Avapritinib: First Approval.

Abstract:

:Avapritinib (AYVAKIT™) is a potent and selective tyrosine kinase inhibitor of platelet-derived growth factor receptor alpha (PDGFRA) and KIT activation loop mutants. It is being developed by Blueprint Medicines for the treatment of gastrointestinal stromal tumours (GIST), solid tumours and systemic mastocytosis. Avapritinib is approved in the USA for PDGFRA exon 18 (including D842V) mutant GIST and is undergoing regulatory assessment in the USA as a 4th-line treatment for GIST. Avapritinib is also undergoing regulatory assessment in the EU for PDGFRA D842V mutant GIST. This article summarizes the milestones in the development of avapritinib leading to this first approval for the treatment of adults with unresectable or metastatic GIST harbouring a PDGFRA exon 18 mutation, including PDGFRA D842V mutations. Clinical development of avapritinib is also underway for the treatment of systemic mastocytosis and late-stage solid tumours in several countries.

journal_name

Drugs

journal_title

Drugs

authors

Dhillon S

doi

10.1007/s40265-020-01275-2

subject

Has Abstract

pub_date

2020-03-01 00:00:00

pages

433-439

issue

4

eissn

0012-6667

issn

1179-1950

pii

10.1007/s40265-020-01275-2

journal_volume

80

pub_type

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