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

Stem definitionDrug idCAS RN
thrombopoietin agonists 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: 4.81
  • 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:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.01 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
May 21, 2018 FDA AKARX INC
March 27, 2023 PMDA Swedish Orphan Biovitrum Japan Co., Ltd.

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 92.37 43.65 22 427 17689 63470884
Platelet count decreased 83.42 43.65 31 418 116091 63372482
Platelet count abnormal 62.87 43.65 12 437 3352 63485221
Headache 58.12 43.65 42 407 633199 62855374

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 61.80 39.58 23 320 62273 34894315
Platelet count decreased 53.47 39.58 25 318 119692 34836896

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 44.37 40.22 12 387 22394 79721595
Platelet count decreased 41.88 40.22 20 379 194644 79549345

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Thrombocytopenic disorder indication 302215000 DOID:1588




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 20MG BASE DOPTELET AKARX INC N210238 May 21, 2018 RX TABLET ORAL 8765764 Jan. 15, 2023 TREATMENT OF THROMBOCYTOPENIA IN AN ADULT PATIENT WITH CHRONIC LIVER DISEASE WHO IS SCHEDULED TO UNDERGO A PROCEDURE
EQ 20MG BASE DOPTELET AKARX INC N210238 May 21, 2018 RX TABLET ORAL 8765764 Jan. 15, 2023 TREATMENT OF THROMBOCYTOPENIA IN AN ADULT PATIENT WITH CHRONIC LIVER DISEASE WHO IS SCHEDULED TO UNDERGO A PROCEDURE USING DOPTELET
EQ 20MG BASE DOPTELET AKARX INC N210238 May 21, 2018 RX TABLET ORAL 8338429 June 30, 2023 TREATMENT OF THROMBOCYTOPENIA IN AN ADULT PATIENT WITH CHRONIC IMMUNE THROMBOCYTOPENIA WHO HAS HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

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 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
C3886460 UMLSCUI
CHEMBL2103883 ChEMBL_ID
9852519 PUBCHEM_CID
DB11995 DRUGBANK_ID
CHEMBL2105758 ChEMBL_ID
D10306 KEGG_DRUG
9571 INN_ID
9953 IUPHAR_LIGAND_ID
279520 MMSL
34258 MMSL
d08798 MMSL
017566 NDDF
017567 NDDF
770717002 SNOMEDCT_US
771571004 SNOMEDCT_US
895433008 SNOMEDCT_US
4037588 VANDF
2045726 RXNORM
C533238 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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