Leuprorelin acetate

Leuprorelin acetate also known as leuprolide is a manmade version of a hormone. It treats hormone-responsive cancers such as prostate & breast cancers and estrogen-dependent conditions such as endometriosis, uterine fibroids, and early puberty. It can also reduce the risk of premature ovarian failure in females on cyclophosphamide-based chemotherapy. Leuprorelin acetate in combination with triptorelin and Goserelin delays puberty in transgender youth, till they reach the age for hormone replacement therapy. It is considered for treating paraphilias and tested for reducing sexual urges in pedophiles and other cases of paraphilia. Leuprorelin acetate is sold under the Brand names Eligard, Leuprofact, Lucrin Depot among others. But due to its efficacy, it has found a place on the WHO list of essential medicines. Since the expiry of the initial patent protection, it is now made and sold around the world by several manufacturers. Abbott Laboratories filed the first patent for Leuprorelin in 1973 and was introduced for medical use in 1985. Initially sold only for daily injection, by 1989, a depot injection formulation was introduced to the market.

Dosage and administration

The usual recommended dose is 1 mg or 0.2 mL or 20-unit mark injected in a single daily subcutaneous injection. Like other chronically subcutaneous injections, the sites for injecting are to be varied periodically. Every 0.2 mL contains 1 mg of leuprolide acetate, sodium chloride for tonicity adjustment, and 1.8 mg of benzyl alcohol as preservative and water for injection.

The price of Leuprorelin acetate In the USA, the consumer has to pay an average retail price of $9,652.96 for a supply of 5 kits containing a 2.8ml vial of 1mg/0.2ml. In India, a syringe with 22.5mg costs around USD 273.

How does it work?

Leuprorelin is a gonadotropin-releasing hormone analog. It acts as an agonist at pituitary GnRH receptors. This Agonism of GnRH receptors stimulating of luteinizing hormone and follicle- stimulating hormone secretion by the anterior pituitary. This eventually leads to increased serum estradiol and testosterone levels via the normal physiology of the hypothalamic–pituitary–gonadal axis. A protracted downregulation of GnRH receptor activity is the goal to ultimately decrease LH and FSH secretion. This leads to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels regardless of sex.

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