Category: peptide
Aliases: Leuprorelin, Lupron, Eligard, Lupron Depot
Nonapeptide GnRH analog — D-Leu⁶ + Pro⁹-NEt modifications resist degradation, raise receptor affinity ~15× over native GnRH. Initial pulsatile spike flares LH/FSH → testosterone / oestrogen surge in first week (testosterone-flare in prostate cancer); continuous chronic exposure desensitises and down-regulates pituitary GnRH-R → castrate gonadal steroid levels within ~3–4 weeks. Depot microspheres / in-situ-forming gel formulations release drug over 1, 3, 4, or 6 months.
SC: 3h