Goserelin
Zoladex, Zoladex LA, ICI 118630, goserelin acetate
1What it is
Goserelin is a GnRH superagonist developed by ICI (later AstraZeneca) in the late 1970s and launched in 1987 as Zoladex. Its distinguishing feature is not the peptide but the delivery: it is embedded in a small rod of biodegradable lactide-glycolide polymer that is injected under the skin of the abdomen with a pre-loaded 16-gauge needle and dissolves over one or three months. That made it the first long-acting depot GnRH and it remains a standard hormone therapy in prostate cancer, premenopausal breast cancer, endometriosis and before uterine surgery. The US rights now sit with a smaller specialty company; AstraZeneca retains it in many other markets.
Community or self-directed use is essentially absent — the product is an implant placed by a clinician.
2How it's thought to work
Identical in principle to the other (see Buserelin, #211). After an initial LH/FSH surge over 1–2 weeks, pituitary GnRH receptors are down-regulated and testosterone falls to castrate levels by about day 21; oestradiol in women falls to postmenopausal levels within about 3 weeks. Effects reverse after the implant is exhausted, typically over 2–3 months, though recovery can be slower after prolonged use or in older men.
3What the research shows
Advanced prostate cancer
Locally advanced prostate cancer with radiotherapy
Premenopausal breast cancer
Ovarian protection during chemotherapy
Endometriosis and pre-operative fibroid/endometrial thinning
4Reported side effects and interactions
Literature-reported
hot flushes (very common), loss of libido, erectile dysfunction, gynaecomastia and breast tenderness in men; vaginal dryness, headache, mood change and bone loss in women; injection-site bruising or haematoma (occasionally serious, including vascular injury from the large needle, which prompted a label warning); tumour flare in the first weeks with possible ureteric obstruction or spinal-cord compression in men with metastases. Long-term androgen deprivation is associated with bone fracture, diabetes, cardiovascular events and QT prolongation.Community-reported
essentially none documented outside prescribed use.Theoretical. pituitary apoplexy has been reported very rarely after first dose in people with undiagnosed pituitary adenomas (class effect).
Interactions. additive QT-prolonging risk with antiarrhythmics and some antipsychotics; concurrent anti-androgens for flare cover; glucose-lowering drugs may need adjustment over long courses.
Markers researchers commonly monitor
Drawn from label and oncology guideline monitoring:
| Marker | Why it's watched |
|---|---|
| Testosterone and PSA (men) | confirms castrate suppression and tumour response; a rising PSA at castrate testosterone signals castration resistance. |
| Oestradiol, LH, FSH (women) | confirms ovarian suppression; relevant when combined with an aromatase inhibitor, which requires full suppression. |
| Bone mineral density (DEXA) | baseline and periodic for courses beyond 6 months. |
| HbA1c, lipid panel, blood pressure, weight | metabolic consequences of long-term androgen deprivation. |
| ECG (QTc) | in men with cardiac history or on QT-prolonging co-medication. |
| Haemoglobin | mild anaemia is common under long-term androgen deprivation. |
Free for everyone. Safety information is never behind a paywall.
5Reconstitution and handling
A pre-filled implant-and-applicator unit; no or calculation is involved. Placed subcutaneously in the anterior abdominal wall below the navel by a trained clinician, avoiding the inferior epigastric vessels. The calculator is not applicable.
6Commonly studied alongside
Bicalutamide or flutamide (flare cover and combined androgen blockade), radiotherapy (EORTC 22863), tamoxifen or aromatase inhibitors (ovarian suppression in breast cancer), buserelin (#211), histrelin (#213), degarelix (#214), and the other GnRH analogue profiles (#102–#108).
Informational cross-links. Not stack recommendations.
7Regulatory status by region
| Region | Status (checked —) |
|---|---|
| United States | FDA-approved (Zoladex 3.6 mg and 10.8 mg): prostate cancer palliation; with flutamide and radiotherapy for locally advanced disease; endometriosis, endometrial thinning and advanced breast cancer (3.6 mg); 10.8 mg indications in women † |
| European Union | Nationally authorised in all major markets (Zoladex / Zoladex LA) |
| United Kingdom | MHRA-licensed; prescription-only |
| Australia | TGA-registered (Zoladex 3.6 mg and 10.8 mg); PBS-listed |
| South Africa | SAHPRA-registered; prescription-only |
| Sport (WADA) | Prohibited in males under S2 (goserelin named among LH-releasing factors); not prohibited in females |
8Open questions
- Whether GnRH antagonists reduce cardiovascular events compared with in men with existing heart disease (PRONOUNCE was inconclusive; see Degarelix, #214).
- Intermittent versus continuous androgen deprivation: non-inferiority remains debated for metastatic disease.
- How durable fertility preservation is after goserelin-protected chemotherapy.
9References
- 1Bolla M et al. (1997). Improved survival in patients with locally advanced prostate cancer treated with radiotherapy and goserelin. NEJM. PubMed · DOI
- 2Bolla M et al. (2010). External irradiation with or without long-term androgen suppression for prostate cancer with high metastatic risk: 10-year results of an EORTC randomised study. Lancet Oncol. PubMed · DOI
- 3Jonat W et al. (2002). Goserelin versus cyclophosphamide, methotrexate, and fluorouracil as adjuvant therapy in premenopausal patients with node-positive breast cancer: the ZEBRA study. J Clin Oncol. PubMed · DOI
- 4Moore HCF et al. (2015). Goserelin for ovarian protection during breast-cancer adjuvant chemotherapy (POEMS). NEJM. PubMed · DOI
- 5Kaisary AV et al. (1991). Comparison of LHRH analogue (Zoladex) with orchiectomy in patients with metastatic prostatic carcinoma. Br J Urol. PubMed · DOI
- 6Zoladex (goserelin acetate implant) US prescribing information (current label). PubMed
References are being resolved to PubMed/DOI identifiers; links search PubMed for the citation until then.
† Being confirmed by our reviewers against current sources.
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Self-reported side effects Phase 2
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