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Antitumoral effects of R 75251 on the growth of transplantable R3327 prostatic adenocarcinoma in rats
Author(s) -
Van Ginckel R.,
De Coster R.,
Wouters W.,
Vanherck W.,
Van Veer R. Der,
Goeminne N.,
Jagers E.,
Van Cauteren H.,
Wouters L.,
Distelmans W.,
Janssen P. A. J.
Publication year - 1990
Publication title -
the prostate
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.295
H-Index - 123
eISSN - 1097-0045
pISSN - 0270-4137
DOI - 10.1002/pros.2990160406
Subject(s) - castration , endocrinology , medicine , testosterone (patch) , androgen , seminal vesicle , prostate , adenocarcinoma , renal capsule , capsule , kidney , biology , hormone , cancer , botany
The antitumoral activity of a novel imidazole derivative, R 75251, has been studied in the androgen‐dependent R3327G Dunning prostate adenocarcinoma grafted subcutaneously in syngeneic rats. Dietary application resulting approximately in dose levels of 80, 120, and 160 mg/kg reduced tumor weight by 66, 81, and 79%, respectively. This effect was not significantly different from that measured after castration (‐ 82%). In intact animals, however, serum testosterone levels were almost not affected by R 75 251 treatment while LH levels rose two‐ to threefold. In castrated rats a tenfold increase in LH was observed. Moreover, prostate and seminal vesicles weights decreased much less after R 75 251 treatment than after castration. In castrated animals, treatment with R 75 251 induced a slight, non‐significant reduction in tumor weight (‐ 36%) compared with castration alone. In castrated animals, tumor growth was restored by exogenous administration of testosterone. In such animals R 75 251 also significantly reduced tumor weight by 57%. Similar results were obtained with Dunning R3327G prostate adenocarcinoma grafted beneath the renal capsule in male syngeneic rats receiving twice daily orally by gavage a dose of 80 mg/kg of R 75 251. These data suggest that R 75 251 exerts an antitumoral effect independent of its inhibition of androgen biosynthesis.