Leuprolide
A GnRH agonist that suppresses the axis through continuous stimulation.
Identity
- Class
- GnRH receptor agonist (nonapeptide analog)
- Source
- Synthetic analog of GnRH
- Receptor
- GnRH receptor (GnRHR)
Key properties
Molecular weight
~1,209.4 Da
Approximate values for the native hormone. Engineered analogs are often deliberately larger and far longer-acting.
Mechanism
Leuprolide is a long-acting GnRH agonist. Because GnRH normally signals in pulses, continuous agonist exposure first causes a transient surge ('flare') and then desensitizes the receptor — paradoxically shutting the axis down. Depot formulations exploit this to maintain chronic suppression.
Reference notes
- It suppresses the reproductive axis by overriding GnRH's required pulsatility — continuous stimulation desensitizes the receptor.
- An initial hormonal 'flare' precedes suppression — a direct consequence of the agonist mechanism.
- Depot formulations release the drug over months to sustain the effect.
Selected literature
Curated peer-reviewed reviews, sourced from PubMed. Selected for relevance, not exhaustive — open any entry on PubMed for the full record and its primary citations.
- 1.Leuprorelin. A review of its pharmacology and therapeutic use in prostatic disorders · Drugs & aging, 1991 · PMID 1794035
- 2.Clinical pharmacokinetics of depot leuprorelin · Clinical pharmacokinetics, 2002 · PMID 12083977