DISEASE FLARE INDUCED BY D-Trp6-LHRH ANALOGUE IN PATIENTS WITH METASTATIC PROSTATIC CANCER

Pharmacological Profile of a New, Potent, and Long-Acting Gonadotropin-Releasing Hormone Antagonist: Degarelix

“…Such pathologies are currently managed with longacting (1 or 3 months) formulations of GnRH agonists that initially stimulate pituitary LH and follicle-stimulating hormone release as well as gonadal steroids, and then, after 2 to 4 weeks, desensitize the gonadotrophs, leading to suppression of gonadotropin and sex steroids. However, in clinical situations where an immediate suppression of the gonadotropins is required, the major disadvantage of agonists is their initial stimulatory effect on hormone release that may lead to a transient flare-up of the disease (Kahan et al, 1984). In this context, competitive GnRH antagonists are expected to have significant clinical advantages on the basis of the avoidance of this initial stimulation of gonadotropin release and a faster onset of action (Balmaceda et al, 1983;Cetel et al, 1983).…”

A Randomized Comparison of the Clinical and Hormonal Effects of Two GnRH Agonists in Patients with Prostate Cancer

“…These characteristics are not similar from one GnRHa to another given as treat ment of prostate cancer [15][16][17] and may lead to different effects in terms of hormonal castration. On the other hand, an increase in plasma testosterone levels following the first injection is well known to occur [2,19] and can be responsible in some cases for a disease flare [4,7,20,21]. Such an effect can be prevented by the concomitant administration of antiandrogen to GnRHa during the first month of treatment [18,[22][23][24][25].…”

Inhibition of PSA flare in prostate cancer patients by administration of flutamide for 2 weeks before initiation of treatment with slow-releasing LH-RH agonist

“…1 Disease flare symptoms and elevation of tumor marker levels may follow in 5%-10% of patients treated with LHRHa 2-4 because of the elevation in testosterone levels. Although these symptoms are usually transient and are observed only after the first injection of LH-RHa, sudden death caused by LH-RHa has been reported.…”