodoneThe metabolism of Trazodone can be decreased when combined with Cinacalcet.Approved, Investigational
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Cinacalcet.Approved
UmeclidiniumThe metabolism of Umeclidinium can be decreased when combined with Cinacalcet.Approved
VemurafenibThe serum concentration of Cinacalcet can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Venlafaxine can be decreased when combined with Cinacalcet.Approved
VerapamilThe metabolism of Cinacalcet can be decreased when combined with Verapamil.Approved
VilazodoneThe metabolism of Vilazodone can be decreased when combined with Cinacalcet.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Cinacalcet.Approved
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Cinacalcet.Approved, Investigational
VoriconazoleThe metabolism of Cinacalcet can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe serum concentration of Vortioxetine can be increased when it is combined with Cinacalcet.Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Cinacalcet.Approved, Vet Approved
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Cinacalcet.Approved
ZiprasidoneThe metabolism of Cinacalcet can be decreased when combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Cinacalcet.Approved
ZuclopenthixolThe metabolism of Zuclopenthixol can be decreased when combined with Cinacalcet.Approved, Investigational
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
ATC CodesH05BX01
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (278 KB)
MSDSNot Available
ADMET
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 )
Pharmacoeconomics
Manufacturers
  • Amgen inc
Packagers
Dosage forms
FormRouteStrength
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)
CA2202879 No2005-08-302015-10-23Canada
US6011068 No1998-03-082018-03-08Us
US6031003 No1996-12-142016-12-14Us
US6211244 No1995-10-232015-10-23Us
US6313146 No1996-12-142016-12-14Us
US7829595 No2006-09-222026-09-22Us
Properties
StateSolid
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 FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassNaphthalenes
Sub ClassNot Available
Direct ParentNaphthalenes
Alternative Parents
Substituents
  • Phenylpropylamine
  • Naphthalene
  • Aralkylamine
  • Monocyclic benzene moiety
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External Descriptors

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
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 07, 2016 02:38