anagrelide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
platelet aggregation inhibitors 209 68475-42-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • anagrelide
  • xagrid
  • anagrelide hydrochloride
  • anagrelide hydrochloride hydrate
  • anagrelide HCl
  • anagrelide hydrochloride monohydrate
imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia
  • Molecular weight: 256.09
  • Formula: C10H7Cl2N3O
  • CLOGP: 1.02
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 44.70
  • ALOGS: -2.96
  • ROTB: 0

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.56 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 75 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Nov. 15, 2004 EMA SHIRE PHARMACEUTICALS IRELAND LIMITED
March 14, 1997 FDA SHIRE LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Myelofibrosis 103.66 43.69 15 271 323 2357476
Platelet count increased 93.79 43.69 18 268 2219 2355580
Acute myeloid leukaemia 78.36 43.69 16 270 2694 2355105
Palpitations 58.09 43.69 18 268 16438 2341361

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Platelet count increased 81.36 41.33 16 225 1605 1744935
Haemoglobin decreased 51.64 41.33 18 223 17096 1729444
Acute myeloid leukaemia 49.96 41.33 12 229 3029 1743511
Myelofibrosis 45.99 41.33 8 233 402 1746138

Pharmacologic Action:

SourceCodeDescription
ATC L01XX35 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
CHEBI has role CHEBI:48675 antifibrinolytic drug
CHEBI has role CHEBI:35554 cardiovascular drug
MeSH PA D002317 Cardiovascular Agents
MeSH PA D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
FDA PE N0000175972 Decreased Platelet Production
FDA EPC N0000175638 Platelet-reducing Agent
FDA MoA N0000175086 Phosphodiesterase 3 Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Essential thrombocythemia indication 109994006 DOID:2224
Thrombocytosis in Myeloproliferative Disease indication
High output heart failure contraindication 10091002
Heart disease contraindication 56265001 DOID:114
Hepatic failure contraindication 59927004
Interstitial pneumonia contraindication 64667001
Blood coagulation disorder contraindication 64779008 DOID:1247
Kidney disease contraindication 90708001 DOID:557
Interstitial lung disease contraindication 233703007 DOID:3082
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Eosinophilic asthma contraindication 367542003 DOID:9498

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.12 acidic
pKa2 3.82 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Enzyme INHIBITOR IC50 7.27 IUPHAR CHEMBL
cGMP-dependent 3',5'-cyclic phosphodiesterase Enzyme IC50 4.47 CHEMBL

External reference:

IDSource
4024077 VUID
N0000022082 NUI
C0051809 UMLSCUI
D02933 KEGG_DRUG
108976008 SNOMEDCT_US
d04126 MMSL
372561005 SNOMEDCT_US
596724 RXNORM
4024077 VANDF
006435 NDDF
CHEBI:142290 CHEBI
CHEMBL760 ChEMBL_ID
DB00261 DRUGBANK_ID
CHEMBL1200759 ChEMBL_ID
K9X45X0051 UNII
4672 INN_ID
58579-51-4 SECONDARY_CAS_RN
7114 IUPHAR_LIGAND_ID
135409400 PUBCHEM_CID
C021139 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Anagrelide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0172-5240 CAPSULE 1 mg ORAL ANDA 16 sections
Anagrelide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0172-5241 CAPSULE 0.50 mg ORAL ANDA 16 sections
anagrelide HUMAN PRESCRIPTION DRUG LABEL 1 13668-453 CAPSULE 0.50 mg ORAL ANDA 16 sections
anagrelide HUMAN PRESCRIPTION DRUG LABEL 1 13668-462 CAPSULE 1 mg ORAL ANDA 16 sections
Agrylin HUMAN PRESCRIPTION DRUG LABEL 1 54092-063 CAPSULE 0.50 mg ORAL NDA 17 sections
Anagrelide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54868-5385 CAPSULE 1 mg ORAL ANDA 11 sections
Anagrelide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54868-5443 CAPSULE 0.50 mg ORAL ANDA 11 sections
Anagrelide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68151-2959 CAPSULE 0.50 mg ORAL ANDA 17 sections