avatrombopag 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,EIF2AK3,GRK2,ITK,MAPK10,MAPK7,PDK1,PDK2,PDK4,PRKDC,TTK 14
kinase-selectivity-class AXL,BRAF,CAMK2D,GRK2,MAPK7,MARK4,SIK2,STK33,TTK 9
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 decreased 205.54 41.08 73 1051 136896 90490427
Platelet count increased 137.56 41.08 35 1089 20824 90606499
Platelet count abnormal 116.64 41.08 23 1101 4312 90623011
Thrombocytosis 57.33 41.08 14 1110 6987 90620336
Myelofibrosis 52.50 41.08 10 1114 1557 90625766
Pulmonary embolism 50.83 41.08 27 1097 130793 90496530
Headache 48.32 41.08 56 1068 862690 89764633

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 decreased 107.32 41.90 48 580 138533 42482174
Platelet count increased 72.48 41.90 19 609 10684 42610023
Inappropriate schedule of product administration 42.95 41.90 23 605 95879 42524828

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 decreased 182.30 35.37 75 1166 230368 110357690
Platelet count increased 95.49 35.37 27 1214 26307 110561751
Platelet count abnormal 81.97 35.37 18 1223 6264 110581794
Thrombocytosis 57.99 35.37 15 1226 10429 110577629
Myelofibrosis 52.58 35.37 11 1230 3040 110585018
Pulmonary embolism 45.88 35.37 29 1212 214445 110373613
Drug ineffective 39.95 35.37 65 1176 1520475 109067583
Antiphospholipid syndrome 37.21 35.37 8 1233 2515 110585543

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
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

B02BX Other systemic hemostatics 10 drugs
carbazochromeconcizumabeltrombopagemicizumabetamsylatefitusiranfostamatiniblusutrombopagmarstacimab-hncqromiplostim

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)

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, 2026 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 July 24, 2028 TREATMENT OF THROMBOCYTOPENIA IN PEDIATRIC PATIENTS 6 YEARS AND OLDER WITH PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA, WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 10MG BASE DOPTELET SPRINKLE AKARX INC N219696 July 24, 2025 RX GRANULE ORAL July 24, 2028 NEW PRODUCT
EQ 20MG BASE DOPTELET AKARX INC N210238 May 21, 2018 RX TABLET ORAL July 24, 2032 TREATMENT OF THROMBOCYTOPENIA IN PEDIATRIC PATIENTS 1 YEAR AND OLDER WITH PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 10MG BASE DOPTELET SPRINKLE AKARX INC N219696 July 24, 2025 RX GRANULE ORAL July 24, 2032 TREATMENT OF THROMBOCYTOPENIA IN PEDIATRIC PATIENTS 1 YEAR AND OLDER WITH PERSISTENT OR 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
C3886460 UMLSCUI
CHEBI:750510 CHEBI
CHEMBL2103883 ChEMBL_ID
9852519 PUBCHEM_CID
DB11995 DRUGBANK_ID
CHEMBL2105758 ChEMBL_ID
D10306 KEGG_DRUG
9571 INN_ID
C533238 MESH_SUPPLEMENTAL_RECORD_UI
9953 IUPHAR_LIGAND_ID
770717002 SNOMEDCT_US
771571004 SNOMEDCT_US
895433008 SNOMEDCT_US
279520 MMSL
338087 MMSL
338089 MMSL
34258 MMSL
d08798 MMSL
017566 NDDF
017567 NDDF
2045726 RXNORM
3H8GSZ4SQL INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Doptelet Sprinkle HUMAN PRESCRIPTION DRUG LABEL 1 71369-010 GRANULE 10 mg ORAL NDA 31 sections
DOPTELET HUMAN PRESCRIPTION DRUG LABEL 1 71369-020 TABLET, FILM COATED 20 mg ORAL NDA 31 sections