Degarelix

FIRMAGON

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Pronunciation: deg-a-REL-ix (FIRM-a-gon)

Degarelix ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Degarelix ballicule

Degarelix FIRMAGON mascot mnemonic cartoon — Visual mnemonic: Degarelix mascot
**“Dega really likes Firmer gonads”**

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.

Degarelix molecular structure (skeletal formula) — Molecular structure: Degarelix

FDA-approved for

Advanced prostate cancer (2008)

FDA label

Read the full label on DailyMed ↗

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

Available strengths

inj 80, 120 mg

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

Cost

Degarelix (FIRMAGON)

Strength		#/mo	generic $/unit	CostPlus
80 mg	inj	per unit		not offered
120 mg	inj	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Degarelix is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskInjection-site reactions; QT prolongation

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Weight-gain liability2 / 4

Sedation liability0 / 4

QT / Torsades1 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryX

Defining liabilityInjection reactions and sustained androgen-deprivation effects

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Memory aids: interaction avatars

Box: minimal PK interactions

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