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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5379 1703793-34-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • avapritinib
  • BLU-285
  • ayvakit
Avapritinib is a tyrosine kinase inhibitor that targets PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants with half maximal inhibitory concentrations (IC50s) less than 25 nM. Certain mutations in PDGFRA and KIT can result in the autophosphorylation and constitutive activation of these receptors which can contribute to tumor cell proliferation. Other potential targets for avapritinib include wild type KIT, PDGFRB, and CSFR1.
  • Molecular weight: 498.57
  • Formula: C26H27FN10
  • CLOGP: 1.60
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 1
  • TPSA: 106.29
  • ALOGS: -4.22
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 24, 2020 EMA Blueprint Medicines (Netherlands) B.V.
Jan. 9, 2020 FDA BLUEPRINT MEDICINES

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX18 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
FDA MoA N0000020001 Tyrosine Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000185504 Cytochrome P450 2C9 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000191423 Multidrug and Toxin Extrusion Transporter 1 Inhibitors
FDA MoA N0000193845 Bile Salt Export Pump Inhibitors
FDA MoA N0000193932 Multidrug and Toxin Extrusion Transporter 2 K Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Gastrointestinal stromal tumor indication 420120006 DOID:9253

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.82 Basic
pKa2 6.22 Basic
pKa3 1.64 Basic
pKa4 1.05 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL Jan. 9, 2025 NEW CHEMICAL ENTITY
200MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL Jan. 9, 2025 NEW CHEMICAL ENTITY
300MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL Jan. 9, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Platelet-derived growth factor receptor alpha Kinase INHIBITOR IC50 9.62 SCIENTIFIC LITERATURE DRUG LABEL
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 9.57 SCIENTIFIC LITERATURE DRUG LABEL
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 7.66 SCIENTIFIC LITERATURE

External reference:

IDSource
513P80B4YJ UNII
4039082 VANDF
C4743552 UMLSCUI
CHEMBL4204794 ChEMBL_ID
DB15233 DRUGBANK_ID
118023034 PUBCHEM_CID
10613 INN_ID
C000707147 MESH_SUPPLEMENTAL_RECORD_UI
D11279 KEGG_DRUG
10368 IUPHAR_LIGAND_ID
2272107 RXNORM
329235 MMSL
37922 MMSL
d09480 MMSL
018251 NDDF
838409003 SNOMEDCT_US
838462005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-110 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-120 TABLET, FILM COATED 200 mg ORAL NDA 32 sections
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-125 TABLET, FILM COATED 25 mg ORAL NDA 32 sections
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-130 TABLET, FILM COATED 300 mg ORAL NDA 32 sections
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-150 TABLET, FILM COATED 50 mg ORAL NDA 32 sections