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histrelin
- Development stage
- Approved
- Lead developer
- Endo International
- Modality
- Peptides, Small Molecules
- Administration
- Subcutaneous
01
Overview
Histrelin is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH). It acts as a potent GnRH agonist and is administered via subcutaneous implant. Histrelin initially stimulates the pituitary to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), causing a transient increase in sex steroids such as testosterone and estrogen. With continuous administration, it downregulates GnRH receptors in the pituitary gland, leading to decreased LH and FSH secretion and subsequent suppression of gonadal steroidogenesis. This results in reduced levels of sex hormones. Histrelin is primarily used for the palliative treatment of advanced prostate cancer in adults (Vantas) by lowering testosterone levels, which can slow cancer progression but does not cure it. It is also indicated for central precocious puberty (CPP) in children (Supprelin LA), where it halts premature sexual development by reducing sex steroid production[1][3][4][7].
- Brand names
- Supprelin LAVantasSupprelin
- Other names
- histrelin acetate
02
Targets
GnRHR (Gonadotropin-releasing hormone receptor)
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