ApprovedReproductive & hormoneSubcutaneousEvidence 4/5

Buserelin

Also known as: Suprefact

Buserelin is a GnRH receptor superagonist that initially stimulates and then, with continuous non-pulsatile exposure, desensitizes pituitary gonadotrophs to suppress LH, FSH and downstream testosterone or estradiol production.

Buserelin
Drug class
GnRH agonist (LHRH analogue)
Primary targets
GnRH/LHRH receptor, Pituitary gonadotrophs, LH, FSH
Dose reference
Label/trial reference figures, not recommendations: advanced prostate cancer 500 mcg SC every 8 hours for 7 days, then 200 mcg SC daily or 400 mcg intranasally three times daily; endometriosis 400 mcg intranasally three times daily for up to ~6 months.
Half-life
Short elimination half-life, reported around 72-80 minutes (about 1-2 hours) regardless of route.
Developer / origin
Hoechst AG (Frankfurt, Germany); rights now held by Sanofi
Reference year
1984
Evidence score
4/5 - Approved GnRH agonist with label and trial support

Approved uses

  • Hormone-dependent advanced (metastatic) prostate cancer (e.g. Health Canada Suprefact label)
  • Endometriosis
  • Pituitary down-regulation in assisted reproduction/IVF (protocol use)
Evidence 4/5

Approved GnRH agonist with label and trial support

Buserelin is an approved GnRH agonist (Suprefact) in Canada and parts of Europe for hormone-dependent advanced prostate cancer and endometriosis, with a substantial randomized/comparative trial record for IVF down-regulation; it is not FDA-approved in the US.

Investigational compound with human randomized or phase 2/3 evidence.

Evidence basis

  • Health Canada Suprefact product monograph documents approved prostate cancer and endometriosis indications, dosing and safety
  • Multiple PubMed-indexed randomized and comparative trials evaluate buserelin for IVF down-regulation and GnRH-agonist ovulation triggering
  • Pharmacovigilance and pharmacology literature characterize class mechanism, ~72-80 min half-life and adverse-event profile

How to read this entry

Dose references and half-life values are pulled from trial protocols, labels, reviews, or published summaries where available. They are context for research and comparison, not a personal dosing recommendation.

Status matters: approved drugs have regulated indications; investigational compounds are still being studied; research-only peptides do not have established human dosing, safety, or efficacy for consumer use.

Buserelin guides

Read the matching guide or adjacent research pages for more context.

Peptide calculators

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Compare with related peptides

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Triptorelin

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5/5
Reproductive & hormoneApproved

Triptorelin is a potent GnRH-receptor agonist that first transiently stimulates LH and FSH release, then, with continuous exposure, downregulates and desensitizes pituitary GnRH receptors to suppress gonadotropins and sex steroids.

Goserelin

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5/5
Reproductive & hormoneApproved

Goserelin is a synthetic decapeptide GnRH agonist that first stimulates and then, with continuous depot exposure, downregulates pituitary GnRH receptors to suppress LH, FSH and downstream sex steroids toward castrate or postmenopausal levels.

Nafarelin

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4/5
Reproductive & hormoneApproved

Nafarelin is a potent GnRH receptor agonist that initially stimulates pituitary LH and FSH release but with continued dosing downregulates the receptor, suppressing gonadotropins and sex steroid production.

Histrelin

Supprelin LA, Vantas

4/5
Reproductive & hormoneApproved

Histrelin is a GnRH receptor agonist that initially stimulates and then, through continuous implant delivery, downregulates pituitary GnRH receptors to suppress LH, FSH and sex steroid production.

Research & educational purposes only

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