Leuprorelin acetate

CAS: 74381-53-6

MF: C59H84N16O12.C2H4O2

MW: 1269.46

EINECS: 686-285-8

Melting point  150-155°C

storage temp.  −20°C

Merck  14,5457

Leuprolide acetate is a commonly used hormone anti-cancer drug, , it is a acetate of leuprolide which is a nonapeptide synthetic analogue of LHRH( one kind decapeptide), it is a LH-RH antagonist, LHRH is produced by the hypothalamus, it can promote pituitary for the release of gonadotropins and follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This product’s structure is similar to LHRH, its acting on the anterior pituitary which prompts FSH, LH release function, increases serum concentrations of testosterone and dihydro testosterone. It is used as maintenance therapy for advanced prostate cancer clinically, but in about one week after use of the product, the number of active receptors will be reduced, and gonadotropin secretion will be reduced.After 2 to 4 weeks, the concentration of testosterone and dihydro testosterone can be reduced to castration levels. After the withdrawal, gonadotropin and androgen concentrations can be recovered to normal. 

Note that this product is not effective when administered orally, subcutaneous or intramuscular administration has good absorption. T1/2 of parenteral administration is 3 h. There is no accumulation in the body, unchanged drugs and its metabolites in urine excretion rates are2.9% and 1.5%, respectively. Ethanol can enhance the role of this product, the course of treatment should not drink, in case it is difficult to control the incidence of adverse reactions. In the first week of the course of treatment ,patients should try to be hospitalized for monitoring, choose an experienced physician to guide treatment to prevent severe neurological complications, urinary tract obstruction. Injection site should often vary.