anagrelide ๐Ÿถ Veterinary Use | 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 ยตM/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 81.77 27.47 24 1019 14516 50589565
Myelofibrosis 62.85 27.47 12 1031 1135 50602946
Thrombocytosis 35.91 27.47 10 1033 4986 50599095
Adenocarcinoma metastatic 35.10 27.47 5 1038 75 50604006
Stress cardiomyopathy 31.40 27.47 10 1033 7877 50596204

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 51.43 28.82 16 831 8447 29565233
Myelofibrosis 34.10 28.82 8 839 1454 29572226

FDA Adverse Event Reporting System (Geriatric)

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 90.06 24.78 29 1662 18667 64478374
Thrombocytosis 46.62 24.78 14 1677 7142 64489899
Myelofibrosis 36.56 24.78 9 1682 2184 64494857
Stress cardiomyopathy 35.09 24.78 12 1679 9245 64487796
Congestive cardiomyopathy 33.79 24.78 12 1679 10332 64486709
Adenocarcinoma metastatic 32.68 24.78 5 1686 97 64496944
Platelet count abnormal 26.58 24.78 8 1683 4104 64492937

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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
D02933 KEGG_DRUG
823178-43-4 SECONDARY_CAS_RN
236612 RXNORM
C0051809 UMLSCUI
CHEBI:55345 CHEBI
J33 PDB_CHEM_ID
CHEMBL760 ChEMBL_ID
CHEMBL1200759 ChEMBL_ID
DB00261 DRUGBANK_ID
C021139 MESH_SUPPLEMENTAL_RECORD_UI
135409400 PUBCHEM_CID
7114 IUPHAR_LIGAND_ID
4672 INN_ID
K9X45X0051 UNII
4199 MMSL
58814 MMSL
d04126 MMSL
006435 NDDF
006436 NDDF
4021052 VANDF
4024077 VANDF
108976008 SNOMEDCT_US
108977004 SNOMEDCT_US
372561005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Anagrelide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0172-5240 CAPSULE 1 mg ORAL ANDA 26 sections
Anagrelide Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0172-5241 CAPSULE 0.50 mg ORAL ANDA 26 sections