Tumor localization of 16β-(18)F-fluoro-5α- dihydrotestosterone versus (18)F-FDG in patients with progressive, metastatic prostate cancer Journal Article


Authors: Larson, S. M.; Morris, M.; Guenther, I.; Beattie, B.; Humm, J. L.; Akhurst, T.; Finn, R. D.; Erdi, Y.; Pentlow, K.; Dyke, J.; Squire, O.; Bornmann, W.; McCarthy, T.; Welch, M.; Scher, H.
Article Title: Tumor localization of 16β-(18)F-fluoro-5α- dihydrotestosterone versus (18)F-FDG in patients with progressive, metastatic prostate cancer
Abstract: This trial was an initial assessment of the feasibility, in vivo targeting, and biokinetics of 16β-18F-fluoro-5α-dihydrotestosterone (18F-FDHT) PET in patients with metastatic prostate cancer to assess androgen receptor expression. Methods: Seven patients with progressive clinically metastatic prostate cancer underwent 18F-FDG and 18F-FDHT PET scans in addition to conventional imaging methods. Three patients had their studies repeated 1 mo later, 2 while on testosterone therapy, and the third after treatment with 17-allylamino-17- demethoxygeldanamycin (17-AAG). High-pressure liquid radiochromatography was used to separate 18F-FDHT from radiolabeled metabolites. Lesion-by-lesion comparisons between the 18F-FDHT, 18F-FDG, and conventional imaging methods were performed. Results: Metabolism of 18F-FDHT was rapid, with 80% conversion within 10 min to radiolabeled metabolites that circulated bound to plasma proteins. Tumor uptake was rapid and tumor retention was prolonged. Fifty-nine lesions were identified by conventional imaging methods. 18F-FDG PET was positive in 57 of 59 lesions (97%), with an average lesion maximum standardized uptake value (SUVmax) = 5.22. 18F-FDHT PET was positive in 46 of 59 lesions (78%), with the average positive lesion SUVmax = 5.28. Treatment with testosterone resulted in diminished 18F-FDHT uptake at the tumor site. Conclusion: 18F-FDHT localizes to tumor sites in patients with progressive clinically metastatic prostate cancer and may be a promising agent to analyze antigen receptors and their impact on the clinical management of prostate cancer.
Keywords: adult; clinical article; controlled study; aged; bone neoplasms; middle aged; bone tumor; unclassified drug; clinical trial; cancer growth; comparative study; methodology; sensitivity and specificity; radiopharmaceuticals; reproducibility; reproducibility of results; metabolism; tumor localization; metastasis; validation study; prostate cancer; prostatic neoplasms; goserelin; leuprorelin; diagnostic agent; tissue distribution; celecoxib; prostate tumor; fluorodeoxyglucose f 18; computer assisted emission tomography; fluorodeoxyglucose f18; radiopharmaceutical agent; drug derivative; scintiscanning; metabolic clearance rate; androgen receptor; orchiectomy; receptors, androgen; whole body counting; whole-body counting; fluorine 18; pet; 16beta fluoro 5alpha dihydrotestosterone f 18; testosterone; androstanolone; tomography, emission-computed; geldanamycin; pamidronic acid; dihydrotestosterone; humans; human; male; priority journal; article; 16β-18f-fluoro-5α-dihydrotestosterone; 17 allyamno 17 demethoxygeldanamycin; 11 fluoro dihydro testosterone; 11-fluoro-dihydro-testosterone
Journal Title: Journal of Nuclear Medicine
Volume: 45
Issue: 3
ISSN: 0161-5505
Publisher: Society of Nuclear Medicine  
Date Published: 2004-03-01
Start Page: 366
End Page: 373
Language: English
PROVIDER: scopus
DOI/URL:
Notes: J. Nucl. Med. -- Cited By (since 1996):160 -- Export Date: 16 June 2014 -- CODEN: JNMEA -- Source: Scopus