Buserelin

Summary

Buserelin is a synthetic GnRH agonist used to suppress gonadal steroid production in hormone-sensitive conditions including prostate cancer, endometriosis, uterine fibroids, and for pituitary desensitization in assisted reproduction protocols.

Mechanism of Action

Synthetic analogue of gonadotropin-releasing hormone (GnRH). Initial stimulation of LH and FSH release is followed by downregulation and desensitization of pituitary GnRH receptors, leading to suppression of gonadotropins and subsequent reduction in sex steroid (testosterone/estrogen) production.

Routes of Administration

Goals & Uses

• Controlled ovarian stimulation / ARTReproductive MedicineHigh
• Precocious pubertyPediatric EndocrinologyModerate
• Prostate cancer treatment (androgen deprivation)OncologyHigh
• Uterine fibroids (leiomyomata)GynecologyHigh
• Endometriosis managementGynecologyHigh
• Gender-affirming hormone therapy (puberty suppression)EndocrinologyModerate

Contraindications

• Hypersensitivity to GnRH or analoguesImmunologicalHigh
• Osteoporosis (pre-existing severe)MusculoskeletalModerate
• Undiagnosed vaginal bleedingGynecologicalHigh
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• BreastfeedingPopulationModeratePotential transfer into breast milk or insufficient safety data

Adverse Effects

• Hot flushes / vasomotor symptomsEndocrine/VasomotorCommon
• Injection site reactionsLocalCommon
• Decreased bone mineral densityMusculoskeletalCommon
• Mood changes / depressionPsychiatricUncommon
• Sexual dysfunction / loss of libidoSexual HealthCommon
• Tumor flare (prostate cancer)OncologicalUncommon

Drug Interactions

• Gonadotropins (FSH/LH preparations)Low
• Insulin / antidiabetic agentsModerate
• QT-prolonging agentsModerate
• Anti-androgens (e.g., flutamide, bicalutamide)Low

Population Constraints

• Patients with depression or psychiatric historyPsychiatricRelative
• Elderly patients with cardiovascular diseaseCardiovascularRelative
• Patients with osteopenia/osteoporosisMusculoskeletalRelative
• Pediatric use (prepubertal / early pubertal)AgeRelative

Regulatory Status

• European UnionApprovedApproved: Prostate cancer (hormone-sensitive), Endometriosis, Uterine fibroids (preoperative), Assisted reproduction (pituitary desensitization)Approved in multiple EU member states under brand names including Suprefact and Profact.
• United StatesUnapprovedNot FDA-approved; other GnRH agonists (leuprolide, goserelin, histrelin) used instead. May be available via compounding pharmacies.
• United KingdomApprovedApproved: Prostate cancer, Endometriosis, Assisted reproductionLicensed in the UK; nasal spray and injection formulations available.

Approved in multiple countries including EU member states and Canada. Not FDA-approved in the United States; leuprolide and other GnRH agonists are preferred in the US market. Available as nasal spray, subcutaneous injection, and implant formulations depending on jurisdiction.

Evidence & Sources

No sources recorded yet.