Degarelix for advanced prostate cancer treatment

Degarelix is a medication used to treat patients with advanced prostate cancer. It is given as a subcutaneous injection and works by suppressing hormones that stimulate prostate cancer growth.

Degarelix is indicated for the treatment of patients with advanced prostate cancer.

Degarelix

Degarelix is a gonadotropin-releasing hormone (GnRH) receptor antagonist. It works by binding reversibly to GnRH receptors in the pituitary gland, which reduces the release of gonadotropins and subsequently lowers testosterone levels. This hormone suppression helps control the growth of prostate cancer.

General Administration

Degarelix is administered by a healthcare professional only, as a subcutaneous injection into the abdominal region. Injection sites should vary periodically and avoid areas exposed to pressure, such as near waistband or ribs.

Starting Dose

• 240 mg given as two subcutaneous injections of 120 mg each (at 40 mg/mL concentration)

Maintenance Dose

• 80 mg given as one subcutaneous injection every 28 days (at 20 mg/mL concentration)
• The first maintenance dose should be given 28 days after the starting dose

Preparation and Injection Instructions

• Supplied as lyophilized powder to be reconstituted with sterile water for injection
• Starting dose vials are reconstituted with 3 mL sterile water; maintenance dose vials with 4.2 mL sterile water
• Reconstituted solution must be administered within one hour
• Do not shake vials; use aseptic technique
• Inject at a 45-degree angle into the abdominal subcutaneous tissue; do not inject into muscle or veins
• Perform a slow deep injection over 30 seconds
• Do not rub injection site after needle removal

Degarelix is contraindicated in patients with a history of severe hypersensitivity to degarelix or any of its components.

Serious Hypersensitivity Reactions

Anaphylaxis, urticaria, and angioedema have been reported. Discontinue degarelix immediately if a severe hypersensitivity reaction occurs and manage appropriately. Do not re-challenge patients with a known history of severe hypersensitivity.

QT Interval Prolongation

Degarelix may prolong the QT interval. Use caution in patients with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities, or concurrent use of QT-prolonging drugs. Correct electrolyte imbalances and consider ECG monitoring during treatment.

Embryo-Fetal Toxicity

Degarelix can cause fetal harm and pregnancy loss. Women of reproductive potential should be advised of potential risks. Use contraception during treatment.

Monitoring

Monitor serum prostate-specific antigen (PSA) periodically to assess therapeutic effect. If PSA increases, measure serum testosterone to evaluate disease control.

Common Adverse Reactions (≥10%)

• Injection site reactions (pain, erythema, swelling, induration, nodules)
• Hot flashes
• Elevated liver enzymes (transaminases and gamma-glutamyltransferase)

Other Adverse Reactions (≥5%)

• Weight increase
• Chills
• Hypertension
• Constipation
• Back pain
• Arthralgia
• Urinary tract infection

Less Common (1-

• Fatigue, fever, night sweats
• Nausea
• Dizziness, headache, insomnia
• Erectile dysfunction, testicular atrophy
• Gynecomastia
• Hyperhidrosis
• Diarrhea

Injection Site Reactions

Mostly mild or moderate; may include pain (28%), erythema (17%), swelling (6%), induration (4%), and nodules (3%). Usually transient and more frequent with starting dose. Grade 3 reactions occurred in ≤2% of patients.

Hepatic Laboratory Abnormalities

Primarily mild to moderate; Grade 3 abnormalities occurred in

Long-term Safety

In extension studies, common adverse reactions included injection site reactions, pyrexia, hot flushes, weight changes, fatigue, and increased liver enzymes; injection site infections occurred in about 1%.

Immunogenicity

Anti-degarelix antibodies developed in about 10% of patients after one year without apparent effect on safety or efficacy.

No drug-drug interaction studies have been conducted. Degarelix is not metabolized by or an inducer/inhibitor of cytochrome P450 enzymes, so clinically relevant CYP450 interactions are unlikely.

Pregnancy

Degarelix can cause fetal harm and pregnancy loss based on animal studies. There are no human data. Women of reproductive potential should be advised of the risks.

Lactation

Safety and efficacy in breastfeeding women have not been established. Because of potential serious adverse reactions in a breastfed child, nursing should be discontinued or degarelix stopped considering the importance to the mother.

Fertility

Degarelix may impair fertility in males and females of reproductive potential based on animal data and mechanism of action.

There have been no reports of overdose. In the event of overdose, discontinue degarelix and provide symptomatic and supportive treatment.