Histrelin is a synthetic gonadotropin-releasing hormone (GnRH) agonist. It is a peptide analogue of naturally occurring GnRH and acts on GnRH receptors in the pituitary gland.
When administered continuously, histrelin initially stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Continued exposure subsequently suppresses gonadotropin secretion and reduces production of sex hormones.
Histrelin is commonly used in the form of histrelin acetate in long-acting implant formulations.
Histrelin is a specialized synthetic peptide pharmaceutical API requiring controlled peptide synthesis, purification and comprehensive structural characterization. Quality control is particularly important for peptide identity, purity, related peptides, residual solvents, water content and biological activity.
CAS Number: 76712-82-8
Molecular Formula: C66H86N18O12
Molecular Weight: 1323.54 g/mol
Common Salt Form: Histrelin Acetate
Drug Class: GnRH Agonist
Pharmacological Class: Gonadotropin-Releasing Hormone Analogue
Therapeutic Class: Endocrine / Hormonal Agent
Therapeutic Area: Endocrinology / Reproductive Medicine
Histrelin binds to GnRH receptors on pituitary gonadotroph cells. Continuous administration produces an initial increase in LH and FSH secretion, followed by desensitization and downregulation of GnRH receptors.
This results in suppression of gonadal steroid production, including decreased testosterone in males and decreased estrogen production in females.
Histrelin is used in approved formulations for conditions including:
The specific indication depends on the formulation and regulatory approval in the relevant market.
Long-acting histrelin implants provide continuous GnRH agonist exposure. This suppresses premature activation of the hypothalamic-pituitary-gonadal axis and helps reduce the excessive production of sex hormones associated with central precocious puberty.
Histrelin is a synthetic peptide analogue containing 10 amino-acid residues. It is structurally related to GnRH but contains modifications that provide substantially greater potency and resistance to enzymatic degradation.
Histrelin acetate is used in pharmaceutical formulations, particularly long-acting implant systems.
Histrelin API quality evaluation may include:
Histrelin should be stored under validated, controlled pharmaceutical conditions and protected from excessive heat, moisture and direct light. Because it is a peptide, appropriate temperature and humidity control is important to maintain chemical and biological stability.
Histrelin is an established peptide therapeutic relevant to research involving GnRH receptor activation, pituitary gonadotropin suppression, sex-hormone regulation and endocrine disorders.
Histrelin is a synthetic GnRH agonist peptide with CAS Number 76712-82-8, molecular formula C66H86N18O12, and molecular weight approximately 1323.54 g/mol. Continuous exposure suppresses LH and FSH secretion after an initial stimulatory phase. Histrelin acetate is used in long-acting pharmaceutical implant formulations, particularly for central precocious puberty.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 95.0% – 105.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| Total Impurities | NMT 5.0% |
| Water Content | NMT 5.0% |