Degarelix

Dosage Forms & Strengths

powder for injection

• 80mg
• 120mg

Hormone-dependent Advanced Prostate Carcinoma (Stage D)

Initial: 120 mg SC for 2 doses (ie, 2 separate injections totaling 240 mg), THEN after 28 days, begin maintenance dose of 80 mg SC q28Days

Renal Impairment

≥50 mL/min: Dose adjustment not necessary

<50 mL/min: Use caution

Hepatic Impairment

Mild-to-moderate: Dose adjustment not necessary

Severe: Safety and efficacy not established; use caution

Administration

Initiation pack contains 2 vials each with 120 mg per vial & 6 mL sterile water for injection diluent

Withdraw 3 mL of sterile water for injection diluent (supplied) & add to 1 of the 2 vials, swirl to mix - keep vial vertical at all times, do not shake

Inject SC in abdomen within 1 hour of reconstitution

Repeat for 2nd injection and use different injection site

Maintenance pack contains 1 vial of 80 mg per vial & 4.2 mL sterile water for injection diluent

Use 4.2 mL to reconstitute, withdraw 4 mL for dose of 80 mg

Not indicated

Degarelix may be found in some form under the following brand names:

• Firmagon

Degarelix comes as a liquid to be injected under the skin (subcutaneously) of the stomach area, usually once every 28 days. The area where the medication is injection should change with each dosage. It should not be injected in the area of the ribs or waistline as these areas could be easily rubbed against or receive pressure.

This medication is usually given by a doctor or nurse in a medical facility, such as the doctor's office, clinic, or hospital.

• The injected medicine gives you a continuous release of degarelix over one month.
• Two injections are given as a first dose and the following monthly doses are one injection.
• Always set up an appointment for your next injection.
• If you miss a dose of degarelix, or if you think you forgot to get your monthly dose of degarelix, talk to your healthcare provider about how to get your next dose.

On the day of your injection, avoid wearing a belt, tight waistband, or tight clothing around your stomach where the injection will be given.

This medicine can pass into body fluids (urine, feces, vomit). For at least 48 hours after you receive a dose, avoid allowing your body fluids to come into contact with your hands or other surfaces. Caregivers should wear rubber gloves while cleaning up a patient's body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.

Tell your doctor about all your current medicines and any you start or stop using, especially:

• heart rhythm medicine--amiodarone, disopyramide, dofetilide, dronedarone, flecainide, procainamide, quinidine, sotalol, and others.

This list is not complete. Other drugs may interact with degarelix, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

• It is used to treat prostate cancer.
• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Weight gain.
• Change in sex ability.
• Lowered interest in sex.
• Feeling tired or weak.
• Hot flashes.
• Back pain.
• Joint pain.
• Chills.
• Hard stools (constipation).
• Redness or swelling where the shot is given.
• Itching where the shot is given.
• Pain where the shot was given.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

(deg a REL ix)

A single dose of degarelix 1 mg was administered intravenously to subjects without prostate cancer with mild (Child Pugh class A) or moderate (Child Pugh class B) impairment; degarelix exposure was decreased 10% for mild impairment, and 18% for moderate impairment (when compared to patients without prostate cancer and with normal hepatic function).

Administer (deep) SubQ in the abdominal area by pinching skin and elevating SubQ tissue; insert needle at a 45 degree angle. Gently pull plunger back to check for aspiration (if blood is aspirated into syringe, do not inject; discard and reconstitute a new dose); slowly inject over 30 seconds, remove needle and then release skin. For SubQ administration only; do not inject into a vein or into muscle. Avoid pressure exposed areas (eg, waistband, belt, or near ribs). Rotate injection site. Inject loading dose as two 3 mL injections (40 mg/mL) in different sites; maintenance dose should be administered as a single 4 mL injection (20 mg/mL); begin maintenance dose 28 days after initial loading dose.

-Mild Renal Impairment (CrCl 50 to 80 mL/min): No adjustment recommended.
-Moderate to Severe Renal Impairment (CrCl less than 50 mL/min): Use with caution.

Administration Advice:
-Administer this drug in the abdominal region only.
-Vary the injection site periodically to minimize patient discomfort, and administer in abdomen areas not exposed to pressure (e.g., not close to waistband or belt, not close to the ribs).
-Perform a slow, deep subcutaneous injection over 30 seconds.
-This drug is for subcutaneous injection only; do not administer intravenously or intramuscularly.
-Use this drug only as a first-line androgen deprivation therapy; there is no data available on use of this drug in patients who have failed treatment with GnRH agonists (e.g., leuprorelin, goserelin).
-Confirm serum testosterone levels are remaining sufficiently suppressed if a patient's clinical response appears to be sub-optimal.

Reconstitution/Preparation Techniques:
-Consult the manufacturer product information.

General:
-This drug has shown to be effective in achieving and maintaining testosterone suppression below the medical castration level of 0.5 ng/mL.
-There is no clinical experience with the effects of an acute overdose.

Monitoring:
-PSA serum concentrations; testosterone serum concentrations of testosterone (if PSA increases)
-ECG and electrolytes

Patient Advice:
-Do not rub, massage, or scratch the injection site.