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Androgen receptors (AR) mediated imaging of prostate in non-human primates (NHP) using F-18 FMDHT: Potential application to image human prostate cancer (PC)

¹ Radiology/PET Center, Wake Forest University Health Sciences, Winston-Salem, North Carolina; ² Psychiatry, Duke University Medical Center, Durham, North Carolina

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Objectives: While our main goal is to evaluate the efficacy of F-18 FMDHT to image PC in humans, current study focused on assessing the safety, in vivo kinetics, and imaging characteristics of F-18 FMDHT in NHP.

Methods: 9 whole body PET scans were performed in 3 NHP after injecting 7.5 ± 2.1 mCi F-18 FMDHT and scaning over 150 min. Depletion studies (1 mg Cetrorelix) and displacement studies (3.5 mg/kg 5-dihydrotestosterone (5-DHT)) were performed.

Results: The F-18 FMDHT was well tolerated by NHP (no adverse event) and showed favorable kinetics. Initial accumulation of tracer in various tissues was in concert with blood flow and rapidly cleared with time via the hipatobilliary excretion. No F-18 accumulation was seen in urinary bladder before 20 min. By 100 min, 2 ± 0.4 %ID was in urinary bladder, aiding better visualization of prostate. After initial peak, the prostate to muscle ratios (P:M) increased asymptotically and reached to 90% of the maximal values at 90 ± 7 min (P:M 4.5±0.8). Depletion of endogenous testosterone to increase available AR resulted in 20% P:M. In contrast, blockade of AR with 5-DHT resulted in two fold P:M. Most of the prostate uptake appeared to be AR dependent.

Conclusions: Tracer uptake in prostate corresponded to AR availability. These results show F-18 FMDHT is safe and effective ligand to image AR in NHP and has the potential to image PC in humans. Further studies are warranted to establish its role to image prostate cancer.

Research Support: NIH grant (RO1 to PKG; CA 105382).

This Article Services Email this article to a friend Similar articles in this journal Alert me to new issues of the journal Download to citation manager Google Scholar Articles by Garg, S. Articles by Garg, P. PubMed Articles by Garg, S. Articles by Garg, P.