TY - JOUR
T1 - Targeted Therapy for RET Fusion Lung Cancer
T2 - Breakthrough and Unresolved Issue
AU - Takamori, Shinkichi
AU - Matsubara, Taichi
AU - Haratake, Naoki
AU - Toyokawa, Gouji
AU - Fujishita, Takatoshi
AU - Toyozawa, Ryo
AU - Ito, Kensaku
AU - Yamaguchi, Masafumi
AU - Taguchi, Kenichi
AU - Okamoto, Tatsuro
AU - Seto, Takashi
N1 - Publisher Copyright:
© Copyright © 2021 Takamori, Matsubara, Haratake, Toyokawa, Fujishita, Toyozawa, Ito, Yamaguchi, Taguchi, Okamoto and Seto.
PY - 2021/8/23
Y1 - 2021/8/23
N2 - Molecular drugs targeting mutated or rearranged oncogene drivers have become one of the standard recognized treatments in patients with advanced and recurrent non-small cell lung cancer. RET is located in the long arm of human chromosome 10 and encodes a receptor tyrosine kinase protein, and RET fusion-positive lung adenocarcinoma occurs in 1%–2% of cases. Clinical trials of multikinase inhibitors, including cabozantinib, vandetanib, sorafenib, and lenvatinib, that inhibit RET oncogene activity have shown their antitumor efficacy. Recently, RET inhibitors such as pralsetinib and selpercatinib that are specialized for RET kinase have also been developed, and their efficacy was investigated in previous clinical trials (BLU-667 and LOXO-292). In this review, we summarized the effects and adverse events of multikinase and selective RET inhibitors and the various diagnostic techniques for RET gene fusion. In the perspective part, we focused on the unsolved issues on treatment for RET fusion-positive lung cancer and future developments.
AB - Molecular drugs targeting mutated or rearranged oncogene drivers have become one of the standard recognized treatments in patients with advanced and recurrent non-small cell lung cancer. RET is located in the long arm of human chromosome 10 and encodes a receptor tyrosine kinase protein, and RET fusion-positive lung adenocarcinoma occurs in 1%–2% of cases. Clinical trials of multikinase inhibitors, including cabozantinib, vandetanib, sorafenib, and lenvatinib, that inhibit RET oncogene activity have shown their antitumor efficacy. Recently, RET inhibitors such as pralsetinib and selpercatinib that are specialized for RET kinase have also been developed, and their efficacy was investigated in previous clinical trials (BLU-667 and LOXO-292). In this review, we summarized the effects and adverse events of multikinase and selective RET inhibitors and the various diagnostic techniques for RET gene fusion. In the perspective part, we focused on the unsolved issues on treatment for RET fusion-positive lung cancer and future developments.
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U2 - 10.3389/fonc.2021.704084
DO - 10.3389/fonc.2021.704084
M3 - Review article
AN - SCOPUS:85114357955
VL - 11
JO - Frontiers in Oncology
JF - Frontiers in Oncology
SN - 2234-943X
M1 - 704084
ER -