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Identification
NameAnagrelide
Accession NumberDB00261  (APRD00798)
TypeSmall Molecule
GroupsApproved
DescriptionAnagrelide is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It also has been used in the treatment of chronic myeloid leukemia. [Wikipedia]
Structure
Thumb
Synonyms
Anagrelida
Anagrelidum
External Identifiers
  • BL-4162A
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Agrylincapsule.5 mg/1oralShire US Manufacturing Inc.1997-03-14Not applicableUs
Agrylincapsule0.5 mgoralShire Pharma Canada Ulc1998-01-06Not applicableCanada
Dom-anagrelidecapsule0.5 mgoralDominion Pharmacal2006-08-02Not applicableCanada
Mylan-anagrelidecapsule0.5 mgoralMylan Pharmaceuticals Ulc2005-04-112016-06-28Canada
PHL-anagrelidecapsule0.5 mgoralPharmel Inc2006-07-212009-10-26Canada
PMS-anagrelidecapsule0.5 mgoralPharmascience Inc2006-01-06Not applicableCanada
Sandoz Anagrelidecapsule0.5 mgoralSandoz Canada Incorporated2004-11-05Not applicableCanada
XagridCapsule, hard0.5 mgOral useShire Pharmaceutical Contracts Limited2004-11-16Not applicableEu
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Anagrelide Hydrochloridecapsule1 mg/1oralIVAX Pharmaceuticals, Inc.2005-04-18Not applicableUs
Anagrelide Hydrochloridecapsule.5 mg/1oralAvera Mc Kennan Hospital2015-07-15Not applicableUs
Anagrelide Hydrochloridecapsule.5 mg/1oralIVAX Pharmaceuticals, Inc.2005-04-18Not applicableUs
Anagrelide Hydrochloridecapsule.5 mg/1oralPhysicians Total Care, Inc.2007-07-19Not applicableUs
Anagrelide Hydrochloridecapsule.5 mg/1oralCarilion Materials Management2005-04-18Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
XagridNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Anagrelide Hydrochloride
58579-51-4
Thumb
  • InChI Key: TVWRQCIPWUCNMI-UHFFFAOYSA-N
  • Monoisotopic Mass: 290.973295014
  • Average Mass: 292.549
DBSALT000379
Categories
UNIIK9X45X0051
CAS number68475-42-3
WeightAverage: 256.088
Monoisotopic: 254.996617275
Chemical FormulaC10H7Cl2N3O
InChI KeyInChIKey=OTBXOEAOVRKTNQ-UHFFFAOYSA-N
InChI
InChI=1S/C10H7Cl2N3O/c11-6-1-2-7-5(9(6)12)3-15-4-8(16)14-10(15)13-7/h1-2H,3-4H2,(H,13,14,16)
IUPAC Name
6,7-dichloro-1H,2H,3H,5H-imidazolidino[2,1-b]quinazolin-2-one
SMILES
ClC1=CC=C2N=C3NC(=O)CN3CC2=C1Cl
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinazolines. These are compounds containing a quinazoline moiety, which is made up of two fused six-member aromatic rings, a benzene ring and a pyrimidine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassNaphthyridines
Sub ClassQuinazolines
Direct ParentQuinazolines
Alternative Parents
Substituents
  • Quinazoline
  • 1,2-dichlorobenzene
  • Chlorobenzene
  • Benzenoid
  • Imidazolidinone
  • Aryl halide
  • Aryl chloride
  • Imidazolidine
  • Tertiary amine
  • Guanidine
  • Carboxamide group
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of patients with thrombocythemia, secondary to myeloproliferative disorders, to reduce the elevated platelet count and the risk of thrombosis and to ameliorate associated symptoms including thrombo-hemorrhagic events.
PharmacodynamicsAnagrelide is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It works by inhibiting the maturation of megakaryocytes into platelets. The exact mechanism of action is unclear, although it is known to be a potent (IC50 = 36nM) inhibitor of phosphodiesterase-III.
Mechanism of actionThe mechanism by which anagrelide reduces blood platelet count is still under investigation. Studies in patients support a hypothesis of dose-related reduction in platelet production resulting from a decrease in megakaryocyte hypermaturation. In blood withdrawn from normal volunteers treated with anagrelide, a disruption was found in the postmitotic phase of megakaryocyte development and a reduction in megakaryocyte size and ploidy. At therapeutic doses, anagrelide does not produce significant changes in white cell counts or coagulation parameters, and may have a small, but clinically insignificant effect on red cell parameters. Anagrelide inhibits cyclic AMP phosphodiesterase III (PDEIII). PDEIII inhibitors can also inhibit platelet aggregation. However, significant inhibition of platelet aggregation is observed only at doses of anagrelide higher than those required to reduce platelet count.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Extensive, with < 1% recovered unchanged in the urine. Metabolized primarily in the liver by cytochrome P450 1A2 (CYP1A2). Recently, it was found that anagrelide is bio-transformed in humans into two major metabolites (6,7-dichloro-3-hydroxy-1,5 dihydro-imidazo[2,1-b]quinazolin-2-one (BCH24426) and 2-amino-5,6-dichloro-3,4,-dihydroquinazoline (RL603). Whether these metabolites have biological activities that may underlie the mode of action of the parent drug is presently unclear.

SubstrateEnzymesProduct
Anagrelide
Not Available
2-amino-5,6-dichloro-3,4,-dihydroquinazolineDetails
Anagrelide
Not Available
6,7-dichloro-3-hydroxy-1,5 dihydro-imidazo[2,1-b]quinazolin-2-oneDetails
Route of eliminationNot Available
Half lifeAt fasting and at a dose of 0.5 mg of anagrelide, the plasma half-life is 1.3 hours.
ClearanceNot Available
ToxicityThere are no reports of overdosage with anagrelide, however thrombocytopenia, which can potentially cause bleeding, is expected from overdosage. Single oral doses of anagrelide at 2,500, 1,500 and 200 mg/kg in mice, rats and monkeys, respectively, were not lethal. Symptoms of acute toxicity were: decreased motor activity in mice and rats and softened stools and decreased appetite in monkeys.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9972
Blood Brain Barrier+0.848
Caco-2 permeable+0.5826
P-glycoprotein substrateSubstrate0.7133
P-glycoprotein inhibitor INon-inhibitor0.5302
P-glycoprotein inhibitor IINon-inhibitor0.8438
Renal organic cation transporterInhibitor0.7044
CYP450 2C9 substrateNon-substrate0.8171
CYP450 2D6 substrateNon-substrate0.7564
CYP450 3A4 substrateSubstrate0.725
CYP450 1A2 substrateInhibitor0.688
CYP450 2C9 inhibitorNon-inhibitor0.7769
CYP450 2D6 inhibitorNon-inhibitor0.736
CYP450 2C19 inhibitorNon-inhibitor0.6425
CYP450 3A4 inhibitorNon-inhibitor0.5974
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6563
Ames testNon AMES toxic0.6107
CarcinogenicityNon-carcinogens0.8902
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8127 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8386
hERG inhibition (predictor II)Non-inhibitor0.8405
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Shire development inc
  • Alphapharm pty ltd
  • Barr laboratories inc
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan laboratories inc
  • Roxane laboratories inc
  • Sandoz inc
  • Watson laboratories
Packagers
Dosage forms
FormRouteStrength
Capsuleoral.5 mg/1
Capsuleoral1 mg/1
Capsuleoral0.5 mg
Capsule, hardOral use0.5 mg
Prices
Unit descriptionCostUnit
Agrylin 1 mg capsule13.03USD each
Anagrelide hcl 1 mg capsule11.91USD each
Agrylin 0.5 mg capsule7.37USD each
Anagrelide hcl 0.5 mg capsule5.94USD each
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point280 °CNot Available
water solubilityVery slightly solubleNot Available
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.279 mg/mLALOGPS
logP1.95ALOGPS
logP1.94ChemAxon
logS-3ALOGPS
pKa (Strongest Acidic)12.55ChemAxon
pKa (Strongest Basic)3.62ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area44.7 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity63.25 m3·mol-1ChemAxon
Polarizability23.61 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
References
Synthesis Reference

DrugSyn.org

US3932407
General References
  1. Voglova J, Maisnar V, Beranek M, Chrobak L: [Combination of imatinib and anagrelide in treatment of chronic myeloid leukemia in blastic phase]. Vnitr Lek. 2006 Sep;52(9):819-22. [PubMed:17091608 ]
  2. Petrides PE: Anagrelide: what was new in 2004 and 2005? Semin Thromb Hemost. 2006 Jun;32(4 Pt 2):399-408. [PubMed:16810615 ]
  3. Harrison CN, Campbell PJ, Buck G, Wheatley K, East CL, Bareford D, Wilkins BS, van der Walt JD, Reilly JT, Grigg AP, Revell P, Woodcock BE, Green AR: Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. N Engl J Med. 2005 Jul 7;353(1):33-45. [PubMed:16000354 ]
External Links
ATC CodesL01XX35
AHFS Codes
  • 10:00.00
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (295 KB)
MSDSDownload (97.3 KB)
Interactions
Drug Interactions
Drug
AbciximabAnagrelide may increase the anticoagulant activities of Abciximab.
AbirateroneThe serum concentration of Anagrelide can be increased when it is combined with Abiraterone.
AcenocoumarolAnagrelide may increase the anticoagulant activities of Acenocoumarol.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Anagrelide.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Anagrelide.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Anagrelide.
AlprostadilAlprostadil may increase the anticoagulant activities of Anagrelide.
AlprostadilAnagrelide may increase the antiplatelet activities of Alprostadil.
AlteplaseAnagrelide may increase the anticoagulant activities of Alteplase.
ALX-0081Anagrelide may increase the anticoagulant activities of ALX-0081.
AmantadineAmantadine may increase the QTc-prolonging activities of Anagrelide.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Anagrelide.
AmiodaroneAnagrelide may increase the QTc-prolonging activities of Amiodarone.
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Anagrelide.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Anagrelide.
AncrodAnagrelide may increase the anticoagulant activities of Ancrod.
AnistreplaseAnagrelide may increase the anticoagulant activities of Anistreplase.
Antithrombin III humanAnagrelide may increase the anticoagulant activities of Antithrombin III human.
ApixabanAnagrelide may increase the anticoagulant activities of Apixaban.
ApomorphineApomorphine may increase the QTc-prolonging activities of Anagrelide.
AprotininThe therapeutic efficacy of Anagrelide can be decreased when used in combination with Aprotinin.
ArdeparinAnagrelide may increase the anticoagulant activities of Ardeparin.
ArformoterolArformoterol may increase the QTc-prolonging activities of Anagrelide.
ArgatrobanAnagrelide may increase the anticoagulant activities of Argatroban.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Anagrelide.
Arsenic trioxideAnagrelide may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherAnagrelide may increase the QTc-prolonging activities of Artemether.
AsenapineAnagrelide may increase the QTc-prolonging activities of Asenapine.
AstaxanthinAnagrelide may increase the anticoagulant activities of Astaxanthin.
AtazanavirAtazanavir may increase the QTc-prolonging activities of Anagrelide.
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Anagrelide.
AzelastineAzelastine may increase the anticoagulant activities of Anagrelide.
AzelastineAnagrelide may increase the antiplatelet activities of Azelastine.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Anagrelide.
BatroxobinAnagrelide may increase the anticoagulant activities of Batroxobin.
BecaplerminAnagrelide may increase the anticoagulant activities of Becaplermin.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Anagrelide.
BemiparinAnagrelide may increase the anticoagulant activities of Bemiparin.
BeraprostAnagrelide may increase the anticoagulant activities of Beraprost.
BevacizumabBevacizumab may increase the cardiotoxic activities of Anagrelide.
BivalirudinAnagrelide may increase the anticoagulant activities of Bivalirudin.
BortezomibThe metabolism of Anagrelide can be decreased when combined with Bortezomib.
BuserelinBuserelin may increase the QTc-prolonging activities of Anagrelide.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Anagrelide.
CaffeineThe metabolism of Anagrelide can be decreased when combined with Caffeine.
CangrelorAnagrelide may increase the anticoagulant activities of Cangrelor.
CarbamazepineThe metabolism of Anagrelide can be increased when combined with Carbamazepine.
CeritinibCeritinib may increase the QTc-prolonging activities of Anagrelide.
CertoparinAnagrelide may increase the anticoagulant activities of Certoparin.
ChloroquineChloroquine may increase the QTc-prolonging activities of Anagrelide.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Anagrelide.
CilostazolThe risk or severity of adverse effects can be increased when Anagrelide is combined with Cilostazol.
CilostazolCilostazol may increase the anticoagulant activities of Anagrelide.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Anagrelide.
CisaprideAnagrelide may increase the QTc-prolonging activities of Cisapride.
CitalopramCitalopram may increase the QTc-prolonging activities of Anagrelide.
Citric AcidAnagrelide may increase the anticoagulant activities of Citric Acid.
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Anagrelide.
ClomipramineClomipramine may increase the QTc-prolonging activities of Anagrelide.
ClopidogrelAnagrelide may increase the anticoagulant activities of Clopidogrel.
ClotrimazoleThe metabolism of Anagrelide can be decreased when combined with Clotrimazole.
ClozapineClozapine may increase the QTc-prolonging activities of Anagrelide.
CollagenaseThe risk or severity of adverse effects can be increased when Anagrelide is combined with Collagenase.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Anagrelide.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Anagrelide.
Cyproterone acetateThe serum concentration of Anagrelide can be decreased when it is combined with Cyproterone acetate.
Dabigatran etexilateAnagrelide may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibDabrafenib may increase the QTc-prolonging activities of Anagrelide.
DalteparinAnagrelide may increase the anticoagulant activities of Dalteparin.
DanaparoidAnagrelide may increase the anticoagulant activities of Danaparoid.
DasatinibDasatinib may increase the anticoagulant activities of Anagrelide.
DeferasiroxThe serum concentration of Anagrelide can be increased when it is combined with Deferasirox.
DefibrotideAnagrelide may increase the anticoagulant activities of Defibrotide.
DegarelixDegarelix may increase the QTc-prolonging activities of Anagrelide.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Anagrelide is combined with Deoxycholic Acid.
DesfluraneDesflurane may increase the QTc-prolonging activities of Anagrelide.
DesipramineDesipramine may increase the QTc-prolonging activities of Anagrelide.
DesirudinAnagrelide may increase the anticoagulant activities of Desirudin.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Anagrelide.
DesmoteplaseAnagrelide may increase the anticoagulant activities of Desmoteplase.
DextranAnagrelide may increase the anticoagulant activities of Dextran.
Dextran 40Anagrelide may increase the anticoagulant activities of Dextran 40.
Dextran 70Anagrelide may increase the anticoagulant activities of Dextran 70.
Dextran 75Anagrelide may increase the anticoagulant activities of Dextran 75.
DicoumarolAnagrelide may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Anagrelide.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Anagrelide.
DigoxinDigoxin may decrease the cardiotoxic activities of Anagrelide.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Anagrelide.
DipyridamoleAnagrelide may increase the anticoagulant activities of Dipyridamole.
DisopyramideAnagrelide may increase the QTc-prolonging activities of Disopyramide.
DitazoleAnagrelide may increase the anticoagulant activities of Ditazole.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Anagrelide.
DofetilideDofetilide may increase the QTc-prolonging activities of Anagrelide.
DolasetronDolasetron may increase the QTc-prolonging activities of Anagrelide.
DomperidoneAnagrelide may increase the QTc-prolonging activities of Domperidone.
DoxepinDoxepin may increase the QTc-prolonging activities of Anagrelide.
DronedaroneAnagrelide may increase the QTc-prolonging activities of Dronedarone.
DroperidolDroperidol may increase the QTc-prolonging activities of Anagrelide.
Drotrecogin alfaAnagrelide may increase the anticoagulant activities of Drotrecogin alfa.
Edetic AcidAnagrelide may increase the anticoagulant activities of Edetic Acid.
EdoxabanAnagrelide may increase the anticoagulant activities of Edoxaban.
EliglustatAnagrelide may increase the QTc-prolonging activities of Eliglustat.
EnoxaparinAnagrelide may increase the anticoagulant activities of Enoxaparin.
EpinastineEpinastine may increase the anticoagulant activities of Anagrelide.
EpinastineAnagrelide may increase the antiplatelet activities of Epinastine.
EpoprostenolAnagrelide may increase the anticoagulant activities of Epoprostenol.
EptifibatideEptifibatide may increase the anticoagulant activities of Anagrelide.
EribulinEribulin may increase the QTc-prolonging activities of Anagrelide.
ErythromycinErythromycin may increase the QTc-prolonging activities of Anagrelide.
EscitalopramAnagrelide may increase the QTc-prolonging activities of Escitalopram.
Ethyl biscoumacetateAnagrelide may increase the anticoagulant activities of Ethyl biscoumacetate.
EzogabineEzogabine may increase the QTc-prolonging activities of Anagrelide.
FamotidineFamotidine may increase the QTc-prolonging activities of Anagrelide.
FelbamateFelbamate may increase the QTc-prolonging activities of Anagrelide.
FibrinolysinAnagrelide may increase the anticoagulant activities of Fibrinolysin.
FingolimodFingolimod may increase the QTc-prolonging activities of Anagrelide.
FlecainideFlecainide may increase the QTc-prolonging activities of Anagrelide.
FluconazoleFluconazole may increase the QTc-prolonging activities of Anagrelide.
FluoxetineAnagrelide may increase the QTc-prolonging activities of Fluoxetine.
FlupentixolAnagrelide may increase the QTc-prolonging activities of Flupentixol.
FluvoxamineThe metabolism of Anagrelide can be decreased when combined with Fluvoxamine.
Fondaparinux sodiumAnagrelide may increase the anticoagulant activities of Fondaparinux sodium.
FormoterolFormoterol may increase the QTc-prolonging activities of Anagrelide.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Anagrelide.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Anagrelide.
GalantamineGalantamine may increase the QTc-prolonging activities of Anagrelide.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Anagrelide.
GlucosamineGlucosamine may increase the antiplatelet activities of Anagrelide.
GoserelinGoserelin may increase the QTc-prolonging activities of Anagrelide.
GranisetronGranisetron may increase the QTc-prolonging activities of Anagrelide.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Anagrelide.
HeparinAnagrelide may increase the anticoagulant activities of Heparin.
HirulogAnagrelide may increase the anticoagulant activities of Hirulog.
HistrelinHistrelin may increase the QTc-prolonging activities of Anagrelide.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Anagrelide.
IbandronateIbandronate may increase the QTc-prolonging activities of Anagrelide.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Anagrelide is combined with Ibritumomab tiuxetan.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Anagrelide.
IbudilastIbudilast may increase the anticoagulant activities of Anagrelide.
IbudilastAnagrelide may increase the antiplatelet activities of Ibudilast.
IbutilideAnagrelide may increase the QTc-prolonging activities of Ibutilide.
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Anagrelide.
Icosapent ethylAnagrelide may increase the antiplatelet activities of Icosapent ethyl.
IfenprodilIfenprodil may increase the anticoagulant activities of Anagrelide.
IfenprodilAnagrelide may increase the antiplatelet activities of Ifenprodil.
IloperidoneAnagrelide may increase the QTc-prolonging activities of Iloperidone.
IloprostAnagrelide may increase the anticoagulant activities of Iloprost.
ImipramineImipramine may increase the QTc-prolonging activities of Anagrelide.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Anagrelide.
IndapamideIndapamide may increase the QTc-prolonging activities of Anagrelide.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Anagrelide.
IsradipineIsradipine may increase the QTc-prolonging activities of Anagrelide.
ItraconazoleItraconazole may increase the QTc-prolonging activities of Anagrelide.
IvabradineIvabradine may increase the QTc-prolonging activities of Anagrelide.
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Anagrelide.
LapatinibLapatinib may increase the QTc-prolonging activities of Anagrelide.
LenvatinibLenvatinib may increase the QTc-prolonging activities of Anagrelide.
LepirudinAnagrelide may increase the anticoagulant activities of Lepirudin.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Anagrelide.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Anagrelide.
LidocaineThe metabolism of Anagrelide can be decreased when combined with Lidocaine.
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Anagrelide.
LithiumLithium may increase the QTc-prolonging activities of Anagrelide.
LopinavirAnagrelide may increase the QTc-prolonging activities of Lopinavir.
LumefantrineAnagrelide may increase the QTc-prolonging activities of Lumefantrine.
MaprotilineMaprotiline may increase the QTc-prolonging activities of Anagrelide.
MefloquineMefloquine may increase the QTc-prolonging activities of Anagrelide.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Anagrelide.
MethadoneMethadone may increase the QTc-prolonging activities of Anagrelide.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Anagrelide.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Anagrelide.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Anagrelide.
MexiletineThe metabolism of Anagrelide can be decreased when combined with Mexiletine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Anagrelide.
MilrinoneMilrinone may increase the anticoagulant activities of Anagrelide.
MilrinoneAnagrelide may increase the antiplatelet activities of Milrinone.
MirabegronMirabegron may increase the QTc-prolonging activities of Anagrelide.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Anagrelide.
MoexiprilMoexipril may increase the QTc-prolonging activities of Anagrelide.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Anagrelide.
NadroparinAnagrelide may increase the anticoagulant activities of Nadroparin.
NCX 4016Anagrelide may increase the anticoagulant activities of NCX 4016.
NelfinavirNelfinavir may increase the QTc-prolonging activities of Anagrelide.
NevirapineThe metabolism of Anagrelide can be decreased when combined with Nevirapine.
NicardipineNicardipine may increase the QTc-prolonging activities of Anagrelide.
NilotinibAnagrelide may increase the QTc-prolonging activities of Nilotinib.
NimesulideNimesulide may increase the anticoagulant activities of Anagrelide.
NimesulideAnagrelide may increase the antiplatelet activities of Nimesulide.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Anagrelide.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Anagrelide.
ObinutuzumabThe risk or severity of adverse effects can be increased when Anagrelide is combined with Obinutuzumab.
OctreotideOctreotide may increase the QTc-prolonging activities of Anagrelide.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Anagrelide.
OlanzapineOlanzapine may increase the QTc-prolonging activities of Anagrelide.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Anagrelide.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Anagrelide.
OndansetronOndansetron may increase the QTc-prolonging activities of Anagrelide.
OsimertinibThe serum concentration of Anagrelide can be decreased when it is combined with Osimertinib.
OtamixabanAnagrelide may increase the anticoagulant activities of Otamixaban.
OuabainOuabain may decrease the cardiotoxic activities of Anagrelide.
OxytocinOxytocin may increase the QTc-prolonging activities of Anagrelide.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Anagrelide.
PaliperidoneAnagrelide may increase the QTc-prolonging activities of Paliperidone.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Anagrelide.
ParnaparinAnagrelide may increase the anticoagulant activities of Parnaparin.
ParoxetineParoxetine may increase the QTc-prolonging activities of Anagrelide.
PasireotidePasireotide may increase the QTc-prolonging activities of Anagrelide.
PazopanibPazopanib may increase the QTc-prolonging activities of Anagrelide.
Peginterferon alfa-2bThe serum concentration of Anagrelide can be increased when it is combined with Peginterferon alfa-2b.
PentamidinePentamidine may increase the QTc-prolonging activities of Anagrelide.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Anagrelide.
Pentosan PolysulfateAnagrelide may increase the anticoagulant activities of Pentosan Polysulfate.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Anagrelide.
PerflutrenPerflutren may increase the QTc-prolonging activities of Anagrelide.
PhenindioneAnagrelide may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe metabolism of Anagrelide can be increased when combined with Phenobarbital.
PhenprocoumonAnagrelide may increase the anticoagulant activities of Phenprocoumon.
PimozideAnagrelide may increase the QTc-prolonging activities of Pimozide.
PlasminAnagrelide may increase the anticoagulant activities of Plasmin.
PosaconazolePosaconazole may increase the QTc-prolonging activities of Anagrelide.
PrasugrelAnagrelide may increase the anticoagulant activities of Prasugrel.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Anagrelide.
PrimidoneThe metabolism of Anagrelide can be increased when combined with Primidone.
ProcainamideAnagrelide may increase the QTc-prolonging activities of Procainamide.
PromazinePromazine may increase the QTc-prolonging activities of Anagrelide.
PromethazinePromethazine may increase the QTc-prolonging activities of Anagrelide.
PropafenonePropafenone may increase the QTc-prolonging activities of Anagrelide.
PropofolPropofol may increase the QTc-prolonging activities of Anagrelide.
Protein CAnagrelide may increase the anticoagulant activities of Protein C.
ProtocatechualdehydeAnagrelide may increase the anticoagulant activities of Protocatechualdehyde.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Anagrelide.
QuetiapineAnagrelide may increase the QTc-prolonging activities of Quetiapine.
QuinidineAnagrelide may increase the QTc-prolonging activities of Quinidine.
QuinineAnagrelide may increase the QTc-prolonging activities of Quinine.
RanolazineRanolazine may increase the QTc-prolonging activities of Anagrelide.
ResveratrolResveratrol may increase the anticoagulant activities of Anagrelide.
ResveratrolAnagrelide may increase the antiplatelet activities of Resveratrol.
ReteplaseAnagrelide may increase the anticoagulant activities of Reteplase.
ReviparinAnagrelide may increase the anticoagulant activities of Reviparin.
RidogrelRidogrel may increase the anticoagulant activities of Anagrelide.
RidogrelAnagrelide may increase the antiplatelet activities of Ridogrel.
RifampicinThe metabolism of Anagrelide can be increased when combined with Rifampicin.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Anagrelide.
RiociguatAnagrelide may increase the hypotensive activities of Riociguat.
RisperidoneRisperidone may increase the QTc-prolonging activities of Anagrelide.
RitonavirRitonavir may increase the QTc-prolonging activities of Anagrelide.
RivaroxabanAnagrelide may increase the anticoagulant activities of Rivaroxaban.
RopiniroleThe metabolism of Anagrelide can be decreased when combined with Ropinirole.
RosiglitazoneAnagrelide may increase the anticoagulant activities of Rosiglitazone.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Anagrelide.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Anagrelide.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Anagrelide.
SaquinavirSaquinavir may increase the QTc-prolonging activities of Anagrelide.
SCH-530348SCH-530348 may increase the anticoagulant activities of Anagrelide.
SCH-530348Anagrelide may increase the antiplatelet activities of SCH-530348.
SelexipagAnagrelide may increase the anticoagulant activities of Selexipag.
SertralineSertraline may increase the QTc-prolonging activities of Anagrelide.
SevofluraneSevoflurane may increase the anticoagulant activities of Anagrelide.
SevofluraneAnagrelide may increase the antiplatelet activities of Sevoflurane.
SimeprevirThe metabolism of Anagrelide can be decreased when combined with Simeprevir.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Anagrelide.
SorafenibSorafenib may increase the QTc-prolonging activities of Anagrelide.
SotalolAnagrelide may increase the QTc-prolonging activities of Sotalol.
SRT501SRT501 may increase the anticoagulant activities of Anagrelide.
SRT501Anagrelide may increase the antiplatelet activities of SRT501.
StreptokinaseAnagrelide may increase the anticoagulant activities of Streptokinase.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Anagrelide.
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Anagrelide.
SulodexideAnagrelide may increase the anticoagulant activities of Sulodexide.
SunitinibSunitinib may increase the QTc-prolonging activities of Anagrelide.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Anagrelide.
TelavancinTelavancin may increase the QTc-prolonging activities of Anagrelide.
TelithromycinTelithromycin may increase the QTc-prolonging activities of Anagrelide.
TenecteplaseAnagrelide may increase the anticoagulant activities of Tenecteplase.
TenofovirThe metabolism of Anagrelide can be decreased when combined with Tenofovir.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Anagrelide.
TeriflunomideThe serum concentration of Anagrelide can be decreased when it is combined with Teriflunomide.
TesmilifeneTesmilifene may increase the anticoagulant activities of Anagrelide.
TesmilifeneAnagrelide may increase the antiplatelet activities of Tesmilifene.
TetrabenazineAnagrelide may increase the QTc-prolonging activities of Tetrabenazine.
TheophyllineThe metabolism of Anagrelide can be decreased when combined with Theophylline.
ThioridazineAnagrelide may increase the QTc-prolonging activities of Thioridazine.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Anagrelide.
TicagrelorAnagrelide may increase the anticoagulant activities of Ticagrelor.
TiclopidineTiclopidine may increase the anticoagulant activities of Anagrelide.
TinzaparinAnagrelide may increase the anticoagulant activities of Tinzaparin.
TipranavirTipranavir may increase the antiplatelet activities of Anagrelide.
TirofibanAnagrelide may increase the anticoagulant activities of Tirofiban.
TizanidineTizanidine may increase the QTc-prolonging activities of Anagrelide.
TolterodineTolterodine may increase the QTc-prolonging activities of Anagrelide.
ToremifeneAnagrelide may increase the QTc-prolonging activities of Toremifene.
TositumomabThe risk or severity of adverse effects can be increased when Anagrelide is combined with Tositumomab.
TranilastTranilast may increase the anticoagulant activities of Anagrelide.
TranilastAnagrelide may increase the antiplatelet activities of Tranilast.
TrapidilTrapidil may increase the anticoagulant activities of Anagrelide.
TrapidilAnagrelide may increase the antiplatelet activities of Trapidil.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Anagrelide.
TrazodoneTrazodone may increase the QTc-prolonging activities of Anagrelide.
TreprostinilAnagrelide may increase the anticoagulant activities of Treprostinil.
TreprostinilTreprostinil may increase the antiplatelet activities of Anagrelide.
TriflusalAnagrelide may increase the anticoagulant activities of Triflusal.
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Anagrelide.
TrimipramineTrimipramine may increase the QTc-prolonging activities of Anagrelide.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Anagrelide.
UrokinaseAnagrelide may increase the anticoagulant activities of Urokinase.
VandetanibAnagrelide may increase the QTc-prolonging activities of Vandetanib.
VardenafilVardenafil may increase the QTc-prolonging activities of Anagrelide.
VemurafenibAnagrelide may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Anagrelide.
VilanterolVilanterol may increase the QTc-prolonging activities of Anagrelide.
Vitamin EVitamin E may increase the antiplatelet activities of Anagrelide.
VorapaxarAnagrelide may increase the anticoagulant activities of Vorapaxar.
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Anagrelide.
VorinostatVorinostat may increase the QTc-prolonging activities of Anagrelide.
WarfarinAnagrelide may increase the anticoagulant activities of Warfarin.
XimelagatranAnagrelide may increase the anticoagulant activities of Ximelagatran.
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Anagrelide.
ZuclopenthixolAnagrelide may increase the QTc-prolonging activities of Zuclopenthixol.
Food Interactions
  • Food appears to reduce the area under the curve by 13.8%, without clinical consequence.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
Gene Name:
PDE3A
Uniprot ID:
Q14432
Molecular Weight:
124978.06 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Venuti MC, Stephenson RA, Alvarez R, Bruno JJ, Strosberg AM: Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline. J Med Chem. 1988 Nov;31(11):2136-45. [PubMed:2846839 ]
  4. 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:
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23