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Comment
. 2018 Jul;8(7):797-799.
doi: 10.1158/2159-8290.CD-18-0489.

Stop fRETting the Target: Next-Generation RET Inhibitors Have Arrived

Wade T Iams  1 , Christine M Lovly  2
Affiliations
Comment

Stop fRETting the Target: Next-Generation RET Inhibitors Have Arrived

Wade T Iams et al. Cancer Discov. 2018 Jul.

Abstract

BLU-667 is a next-generation RET inhibitor that maximizes on-target and minimizes off-target effects. It is an exemplar of genotype-driven drug development followed by multi-histology basket trial validation that is becoming a paradigm for precision oncology. Cancer Discov; 8(7); 797-9. ©2018 AACRSee related article by Subbiah et al., p. 836.

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Conflict of interest statement

Disclosure of Potential Conflicts of Interest

C.M. Lovly reports receiving commercial research support from Novartis, Xcovery, and AstraZeneca and is a consultant/advisory board member for Cepheid, Foundation Medicine, Takeda, Pfizer. Ariad, AstraZeneca, Novartis, Clovis, and Genoptix. No potential conflicts of interest were disclosed by the other author.

Figures

Figure 1.
Figure 1.
RET alterations by histology and mutation type with current RET Inhibitors. RET-driven cancers tend to harbor either chromosomal rearrangements or point mutations in the RET extracellular domain or tyrosine kinase domain. A variety of multikinase inhibitors have been applied in patients with RET-driven cancer; however, BLU-667 and LOXO-292 are two next-generation RET inhibitors now being broadly applied to patients whose tumors harbor these oncogenic RET alterations.
See this image and copyright information in PMC

Comment on

  • Precision Targeted Therapy with BLU-667 for RET-Driven Cancers.
    Subbiah V, Gainor JF, Rahal R, Brubaker JD, Kim JL, Maynard M, Hu W, Cao Q, Sheets MP, Wilson D, Wilson KJ, DiPietro L, Fleming P, Palmer M, Hu MI, Wirth L, Brose MS, Ou SI, Taylor M, Garralda E, Miller S, Wolf B, Lengauer C, Guzi T, Evans EK. Subbiah V, et al. Cancer Discov. 2018 Jul;8(7):836-849. doi: 10.1158/2159-8290.CD-18-0338. Epub 2018 Apr 15. Cancer Discov. 2018. PMID: 29657135

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