ApprovedReproductive & hormoneIntranasalEvidence 4/5

Nafarelin

Also known as: Synarel

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.

Nafarelin
Drug class
GnRH agonist (gonadotropin-releasing hormone analog)
Primary targets
GnRH receptor (pituitary gonadotrophs), LH, FSH, estradiol, testosterone
Dose reference
Per the FDA label (reference only, not a recommendation): endometriosis 400 mcg/day (one 200 mcg spray per nostril twice daily), increasable to 800 mcg/day; central precocious puberty 1600 mcg/day, increasable to 1800 mcg/day.
Half-life
Approximately 3 hours in adults (about 2.5 hours in children) after intranasal administration
Developer / origin
Syntex (now part of Pfizer)
Reference year
1990
Evidence score
4/5 - Approved with controlled-trial evidence

Approved uses

  • Endometriosis (management including pain relief and lesion reduction, up to 6 months)
  • Central precocious puberty
Evidence 4/5

Approved with controlled-trial evidence

Nafarelin (Synarel) is FDA-approved with randomized controlled-trial evidence for endometriosis (comparable to danazol for symptom control) and effective LH suppression in central precocious puberty, though benefits are duration-limited and constrained by hypoestrogenic bone-density loss.

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

Evidence basis

  • FDA-approved label (DailyMed) with two indications and defined dosing
  • NEET large danazol-controlled randomized trial in endometriosis
  • Multiple double-blind nafarelin-versus-danazol endometriosis trials
  • Manufacturer clinical pharmacology documenting LH/FSH suppression and prepubertal LH response in CPP
  • Label-documented ~8.7% trabecular bone-density loss at 6 months limiting duration

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.

Nafarelin 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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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.

Buserelin

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4/5
Reproductive & hormoneApproved

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.

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

The information on PeptideStat is for educational and research purposes only and is not medical advice. Many peptides discussed are research compounds not approved for human use. Always consult a qualified healthcare professional before making any health decisions. Articles may contain affiliate links — we may earn a commission at no extra cost to you.