Goserelin Research & Studies

Goserelin is a gonadotropin-releasing hormone (GnRH) agonist with a long history of clinical application and well-established efficacy and safety profile. Its mechanism of action centers on sustained GnRH receptor desensitization, leading to pituitary downregulation, ovarian suppression, and reduction of estradiol and progesterone to postmenopausal levels; this forms the basis for its efficacy in hormone-dependent gynecological conditions. Over the past three decades, the use of goserelin has been expanded to an increasing number of indications and clinical scenarios. Approved gynecological indications of goserelin include endometriosis, uterine fibroids, usage as an agent for endometrial thinning, and usage as an agent for ovarian downregulation prior to assisted reproduction. More recent research continues to explore the use of goserelin in gynecological diseases such as adenomyosis and different types of female cancers. Goserelin may also be a useful tool in clinical scenarios where gynecologic management is required as part of multi-disciplinary therapy. This review consolidates the established and emerging roles of goserelin across the broad spectrum of benign and malignant gynecological conditions, underscoring its remarkable clinical versatility and the breadth of evidence that support its continued expansion of utility in contemporary practice.

Clinical trials demonstrated every 3-month goserelin 10.8 mg to be non-inferior to monthly goserelin 3.6 mg in premenopausal patients with ER-positive breast cancer. However, real-world studies comparing 3-month goserelin 10.8 mg with monthly goserelin 3.6 mg are scarce.

Few studies compared the effectiveness of the 3-monthly goserelin 10.8-mg and the monthly 3.6-mg depot in inducing ovarian function suppression for premenopausal patients with hormone receptor positive (HR+) breast cancer. We conducted a large-scale real-world study (RWS) in China to validate the non-inferiority of goserelin 10.8-mg to the 3.6-mg depot.

Goserelin is widely employed as a form of androgen deprivation therapy in the management of prostate cancer. Given the chronic nature of hormonal therapy, sustained and long-term drug administration is essential to ensure therapeutic efficacy. Goserelin is often formulated as sustained-release implants or microspheres requiring intramuscular injections. Both delivery methods necessitate administration by trained healthcare personnel and are frequently associated with poor patient compliance due to procedural invasiveness and considerable discomfort. Herein, we developed a goserelin microsphere-loaded microneedle (GSR-MN) patch as a minimally invasive alternative. The microneedles exhibit robust mechanical strength and rapid dissolution properties, enabling them to effectively penetrate the stratum corneum and facilitate the delivery of goserelin microspheres into the underlying skin tissue. The GSR-MN patch demonstrates excellent biocompatibility and biosafety, and is capable of sustaining goserelin release over a 28-day period. The therapeutic outcomes were comparable to those of conventional intramuscular goserelin microsphere administration, offering a promising strategy to improve patient adherence and reduce treatment-associated discomfort.

LY01005 (Goserelin acetate sustained-release microsphere injection) is a modified gonadotropin-releasing hormone (GnRH) agonist injected monthly. This phase III trial study aimed to evaluated the efficacy and safety of LY01005 in Chinese patients with prostate cancer.

To assess the long-term (20-year) endocrine therapy benefit in premenopausal patients with breast cancer.

We investigated the efficacy and safety of fulvestrant plus goserelin (F + G) versus anastrozole plus goserelin (A + G) in comparison with goserelin (G) alone in premenopausal women with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-), tamoxifen-pretreated metastatic breast cancer (MBC).

Acylation of peptides is a well-known but unwanted phenomenon in polyester matrices such as poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres used as controlled release formulations. Acylation normally occurs on lysine residues and the N-terminus of the peptide. The purpose of the present work was to assess other possible acylation sites on peptides. Goserelin was used as a model peptide that lacks lysine and a free N-terminus, but contains other nucleophilic residues, i.e. serine, tyrosine and arginine, which potentially can be acylated. Goserelin loaded PLGA microspheres were prepared by a double emulsion solvent evaporation technique. Liquid chromatography ion-trap mass spectrometry (LC-ITMS) was used for determining and monitoring acylation of released goserelin. It is demonstrated that arginine is subjected to acylation with glycolic acid and lactic acid units of PLGA, which was followed by loss of NH3 from the guanidine group to obtain 2-oxazolin-4-one and 5-methyl-2-oxazolin-4-one residues with masses that are 41 and 55Da higher, respectively, than the native goserelin. There was no evidence for acylation of serine and tyrosine in goserelin. Our results demonstrate that beside lysine also acylation of arginine can occur in peptides and proteins that are loaded and released from PLGA matrixes.

Ovarian failure is a common toxic effect of chemotherapy. Studies of the use of gonadotropin-releasing hormone (GnRH) agonists to protect ovarian function have shown mixed results and lack data on pregnancy outcomes.

Women with symptomatic uterine leiomyomas (fibroids) may have iron-deficiency anemia (IDA); therefore, surgery places them at risk of blood-borne morbidity from perioperative transfusions. Such women might benefit from a preoperative treatment that restores hematologic normality and alleviates fibroid symptoms.

The luteinising hormone-releasing hormone analogue goserelin ('Zoladex') suppresses ovarian oestrogen production in pre- and perimenopausal women. Goserelin is a biodegradable, sustained-release 3.6 mg depot that is administered by subcutaneous injection every 28 days. Clinical trials in premenopausal women with hormone-sensitive early breast cancer have demonstrated that goserelin alone, or in combination with tamoxifen, is at least as effective as cyclophosphamide, methotrexate, 5-fluorouracil (CMF) chemotherapy. Goserelin plus tamoxifen after cyclophosphamide, doxorubicin and 5-fluorouracil (CAF) chemotherapy resulted in improved disease-free survival compared with CAF alone. These trials have also shown that goserelin is well tolerated and is associated with less acute toxicity than cytotoxic chemotherapy. Early improvements in quality of life over the first 3-6 months of goserelin treatment support the use of this agent as an alternative to chemotherapy in this patient population. Patients should be provided with information on the benefits and risks associated with available treatment options so that they can be involved in the decision-making process.

Goserelin is a synthetic decapeptide analogue of luteinising hormone-releasing hormone (LHRH). For experimental purposes it has been administered subcutaneously as an aqueous solution, but for therapeutic use it is formulated as subcutaneous depots releasing goserelin over periods of 1 (3.6 mg) or 3 (10.8 mg) months. Pharmacokinetic data have been generated using a specific radioimmunoassay. When administered as a solution, goserelin is rapidly absorbed and eliminated from serum with a mean elimination half-life (t1/2beta) of 4.2 hours in males and 2.3 hours in females. The shapes of the observed serum goserelin profiles following administration of the depots are primarily determined by the rate of goserelin release from the biodegradable lactide-glycolide copolymer matrix over periods of 1 or 3 months. There is no clinically relevant accumulation of goserelin during multiple administration of these depots. Goserelin is extensively metabolised prior to excretion. Its pharmacokinetics are unaffected by hepatic impairment, but the mean t1/2beta increases to 12.1 hours in patients with severe renal impairment. This suggests that the total renal clearance (renal metabolism and unchanged drug) is decreased in patients with renal dysfunction. It is unnecessary to adjust the dose or administration interval when the depot formulations are administered to elderly patients or to those with impaired renal or hepatic function. Administration of a goserelin 3.6 mg or 10.8 mg depot results in an initial increase of luteinising hormone (LH) levels and in increases of serum testosterone or oestradiol levels in males and females, respectively. This is followed by a decrease in serum LH levels and suppression of testosterone or oestradiol to within the castrate or menopausal range, respectively. Subsequently, throughout treatment with goserelin depots, serum testosterone or oestradiol levels remain suppressed. Clinical outcomes following treatment of patients with prostate cancer, breast cancer and benign gynaecological conditions with goserelin are described briefly.