@article{ca27d28b446c4e0eb13a56e6e06b3eb4,
title = "Precision therapy for RET-altered cancers with RET inhibitors",
abstract = "Rearranged during transfection (RET) is involved in the physiological development of some organ systems. Activating RET alterations via either gene fusions or point mutations are potent oncogenic drivers in non-small cell lung cancer, thyroid cancer, and in multiple diverse cancers. RET-altered cancers were initially treated with multikinase inhibitors (MKIs). The efficacy of MKIs was modest at the expense of notable toxicities from their off-target activity. Recently, highly potent and RET-specific inhibitors selpercatinib and pralsetinib were successfully translated to the clinic and FDA approved. We summarize the current state-of-the-art therapeutics with preclinical and clinical insights of these novel RET inhibitors, acquired resistance mechanisms, and future outlooks.",
keywords = "BLU-667 (pralsetinib), LOXO-292 (selpercatinib), RET-altered cancers, lung cancer, multikinase inhibitors, thyroid cancer",
author = "Thein, {Kyaw Z.} and Vamsidhar Velcheti and Mooers, {Blaine H.M.} and Jie Wu and Vivek Subbiah",
note = "Funding Information: National Institutes of Health grant R01CA242845 (to B.H.M.M., V.S., and J.W.). V.S. is an Andrew Sabin Family Foundation Fellow at The University of Texas MD Anderson Cancer Center. V.S. acknowledges support of The Jacquelyn A. Brady Fund. MD Anderson Cancer Center Department of Investigational Cancer Therapeutics is supported by the Cancer Prevention and Research Institute of Texas ( RP1100584 ), the Sheikh Khalifa Bin Zayed Al Nahyan Institute for Personalized Cancer Therapy , 1U01 CA180964 , NCATS Grant UL1 TR000371 ( Center for Clinical and Translational Sciences ), and the MD Anderson Cancer Center Support Grant ( P30 CA016672 ). Funding Information: National Institutes of Health grant R01CA242845 (to B.H.M.M. V.S. and J.W.). V.S. is an Andrew Sabin Family Foundation Fellow at The University of Texas MD Anderson Cancer Center. V.S. acknowledges support of The Jacquelyn A. Brady Fund. MD Anderson Cancer Center Department of Investigational Cancer Therapeutics is supported by the Cancer Prevention and Research Institute of Texas (RP1100584), the Sheikh Khalifa Bin Zayed Al Nahyan Institute for Personalized Cancer Therapy, 1U01 CA180964, NCATS Grant UL1 TR000371 (Center for Clinical and Translational Sciences), and the MD Anderson Cancer Center Support Grant (P30 CA016672). V.S. reports research funding/grant support for clinical trials: Roche/Genentech, Novartis, Bayer, GlaxoSmithKline, Nanocarrier, Vegenics, Celgene, Northwest Biotherapeutics, Berghealth, Incyte, Fujifilm, Pharmamar, D3, Pfizer, Multivir, Amgen, Abbvie, Alfa-sigma, Agensys, Boston Biomedical, Idera Pharma, Inhibrx, Exelixis, Blueprint Medicines, Loxo Oncology, Medimmune, Altum, Dragonfly Therapeutics, Takeda and National Comprehensive Cancer Network, NCI-CTEP and UT MD Anderson Cancer Center, Turning Point Therapeutics, Boston Pharmaceuticals; Travel: Novartis, Pharmamar, ASCO, ESMO, Helsinn, Incyte. Consultancy/advisory board: Helsinn, LOXO Oncology/Eli Lilly, R-Pharma US, INCYTE, QED pharma, Medimmune, Novartis. Other: Medscape. All remaining authors have declared no conflicts of interest. Publisher Copyright: {\textcopyright} 2021 The Authors",
year = "2021",
month = dec,
doi = "10.1016/j.trecan.2021.07.003",
language = "English (US)",
volume = "7",
pages = "1074--1088",
journal = "Trends in Cancer",
issn = "2405-8033",
publisher = "Cell Press",
number = "12",
}