Avapritinib

Chemical formula: C₂₆H₂₇FN₁₀  Molecular mass: 498.57 g/mol  PubChem compound: 118023034

Active ingredient description

Avapritinib is a Type 1 kinase inhibitor that has demonstrated biochemical in vitro activity on the PDGFRA D842V and KIT D816V mutants associated with resistance to imatinib, sunitinib and regorafenib with half maximal inhibitory concentrations (IC50) of 0.24 nM and 0.27 nM, respectively, and greater potency against clinically relevant KIT exon 11, KIT exon 11/17 and KIT exon 17 mutants than against the KIT wild-type enzyme.

Medicine classification

This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:

ATC Group Classification
L01EX18 L Antineoplastic and immunomodulating agents → L01 Antineoplastic agents → L01E Protein kinase inhibitors → L01EX Other protein kinase inhibitors
Discover more medicines within L01EX18

Product monographs

Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):

Document Type Information Source  
 AYVAKIT Film-coated tablet MPI, US: SPL/PLR FDA, National Drug Code (US)
 AYVAKYT Film-coated tablet MPI, EU: SmPC European Medicines Agency (EU)

Structural formula

Graphic representation of the active ingredient's molecular structure

External identifiers

CAS Substance: 1703793-34-3
DrugBank Drug: DB15233
PubChem Compound: 118023034
RxNorm Ingredient: 2272107
SNOMED-CT Concept: 838462005
Avapritinib (substance)
UNII Identifier: 513P80B4YJ
AVAPRITINIB

Medicines

Avapritinib is an active ingredient of these brands:

Austria (AT)

Croatia (HR)

Estonia (EE)

France (FR)

Ireland (IE)

Lithuania (LT)

Poland (PL)

Romania (RO)

United Kingdom (UK)

United States (US)

Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide.

 
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