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Review
. 2022 Feb;24(2):151-159.
doi: 10.1007/s11912-021-01165-0. Epub 2022 Jan 21.

New Tyrosine Kinase Inhibitors for the Treatment of Gastrointestinal Stromal Tumors

César Serrano  1   2 , Sebastian Bauer  3   4
Affiliations
Review

New Tyrosine Kinase Inhibitors for the Treatment of Gastrointestinal Stromal Tumors

César Serrano et al. Curr Oncol Rep. 2022 Feb.

Abstract

Purpose of review: This article critically revisits novel data on tyrosine kinase inhibitors that have shown clinical activity in the treatment of gastrointestinal stromal tumor (GIST).

Recent findings: GIST therapeutic development exploits the oncogene addiction to KIT or PDGFRA receptor tyrosine kinases. Based on this principle, two new drugs were approved in 2020: ripretinib in GIST patients after progression to all standard treatments and avapritinib, the first agent ever active in the multiresistant PDGFRA D842V-mutant GIST. Additionally, cabozantinib has also shown encouraging activity in imatinib-resistant GIST patients. Finally, novel agents targeting NTRK-driven GIST have emerged as a breakthrough for the treatment of a subset of KIT/PDGFRA wild-type GIST patients. GIST is a paradigmatic tumor model for the rational and successful development of molecularly targeted agents directed against driver mutations in cancer.

Keywords: Avapritinib; Cabozantinib; GIST; Imatinib; NTRK; Ripretinib.

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References

Papers of particular interest, published recently, have been highlighted as: • Of importance •• Of major importance
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