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
Platelet count increased 122.56 25.77 37 1559 14837 46669629
Myelofibrosis 84.77 25.77 17 1579 1242 46683224
Acute myeloid leukaemia 45.77 25.77 18 1578 15760 46668706
Thrombocytosis 39.23 25.77 12 1584 4990 46679476
Adenocarcinoma metastatic 32.96 25.77 5 1591 69 46684397
Transient ischaemic attack 32.13 25.77 18 1578 34885 46649581
Haemoglobin decreased 28.35 25.77 28 1568 128921 46555545

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 66.60 26.34 21 1117 8721 29942619
Myelofibrosis 51.77 26.34 12 1126 1559 29949781
Essential thrombocythaemia 33.82 26.34 5 1133 51 29951289
Thrombocytosis 33.63 26.34 10 1128 3403 29947937
Community acquired infection 27.54 26.34 3 1135 0 29951340
Haemoglobin decreased 26.95 26.34 27 1111 114071 29837269

Pharmacologic Action:

SourceCodeDescription
ATC L01XX35 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
FDA MoA N0000175086 Phosphodiesterase 3 Inhibitors
FDA EPC N0000175638 Platelet-reducing Agent
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
CHEBI has role CHEBI:48675 antifibrinolytic agents
CHEBI has role CHEBI:50427 platelet aggregation inhibitors
CHEBI has role CHEBI:35554 cardiovascular drugs
CHEBI has role CHEBI:50249 anticoagulante

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
K9X45X0051 UNII
4024077 VUID
N0000022082 NUI
D02933 KEGG_DRUG
823178-43-4 SECONDARY_CAS_RN
C0051809 UMLSCUI
CHEBI:55345 CHEBI
CHEMBL760 ChEMBL_ID
CHEMBL1200759 ChEMBL_ID
DB00261 DRUGBANK_ID
135409400 PUBCHEM_CID
4672 INN_ID
C021139 MESH_SUPPLEMENTAL_RECORD_UI
7114 IUPHAR_LIGAND_ID
236612 RXNORM
4199 MMSL
58814 MMSL
d04126 MMSL
006435 NDDF
006436 NDDF
108976008 SNOMEDCT_US
108977004 SNOMEDCT_US
372561005 SNOMEDCT_US
4021052 VANDF
4024077 VANDF

Pharmaceutical products:

None