Goserelin
Also known as: Goserelin acetate, Zoladex, ICI-118630
Goserelin is a GnRH agonist delivered as a slowly releasing implant. It suppresses testosterone or ovarian estrogen after an initial flare and has approved uses in prostate cancer, selected breast cancer and gynecologic care.
Quick Facts
What is goserelin?
Goserelin acetate, marketed as Zoladex and developed as ICI-118630, is a ten-amino-acid GnRH/LHRH analog. A wax-like cylinder inserted under abdominal skin releases the drug gradually. Its stronger, sustained signal differs from natural hypothalamic pulses. It received US approval in 1989.
How does goserelin work?
The first dose briefly increases pituitary LH and sex-hormone levels. With continuous implant exposure, receptors downregulate and desensitize; within a few weeks, LH and FSH decrease. Testosterone can reach castrate levels in men, and ovarian estrogen can reach postmenopausal levels in women.
Testosterone suppression targets hormone-sensitive prostate cancer. Ovarian-estrogen suppression can treat estrogen-receptor-positive premenopausal breast cancer. A reversible low-estrogen state also reduces endometriosis lesions.
In long-term ZEBRA follow-up, goserelin matched standard CMF chemotherapy for disease-free and overall survival in premenopausal women with estrogen-receptor-positive, node-positive early breast cancer, without chemotherapy’s acute toxicity. That result concerns this defined population and comparison.
Sources: [1]
Is it FDA-approved?
FDA approved goserelin in 1989 following development by ICI Pharmaceuticals, later Zeneca and AstraZeneca. Implant strengths are 3.6 mg for monthly administration and 10.8 mg for three-month administration. Approved uses and strengths are product specific.
Sources: [2]
What is goserelin prescribed for?
Prescribing uses include advanced prostate cancer, sometimes with radiotherapy or an anti-androgen; advanced breast cancer in pre- and perimenopausal women; endometriosis; and endometrial thinning before surgical ablation for heavy uterine bleeding. It is contraindicated during pregnancy.
What are the side effects?
Common effects include hot flashes, sweating, sexual dysfunction, vaginal dryness, headache and implant-site reactions. Long-term suppression can reduce bone density. Prostate-cancer symptoms may flare initially, sometimes prompting temporary anti-androgen use. Longer-term androgen deprivation also carries hyperglycemia and cardiovascular risks; pituitary apoplexy is rare.
References and further reading
This reference draws on Superpower’s Peptide Library and the research linked below. Peptide Dossier’s editorial team adapted and integrated the material on .
- 10.1016/s0959-8049(03)00392-7How does goserelin work?Cited in: How does goserelin work?
- accessdata.fda.govIs it FDA-approved?Cited in: Is it FDA-approved?
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Disclaimer: This article is for informational and educational purposes only. It is not intended as medical advice. The information presented is based on published research and should not be used as a substitute for professional medical guidance. Always consult a qualified healthcare provider before starting any peptide protocol. Some peptides discussed may not be approved for human use by the FDA or equivalent regulatory bodies.