Overview
Leuprolide is a nonapeptide GnRH agonist used clinically as a depot injection to suppress the HPG axis in hormone-responsive disease.
- Approved pharmaceutical
- Depot intramuscular and subcutaneous injection
Mechanism of action
Continuous receptor stimulation desensitizes the pituitary, suppressing LH, FSH, and downstream sex steroids after an initial flare.
- · GnRH receptor desensitization
- · LH and FSH suppression
- · Gonadal steroid suppression
- · GnRH
- · LH
- · FSH
- · Testosterone
- · Estradiol
How it acts on the body
Leuprolide produces medical castration after an initial 1-2 week flare. In prostate cancer it suppresses androgen-driven growth; in endometriosis and uterine fibroids it suppresses estrogen-driven lesion activity; in central precocious puberty it halts premature pubertal progression.
Flare prophylaxis (e.g. with an androgen receptor antagonist in prostate cancer) is essential because rising testosterone in the first weeks can worsen disease before suppression begins.
Hormonal & endocrine impact
How this peptide is reported to shift specific hormones and signaling molecules. Directionality reflects research literature and preclinical models, not clinical prescribing data.
Curves are schematic shapes (sigmoid for increases/decreases, damped oscillation for modulation/stabilization) anchored to a 100% baseline. They communicate direction and tempo of change reported in research literature — not absolute hormone concentrations.
Effects on the body
Organ system effects
Pituitary downregulation.
HPG suppression.
Density loss with chronic use without add-back.
Reported effects
Drawn from preclinical research, anecdote, and small-scale clinical observation. No evidence grades are assigned — most peptides on this page lack rigorous human trials.
- Depot dosing for convenience
- Strong evidence base across indications
Potential side effects
- · Hot flashes
- · Decreased libido
- · Mood changes
- · Injection-site reactions
- · Tumor flare
- · Bone loss
- · QT prolongation with some formulations
Drug interactions
Pairing context
- Add-back therapy in benign indicationsMitigates bone and vasomotor effects.
- PregnancyContraindicated.