PET Imaging of Steroid Hormone Receptor Expression

Abstract

Steroid hormone receptor (SHR) expression and changes in SHR expression compared to basal levels, whether upregulated, downregulated, or mutated, form a distinguishing feature of some breast, ovarian, and prostate cancers. These receptors act to induce tumor proliferation. In the imaging context, total expression together with modulation of expression can yield predictive and prognostic information. Currently, biopsy for histologic assessment of SHR expression is routine for breast and prostate cancer; however, the technique is not well suited to the heterogeneous tumor environment and can lead to incorrect receptor expression assignment, which precludes effective treatment. The development of positron emission tomography (PET) radioligands to image receptor expression may overcome the difficulties associated with tumor heterogeneity and facilitate the assessment of metastatic disease.

Recent Advances in Imaging Steroid Hormone Receptors in Breast Cancer

“…In a retrospective study of 46 patients with histologically confirmed invasive breast cancer reported by Yang et al, the optimal 18 F-fluoroestradiol threshold was 1.21 for SUV mean and 1.82 for SUV max (8). Thus, including previously published data, optimal 18 F-fluoroestradiol SUV max thresholds for distinguishing between ER-positive and ER-negative lesions ranged from 1.5 to 2.0 (1)(2)(3)(4)6).…”

“…The study highlighted the potential for 18 F-fluoroestradiol imaging to identify patients with acquired endocrine resistance who are unlikely to benefit from estradiol therapy indicated by poor 18 F-fluoroestradiol uptake. This study adds to landmark studies from Washington University and the University of Washington, which demonstrated a predictive value of 18 F-fluoroestradiol imaging for endocrine therapy benefit (1)(2)(3)(4).…”

“…Additional work has been published from teams at Memorial Sloan Kettering Cancer Center, The Netherlands, China, and Canada. Details of these articles are summarized in multiple review articles (1)(2)(3)(4). Recent investigations have built on this foundation and are highlighted herein.…”

PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging

“…The biodistribution of some radioiodinated nonsteroidal estrogens also looks very promising [ 56 ], and some work has been done to advance these and related agents for both imaging and targeted in vivo radiotherapy in preclinical breast cancer models [ 57 , 58 ]. Note is made of other recent reviews covering the development of PET imaging agents for ER [ 47 , 59 ].…”

Synthesis and pre-clinical evaluation of a [18F]fluoromethyl-tanaproget derivative for imaging of progesterone receptor expression

“…The use of the ER-targeted radioligand, 16α- involving primary and metastatic breast cancer. [8][9][10][11][12][13][14][15][16][17][18] Further integration of […”