@article{6cfb4c7f8a254ebb84d9f38f261f7c64,
title = "Pet imaging agents (Fes, ffnp, and fdht) for estrogen, androgen, and progesterone receptors to improve management of breast and prostate cancers by functional imaging",
abstract = "Many breast and prostate cancers are driven by the action of steroid hormones on their cognate receptors in primary tumors and in metastases, and endocrine therapies that inhibit hormone production or block the action of these receptors provide clinical benefit to many but not all of these cancer patients. Because it is difficult to predict which individuals will be helped by endocrine therapies and which will not, positron emission tomography (PET) imaging of estrogen receptor (ER) and progesterone receptor (PgR) in breast cancer, and androgen receptor (AR) in prostate cancer can provide useful, often functional, information on the likelihood of endocrine therapy response in individual patients. This review covers our development of three PET imaging agents, 16α-[18 F]fluoroestradiol (FES) for ER, 21-[18 F]fluoro-furanyl-nor-progesterone (FFNP) for PgR, and 16β-[18 F]fluoro-5α-dihydrotestosterone (FDHT) for AR, and the evolution of their clinical use. For these agents, the pathway from concept through development tracks with an emerging understanding of critical performance criteria that is needed for successful PET imaging of these low-abundance receptor targets. Progress in the ongoing evaluation of what they can add to the clinical management of breast and prostate cancers reflects our increased understanding of these diseases and of optimal strategies for predicting the success of clinical endocrine therapies.",
keywords = "Breast cancer, Endocrine therapy, FDHT, FES, FFNP, Hormone-challenge test, PET imaging, Prostate cancer, Radiopharmaceuticals, Receptor-targeting",
author = "Katzenellenbogen, {John A.}",
note = "Funding Information: Funding: My research on the development of PET imaging agents for breast and prostate cancer has been funded over an extended period of time by grants from the National Institutes of Health (PHS 5R01CA015556) and the Department of Energy (DE FG02 86ER60401) Acknowledgments: I am grateful to the many graduate students and postdoctoral scientists in my laboratory who have contributed to the development of our ER, PR, and AR-targeted PET imaging agents. Although I am not able to name them all (see references from my laboratory cited in this review), I wish to acknowledge, as particularly central to this work, the contributions by Steven Senderoff, Scott Landvatter, Dale Kiesewetter, Kathryn Carlson, Martin Pomper, Aijun Liu, Henry VanBrocklin, Brad Buckman, and Sung Hoon Kim. At Washington University Medical School, the support of Mike Welch, as well as his friendship and that of his family, were immensely beneficial; critical as well was the help of many of his coworkers and colleagues, in particular, Karen McElvany, Carla, Mathias, Tim Tewson, Mike Kilbourn, and Dong Zhou, as well as Barry Siegel, Farrokh Dehdashti, Mark Mintun, Andrea McGuire, Joanne Mortimer, Ruby Chan, Amy Fowler, and Sally Schwarz. Support of my research over many years by grants from the National Institutes of Health, the Department of Energy, the American Cancer Society, and the Breast Cancer Research Foundation is gratefully acknowledged. I thank Farrokh Dehdashti and Barry Siegel (Washington University, St. Louis) and Steven Larson (Memorial Sloan Kettering Cancer Center, New York) for providing PET images used in this article. Publisher Copyright: {\textcopyright} 2020 by the author. Licensee MDPI, Basel, Switzerland.",
year = "2020",
month = aug,
doi = "10.3390/cancers12082020",
language = "English (US)",
volume = "12",
pages = "1--32",
journal = "Cancers",
issn = "2072-6694",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "8",
}