Degarelix

FIRMAGON

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What it isGnRH receptor antagonist; advanced prostate cancer.

Why this oneImmediate testosterone suppression with NO flare, so no antiandrogen cover is needed and it suits cord compression or severe obstruction.

What limits itMonthly subcutaneous injection with frequent injection-site reactions. QT prolongation.

FDA-approved for

Advanced prostate cancer (2008)

FDA label

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FDA dosing	Population	Start	Target	Max
Prostate cancer (androgen deprivation therapy)	adult men	240 mg SC (two 120-mg injections at 40 mg/mL) in abdominal region	Maintenance: 80 mg SC (20 mg/mL) every 28 days; first maintenance dose 28 days after starting dose

Renal Mild impairment (CrCl 50–80 mL/min): no significant effect; CrCl <50 mL/min: use with caution (limited data; severe not studied)

Hepatic Mild–moderate (Child-Pugh A/B): no dose adjustment; severe: not studied — caution

Instructions

Administered by healthcare professional only; SC injection in abdominal region only, avoiding areas exposed to pressure (waistband, belt, near ribs); vary injection site periodically
Reconstitute powder with supplied Sterile Water for Injection using vial adapter; do not shake; administer within 1 hour of reconstitution
Monitor PSA periodically; if PSA rises, measure serum testosterone

Cautions

Hypersensitivity incl. anaphylaxis, urticaria, angioedema (postmarketing) — discontinue immediately for severe reactions; do not rechallenge
QT prolongation (androgen deprivation therapy): weigh benefit/risk with congenital long QT, CHF, frequent electrolyte abnormalities, or QT-prolonging drugs; correct electrolytes; consider periodic ECG and electrolytes
Suppresses pituitary-gonadal system — affects gonadotropic/gonadal diagnostic test results
Embryo-fetal toxicity: can cause fetal harm and pregnancy loss

Adverse reactions

Injection-site reactions (35%: pain 28%, erythema 17%, swelling, induration, nodule) — mostly transient, primarily with starting dose
Hot flashes (26%)
Transaminase and GGT increases (10%)
Weight increase, hypertension, chills, constipation, back pain, arthralgia, UTI
Erectile dysfunction, testicular atrophy, gynecomastia, night sweats

Pregnancy Not established in women; can cause fetal harm and pregnancy loss — embryo-fetal lethality/abortion in animals at doses far below the clinical loading dose

Lactation Not established in females; no data on milk presence — decide between discontinuing nursing or discontinuing drug

NO BOXED WARNINGS

Principal riskInjection-site reactions; QT prolongation