1992
DOI: 10.1002/pros.2990200306
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Blockade of the LH response induced by the agonist D‐Trp‐6‐LHRH in rats by a highly potent LH‐RH antagonist SB‐75

Abstract: During treatment of prostate cancer patients with luteinizing hormone-releasing hormone agonist, a transient LH and sex steroid release, which precedes the secretion blockade, may result in a flare-up of the disease, whereas the antagonists induce an immediate suppression. The administration of the modern, superactive LHRH antagonist SB-75 before or together with the agonist D-Trp-6-LHRH should prevent the "flare-up" phenomena. In order to demonstrate that the LHRH antagonist can prevent the initial stimulatio… Show more

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Cited by 14 publications
(10 citation statements)
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References 37 publications
(35 reference statements)
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“…The apparently opposing impact of GnRHant on GnRHa-induced down-regulation of pituitary receptors raises interesting questions regarding the potential effects of concurrent administration. Regarding the impact of GnRHant on the GnRHa-induced flare-up phenomenon, GnRHant partially inhibited the initial flare-up caused by GnRHa treatment in this study, and Pinski et al [15] described that pretreatment with GnRHant (500 or 1000 mg/rat) 1 hour before GnRHa (50 mg/rat) in male rats could completely prevent the elevation of LH. However, GnRHant did not diminish GnRHa-induced gonadotropin desensitization during prolonged treatment in the present study.…”
Section: Discussionsupporting
confidence: 57%
“…The apparently opposing impact of GnRHant on GnRHa-induced down-regulation of pituitary receptors raises interesting questions regarding the potential effects of concurrent administration. Regarding the impact of GnRHant on the GnRHa-induced flare-up phenomenon, GnRHant partially inhibited the initial flare-up caused by GnRHa treatment in this study, and Pinski et al [15] described that pretreatment with GnRHant (500 or 1000 mg/rat) 1 hour before GnRHa (50 mg/rat) in male rats could completely prevent the elevation of LH. However, GnRHant did not diminish GnRHa-induced gonadotropin desensitization during prolonged treatment in the present study.…”
Section: Discussionsupporting
confidence: 57%
“…Experimental data were conducted using LHRH antagonists which directly block the LHRH receptor and result in immediate suppression of androgen production (Pinski et al 1992). Unfortunately, early results were associated with histamine releasing anaphylactoid reaction, relative water insolubility, and the necessity of using acidic formulation for delivery (Garnick 1997).…”
Section: Results Of Androgen Withdrawal Monotherapymentioning
confidence: 99%
“…These experimental results suggest a regulatory role for LHRH-like peptides on tumor growth (14,18,21,27,28). Consequently LHRH antagonists like Cetrorelix could be considered for the development of new therapies for LHRH receptor positive cancers (17).…”
Section: Introductionmentioning
confidence: 88%