Overview
Buserelin is a synthetic nonapeptide analogue of gonadotropin-releasing hormone developed by Hoechst in the 1970s and 1980s. It carries a tert-butyl-protected D-serine at position 6 and a C-terminal proline ethylamide in place of the native glycine amide, giving it much greater potency and a longer duration of action than natural GnRH. It is marketed in several European and other countries as Suprefact, but it has not been marketed in the United States.
Buserelin has a long history in assisted reproduction research, where GnRH agonists are used to down-regulate the pituitary before controlled ovarian stimulation so that premature LH surges are prevented. It has also been studied in endometriosis and prostate cancer, and it is used in veterinary reproductive management. For researchers, buserelin is a well-characterised agonist for studying pituitary desensitisation, the timing of the LH surge, and the dependence of reproductive tissues on gonadal steroids. Its availability in multiple formulations has also made it a subject of peptide delivery research.
Mechanism studied
- Buserelin
- GnRH receptor
- Pituitary desensitisation
- Sex steroids ↓
Buserelin activates GnRH receptors on anterior pituitary gonadotrophs, initially provoking release of luteinising hormone and follicle-stimulating hormone. Sustained occupancy then leads to receptor desensitisation, uncoupling from intracellular signalling, internalisation and reduced gonadotropin synthesis. The resulting fall in LH and FSH lowers ovarian oestradiol or testicular testosterone production. In assisted reproduction research this suppressed state allows investigators to control follicle development with exogenous gonadotropins and to prevent spontaneous ovulation. The biphasic stimulatory-then-inhibitory response is shared with other GnRH superagonists and is fully reversible after exposure ends.
Research highlights
- 01Synthesised by Hoechst during the first wave of GnRH superagonist development in the 1970s.
- 02Became a common pituitary down-regulation agent in IVF research in Europe during the 1980s and 1990s.
- 03Studied in prostate cancer and endometriosis, often alongside comparative work with other agonists.
- 04Applied in veterinary reproduction to synchronise ovulation in livestock and companion animals.
- 05Open questions include optimal strategies for pituitary suppression and their effects on oocyte and endometrial quality.
Latest published research
1,496 papers on PubMed →Is there a difference in ovarian hyperstimulation syndrome rates in freeze-all treatment cycles in high-risk patients treated with different GnRH agonist triggers?
Shah R et al. · Human fertility (Cambridge, England) · 2026 Dec · PMID 42831293
Ovulation Timing After Recombinant Human Chorionic Gonadotropin, Gonadorelin, or Buserelin Under Estrus-Triggered and Fixed-Time Treatment Protocols for Artificial Insemination in Sows
Fang Z et al. · Animals : an open access journal from MDPI · 2026 Oct 15 · PMID 42939176
Ex Vivo Evaluation of Buserelin Permeation Across Porcine Endometrial Tissue: A Pilot Study
Taechamaeteekul P et al. · Animals : an open access journal from MDPI · 2026 Oct 3 · PMID 42883077
Field Implementation of Buserelin-Supplemented Boar Semen Protocol at the First Insemination: Farrowing Rate and Litter Size in Gilts and Sows Under Tropical Conditions
Taechamaeteekul P et al. · Animals : an open access journal from MDPI · 2026 Oct 2 · PMID 42883070
Buserelin Improves Ovulation-Embryo Synchrony Compared With hCG After eCG-Induced Superovulation in Donor Sows
Lopez-Jara A et al. · Reproduction in domestic animals = Zuchthygiene · 2026 Oct · PMID 42817029
Intravaginal GnRH analogues in rabbits: Fertirelin as the most effective option for ovulation induction
Castillo JJ et al. · Theriogenology · 2026 Oct 1 · PMID 42140155
Superovulation with eCG alone or combined with the GnRH analogue buserelin improves transferable embryo production in weaned sows without affecting day 6 embryo morphological, cellular, and transcriptomic parameters
Lopez-Jara A et al. · Animal reproduction science · 2026 Aug 27 · PMID 42679714
Rapid and harmonized analytical workflow for the determination of peptidic and non-peptidic doping agents in dried and liquid blood matrices
Mazzarino M et al. · The Analyst · 2026 Jul 27 · PMID 42328738
Live feed from PubMed (NCBI) for “Buserelin”, updated 2026-10-30. Listing a paper is not an endorsement of its findings.
Registered studies
42 on ClinicalTrials.gov →- RecruitingPhase 3
Hypo-fractionated Radiation Therapy With or Without Androgen Suppression for Intermediate Risk Prostate Cancer
NCT01492972 · Proton Collaborative Group · 2012-01
- Active not recruitingPhase 3
Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial
NCT04513717 · NRG Oncology · 2021-01-21
- Active not recruitingPhase 3
Two Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a Higher Gene Risk Score, The Guidance Trial
NCT05050084 · NRG Oncology · 2021-12-06
- Active not recruitingPhase 2
A Comparative Dose-finding Study of RS-113 in Patients With Metastatic Castration-resistant Prostate Cancer
NCT07553988 · R-Pharm International, LLC · 2024-10-24
- CompletedPhase 3
Radiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer
NCT00936390 · Radiation Therapy Oncology Group · 2009-09
- CompletedPhase 3
Hormone Therapy, Radiation Therapy, and Steroid 17alpha-monooxygenase TAK-700 in Treating Patients With High-Risk Prostate Cancer
NCT01546987 · Radiation Therapy Oncology Group · 2012-05
- Completed
Cell-free DNA Analysis of Spent Embryo Culture Media as a Non-invasive Approach for Preimplantation Genetic Diagnosis
NCT07076719 · Sohag University · 2023-10-01
- UnknownPhase 3
Prostate Radiation Therapy or Short-Term Androgen Deprivation Therapy and Pelvic Lymph Node Radiation Therapy With or Without Prostate Radiation Therapy in Treating Patients With a Rising Prostate Specific Antigen (PSA) After Surgery for Prostate Cancer
NCT00567580 · Radiation Therapy Oncology Group · 2008-02
From the public ClinicalTrials.gov registry for “Buserelin”, updated 2026-10-30. Shown for research context only; Purity Peptides products are not for human use.
Key references
- [1]Manufacturer's prescribing information — FDA / EMA / ANVISA
- [2]WADA — Prohibited List of Substances and Methods
- [3]PubMed — reviews on buserelin and assisted reproduction
FAQ
Buserelin was developed and registered primarily through European national authorisations and has not been marketed in the US. Other GnRH agonists such as leuprolide fill comparable research and clinical roles there.
It has been used to down-regulate the pituitary before ovarian stimulation, preventing premature LH surges. Researchers study how this suppression affects follicle recruitment, oocyte yield and endometrial receptivity compared with antagonist-based approaches.
Yes. Buserelin is used in veterinary reproductive management, for example to induce or synchronise ovulation in cattle and other species. These applications have produced a substantial body of comparative reproductive physiology research.
FOR RESEARCH USE ONLY.Not for human or veterinary use. Not intended to diagnose, treat, cure, or prevent any disease.



