Goserelin Uses, Dosage, Side Effects and more
Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal.
The pharmacokinetics of goserelin have been determined in both male and female healthy volunteers and patients. In these studies, goserelin was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route.
| Trade Name | Goserelin |
| Availability | Prescription only |
| Generic | Goserelin |
| Goserelin Other Names | Goserelin, Goserelina |
| Related Drugs | estradiol, tamoxifen, Premarin, testosterone, tranexamic acid, norethindrone, medroxyprogesterone, megestrol, Xtandi, Provera |
| Weight | 10.8mg, 3.6mg |
| Type | Subcutaneous, Subcutaneous Implant, Implant |
| Formula | C59H84N18O14 |
| Weight | Average: 1269.4105 Monoisotopic: 1268.641439486 |
| Protein binding | 27.3% |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | January 7, 2025 at 1:49 am |
Uses
Goserelin is a synthetic analog of luteinizing hormone-releasing hormone used to treat breast cancer and prostate cancer by reducing secretion of gonadotropins from the pituitary.
Goserelin is indicated for:
- Use in combination with flutamide for the management of locally confined carcinoma of the prostate
- Palliative treatment of advanced carcinoma of the prostate
- The management of endometriosis
- Use as an endometrial-thinning agent prior to endometrial ablation for dysfunctional uterine bleeding
- Use in the palliative treatment of advanced breast cancer in pre- and perimenopausal women
Goserelin is also used to associated treatment for these conditions: Advanced Breast Cancer, Early Breast Cancer, Endometriosis, Advanced carcinoma of the prostate, Stage M1 hormone dependent carcinoma of the prostate, Stage T2b carcinoma of the prostate, Stage T2c carcinoma of the prostate, Stage T3 carcinoma of the prostate, Stage T4 carcinoma of the prostate, Endometrial thinning prior to endometrial ablation for dysfunctional uterine bleeding
How Goserelin works
Goserelin is a synthetic decapeptide analogue of LHRH. Goserelin acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels.
Toxicity
No experience of overdosage from clinical trials.
Food Interaction
No interactions found.Drug Interaction
Moderate: glycerin, glycerinMinor: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprimUnknown: aspirin, aspirin, calcium / vitamin d, calcium / vitamin d, ubiquinone, ubiquinone, copper gluconate, copper gluconate, acetaminophen, acetaminophen, bioflavonoids, bioflavonoids, valproic acid, valproic acid, cholecalciferol, cholecalciferol
Disease Interaction
Moderate: bone mineral density, CV disease, hyperglycemia, QTc interval prolongation
Volume of Distribution
- 44.1 ± 13.6 L [subcutaneous administration of 250 mcg]
Elimination Route
Inactive orally, rapidly absorbed following subcutaneous administration.
Half Life
4-5 hours
Clearance
- 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot]
Elimination Route
Clearance of goserelin following subcutaneous administration of a radiolabeled solution of goserelin was very rapid and occurred via a combination of hepatic and urinary excretion. More than 90% of a subcutaneous radiolabeled solution formulation dose of goserelin was excreted in urine.
