Firmagon

Degarelix is a man-made form of a protein that reduces the amount of certain hormones in the body, including testosterone.

Degarelix is used to treat prostate cancer.

Degarelix may also be used for purposes not listed in this medication guide.

Although degarelix is not for use by women, this medication should not be used by a woman who is pregnant or breast-feeding, or who may become pregnant.

You should not use degarelix if you are allergic to it.

To make sure degarelix is safe for you, tell your doctor if you have:

• heart disease, heart rhythm disorder;
• a personal or family history of Long QT syndrome;
• liver or kidney disease; or
• an electrolyte imbalance, such as low or high levels of potassium or magnesium in your blood.

Although degarelix is not for use by women, this medicine can cause birth defects if a woman is exposed to it during pregnancy. Degarelix should not be used by a woman who is pregnant.

It is not known whether this medicine passes into breast milk or if it could harm a nursing baby. Degarelix should not be used by a woman who is breast-feeding a baby.

The common side effects include:

• hot flashes
• injection site pain, redness, and swelling, especially with the first dose
• weight gain
• increase in some liver enzymes
• tiredness
• hypertension
• back and joint pain
• chills
• urinary tract infection
• decreased sex drive and trouble with erectile function (impotence)

Tell your doctor if you are pregnant or plan to become pregnant. The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy. This medication falls into category X.

This medication is not intended for use in women and should especially be avoided by pregnant women. Tell your doctor if you are pregnant or plan to become pregnant. Women who are pregnant or may become pregnant should not receive Firmagon. This medication may harm the unborn baby.

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if Firmagon is excreted in human breast milk or if it will harm your nursing baby.

Keep all medical and laboratory appointments while receiving this medication. To get the most benefit from this medication you should not skip doses. If you are unable to make an appointment, reschedule as soon as possible.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

A total of 1325 patients with prostate cancer received FIRMAGON either as a monthly treatment (60-160 mg) or as a single dose (up to 320 mg). A total of 1032 patients (78%) were treated for at least 6 months and 853 patients (64%) were treated for one year or more. The most commonly observed adverse reactions during FIRMAGON therapy included injection site reactions (e.g., pain, erythema, swelling or induration), hot flashes, increased weight, fatigue, and increases in serum levels of transaminases and gamma-glutamyltransferase (GGT). The majority of the adverse reactions were Grade 1 or 2, with Grade 3/4 adverse reaction incidences of 1% or less.

FIRMAGON was studied in an active-controlled trial (N = 610) in which patients with prostate cancer were randomized to receive FIRMAGON (subcutaneous) or leuprolide (intramuscular) monthly for 12 months.Adverse reactions reported in 5% of patients or more are shown in Table 1.

Table 1: Adverse Reactions Reported in ≥ 5% of Patients in an Active Controlled Study

The most frequently reported adverse reactions at the injection sites were pain (28%), erythema (17%), swelling (6%), induration (4%) and nodule (3%). These adverse reactions were mostly transient, of mild to moderate intensity, occurred primarily with the starting dose and led to few discontinuations ( < 1%). Grade 3 injection site reactions occurred in 2% or less of patients receiving degarelix.

Hepatic laboratory abnormalities were primarily Grade 1 or 2 and were generally reversible. Grade 3 hepatic laboratory abnormalities occurred in less than 1% of patients.

In 1-5% of patients the following adverse reactions, not already listed, were considered related to FIRMAGON by the investigator:

Body as a whole: Asthenia, fever, night sweats; Digestive system: Nausea; Nervous system: Dizziness, headache, insomnia.

The following adverse reactions, not already listed, were reported to be drug-related by the investigator in ≥ 1% of patients: erectile dysfunction, gynecomastia, hyperhidrosis, testicular atrophy, and diarrhea.

The safety of FIRMAGON administered monthly was evaluated further in an extension study in 385 patients who completed the above active-controlled trial. Of the 385 patients, 251 patients continued treatment with FIRMAGON and 135 patients crossed over treatment from leuprolide to FIRMAGON. The median treatment duration on the extension study was approximately 43 months (range 1 to 58 months). The most common adverse reactions reported in > 10% of the patients were injection site reactions (e.g., pain, erythema, swelling, induration or inflammation), pyrexia, hot flush, weight loss or gain, fatigue, increases in serum levels of hepatic transaminases and GGT. One percent of patients had injection site infections including abscess. Hepatic laboratory abnormalities in the extension study included the following: Grade ½ elevations in hepatic transaminases occurred in 47% of patients and Grade 3 elevations occurred in 1% of patients.

Decreased bone density has been reported in the medical literature in men who have had orchiectomy or who have been treated with a GnRH agonist. It can be anticipated that long periods of medical castration in men will result in decreased bone density.

Anti-degarelix antibody development has been observed in 10% of patients after treatment with FIRMAGON for 1 year. There is no indication that the efficacy or safety of FIRMAGON treatment is affected by antibody formation.

Read the entire FDA prescribing information for Firmagon (Degarelix for Injection)

Call your doctor for instructions if you miss an appointment for your degarelix injection.

Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• headache with chest pain and severe dizziness, fainting, fast or pounding heartbeats;

• pain or burning when you urinate;

• shortness of breath (even with mild exertion), swelling, rapid weight gain; or

• dangerously high blood pressure--severe headache, blurred vision, pounding in your neck or ears, nosebleed, anxiety, confusion, severe chest pain, shortness of breath, irregular heartbeats.

Common side effects may include:

• feeling tired;

• chills or hot flashes;

• weight gain;

• abnormal liver function tests;

• joint pain, back pain;

• increased blood pressure;

• impotence, loss of interest in sex, trouble having an orgasm; or

• pain, swelling, redness, or a hard lump where the medicine was injected.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Firmagon is contraindicated in patients with known hypersensitivity to degarelix or to any of the product components. [see Warnings and Precautions (5.2)].

Degarelix is contraindicated in women who are or may become pregnant. Degarelix can cause fetal harm when administered to a pregnant woman. Degarelix given to rabbits during organogenesis at doses that were 0.02% of the clinical loading dose (240 mg) on a mg/m2 basis caused embryo/fetal lethality and abortion. When degarelix was given to female rats during organogenesis, at doses that were just 0.036% of the clinical loading dose on an mg/m2 basis, there was an increase post implantation loss and a decrease in the number of live fetuses. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

No drug-drug interaction studies were conducted.

Degarelix is not a substrate for the human CYP450 system. Degarelix is not an inducer or inhibitor of the CYP450 system in vitro. Therefore, clinically significant CYP450 pharmacokinetic drug-drug interactions are unlikely.

You should not use Firmagon if you are allergic to degarelix.

To make sure Firmagon is safe for you, tell your doctor if you have:

• heart disease, heart rhythm disorder;

• a personal or family history of Long QT syndrome;

• liver or kidney disease; or

• an electrolyte imbalance, such as low or high levels of potassium or magnesium in your blood.

Although Firmagon is not for use by women, this medicine can cause birth defects if a woman is exposed to it during pregnancy. Firmagon should not be used by a woman who is pregnant.

It is not known whether degarelix passes into breast milk or if it could harm a nursing baby. Firmagon should not be used by a woman who is breast-feeding a baby.

Firmagon is injected under the skin around your stomach. A healthcare provider will give you this injection.

Firmagon is usually given once every 28 days. Follow your doctor's instructions.

The first time you receive Firmagon, you will be given two injections. At your monthly follow-up visits you will receive only one injection.

While using Firmagon, you may need frequent blood tests at your doctor's office.

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

Degarelix 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.

Applies to degarelix: subcutaneous powder for solution

Along with its needed effects, degarelix (the active ingredient contained in Firmagon) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur while taking degarelix:

• Back pain
• blurred vision
• dizziness
• fever
• flushing or redness of the skin
• hard lump
• headache
• nervousness
• pain
• pounding in the ears
• slow or fast heartbeat
• small lumps under the skin
• swelling
• unusually warm skin

• Bladder pain
• bloody or cloudy urine
• chills
• decrease in testicle size
• decreased interest in sexual intercourse
• difficult, burning, or painful urination
• difficulty in moving
• frequent urge to urinate
• inability to have or keep an erection
• increased sweating
• loss in sexual ability, desire, drive, or performance
• lower back or side pain
• muscle pain or stiffness
• pain in the joints

• Chest pain or discomfort
• fainting
• irregular heartbeat
• pounding heartbeat
• shortness of breath

Some side effects of degarelix may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Difficulty having a bowel movement (stool)
• feeling of warmth
• increased weight
• redness of the face, neck, arms, and occasionally, upper chest
• sudden sweating
• unusual tiredness or weakness

• Diarrhea
• lack or loss of strength
• nausea
• night sweats
• sleeplessness
• swelling of the breasts or breast soreness
• trouble sleeping
• unable to sleep