This investigation on 12 well-defined patients with untreated, advanced prostatic adenocarcinoma establishes the gonadotropin-releasing hormone analogue [D-Ser(Bu^t)6]LH-RH( 1-9)-nonapeptide-ethylamide (Hoe 766) as an effective, safe and non-toxic form of medical castration. Hoe 766 was given either as subcutaneous injections of 2 X 200 μg/day over 14 days and pemasal application (3 X 400 μg/day) thereafter, or as subcutaneous injections of 3 X 1,000 μg/day over 6 days and pemasal application thereafter in the dosage mentioned above. Both dose regimens were equally effective: pituitary overstimulation between days 3 and 6 with a rise of serum LH and testosterone; pituitary and testicular desensitization with LH and testosterone decline between days 6 and 14; medical castration with average serum testosterone levels maintained around 0.5 ng/ml for up to 12 weeks. Except for transient hot flashes in 4 patients, no clinical or laboratory side effects were observed. It is concluded from this study that the gonadotropinreleasing hormone analogue, Hoe 766, is a valuable alternative to conventional contrasexual measures for prostate cancer palliation. To improve the patient’s compliance, however, the smallest single pemasal dosage effective for maintenance of down-regulation and steroidogenic arrest has still to be determined.

Keywords:
Gonadotropin-releasing hormone analogue, Desensitization of gonadotrophs, Luteinizing hormone, Testosterone, Prostatic carcinoma, Medical castration
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1982
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