Androgen deprivation
therapy remains the mainstay of medical treatment for advanced
prostate cancer. Commonly, this is achieved with medical
androgen deprivation rather than surgical intervention as the permanence and psychological effects of the latter are unacceptable for most patients.
Degarelix is a third generation antagonist of
luteinizing hormone-releasing hormone (
LHRH, also termed
gonadotropin-releasing hormone) for the first-line treatment of
androgen-dependent advanced
prostate cancer.
Degarelix acts directly on the pituitary receptors for
LHRH, blocking the action of endogenous
LHRH. The use of
degarelix eliminates the initial undesirable surge in
gonadotropin and
testosterone levels, which is produced by agonists of
LHRH.
Degarelix is the most comprehensively studied and widely available
LHRH antagonist worldwide. Clinical trials have demonstrated that
degarelix has a long-term efficacy similar to the
LHRH agonist
leuprolide in achieving
testosterone suppression in patients with
prostate cancer.
Degarelix, however, produces a faster suppression of
testosterone and
prostate-specific antigen (PSA), with no
testosterone surges or microsurges, and thus prevents the risk of clinical flare in advanced disease. Recent clinical trials demonstrated that treatment with
degarelix results in improved disease control when compared with an
LHRH agonist in terms of superior PSA progression-free survival, suggesting that
degarelix likely delays progression to
castration-resistant disease and has a more significant impact on bone serum
alkaline phosphatase and
follicle-stimulating hormone.
Degarelix is usually well tolerated, with limited toxicity and no evidence of systemic
allergic reactions in clinical studies.
Degarelix thus represents an important addition to the hormonal armamentarium for
therapy of advanced
androgen-dependent
prostate cancer.