Alarelin Acetate 79561-22-1

Function of Alarelin Acetate

Alarelin is a nonapeptide analogue of synthetic gonadotropin-releasing hormone (GnRH), and its efficacy is 15 times that of the parent. In the early stage of medication, it can stimulate the pituitary to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), causing a temporary increase in ovarian-derived steroid hormones; repeated medication can inhibit the release of LH and FSH from the pituitary, and reduce the level of estradiol in the blood. To achieve the effect of drug ovariectomy, at the same time it has a regulatory effect on the expression of the related oncogenes ras, neu, and myc of endometrial cancer. Clinically, it is mainly used to promote ovulation, treat infertility caused by abnormal ovarian function, endometriosis and uterine fibroids, and improve pregnancy rate.

Pharmacological action: This product is a nonapeptide analogue of synthetic gonadotropin releasing hormone (GnRH), which can stimulate the pituitary to release luteinizing hormone (LH) and follicle stimulating hormone (FSH) at the initial stage of treatment, causing transient ovarian-derived steroid hormones Increased; Repeated medication can inhibit the release of LH and FSH from the pituitary gland, reduce the level of estradiol in the blood, and achieve the effect of drug ovariectomy. This inhibitory effect can be used to treat hormone-dependent diseases such as endometriosis. The mechanism of action is to detect the expression of key intermediary proteins Smad2/3 and Smad7 in the TGF-β/smads signal transduction pathway in endometrial cancer transplanted tumor tissue, indicating that the TGF-β1/smads signal transduction pathway may be endometrial An important pathway in the pathogenesis of cancer. Alarelin may inhibit the occurrence and development of endometrial cancer by up-regulating Smad2/3 and down-regulating the expression of Smad7 protein. Pharmacokinetics: This product is rapidly absorbed after intramuscular injection in rats. The blood concentration reaches its peak in about 20 minutes, and the decrease in blood concentration is in line with the two-compartment model. When intramuscularly administered, t1/2α is about 0.2h, and t1/2β is about 1.8h. In intravenous administration, t1/2α is 0.08h, and t1/2β is about 1.2h. Its bioavailability can reach about 80%. The binding rate to plasma protein is 27% to 35%. The tissue distribution is by gonads and pituitary. The drug can be secreted from bile, completely metabolized and decomposed in the body within 24 hours, and all are excreted in urine and feces, of which 80% is in urine discharge.

Application: Clinically, it is mainly used to promote ovulation, treat infertility caused by abnormal ovarian function, endometriosis and uterine fibroids, and improve pregnancy rate.