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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
XagridCapsule0.5 mgOralShire Pharmaceutical Contracts Limited2004-11-16Not applicableEu
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Anagrelide HydrochlorideCapsule.5 mg/1OralPhysicians Total Care, Inc.2007-07-19Not applicableUs
Anagrelide HydrochlorideCapsule.5 mg/1OralCarilion Materials Management2005-04-18Not applicableUs
Anagrelide HydrochlorideCapsule.5 mg/1OralAvera Mc Kennan Hospital2015-07-15Not applicableUs
Anagrelide HydrochlorideCapsule1 mg/1OralTeva Pharmaceuticals Usa, Inc2005-04-18Not applicableUs
Anagrelide HydrochlorideCapsule.5 mg/1OralTeva Pharmaceuticals Usa, Inc2005-04-18Not 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 KeyOTBXOEAOVRKTNQ-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
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.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
cGMP-inhibited 3',5'-cyclic phosphodiesterase AProteinyes
inhibitor
HumanQ14432 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabAnagrelide may increase the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Anagrelide can be increased when it is combined with Abiraterone.Approved
AcenocoumarolAnagrelide may increase the anticoagulant activities of Acenocoumarol.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Anagrelide.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Anagrelide is combined with Acetylsalicylic acid.Approved, Vet Approved
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
AlprostadilAlprostadil may increase the anticoagulant activities of Anagrelide.Approved, Investigational
AlteplaseAnagrelide may increase the anticoagulant activities of Alteplase.Approved
ALX-0081Anagrelide may increase the anticoagulant activities of ALX-0081.Investigational
AmantadineAmantadine may increase the QTc-prolonging activities of Anagrelide.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Anagrelide is combined with Aminosalicylic Acid.Approved
AmiodaroneAnagrelide may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Anagrelide.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Anagrelide.Approved
AncrodAnagrelide may increase the anticoagulant activities of Ancrod.Investigational
AnistreplaseAnagrelide may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanAnagrelide may increase the anticoagulant activities of Antithrombin III human.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Anagrelide.Investigational
ApixabanThe risk or severity of adverse effects can be increased when Anagrelide is combined with Apixaban.Approved
ApomorphineApomorphine may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
AprotininThe therapeutic efficacy of Anagrelide can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinAnagrelide may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArformoterolArformoterol may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
ArgatrobanAnagrelide may increase the anticoagulant activities of Argatroban.Approved, Investigational
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
Arsenic trioxideAnagrelide may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherAnagrelide may increase the QTc-prolonging activities of Artemether.Approved
AsenapineAnagrelide may increase the QTc-prolonging activities of Asenapine.Approved
AstaxanthinAnagrelide may increase the anticoagulant activities of Astaxanthin.Investigational
AtazanavirAtazanavir may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Anagrelide.Approved
AzelastineAzelastine may increase the anticoagulant activities of Anagrelide.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Anagrelide.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Balsalazide.Approved, Investigational
BatroxobinAnagrelide may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminAnagrelide may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BedaquilineBedaquiline may increase the QTc-prolonging activities of Anagrelide.Approved
BemiparinAnagrelide may increase the anticoagulant activities of Bemiparin.Approved
BeraprostAnagrelide may increase the anticoagulant activities of Beraprost.Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Anagrelide.Approved, Investigational
BivalirudinAnagrelide may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BortezomibBortezomib may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
BuserelinBuserelin may increase the QTc-prolonging activities of Anagrelide.Approved
ButylphthalideButylphthalide may increase the anticoagulant activities of Anagrelide.Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Anagrelide.Approved
CaffeineThe metabolism of Anagrelide can be decreased when combined with Caffeine.Approved
CangrelorAnagrelide may increase the anticoagulant activities of Cangrelor.Approved
CarbamazepineThe metabolism of Anagrelide can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibCeritinib may increase the QTc-prolonging activities of Anagrelide.Approved
CertoparinAnagrelide may increase the anticoagulant activities of Certoparin.Approved
ChloroquineChloroquine may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
CilostazolThe risk or severity of adverse effects can be increased when Anagrelide is combined with Cilostazol.Approved
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
CisaprideAnagrelide may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the QTc-prolonging activities of Anagrelide.Approved
Citric AcidAnagrelide may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Anagrelide.Approved
ClomipramineClomipramine may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
ClopidogrelAnagrelide may increase the anticoagulant activities of Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Anagrelide can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineClozapine may increase the QTc-prolonging activities of Anagrelide.Approved
CollagenaseThe risk or severity of adverse effects can be increased when Anagrelide is combined with Collagenase.Approved
CrizotinibCrizotinib may increase the QTc-prolonging activities of Anagrelide.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Anagrelide.Approved, Investigational
Cyproterone acetateThe serum concentration of Anagrelide can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateAnagrelide may increase the anticoagulant activities of Dabigatran etexilate.Approved
DabrafenibDabrafenib may increase the QTc-prolonging activities of Anagrelide.Approved
DalteparinAnagrelide may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidAnagrelide may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DasatinibDasatinib may increase the anticoagulant activities of Anagrelide.Approved, Investigational
DeferasiroxThe serum concentration of Anagrelide can be increased when it is combined with Deferasirox.Approved, Investigational
DefibrotideAnagrelide may increase the anticoagulant activities of Defibrotide.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Anagrelide.Approved
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Anagrelide is combined with Deoxycholic Acid.Approved
dersalazineThe risk or severity of adverse effects can be increased when Anagrelide is combined with dersalazine.Investigational
DesfluraneDesflurane may increase the QTc-prolonging activities of Anagrelide.Approved
DesipramineDesipramine may increase the QTc-prolonging activities of Anagrelide.Approved
DesirudinAnagrelide may increase the anticoagulant activities of Desirudin.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Anagrelide.Approved
DesmoteplaseAnagrelide may increase the anticoagulant activities of Desmoteplase.Investigational
DextranAnagrelide may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Anagrelide may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Anagrelide may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Anagrelide may increase the anticoagulant activities of Dextran 75.Approved
DicoumarolAnagrelide may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Anagrelide is combined with Diflunisal.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Anagrelide.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Anagrelide.Approved
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Anagrelide.Approved
DipyridamoleAnagrelide may increase the anticoagulant activities of Dipyridamole.Approved
DisopyramideAnagrelide may increase the QTc-prolonging activities of Disopyramide.Approved
DitazoleAnagrelide may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Anagrelide.Approved, Investigational
DofetilideDofetilide may increase the QTc-prolonging activities of Anagrelide.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Anagrelide.Approved
DomperidoneAnagrelide may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Anagrelide.Approved
DronedaroneAnagrelide may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
Drotrecogin alfaAnagrelide may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
Edetic AcidAnagrelide may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanAnagrelide may increase the anticoagulant activities of Edoxaban.Approved
EliglustatAnagrelide may increase the QTc-prolonging activities of Eliglustat.Approved
EnoxaparinAnagrelide may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Anagrelide.Approved, Investigational
eplivanserineAnagrelide may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Anagrelide.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Anagrelide.Approved, Investigational
EribulinEribulin may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
ErythromycinErythromycin may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
EscitalopramAnagrelide may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Ethyl biscoumacetateAnagrelide may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EzogabineEzogabine may increase the QTc-prolonging activities of Anagrelide.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Anagrelide.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Anagrelide.Approved
FibrinolysinAnagrelide may increase the anticoagulant activities of Fibrinolysin.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
FlecainideFlecainide may increase the QTc-prolonging activities of Anagrelide.Approved, Withdrawn
FluconazoleFluconazole may increase the QTc-prolonging activities of Anagrelide.Approved
FluindioneAnagrelide may increase the anticoagulant activities of Fluindione.Investigational
FluoxetineAnagrelide may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolAnagrelide may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluvoxamineThe metabolism of Anagrelide can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxAnagrelide may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumAnagrelide may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FormoterolFormoterol may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
FoscarnetFoscarnet may increase the QTc-prolonging activities of Anagrelide.Approved
GabexateAnagrelide may increase the anticoagulant activities of Gabexate.Investigational
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Anagrelide.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Anagrelide.Approved
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
GlucosamineGlucosamine may increase the antiplatelet activities of Anagrelide.Approved
GoserelinGoserelin may increase the QTc-prolonging activities of Anagrelide.Approved
GranisetronGranisetron may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
HaloperidolHaloperidol may increase the QTc-prolonging activities of Anagrelide.Approved
HeparinAnagrelide may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineAnagrelide may increase the anticoagulant activities of Higenamine.Investigational
HirulogAnagrelide may increase the anticoagulant activities of Hirulog.Experimental
HistrelinHistrelin may increase the QTc-prolonging activities of Anagrelide.Approved
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Anagrelide.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Anagrelide is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Anagrelide.Approved
IbudilastIbudilast may increase the anticoagulant activities of Anagrelide.Approved, Investigational
IbutilideAnagrelide may increase the QTc-prolonging activities of Ibutilide.Approved
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Anagrelide.Approved, Nutraceutical
idraparinuxAnagrelide may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Anagrelide.Approved, Withdrawn
IloperidoneAnagrelide may increase the QTc-prolonging activities of Iloperidone.Approved
IloprostIloprost may increase the antiplatelet activities of Anagrelide.Approved, Investigational
ImipramineImipramine may increase the QTc-prolonging activities of Anagrelide.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Anagrelide.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Anagrelide.Approved
IndobufenAnagrelide may increase the anticoagulant activities of Indobufen.Investigational
IsofluraneIsoflurane may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
IsradipineIsradipine may increase the QTc-prolonging activities of Anagrelide.Approved
ItraconazoleItraconazole may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Anagrelide.Approved
Kct 0809Anagrelide may increase the anticoagulant activities of Kct 0809.Investigational
KetanserinKetanserin may increase the anticoagulant activities of Anagrelide.Investigational
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
LenvatinibLenvatinib may increase the QTc-prolonging activities of Anagrelide.Approved
LepirudinAnagrelide may increase the anticoagulant activities of Lepirudin.Approved
LeuprolideLeuprolide may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
LidocaineThe metabolism of Anagrelide can be decreased when combined with Lidocaine.Approved, Vet Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Anagrelide.Approved
LithiumLithium may increase the QTc-prolonging activities of Anagrelide.Approved
LopinavirAnagrelide may increase the QTc-prolonging activities of Lopinavir.Approved
LumefantrineAnagrelide may increase the QTc-prolonging activities of Lumefantrine.Approved
MaprotilineMaprotiline may increase the QTc-prolonging activities of Anagrelide.Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Anagrelide.Approved
MesalazineThe risk or severity of adverse effects can be increased when Anagrelide is combined with Mesalazine.Approved
MethadoneMethadone may increase the QTc-prolonging activities of Anagrelide.Approved
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Anagrelide.Approved
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Anagrelide.Approved
MexiletineThe metabolism of Anagrelide can be decreased when combined with Mexiletine.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
MilrinoneMilrinone may increase the anticoagulant activities of Anagrelide.Approved
MirabegronMirabegron may increase the QTc-prolonging activities of Anagrelide.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Anagrelide.Approved
MoexiprilMoexipril may increase the QTc-prolonging activities of Anagrelide.Approved
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
NadroparinAnagrelide may increase the anticoagulant activities of Nadroparin.Approved
NafamostatAnagrelide may increase the anticoagulant activities of Nafamostat.Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Anagrelide.Investigational
NCX 4016The risk or severity of adverse effects can be increased when Anagrelide is combined with NCX 4016.Investigational
NelfinavirNelfinavir may increase the QTc-prolonging activities of Anagrelide.Approved
NevirapineThe metabolism of Anagrelide can be decreased when combined with Nevirapine.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Anagrelide.Approved
NilotinibAnagrelide may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NimesulideNimesulide may increase the anticoagulant activities of Anagrelide.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Anagrelide is combined with Nitroaspirin.Investigational
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Anagrelide.Approved
NortriptylineNortriptyline may increase the QTc-prolonging activities of Anagrelide.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Anagrelide is combined with Obinutuzumab.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
OfloxacinOfloxacin may increase the QTc-prolonging activities of Anagrelide.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
OlodaterolOlodaterol may increase the QTc-prolonging activities of Anagrelide.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Anagrelide is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Anagrelide.Approved
OndansetronOndansetron may increase the QTc-prolonging activities of Anagrelide.Approved
OsimertinibThe serum concentration of Anagrelide can be decreased when it is combined with Osimertinib.Approved
OtamixabanAnagrelide may increase the anticoagulant activities of Otamixaban.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Anagrelide.Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Anagrelide.Approved, Vet Approved
PaliperidoneAnagrelide may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatPanobinostat may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
ParnaparinAnagrelide may increase the anticoagulant activities of Parnaparin.Approved
ParoxetineParoxetine may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Anagrelide.Approved
PazopanibPazopanib may increase the QTc-prolonging activities of Anagrelide.Approved
Peginterferon alfa-2bThe serum concentration of Anagrelide can be increased when it is combined with Peginterferon alfa-2b.Approved
PentamidinePentamidine may increase the QTc-prolonging activities of Anagrelide.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Anagrelide.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Anagrelide.Approved, Investigational
PerflutrenPerflutren may increase the QTc-prolonging activities of Anagrelide.Approved
PhenindioneAnagrelide may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe metabolism of Anagrelide can be increased when combined with Phenobarbital.Approved
PhenprocoumonAnagrelide may increase the anticoagulant activities of Phenprocoumon.Approved
PimozideAnagrelide may increase the QTc-prolonging activities of Pimozide.Approved
PlasminAnagrelide may increase the anticoagulant activities of Plasmin.Investigational
PosaconazolePosaconazole may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational, Vet Approved
PrasugrelAnagrelide may increase the anticoagulant activities of Prasugrel.Approved
PrimaquinePrimaquine may increase the QTc-prolonging activities of Anagrelide.Approved
PrimidoneThe metabolism of Anagrelide can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideAnagrelide may increase the QTc-prolonging activities of Procainamide.Approved
PromazinePromazine may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Anagrelide.Approved
PropafenonePropafenone may increase the QTc-prolonging activities of Anagrelide.Approved
PropofolPropofol may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational, Vet Approved
Protein CAnagrelide may increase the anticoagulant activities of Protein C.Approved
Protein S humanAnagrelide may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeAnagrelide may increase the anticoagulant activities of Protocatechualdehyde.Approved
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Anagrelide.Approved
QuetiapineAnagrelide may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineAnagrelide may increase the QTc-prolonging activities of Quinidine.Approved
QuinineAnagrelide may increase the QTc-prolonging activities of Quinine.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Anagrelide.Investigational
RanolazineRanolazine may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Anagrelide.Experimental, Investigational
ReteplaseAnagrelide may increase the anticoagulant activities of Reteplase.Approved
ReviparinAnagrelide may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Anagrelide.Approved
RifampicinThe metabolism of Anagrelide can be increased when combined with Rifampicin.Approved
RilpivirineRilpivirine may increase the QTc-prolonging activities of Anagrelide.Approved
RiociguatAnagrelide may increase the hypotensive activities of Riociguat.Approved
RisperidoneRisperidone may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
RitonavirRitonavir may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
RivaroxabanAnagrelide may increase the anticoagulant activities of Rivaroxaban.Approved
RopiniroleThe metabolism of Anagrelide can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneAnagrelide may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
SalbutamolSalbutamol may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Anagrelide is combined with Salicylic acid.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Anagrelide.Approved
SaquinavirSaquinavir may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
SCH-530348SCH-530348 may increase the anticoagulant activities of Anagrelide.Investigational
SelexipagAnagrelide may increase the anticoagulant activities of Selexipag.Approved
SertralineSertraline may increase the QTc-prolonging activities of Anagrelide.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
SimeprevirThe metabolism of Anagrelide can be decreased when combined with Simeprevir.Approved
SolifenacinSolifenacin may increase the QTc-prolonging activities of Anagrelide.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
SotalolAnagrelide may increase the QTc-prolonging activities of Sotalol.Approved
SRT501SRT501 may increase the anticoagulant activities of Anagrelide.Investigational
StreptokinaseAnagrelide may increase the anticoagulant activities of Streptokinase.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Anagrelide.Approved
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
SulodexideAnagrelide may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SunitinibSunitinib may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
TamoxifenTamoxifen may increase the QTc-prolonging activities of Anagrelide.Approved
TelavancinTelavancin may increase the QTc-prolonging activities of Anagrelide.Approved
TelithromycinTelithromycin may increase the QTc-prolonging activities of Anagrelide.Approved
TenecteplaseAnagrelide may increase the anticoagulant activities of Tenecteplase.Approved
TenofovirThe metabolism of Anagrelide can be decreased when combined with Tenofovir.Approved, Investigational
TerbutalineTerbutaline may increase the QTc-prolonging activities of Anagrelide.Approved
TeriflunomideThe serum concentration of Anagrelide can be decreased when it is combined with Teriflunomide.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Anagrelide.Investigational
TetrabenazineAnagrelide may increase the QTc-prolonging activities of Tetrabenazine.Approved
TheophyllineThe metabolism of Anagrelide can be decreased when combined with Theophylline.Approved
ThioridazineAnagrelide may increase the QTc-prolonging activities of Thioridazine.Approved
ThiothixeneThiothixene may increase the QTc-prolonging activities of Anagrelide.Approved
TicagrelorAnagrelide may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineThe metabolism of Anagrelide can be decreased when combined with Ticlopidine.Approved
TinzaparinAnagrelide may increase the anticoagulant activities of Tinzaparin.Approved
TipranavirTipranavir may increase the antiplatelet activities of Anagrelide.Approved, Investigational
TirofibanAnagrelide may increase the anticoagulant activities of Tirofiban.Approved
TizanidineTizanidine may increase the QTc-prolonging activities of Anagrelide.Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
ToremifeneAnagrelide may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TositumomabThe risk or severity of adverse effects can be increased when Anagrelide is combined with Tositumomab.Approved
TranilastTranilast may increase the anticoagulant activities of Anagrelide.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Anagrelide.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Anagrelide.Approved, Investigational
TrazodoneTrazodone may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
TriflusalAnagrelide may increase the anticoagulant activities of Triflusal.Approved
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Anagrelide.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Anagrelide.Approved, Vet Approved
UrokinaseAnagrelide may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
VandetanibAnagrelide may increase the QTc-prolonging activities of Vandetanib.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Anagrelide.Approved
VemurafenibThe serum concentration of Anagrelide can be increased when it is combined with Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Anagrelide.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Anagrelide.Approved
Vitamin EVitamin E may increase the antiplatelet activities of Anagrelide.Approved, Nutraceutical, Vet Approved
VorapaxarAnagrelide may increase the anticoagulant activities of Vorapaxar.Approved
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Anagrelide.Approved, Investigational
WarfarinAnagrelide may increase the anticoagulant activities of Warfarin.Approved
XimelagatranAnagrelide may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Ym150Anagrelide may increase the anticoagulant activities of Ym150.Investigational
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Anagrelide.Approved
ZuclopenthixolAnagrelide may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food Interactions
  • Food appears to reduce the area under the curve by 13.8%, without clinical consequence.
  • Take without regard to meals.
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)
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
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
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

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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23