avapritinib Indications/Contra | FAERs | Orange Book | 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

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 9, 2020 FDA BLUEPRINT MEDICINES

FDA Adverse Event Reporting System

None

Pharmacologic Action:

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9200002 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
100MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9944651 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
100MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9994575 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
200MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9200002 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
200MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9944651 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
200MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9994575 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
300MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9200002 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
300MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9944651 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
300MG AYVAKIT BLUEPRINT MEDICINES N212608 Jan. 9, 2020 RX TABLET ORAL 9994575 Oct. 15, 2034 TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION

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
10613 INN_ID
2272107 RXNORM
4039082 VANDF
37922 MMSL
d09480 MMSL
018251 NDDF
118023034 PUBCHEM_CID
10368 IUPHAR_LIGAND_ID
DB15233 DRUGBANK_ID
CHEMBL4204794 ChEMBL_ID
D11279 KEGG_DRUG

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-110 TABLET, FILM COATED 100 mg ORAL NDA 17 sections
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-120 TABLET, FILM COATED 200 mg ORAL NDA 17 sections
Ayvakit HUMAN PRESCRIPTION DRUG LABEL 1 72064-130 TABLET, FILM COATED 300 mg ORAL NDA 17 sections