Goserelin

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

Call your doctor at once if you have:

• painful or difficult urination;
• pain, bruising, swelling, redness, oozing, or bleeding where the implant was injected;
• high blood sugar--increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss;
• high calcium levels--nausea, vomiting, constipation, increased thirst or urination, muscle pain or weakness, bone pain, confusion, and feeling tired or restless;
• heart attack symptoms--chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating;
• nerve problems--back pain, muscle weakness, problems with balance or coordination, severe numbness or tingling in your legs or feet, loss of bladder or bowel control; or
• signs of a stroke--sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech, problems with vision or balance.

Common side effects may include:

• hot flashes, sweating;
• mood changes, increased or decreased interest in sex;
• changes in sexual function, fewer erections than normal;
• headache;
• swelling in your hands or feet;
• vaginal dryness, itching, or discharge;
• changes in breast size; or
• acne, mild skin rash or itching.

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.

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

• Zoladex

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of goserelin there are no specific foods that you must exclude from your diet when receiving goserelin.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if goserelin is excreted in human breast milk or if it will harm your nursing baby.

• Goserelin Acetate
• ICI-118630
• ZDX

Breast cancer, advanced (second-line endocrine-based combination therapy)

Data from a large, randomized phase III study supports the use of goserelin in pre- or perimenopausal women (in combination with palbociclib and fulvestrant) as second-line endocrine-based combination therapy in estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer with progression on prior endocrine therapy [Turner 2015].

Prevention of early menopause during chemotherapy for early stage hormone receptor negative breast cancer

Data from a randomized phase III study supports the use of goserelin (starting 1 week prior to chemotherapy initiation) to prevent premature ovarian failure in women with early stage hormone receptor negative breast cancer [Moore, 2015].

US labeling:

Prostate cancer, advanced: Males: SubQ:

28-day implant: 3.6 mg every 28 days

12-week implant: 10.8 mg every 12 weeks

Prostate cancer, stage B2 to C (in combination with an antiandrogen and radiotherapy; begin 8 weeks prior to radiotherapy): Males: SubQ:

Combination 28-day/12-week implant: 3.6 mg implant, followed in 28 days by 10.8 mg implant

28-day implant (alternate dosing): 3.6 mg; repeated every 28 days for a total of 4 doses

Breast cancer, advanced: Females: SubQ: 3.6 mg every 28 days

Endometriosis: Females: SubQ: 3.6 mg every 28 days for 6 months

Endometrial thinning: Females: SubQ: 3.6 mg every 28 days for 1 or 2 doses

Canadian labeling:

Prostate cancer, advanced: Males: SubQ:

28-day implant: 3.6 mg every 28 days

3-month implant: 10.8 mg every 13 weeks

Prostate cancer, stage B2 to C (in combination with an antiandrogen and radiotherapy; begin 8 weeks prior to radiotherapy): Males: SubQ:

Combination 28-day/3-month implant: 3.6 mg implant, followed in 28 days by 10.8 mg implant

28-day implant (alternate dosing): 3.6 mg; repeated every 28 days for a total of 4 doses

Breast cancer, advanced: Females: SubQ: 3.6 mg every 28 days

Breast cancer, early: Females: SubQ: 3.6 mg every 28 days

Endometriosis: Females: SubQ:

28-day implant: 3.6 mg every 28 days for 6 months

3-month implant: 10.8 mg every 12 weeks for 6 months

Endometrial thinning: Females: SubQ: 3.6 mg every 28 days for 2 doses

Off-label dosing:

Prevention of early menopause during chemotherapy for early stage hormone receptor negative breast cancer (off-label use): Adult females: SubQ: 3.6 mg every 28 days starting 1 week prior to the first chemotherapy dose; continue until within 2 weeks before or after the final chemotherapy dose (Moore, 2015).

No dosage adjustment necessary.

Some frequencies not defined. Percentages reported with the 1-month implant:

>10%:

Cardiovascular: Vasodilatation (females 57%), peripheral edema (females 21%)

Central nervous system: Headache (females 32% to 75%; males 1% to 5%), emotional lability (females 60%), depression (females 54%; males 1% to 5%), pain (8% to 17%), dyspareunia (females 14%), insomnia (5% to 11%)

Dermatologic: Diaphoresis (females 16% to 45%; males 6%), acne vulgaris (females 42%; usually within 1 month after starting treatment), seborrhea (females 26%)

Endocrine & metabolic: Hot flash (females 57% to 96%; males 64%), decreased libido (females 48% to 61%), increased libido (females 12%)

Gastrointestinal: Abdominal pain (females 7% to 11%), nausea (5% to 11%)

Genitourinary: Vaginitis (75%), breast atrophy (females 33%), sexual disorder (males 21%), breast hypertrophy (females 18%), decrease in erectile frequency (18%), pelvic symptoms (females 18%), genitourinary signs and symptoms (lower; males 13%)

Hematologic & oncologic: Tumor flare (females 23%; males: Incidence not reported)

Infection: Infection (females 13%; males: Incidence not reported)

Neuromuscular & skeletal: Decreased bone mineral density (females 23%; ~4% decrease from baseline in 6 months; male: Incidence not reported), weakness (females 11%)

1% to 10%:

Cardiovascular: Edema (females 5%; male 7%), hypertension (1% to 6%), cardiac failure (males 5%), cardiac arrhythmia (males >1% to <5%), cerebrovascular accident (males >1% to <5%), peripheral vascular disease (males >1% to <5%), varicose veins (males >1% to <5%), chest pain (1% to <5%), myocardial infarction (males <1% to <5%), palpitations, tachycardia (females)

Central nervous system: Lethargy (females ≤8%), migraine (females 1% to 7%), dizziness (females 6%; male 5%), malaise (females ≤5%), chills (males >1% to <5%), anxiety (1% to <5%), nervousness (females 3% to 5%), voice disorder (females 3%), abnormality in thinking, drowsiness, paresthesia

Dermatologic: Skin rash (males 6% to 8%; female frequency not reported), hair disease (females 4%), pruritus (females 2%), alopecia, skin discoloration, xeroderma

Endocrine & metabolic: Gynecomastia (males 8%), hirsutism (7%), gout (males >1% to <5%), hyperglycemia (males >1% to <5%), weight gain (>1% to <5%)

Gastrointestinal: Anorexia (1% to 5%), gastric ulcer (males >1% to <5%), constipation (1% to <5%), diarrhea (1% to <5%), vomiting (1% to <5%), increased appetite (females 2%), dyspepsia, flatulence, xerostomia

Genitourinary: Pelvic pain (females 9%; males 6%), mastalgia (>1% to 7%), uterine hemorrhage (6%), vulvovaginitis (5%), breast swelling (males >1% to <5%), urinary tract obstruction (males: >1% to <5%), urinary tract infection (1% to <5%), urinary frequency, vaginal hemorrhage

Hematologic & oncologic: Anemia (males >1% to <5%), bruise, hemorrhage

Hypersensitivity: Hypersensitivity reaction

Infection: Sepsis (males >1% to <5%)

Local: Application site reaction (females 6%)

Neuromuscular & skeletal: Myalgia (females 3%, males frequency not reported), leg cramps (females 2%, males frequency not reported), hypertonia (females 1%; male frequency not reported), arthralgia, arthropathy

Ophthalmic: Amblyopia, dry eye syndrome

Renal: Renal insufficiency (<1% to >5%)

Respiratory: Upper respiratory tract infection (males 7%), chronic obstructive pulmonary disease (males 5%), flu-like symptoms (females 5%, male frequency not reported), pharyngitis (females 5%), sinusitis (females ≥1%; male frequency not reported), bronchitis, cough, epistaxis, rhinitis

Miscellaneous: Fever

<1% (Limited to important or life-threatening): Anaphylaxis, convulsions, deep vein thrombosis, diabetes mellitus, hypercalcemia, hypercholesterolemia, increased HDL cholesterol, increased serum ALT, increased serum AST, injection site reaction (including vascular injury, pain, hematoma, hemorrhage, hemorrhagic shock), osteoporosis, ovarian cyst, ovarian hyperstimulation syndrome, pituitary apoplexy, pituitary neoplasm (including adenoma), pulmonary embolism, psychotic reaction, transient ischemic attacks

Monitor blood glucose and HbA1c (periodically), bone mineral density, serum calcium, cholesterol/lipids; monitor for signs/symptoms of abdominal hemorrhage following injection.

Prostate cancer: Consider periodic ECG and electrolyte monitoring. Monitor for weakness, paresthesias, tumor flare, urinary tract obstruction, and spinal cord compression in first few weeks of therapy.