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

Stem definitionDrug idCAS RN
5285 570406-98-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • avatrombopag
  • avatrombopag maleate
  • E5501
  • E5501 maleate
  • AKR-501
  • YM477
  • doptelet
Avatrombopag is an orally bioavailable, small molecule TPO receptor agonist that stimulates proliferation and differentiation of megakaryocytes from bone marrow progenitor cells resulting in an increased production of platelets. Avatrombopag does not compete with TPO for binding to the TPO receptor and has an additive effect with TPO on platelet production.
  • Molecular weight: 649.65
  • Formula: C29H34Cl2N6O3S2
  • CLOGP: 4.13
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 2
  • TPSA: 101.90
  • ALOGS: -5.15
  • ROTB: 7

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 21, 2018 FDA AKARX 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
Headache 52.26 46.84 29 168 478323 46207542

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
Inappropriate schedule of product administration 58.99 43.12 18 182 39710 29912568

Pharmacologic Action:

SourceCodeDescription
ATC B02BX08 BLOOD AND BLOOD FORMING ORGANS
ANTIHEMORRHAGICS
VITAMIN K AND OTHER HEMOSTATICS
Other systemic hemostatics

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Thrombocytopenic disorder indication 302215000 DOID:1588

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.35 acidic
pKa2 7.33 acidic
pKa3 8.93 Basic
pKa4 1.19 Basic
pKa5 0.65 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 20MG BASE DOPTELET AKARX INC N210238 May 21, 2018 RX TABLET ORAL June 26, 2022 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 20MG BASE DOPTELET AKARX INC N210238 May 21, 2018 RX TABLET ORAL May 21, 2023 NEW CHEMICAL ENTITY
EQ 20MG BASE DOPTELET AKARX INC N210238 May 21, 2018 RX TABLET ORAL June 26, 2026 TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Thrombopoietin receptor Membrane receptor AGONIST EC50 8.48 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
3H8GSZ4SQL UNII
677007-74-8 SECONDARY_CAS_RN
4037588 VANDF
C2607237 UMLSCUI
CHEMBL2103883 ChEMBL_ID
CHEMBL2105758 ChEMBL_ID
DB11995 DRUGBANK_ID
D10306 KEGG_DRUG
9852519 PUBCHEM_CID
9571 INN_ID
C533238 MESH_SUPPLEMENTAL_RECORD_UI
9953 IUPHAR_LIGAND_ID
2045726 RXNORM
279520 MMSL
34258 MMSL
d08798 MMSL
017566 NDDF
017567 NDDF
770717002 SNOMEDCT_US
771571004 SNOMEDCT_US
895433008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DOPTELET HUMAN PRESCRIPTION DRUG LABEL 1 71369-020 TABLET, FILM COATED 20 mg ORAL NDA 29 sections