Goserelin
Also known as: Zoladex, ICI 118630
A GnRH agonist implant used for prostate cancer, breast cancer, endometriosis and endometrial thinning. FDA-approved as Zoladex. Prescription drug.
Last updated
Mechanism of Action
Goserelin is a synthetic decapeptide analog of GnRH delivered as a small biodegradable implant injected under the skin of the abdomen. Like other GnRH agonists it briefly stimulates LH and FSH release, then continuous exposure desensitizes pituitary GnRH receptors and gonadotropin output falls. Testosterone reaches castrate levels in men and estradiol reaches postmenopausal levels in premenopausal women, typically within 2-4 weeks. The polymer matrix releases drug steadily over 28 days (3.6 mg) or 12 weeks (10.8 mg).
- Half-life
- ~4-5 hours (drug released continuously from the implant)
- Administration Routes
- Subcutaneous implant
- Research Status
- Clinical
Reported Benefits
- Androgen deprivation for prostate cancer, including with radiotherapy for locally advanced disease
- Palliative treatment of advanced breast cancer in pre- and perimenopausal women (3.6 mg)
- Management of endometriosis (3.6 mg)
- Endometrial thinning before endometrial ablation (3.6 mg)
Potential Side Effects
- Hot flashes, sweating and sexual dysfunction
- Injection-site injury and vascular injury, including abdominal bleeding (label warning)
- Transient tumor flare at the start of treatment
- Bone mineral density loss
- Hyperglycemia and increased cardiovascular risk in men
Common Dosing
Goserelin is given by a clinician as a subcutaneous implant into the anterior abdominal wall: the 3.6 mg implant every 28 days and, for prostate cancer only, the 10.8 mg implant every 12 weeks. Treatment length depends on the indication; courses for endometriosis are limited because of bone loss. Dosing is set and supervised by the prescribing clinician.
The dosing information above is aggregated from research literature and anecdotal community reports for educational purposes only. It is not a recommendation, prescription, or medical advice. Peptides are sold as research chemicals only and are not intended for human use.
Contraindications
- Hypersensitivity to GnRH, GnRH agonists or any component
- Pregnancy, unless used for palliative treatment of advanced breast cancer
- The 10.8 mg implant is not indicated in women
No documented stacking partners for Goserelin yet.
- View
Improved survival in patients with locally advanced prostate cancer treated with radiotherapy and goserelin
1997
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Goserelin for ovarian protection during breast-cancer adjuvant chemotherapy
2015
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Goserelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical use in sex hormone-related conditions
1991