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.
- 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
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
Key references
- DailyMedSynarel (nafarelin acetate) nasal spray prescribing information
- PubMedNafarelin for endometriosis: a large-scale, danazol-controlled trial (NEET)
- Pfizer MedicalSynarel (nafarelin acetate) Clinical Pharmacology
- PubMedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone
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
Use calculators for concentration, unit conversion and repeated-dose accumulation math.
Compare with related peptides
Stay inside the same research category and compare mechanism, status and evidence quality.
Triptorelin
Trelstar, Decapeptyl
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
Zoladex
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
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.
Histrelin
Supprelin LA, Vantas
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.