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lüll 4,16alpha- 16alpha-(18)F Difluoro-11beta-methoxyestradiol Leung KMolecular Imaging and Contrast Agent Database (MICAD)-/-ä 2004[]; ä (ä): äEstrogens and progestins are endogenous hormones that produce many physiological effects (1). Estrogens act primarily by regulating gene expression. Estrogen receptors (ERs) are found in the nucleus of cells of the female reproductive tract, breast, pituitary, hypothalamus, bone, liver, and other tissues, and also in various tissues in men. Estrogens are lipophilic in that they enter the cell passively by diffusion through the cellular membrane. They bind to ERs that are present in the nucleus. Breast cancer is the most common malignancy in women. Approximately 33% of women who have this disease will die of disseminated breast cancer. The growth of breast epithelial cells is dependent on estrogen stimulation to induce progestin receptor expression. Two-thirds of breast carcinomas express ERs. It has also been established that the ER status of the tumor is an important prognostic indicator in breast cancer (2). Women with ER-positive breast tumors have a better prognosis than women with ER-negative tumors in terms of responsiveness to anti-estrogen treatment. ER content in breast cancer was assessed in vitro with receptor binding assays, which suffer from interassay variability and are also limited by intrinsic receptor heterogeneity of the tumor. 16alpha-[(18)F]Fluoro-17beta-estradiol ([(18)F]FES) has been proven to be a valuable tracer for studies of the ER status of primary and metastatic breast cancer (3). However, [(18)F]FES is cleared from the blood and metabolized in 20 min with only 20% of [(18)F]FES intact in a study with 15 breast cancer patients (4). A newly developed estradiol analog, 4,16alpha-[16alpha-(18)F]difluoro-11beta-methoxyestradiol (4F-M[(18)F]FES), exhibited favorable biodistribution in small animals and high uterus/background ratios in rodents (5) and humans (6).ä |