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avapritinib

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Associated Genetic Biomarkers
Associated Diseases

Overview

Trade Name(s):
Ayvakit
NCI Definition [1]:
An orally bioavailable inhibitor of specific mutated forms of platelet-derived growth factor receptor alpha (PDGFR alpha; PDGFRa) and mast/stem cell factor receptor c-Kit (SCFR), with potential antineoplastic activity. Upon oral administration, BLU-285 specifically binds to and inhibits specific mutant forms of PDGFRa and c-Kit, including the PDGFRa D842V mutant and various KIT exon 17 mutants. This results in the inhibition of PDGFRa- and c-Kit-mediated signal transduction pathways and the inhibition of proliferation in tumor cells that express these PDGFRa and c-Kit mutants. PDGFRa and c-Kit, protein tyrosine kinases and tumor-associated antigens (TAAs), are mutated in various tumor cell types; they play key roles in the regulation of cellular proliferation.

Biomarker-Directed Therapies

Clinical Trials

View Clinical Trials for avapritinib

Avapritinib has been investigated in 3 clinical trials, of which 3 are open and 0 are closed. Of the trials investigating avapritinib, 1 is phase 1 (1 open), 1 is phase 2 (1 open), and 1 is phase 3 (1 open).

PDGFRA Mutation, KIT Mutation, and AKT1 Amplification are the most frequent biomarker inclusion criteria for avapritinib clinical trials.

Gastrointestinal stromal tumor, hematopoietic and lymphoid system neoplasm, and malignant solid tumor are the most common diseases being investigated in avapritinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Avapritinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating avapritinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
blu-285, pdgfr alpha/kit mutant-specific inhibitor blu-285, avapritinib, ayvakit
Drug Categories [2]:
Tyrosine kinase inhibitors
Drug Target(s) [2]:
KIT, PDGFRA
NCIT ID [1]:
C123827

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.