pharmacopeia
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/api/v1/drug/goserelin

Mechanism of action

Sourced from openFDA

ZOLADEX is a synthetic decapeptide analogue of GnRH. ZOLADEX acts as an inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation.

Gonadotropin Releasing Hormone Receptor

Indications

Sourced from openFDA
  • ZOLADEX is a Gonadotropin Releasing Hormone (GnRH) agonist indicated for: Use in combination with flutamide for the management of locally confined carcinoma of the prostate ( 1.1 ) Palliative treatment of advanced carcinoma of the prostate ( 1.2 ) The management of endometriosis ( 1.3 ) Use as an endometrial-thinning agent prior to endometrial ablation for dysfunctional uterine bleeding ( 1.4 ) Use in the palliative treatment of advanced breast cancer in pre- and perimenopausal women ( 1.5 ) 1.1 Stage B2-C Prostatic Carcinoma ZOLADEX is indicated for use in combination with flutamide for the management of locally confined Stage T2b-T4 (Stage B2-C) carcinoma of the prostate. Treatment with ZOLADEX and flutamide should start 8 weeks prior to initiating radiation therapy and continue during radiation therapy [see Dosage and Administration ( 2.1 ) and Clinical Studies ( 14.1 )].ICD-10: C50.919, N80.9

Contraindications

Sourced from openFDA
  • Hypersensitivity ( 4.1 ) Pregnancy unless used for treatment of advanced breast cancer ( 4.2 ) 4.1 Hypersensitivity Anaphylactic reactions to ZOLADEX have been reported in the medical literature. ZOLADEX is contraindicated in those patients who have a known hypersensitivity to GnRH, GnRH agonist analogues or any of the components in ZOLADEX [see Warnings and Precautions ( 5.6 )].contraindicated

Dosage & administration

Sourced from openFDA

ZOLADEX, at a dose of 3.6 mg, should be administered subcutaneously every 28 days into the anterior abdominal wall below the navel line using an aseptic technique under the supervision of a physician [see Dosage and Administration ( 2.7 )]. While a delay of a few days is permissible, every effort should be made to adhere to the 28-day schedule. ZOLADEX 3.6 mg should be administered subcutaneously every 28 days ( 2.1 , 2.7 ) For the management of endometriosis, the recommended duration of administration is 6 months for women 18 years of age and older ( 2.3 ) 2.1 Stage B2-C Prostatic Carcinoma When ZOLADEX is given in combination with radiotherapy and flutamide for patients with Stage T2b-T4 (Stage B2-C) prostatic carcinoma, treatment should be started 8 weeks prior to initiating radiotherapy and should continue during radiation therapy. A treatment regimen using a ZOLADEX 3.6 mg depot 8 weeks before radiotherapy, followed in 28 days by the ZOLADEX 10.8 mg depot, can be administered. Alternatively, four injections of 3.6 mg depot can be administered at 28-day intervals, two depots preceding and two during radiotherapy. 2.2 Prostatic Carcinoma For the management of advanced prostate cancer, ZOLADEX is intended for long-term administration unless clinically inappropriate. 2.3 Endometriosis For the management of endometriosis, the recommended duration of administration is 6 months. Currently, there are no clinical data on the effect of treatment of benign gynecological conditions with ZOLADEX for periods in excess of 6 months.

Warnings & precautions

Sourced from openFDA

Women of Childbearing Potential and Pregnancy: Pregnancy must be excluded for use in benign gynecological conditions. Women should avoid pregnancy ( 5.1 ) Tumor Flare Phenomenon: Transient worsening of tumor symptoms may occur during the first few weeks of treatment with ZOLADEX, which may include ureteral obstruction and spinal cord compression. Monitor patients at risk for complications of tumor flare ( 5.2 , 6.2 ) Hyperglycemia and Diabetes: Hyperglycemia and an increased risk of developing diabetes have been reported in men receiving GnRH analogs. Monitor blood glucose level and manage according to current clinical practice ( 5.3 ) Cardiovascular Diseases: Increased risk of myocardial infarction, sudden cardiac death and stroke has been reported in association with use of GnRH analogs in men. Monitor for cardiovascular disease and manage according to current clinical practice ( 5.4 ) Hypercalcemia: Hypercalcemia has been reported in patients with bone metastases treated with ZOLADEX. Monitor and manage appropriately ( 5.5 ) Hypersensitivity: Systemic hypersensitivity has been reported in patients receiving goserelin/ZOLADEX implants ( 4.1 , 5.6 ) Severe Cutaneous Adverse Reactions: ZOLADEX can cause severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome/toxic epidermal necrolysis. Interrupt ZOLADEX if signs or symptoms of SCARs develop. Permanently discontinue ZOLADEX if SCARs are confirmed. ( 5.7 ) Cervical Resistance: Increase in cervical resistance may occur.

Adverse reactions

Sourced from openFDA

The most common, clinically significant adverse reactions occurring in >10% of men: hot flashes, sexual dysfunction, decreased erections and lower urinary tract symptoms ( 6 ) The adverse event profile was similar for women treated for breast cancer, dysfunctional uterine bleeding or endometriosis and included (>20%): hot flushes, headache, sweating, acne, emotional lability, depression, decreased libido, vaginitis, breast atrophy, seborrhea, and peripheral edema ( 6 ) Tumor flare can occur on the initiation of ZOLADEX for both men and women being treated for cancer ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact TerSera Therapeutics at 1-844-334-4035 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Stage B2-C Prostatic Carcinoma Treatment with ZOLADEX and flutamide did not add substantially to the toxicity of radiation treatment alone. The following adverse experiences were reported during a multicenter clinical trial comparing ZOLADEX + flutamide + radiation versus radiation alone.

Use in specific populations

Sourced from openFDA

Nursing mothers: Discontinue drug or nursing taking into account the importance of drug to the mother ( 8.3 ) No information available for use in Pediatric patients ( 8.4 ) Geriatric ( 8.5 ) Renal and Hepatic Impairment: No dose adjustment is necessary ( 2.6 , 8.6 , 8.7 ) 8.1 Pregnancy ZOLADEX is contraindicated during pregnancy unless ZOLADEX is being used for palliative treatment of advanced breast cancer. There are no adequate and well-controlled studies in pregnant women using ZOLADEX. Based on mechanism of action in humans and findings of increased pregnancy loss in animal studies, ZOLADEX can cause fetal harm when administered to a pregnant woman. If this drug is used during pregnancy, the patient should be apprised of the potential hazard to the fetus. There is an increased risk for pregnancy loss due to expected hormone changes that occur with ZOLADEX treatment. ZOLADEX crosses the placenta in rats and rabbits following subcutaneous administration. Administration of goserelin to pregnant rats and rabbits during organogenesis resulted in increased preimplantation loss and increased resorptions. When pregnant rats received goserelin throughout gestation and lactation, there was a dose-related increase in umbilical hernia in offspring. In additional reproduction studies in rats, goserelin decreased fetus and pup survival.

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetics of ZOLADEX have been determined in both male and female healthy volunteers and patients. In these studies, ZOLADEX was administered as a single 250 mcg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route.

Overdosage

Sourced from openFDA

The pharmacologic properties of ZOLADEX and its mode of administration make accidental or intentional overdosage unlikely. There is no experience of overdosage from clinical trials. Animal studies indicate that no increased pharmacologic effect occurred at higher doses or more frequent administration. Subcutaneous doses of the drug as high as 1 mg/kg/day in rats and dogs did not produce any nonendocrine related sequelae; this dose is up to 250 times the estimated human daily dose based on the body surface area. If overdosage occurs, it should be managed symptomatically.

Approval history

Sourced from openFDA
  • Dec 29, 1989NDANDA019726Tersera
  • Jan 11, 1996NDANDA020578Tersera

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
13,078 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Death1,57912%
  2. 2Malignant Neoplasm Progression1,31410%
  3. 3Fatigue8626.6%
  4. 4Metastases To Bone6865.2%
  5. 5Neutropenia6374.9%
  6. 6Nausea5714.4%
  7. 7Hot Flush5143.9%
  8. 8Asthenia5033.8%
  9. 9Diarrhoea4773.6%
  10. 10Pain4713.6%
  11. 11Off Label Use4603.5%
  12. 12Dyspnoea4393.4%
  13. 13Metastases To Liver4343.3%
  14. 14Arthralgia4243.2%
  15. 15Headache3953.0%

Literature

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Recent PubMed references pinned to Goserelin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 407 ClinicalTrials.gov registrations naming Goserelin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Goserelin work?
ZOLADEX is a synthetic decapeptide analogue of GnRH. ZOLADEX acts as an inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation.
What is Goserelin used for?
According to FDA labeling, Goserelin carries indications including: ZOLADEX is a Gonadotropin Releasing Hormone (GnRH) agonist indicated for: Use in combination with flutamide for the management of locally confined carcinoma of the prostate ( 1.1 ) Palliative treatment of advanced carcinoma of the prostate ( 1.2 ) The management of endometriosis ( 1.3 ) Use as an endometrial-thinning agent prior to endometrial ablation for dysfunctional uterine bleeding ( 1.4 ) Use in the palliative treatment of advanced breast cancer in pre- and perimenopausal women ( 1.5 ) 1.1 Stage B2-C Prostatic Carcinoma ZOLADEX is indicated for use in combination with flutamide for the management of locally confined Stage T2b-T4 (Stage B2-C) carcinoma of the prostate. Treatment with ZOLADEX and flutamide should start 8 weeks prior to initiating radiation therapy and continue during radiation therapy [see Dosage and Administration ( 2.1 ) and Clinical Studies ( 14.1 )].. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Goserelin?
Goserelin is classified as Gonadotropin releasing hormone analogues, Gonadotropin Releasing Hormone Receptor Agonist, Gonadotropin Releasing Hormone Receptor Agonists, Pituitary Gland Activity Alteration, Testicular Endocrine Activity Alteration.
What are the brand names for Goserelin?
Goserelin is marketed under brand names including Zoladex.
What are the contraindications for Goserelin?
Goserelin labeling lists contraindications including: Hypersensitivity ( 4.1 ) Pregnancy unless used for treatment of advanced breast cancer ( 4.2 ) 4.1 Hypersensitivity Anaphylactic reactions to ZOLADEX have been reported in the medical literature. ZOLADEX is contraindicated in those patients who have a known hypersensitivity to GnRH, GnRH agonist analogues or any of the components in ZOLADEX [see Warnings and Precautions ( 5.6 )].. Always consult the full prescribing information and a clinician.
Note. Data for goserelin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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