Systemic HormonesWADA Prohibited
Leuprolide
Synonyms: Lupron, Eligard, Leuprorelin, GnRH Agonist
Sequence: Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt
Critical Safety & Regulatory Notice
Leuprolide is classified as a regulated, unapproved, or research-only substance. Doping/Regulatory Status: FDA approved. Prohibited by WADA under Section S2.. Clinical safety profiles for human use are deficient or not approved.
History & Discovery Timeline
Leuprolide was patented in 1973 by Takeda and approved in the USA in 1985 as a synthetic GnRH analog.
What it is: It is a synthetic nonapeptide analog of GnRH. It falls under the Metabolic category (brand name Lupron).
Proposed Mechanisms & Research Findings: It acts as a potent GnRH receptor agonist. Chronic administration leads to receptor downregulation, suppressing LH, FSH, and testosterone/estrogen production.
Regulatory & Safety Status: It is FDA approved for prostate cancer, endometriosis, and precocious puberty. Sourcing must be done by prescription; gray-market compounds are illegal and highly risky.
Athletic & Anti-Doping Status: Strictly prohibited by WADA under Section S2 as a gonadotropin agonist.
Understanding Leuprolide Key Facts
Primary Target System:NEUROENDOCRINE
Residue Count / Length:11 Amino Acids
Primary Action & Category:GnRH Receptor Agonist (Systemic Hormones)
Primary Receptors:GnRH Receptor (GnRHR)
Figure 1: Detailed molecular mechanism pathways of Leuprolide (click to enlarge).