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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5280 901119-35-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tavlesse
  • fostamatinib
  • fostamatinib disodium
  • tavalisse
  • R935788
  • R788
Fostamatinib is a tyrosine kinase inhibitor with demonstrated activity against spleen tyrosine kinase (SYK). The major metabolite of fostamatinib, R406, inhibits signal transduction of Fc-activating receptors and B-cell receptor. The fostamatinib metabolite R406 reduces antibody-mediated destruction of platelets.
  • Molecular weight: 580.47
  • Formula: C23H26FN6O9P
  • CLOGP: 1.47
  • LIPINSKI: 2
  • HAC: 15
  • HDO: 4
  • TPSA: 186.72
  • ALOGS: -4.05
  • ROTB: 10

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 9, 2020 EMA Instituto Grifols S.A.
April 17, 2018 FDA RIGEL PHARMS INC

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 decreased 56.00 40.16 18 131 100006 46585907

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

Pharmacologic Action:

SourceCodeDescription
ATC B02BX09 BLOOD AND BLOOD FORMING ORGANS
ANTIHEMORRHAGICS
VITAMIN K AND OTHER HEMOSTATICS
Other systemic hemostatics

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Immune thrombocytopenia indication 2897005 DOID:1587

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.54 acidic
pKa2 6.59 acidic
pKa3 5.0 Basic
pKa4 4.34 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE TAVALISSE RIGEL PHARMS INC N209299 April 17, 2018 RX TABLET ORAL April 17, 2023 NEW CHEMICAL ENTITY
EQ 150MG BASE TAVALISSE RIGEL PHARMS INC N209299 April 17, 2018 RX TABLET ORAL April 17, 2023 NEW CHEMICAL ENTITY
EQ 100MG BASE TAVALISSE RIGEL PHARMS INC N209299 April 17, 2018 RX TABLET ORAL April 17, 2025 FOR THE TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE TAVALISSE RIGEL PHARMS INC N209299 April 17, 2018 RX TABLET ORAL April 17, 2025 FOR THE TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase SYK Kinase INHIBITOR IC50 7.39 SCIENTIFIC LITERATURE DRUG LABEL
Adenosine receptor A3 GPCR INHIBITOR IC50 7.09 SCIENTIFIC LITERATURE

External reference:

IDSource
914295-16-2 SECONDARY_CAS_RN
841290-80-0 SECONDARY_CAS_RN
4037543 VANDF
C2713632 UMLSCUI
C4730994 UMLSCUI
2RC PDB_CHEM_ID
CHEMBL2103830 ChEMBL_ID
CHEMBL3989516 ChEMBL_ID
DB12010 DRUGBANK_ID
D09347 KEGG_DRUG
C523665 MESH_SUPPLEMENTAL_RECORD_UI
7796 IUPHAR_LIGAND_ID
9022 INN_ID
SQ8A3S5101 UNII
11671467 PUBCHEM_CID
11213558 PUBCHEM_CID
5706 IUPHAR_LIGAND_ID
DB07159 DRUGBANK_ID
RC3A285J2G UNII
2044896 RXNORM
276522 MMSL
d08782 MMSL
017516 NDDF
017517 NDDF
772033003 SNOMEDCT_US
772039004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TAVALISSE HUMAN PRESCRIPTION DRUG LABEL 1 71332-001 TABLET 100 mg ORAL NDA 28 sections
TAVALISSE HUMAN PRESCRIPTION DRUG LABEL 1 71332-002 TABLET 150 mg ORAL NDA 28 sections