Breast cancer, advanced: Females: SubQ: 3.6 mg every 28 days.
Endometrial thinning: Females: SubQ: 3.6 mg every 28 days for 1 or 2 doses.
Endometriosis: Females: SubQ: 3.6 mg every 28 days for 6 months.
Hormone therapy for transgender females (male-to-female) (adjunct) (off-label use): SubQ: 3.6 mg every 4 weeks in combination with other appropriate agents (Mueller 2011).
Prevention of early menopause during chemotherapy for early stage hormone receptor-negative breast cancer (off-label use): Adult females: SubQ: 3.6 mg once every 28 days starting at least 1 week prior to the first chemotherapy dose; continue until within 2 weeks before or after the final chemotherapy dose (Moore 2015; Moore 2019).
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.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
No dosage adjustment necessary.
No dosage adjustment necessary.
Males: Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Implant, Subcutaneous:
Zoladex: 3.6 mg (1 ea); 10.8 mg (1 ea)
No
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Implant, Subcutaneous:
Zoladex: 3.6 mg (1 ea)
Zoladex LA: 10.8 mg (1 ea)
SubQ: Administer implant by inserting needle at a 30- to 45-degree angle into the anterior abdominal wall below the navel line. Use caution while injecting goserelin into the anterior abdominal wall (due to the proximity of underlying inferior epigastric artery and its branches). Goserelin is an implant; therefore, do not attempt to eliminate air bubbles prior to injection (may displace implant). Do not attempt to aspirate prior to injection; if a large vessel is penetrated, blood will be visualized in the syringe chamber (if vessel is penetrated, withdraw needle and inject elsewhere with a new syringe). Do not penetrate into muscle or peritoneum. Implant may be detected by ultrasound if removal is required. Monitor for signs/symptoms of abdominal hemorrhage. Use extra care when administering goserelin to patients with a low BMI and/or to patients receiving full dose anticoagulation.
Hazardous agent (NIOSH 2016 [group 1]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
Breast cancer, advanced (3.6 mg only): Palliative treatment of advanced breast cancer in pre- and perimenopausal women (estrogen and progesterone receptor values may help to predict if goserelin is likely to be beneficial).
Endometrial thinning (3.6 mg only): Endometrial-thinning agent prior to endometrial ablation for dysfunctional uterine bleeding.
Endometriosis (3.6 mg only): Management of endometriosis, including pain relief and reduction of endometriotic lesions for the duration of therapy (goserelin experience for endometriosis has been limited to women 18 years and older treated for 6 months).
Prostate cancer, advanced (3.6 mg or 10.8 mg): Palliative treatment of advanced carcinoma of the prostate.
Prostate cancer, stage B2 to C (3.6 mg or 10.8 mg): Management of locally confined stage T2b to T4 (stage B2 to C) prostate cancer (in combination with an antiandrogen [eg, flutamide]); begin goserelin and antiandrogen therapy 8 weeks prior to initiating radiation therapy and continue during radiation therapy.
Breast cancer, advanced (second-line endocrine-based combination therapy); Hormone therapy for transgender females (male-to-female); Prevention of early menopause during chemotherapy for early stage hormone receptor-negative breast cancer
The Institute for Safe Medication Practices (ISMP) includes this medication (when treating endometriosis or endometrial thinning) among its list of drugs that have a heightened risk of causing significant patient harm when used in error.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Cardiovascular: Peripheral edema (females: 21%; males: 1% to 5%), vasodilation (females: 57%)
Dermatologic: Acne vulgaris (females: 42%), diaphoresis (females: 16% to 45%; males: 6%), seborrhea (females: 26%)
Endocrine & metabolic: Decreased libido (females: 48% to 61%), hot flash (females: 70% to 96%; males: 60% to 62%), increased libido (females: 12%)
Gastrointestinal: Abdominal pain (1% to 11%), nausea (5% to 11%)
Genitourinary: Breast atrophy (females: 33%), breast hypertrophy (females: 18%), decrease in erectile frequency (18%), dyspareunia (females: 14%), genitourinary signs and symptoms (lower; males: 13%), pelvic symptoms (females: 18%), sexual disorder (males: 21%), vaginitis (75%)
Hematologic & oncologic: Tumor flare
Infection: Infection (females: 13%)
Nervous system: Depression (females: 54%; males: 1% to 5%), emotional lability (females: 60%), headache (females: 32% to 75%; males: 1% to 5%), insomnia (5% to 11%), pain (8% to 17%)
Neuromuscular & skeletal: Asthenia (5% to 11%), decreased bone mineral density
1% to 10%:
Cardiovascular: Acute myocardial infarction (males: 1% to 5%), angina pectoris (males: 1% to 5%), cardiac arrhythmia (males: 1% to 5%), cardiac failure (males: 5%), cerebral ischemia (males: 1% to 5%), cerebrovascular accident (males: 1% to 5%), chest pain (1% to 5%), edema (5% to 7%), hypertension (6%), palpitations (females: 1% to 5%), peripheral vascular disease (males: 1% to 5%), pulmonary embolism (males: 1% to 5%), tachycardia (females: 1% to 5%), varicose veins (males: 1% to 5%)
Dermatologic: Alopecia (females: 1% to 5%), ecchymosis (females: 1% to 5%), hair disease (females: 4%), pruritus (2%), skin discoloration (females: 1% to 5%), skin rash (6%), xeroderma (females: 1% to 5%)
Endocrine & metabolic: Diabetes mellitus (males: 1% to 5%), gout (males: 1% to 5%), gynecomastia (males: 8%), hirsutism (females: 7%), hyperglycemia (males: 1% to 5%), weight gain (3%)
Gastrointestinal: Anorexia (5%), constipation (1% to 5%), diarrhea (1% to 5%), dyspepsia (females: 1% to 5%), flatulence (females: 1% to 5%), gastric ulcer (males: 1% to 5%), hematemesis (males: 1% to 5%), increased appetite (females: 2%), vomiting (4%), xerostomia (females: 1% to 5%)
Genitourinary: Breast swelling (males: 1% to 5%), breast tenderness (males: 1% to 5%), dysmenorrhea (1% to 5%), hematuria (males: 1% to 5%), impotence (males: 1% to 5%), mastalgia (7%), pelvic pain (6% to 9%), urinary frequency (1% to 5%), urinary incontinence (males: 1% to 5%), urinary retention (males: 1% to 5%), urinary tract abnormality (males: 1% to 5%), urinary tract infection (1% to 5%), urinary tract obstruction (males: 1% to 5%), urination disorder (males: 1% to 5%), uterine hemorrhage (6%), vaginal hemorrhage (1% to 5%), vulvovaginitis (5%)
Hematologic & oncologic: Anemia (males: 1% to 5%), bladder neoplasm (males: 1% to 5%), hemorrhage (females: 1% to 5%)
Hypersensitivity: Hypersensitivity reaction (females: 1% to 5%)
Infection: Herpes simplex infection (males: 1% to 5%), sepsis (males: 1% to 5%)
Local: Application site reaction (females: 6%)
Nervous system: Abnormality in thinking (females: 1% to 5%), anxiety (1% to 5%), chills (males: 1% to 5%), dizziness (5% to 6%), drowsiness (females: 1% to 5%), fatigue (females: ≤5%), hypertonia (females: 1%), lethargy (≤8%), malaise (females: ≤5%), migraine (females: 7%), nervousness (females: 3% to 5%), paresthesia (1% to 5%), voice disorder (females: 3%)
Neuromuscular & skeletal: Arthralgia (females: 1% to 5%), arthropathy (females: 1% to 5%), back pain (4% to 7%), lower limb cramp (females: 2%), myalgia (females: 3%), ostealgia (males: 6%)
Ophthalmic: Amblyopia (females: 1% to 5%), dry eye syndrome (females: 1% to 5%)
Renal: Renal insufficiency (males: 1% to 5%)
Respiratory: Bronchitis (females: 1% to 5%), chronic obstructive pulmonary disease (males: 5%), cough (1% to 5%), dyspnea (males: 1% to 5%), epistaxis (females: 1% to 5%), flu-like symptoms (5%), pharyngitis (females: 5%), pneumonia (males: 1% to 5%), rhinitis (females: 1% to 5%), sinusitis (females: 1% to 5%), upper respiratory tract infection (males: 7%)
Miscellaneous: Aggravation reaction (males: 1% to 5%), fever (1% to 5%)
<1%:
Hepatic: Increased serum alanine aminotransferase, increased serum aspartate aminotransferase
Local: Injection site reaction
Frequency not defined: Endocrine & metabolic: Decreased HDL cholesterol, increased HDL cholesterol, increased LDL cholesterol, increased serum triglycerides
Postmarketing:
Cardiovascular: Deep vein thrombosis, hypotension, transient ischemic attacks, vascular injury
Endocrine & metabolic: Hypercalcemia (patients with bone metastases), hypovolemic shock, ovarian cyst, pituitary apoplexy
Genitourinary: Ureteral obstruction
Hematologic & oncologic: Pituitary neoplasm (including adenoma)
Hypersensitivity: Anaphylaxis
Local: Bleeding at injection site, hematoma at injection site, pain at injection site
Nervous system: Psychotic reaction, seizure, spinal cord compression
Neuromuscular & skeletal: Bone fracture, osteoporosis
Hypersensitivity to goserelin, gonadotropin-releasing hormone (GnRH), GnRH agonist analogues, or any component of the formulation; during pregnancy for the treatment of endometriosis or endometrial thinning.
Canadian labeling: Additional contraindications (not in the US labeling): Undiagnosed vaginal bleeding, pregnancy, breastfeeding.
Concerns related to adverse effects:
• Cervical resistance: Cervical resistance may be increased; use caution when dilating the cervix for endometrial ablation.
• Decreased bone density: Has been reported in women and may be irreversible; use caution if other risk factors are present; evaluate and institute preventive treatment if necessary.
• Hypercalcemia: Hypercalcemia has been reported in prostate and breast cancer patients with bone metastases. Initiate appropriate management if hypercalcemia occurs.
• Hyperglycemia: Hyperglycemia has been reported in males and may manifest as diabetes or worsening of preexisting diabetes (worsening glycemic control). Monitor blood glucose and HbA1c and manage diabetes appropriately.
• Hypersensitivity: Hypersensitivity reactions (including acute anaphylactic reactions) and antibody formation may occur; monitor.
• Injection site injury: Injection site and vascular injury, including pain, hematoma, hemorrhage, and hemorrhagic shock (requiring blood transfusions or surgical intervention) have been reported with goserelin. Use extra caution when administering to patients with a low BMI and/or to patients receiving full dose anticoagulation. Use caution while injecting goserelin into the anterior abdominal wall (due to the proximity of underlying inferior epigastric artery and its branches). Monitor for signs/symptoms of abdominal hemorrhage. Inform patient to immediately report abdominal pain, abdominal distention, dyspnea, dizziness, hypotension, and/or altered level of consciousness.
• Pituitary apoplexy: Rare cases of pituitary apoplexy (frequently secondary to pituitary adenoma) have been observed with gonadotropin-releasing hormone (GnRH) agonist administration (onset from 1 hour to usually <2 weeks); may present as sudden headache, vomiting, visual or mental status changes, and, infrequently, cardiovascular collapse; immediate medical attention required.
• Tumor flare: Transient increases in serum testosterone (in men with prostate cancer) and estrogen (in women with breast cancer) may result in a worsening of disease signs and symptoms (tumor flare) during the first few weeks of treatment. Some patients experienced a temporary worsening of bone pain, which may be managed symptomatically. Spinal cord compression and urinary tract obstruction have been reported when used for prostate cancer; closely observe patients for symptoms (eg, ureteral obstruction, weakness, paresthesias) in first few weeks of therapy. Manage with standard treatment; consider orchiectomy for extreme cases.
Disease-related concerns:
• Cardiovascular disease: Androgen deprivation therapy may increase the risk for cardiovascular disease (Levine, 2010). An increased risk for myocardial infarction, sudden cardiac death, and stroke has been observed. Monitor for signs/symptoms of cardiovascular disease; manage according to current clinical practice. Androgen deprivation therapy may cause prolongation of the QT/QTc interval; evaluate risk versus benefit in patients with congenital long QT syndrome, heart failure, frequent electrolyte abnormalities, and in patients taking medication known to prolong the QT interval. Correct electrolytes prior to initiation and consider periodic electrolyte and ECG monitoring.
Special populations:
• Obese patients: A decreased AUC may be observed when using the 3-month implant in obese patients. Monitor testosterone levels if desired clinical response is not observed.
• Underweight patients: Use extra care when administering to patients with a low BMI.
Dosage form specific issues:
• Implant removal: If removal is necessary, implant may be located by ultrasound.
None known.
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy
Choline C 11: Luteinizing Hormone-Releasing Hormone Analogs may diminish the therapeutic effect of Choline C 11. Risk C: Monitor therapy
Corifollitropin Alfa: Luteinizing Hormone-Releasing Hormone Analogs may enhance the therapeutic effect of Corifollitropin Alfa. Risk X: Avoid combination
Gallium Ga 68 PSMA-11: Androgen Deprivation Therapy Agents may diminish the therapeutic effect of Gallium Ga 68 PSMA-11. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of gallium Ga 68 PSMA-11 in prostate cancer. The impact of ADT on the performance of gallium Ga 68 PSMA-11 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy
Indium 111 Capromab Pendetide: Luteinizing Hormone-Releasing Hormone Analogs may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Risk X: Avoid combination
Piflufolastat F18: Androgen Deprivation Therapy Agents may diminish the diagnostic effect of Piflufolastat F18. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of ADT on the performance of piflufolastat F18 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
When used for endometriosis or endometrial thinning, females of reproductive potential should not receive goserelin until pregnancy has been excluded. Nonhormonal contraception is recommended for premenopausal women during therapy and for 12 weeks after therapy is discontinued. Although ovulation is usually inhibited and menstruation may stop, pregnancy prevention is not ensured during goserelin therapy. Changes in reproductive function may occur following chronic administration.
Goserelin may prevent premature ovarian failure when added to chemotherapy in women with early stage hormone receptor negative breast cancer. In one study, women followed for 5 years were less likely to experience ovarian failure and more likely to become pregnant than women who did not receive goserelin in addition to their chemotherapy. The desire to become pregnant and the incidence of prior pregnancies was not considered in the analysis, and pregnancies occurred in some women who were not attempting to conceive (Moore 2015; Moore 2019). Use of gonadotropin-releasing hormone (GnRH) agonists such as goserelin for preserving ovarian function and potentially maintaining future fertility may be considered for some premenopausal women undergoing chemotherapy (ACOG 747 2018).
Goserelin induces hormonal changes, which increase the risk for fetal loss.
Use is contraindicated during pregnancy for the treatment of endometriosis or endometrial thinning. If used for the palliative treatment of breast cancer during pregnancy, the potential for increased fetal loss should be discussed with the patient. Outcome information following inadvertent goserelin exposure during pregnancy is limited (Ishizuka 2016).
It is not known if goserelin is present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, a decision should be made to discontinue breastfeeding or to discontinue the drug, considering the importance of treatment to the mother.
Monitor blood glucose and HbA1c (periodically), bone mineral density, serum calcium, cholesterol/lipids; monitor for signs/symptoms of abdominal hemorrhage following injection.
Endometriosis, endometrial thinning: Evaluate pregnancy status prior to use.
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.
Transgender hormone therapy: Serum testosterone levels (goal <50 ng/dL) every 3 months during the first year and then annually or biannually; serum luteinizing hormone (LH), follicle-stimulating hormone (FHS), and prolactin levels at baseline and annually; routine cancer and laboratory screening as in non-transgender individuals for all tissues present (ES [Hembree 2017]; Mueller 2011).
Goserelin (a gonadotropin-releasing hormone [GnRH] analog) causes an initial increase in luteinizing hormone (LH) and follicle stimulating hormone (FSH), chronic administration of goserelin results in a sustained suppression of pituitary gonadotropins. Serum testosterone falls to levels comparable to surgical castration. The exact mechanism of this effect is unknown, but may be related to changes in the control of LH or down-regulation of LH receptors.
Onset:
Females: Estradiol suppression reaches postmenopausal levels within 3 weeks and FSH and LH are suppressed to follicular phase levels within 4 weeks of initiation
Males: Testosterone suppression reaches castrate levels within 2 to 4 weeks after initiation
Duration:
Females: Estradiol, LH and FSH generally return to baseline levels within 12 weeks following the last monthly implant.
Males: Testosterone levels maintained at castrate levels throughout the duration of therapy.
Absorption: SubQ: Rapid and can be detected in serum in 30 to 60 minutes; 3.6 mg: released slowly in first 8 days, then rapid and continuous release for 28 days
Distribution: Vd: Male: 44.1 L; Female: 20.3 L
Protein binding: ~27%
Metabolism: Hepatic hydrolysis of the C-terminal amino acids
Time to peak, serum: SubQ: Male: 12 to 15 days, Female: 8 to 22 days
Excretion: Urine (>90%; 20% as unchanged drug)
Gender: The total body Cl of goserelin was significantly (P <0.05) greater (163.9 vs 110.5 L/min) in women compared with men.
Body weight: A decline in AUC of approximately 1% to 2.5% was observed with a kg increase in body weight.
Implant (Zoladex Subcutaneous)
3.6 mg (per each): $940.33
10.8 mg (per each): $2,636.46
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
