Drug intelligence / Profile preview

degarelix acetate + leuprolide acetate

Development stage
Unknown
Lead developer
Ferring Pharmaceuticals
Modality
Peptides
Administration
Subcutaneous, Intramuscular
01

Overview

This is a combination androgen-deprivation therapy regimen comprising the GnRH antagonist degarelix acetate and the GnRH agonist leuprolide acetate, used sequentially or concomitantly in clinical practice for prostate cancer to achieve rapid testosterone suppression without initial flare (via degarelix) and then continue maintenance suppression with an agonist depot (leuprolide). Degarelix is a competitive gonadotropin-releasing hormone receptor antagonist that rapidly reduces LH and FSH, leading to castrate testosterone levels within days and avoids the testosterone surge seen with GnRH agonists. Leuprolide is a GnRH receptor agonist that initially stimulates LH/FSH causing a transient testosterone surge, followed by receptor downregulation and sustained suppression with depot dosing. Clinical literature describes initiating ADT with degarelix followed by leuprolide to eliminate or minimize the testosterone surge associated with starting an agonist, supporting this combination strategy in advanced prostate cancer.

Brand names
Firmagon
Other names
degarelix + leuprolidedegarelix acetate and leuprolide acetate
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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