Catalog
GnRH receptor superagonist

Leuprolide

aka Lupron

Chemical castration via continuous GnRH agonism — prostate cancer, endometriosis, central precocious puberty, GAHT.

FDA-approvedGrade A — Clinically established
Target
GnRHR — desensitizing agonism

Mechanism of action

Continuous (non-pulsatile) GnRHR activation desensitizes pituitary gonadotrophs → suppression of LH/FSH and downstream sex hormones. Initial 'flare' (1–2 wk) before suppression.

Pharmacokinetics

Depot SC/IM, 1–6 month formulations.

Clinical context

Advanced prostate cancer, endometriosis, central precocious puberty, fibroids, gender-affirming pubertal suppression.

Safety

Contraindications
  • Pregnancy (cat X)
Adverse effects
  • Tumor flare (prostate ca — co-administer antiandrogen)
  • Vasomotor symptoms, BMD loss
  • Mood changes
  • QT prolongation

Covered in modules

Module 11
GnRH Analogs, Somatostatin & Oncology Peptides
Leuprolide, octreotide, lanreotide, pasireotide — the established peptide oncology toolkit.

Related compounds

Somatostatin analog
Octreotide

Generate prescriber-grade deep dive

Pull in expanded mechanism, PK/PD, dosing strategies for special populations, drug interactions, monitoring cadence, head-to-head differentials, prescriber pearls, and patient FAQs for Leuprolide.

Educational reference. Not medical advice. Always verify against current FDA labeling and local regulatory guidance before prescribing or counseling.