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Leuplin SR 11.25 mg
- Development stage
- Approved
- Lead developer
- Takeda
- Modality
- Peptides
- Administration
- Subcutaneous
01
Overview
Leuprolide acetate (marketed by Takeda as Leuplin SR in Japan) is a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH). It functions as a potent GnRH receptor agonist. While initial administration causes a transient surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH), continuous and prolonged exposure leads to the downregulation and desensitization of GnRH receptors in the pituitary gland. This results in the profound suppression of gonadotropin secretion, subsequently reducing serum testosterone levels to castrate levels (androgen deprivation). This mechanism is highly effective in treating hormone-responsive advanced and metastatic prostate cancer. The Leuplin SR 11.25 mg formulation is specifically designed as a sustained-release depot injection using biodegradable microspheres, allowing for subcutaneous administration once every 12 weeks.
- Brand names
- Leuplin SRLupron DepotProstapLeuplin
- Other names
- leuprorelin acetateleuprolide acetateleuprorelin acetate SR 11.25 mg injection kit
02
Targets
GnRHR (Gonadotropin-releasing hormone receptor)
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