|Specific rotation||D25 -31.7° (c = 1 in 1% acetic acid)|
|Acidity coefficient||(pKa) 9.82±0.15 (Predicted)|
|Water solubility||Soluble in water at 1mg/ml|
Leuprolide, goserelin, triprelin, and nafarelin are several drugs commonly used in clinical practice to remove ovaries for the treatment of premenopausal breast cancer and prostate cancer. (referred to as GnRH-a drugs), GnRH-a drugs are similar in structure to GnRH and compete with pituitary GnRH receptors. That is, the gonadotropin secreted by the pituitary decreases, which leads to a significant decrease in the sex hormone secreted by the ovary.
Leuprolide is a gonadotropin-releasing hormone (GnRH) analog, a peptide composed of 9 amino acids. This product can effectively inhibit the function of the pituitary-gonadal system, the resistance to proteolytic enzymes and the affinity to the pituitary GnRH receptor are stronger than GnRH, and the activity of promoting the release of luteinizing hormone (LH) is about 20 times that of GnRH. It also has a stronger inhibitory effect on pituitary-gonad function than GnRH. In the initial stage of treatment, follicle stimulating hormone (FSH), LH, estrogen or androgen may be temporarily increased, and then, due to the decreased responsiveness of the pituitary gland, the secretion of FSH, LH and estrogen or androgen is inhibited, resulting in dependence on sex hormones. Sexual diseases (such as prostate cancer, endometriosis, etc.) have a therapeutic effect.
At present, the acetate salt of leuprolide is mainly used clinically, because the performance of leuprolide acetate is more stable at room temperature. Liquid should be discarded. It can be used for the drug castration treatment of endometriosis and uterine fibroids, central precocious puberty, premenopausal breast cancer and prostate cancer, and also for functional uterine bleeding that is contraindicated or ineffective for conventional hormone therapy. It can also be used as a premedication before endometrial resection, which can evenly thin the endometrium, reduce edema, and reduce the difficulty of surgery.