Degarelix dosing & administration

Klotz L, Boccon-Gibod L, Shore ND, Andreou C, Persson BE, Cantor P, Jensen JK, Olesen TK, Schröder FH · 2008

Pivotal CS21 trial: degarelix 240 mg subcutaneous starting (loading) dose followed by monthly 80 mg maintenance suppressed testosterone to castrate levels (<0.5 ng/mL) in 97.2% of patients from day 28 to day 364, non-inferior to leuprolide 7.5 mg monthly with faster onset.

Ferring Pharmaceuticals (FDA-approved label) · 2020

FDA-approved regimen for advanced prostate cancer: starting dose 240 mg given as two 120 mg deep subcutaneous injections (40 mg/mL) into the abdomen; maintenance dose 80 mg (20 mg/mL) subcutaneous every 28 days, first maintenance dose given 28 days after the starting dose.

Gittelman M, Pommerville PJ, Persson BE, Jensen JK, Olesen TK · 2008

Phase II dose-finding study in 127 North American prostate cancer patients: a 200 mg degarelix starting dose induced rapid testosterone suppression (88% at <=0.5 ng/mL by 1 month), sustained over 12 months with 60 or 80 mg monthly maintenance, with no evidence of testosterone surge; degarelix was well tolerated, 5% withdrew for adverse events.

Carter NJ, Keam SJ · 2014

Review of degarelix (Firmagon/Gonax), approved for prostate cancer in the US, EU and Japan: 240 mg starting dose then 80 mg monthly was non-inferior to leuprolide 7.5 mg monthly for castration, with faster testosterone and PSA suppression and no testosterone surges or microsurges; suppression continued up to 5 years in the trial extension; injection-site reactions and effects of testosterone suppression (hot flushes, weight increase) were the most common adverse events, mostly mild to moderate.

Van Poppel H, Klotz L · 2012

GnRH antagonists act directly to block pituitary GnRH receptors, unlike agonists. Degarelix gives substantially faster onset of castration and faster PSA suppression than leuprolide, with no risk of testosterone surge or clinical flare; other than minor injection-site reactions it is generally well tolerated, with most adverse events consistent with androgen suppression.

Anderson J · 2009

GnRH agonists induce an initial testosterone surge that can cause painful and potentially dangerous clinical flare. Degarelix is a GnRH receptor blocker giving immediate, profound and sustained testosterone reduction without an initial surge; the most common side effects were mild to moderate injection-site reactions and hot flashes.

Nguyen PL, Alibhai SMH, Basaria S, D'Amico AV, Kantoff PW, Keating NL, Penson DF, Rosario DJ, Tombal B, Smith MR · 2015

Systematic review of androgen deprivation therapy harms: decreased bone mineral density; weight gain, decreased muscle mass and increased insulin resistance; decreased libido and sexual dysfunction; hot flashes; gynecomastia; reduced testicle size; anemia and fatigue. Observational studies also suggest increased risk of diabetes and cardiovascular events.

Greenspan SL, Coates P, Sereika SM, Nelson JB, Trump DL, Resnick NM · 2005

Prospective 12-month study of 152 men with prostate cancer: men starting androgen deprivation therapy lost 2.5% bone mineral density at the total hip, 2.4% at the trochanter, 2.6% at the total radius, 3.3% total body and 4.0% at the spine over one year, together with a 10.4% increase in total body fat and a 3.5% loss of lean mass; bone loss was maximal in the first year of therapy.

Nguyen C, Lairson DR, Swartz MD, Du XL · 2018

Propensity-matched SEER-Medicare cohort of 201,797 men aged 66 years and older with prostate cancer: androgen deprivation therapy was associated with higher risk of bone fracture (HR 1.39), diabetes (HR 1.21), dementia (HR 1.16), coronary heart disease (HR 1.12), acute myocardial infarction (HR 1.11) and sexual dysfunction (HR 1.12) than in men not receiving it.

Bultijnck R, De Laere L, De Grande R, Develter T, Vantieghem S, Uvin P, Ghysel C, De Laere B · 2024

Cross-sectional survey of 276 patients on androgen deprivation therapy for advanced prostate cancer: sexual health-related quality of life was low and narrowly distributed, with 84% of patients reporting erectile dysfunction.

Dosani M, Morris WJ, Tyldesley S, Pickles T · 2017

Secondary analysis of 398 men given 12 months of androgen deprivation therapy: hot flashes were reported by 93% and resolved in 99%, at a median 7.6 months after stopping therapy. Median time to testosterone recovery after cessation was 9 months to 5 nmol/L, 13 months to 7.5 nmol/L and 18 months to 10 nmol/L, with recovery rates above 90%.

US Food and Drug Administration, Center for Drug Evaluation and Research · 2008

FIRMAGON (degarelix) was approved by the FDA as a new molecular entity under NDA 022201 on 24 December 2008, with subsequent labeling supplements through February 2020.