Leuprorelin, also called Leuprolide, is a manufactured version of a hormone used to treat
prostate cancer, breast cancer, endometriosis, uterine fibroids, and early puberty. It is also
indicated in the treatment of estrogen-dependent conditions such as endometriosis or uterine
fibroids. It may be used to prevent premature ovulation in cycles of controlled ovarian
stimulation for IVF amongst teens with precocious puberty in both males and females. In
combination with other drugs, it delays puberty in transgender youth until they are old
enough for hormone replacement therapy.
Leuprorelin is sold under the brand name Lupron among others.
Bayer AG markets Leuprorelin under the brand name Viadur. It is also marketed by Tolmar
under the brand names Eligard and Fensolvi and by TAP Pharmaceuticals and Abbott as
Lupron. It was first patented in 1973, and approved for sales in the United States in 1985. It is
on the World Health Organization's List of Essential Medicines. Leuprorelin use is off-label,
for not having the approval of the Food and Drug Administration and without data on long-
term effects of this use. In Europe, In the UK and Ireland, Takeda UK, as Prostap SR and
Prostap 3, markets it.
Forms and Dosage
Leuprorelin is sold as a slow-release implant or subcutaneous/intramuscular injection. It is
sold as Short-acting daily intramuscular injection or as a Long-acting depot intramuscular
injection or as a Long-acting depot subcutaneous injection or Long-acting subcutaneous
injection or a Long-acting subcutaneous implant. In the treatment of Advanced Prostate
Cancer, a standard dose is 7.5 mg IM monthly or 22.5 mg IM every 3 months or 30 mg IM
every 4 months, or 45 mg IM every 6 months. In the treatment of Endometriosis, the dose is
3.75 mg IM monthly for up to 6 months or 11.25 mg IM every 3 months for 2 doses for a
total of 6 months.
How does it work?
Leuprorelin is a gonadotropin-releasing hormone analogue that acts as an agonist at pituitary
GnRH receptors. Initially, Agonism of GnRH receptors results in the stimulation of
luteinizing hormone and follicle-stimulating hormone secretion by the anterior pituitary
eventually leading to increased serum estradiol and testosterone levels via the normal
physiology of the hypothalamic–pituitary–gonadal axis. But, Pituitary GnRH receptors
become de-sensitised after weeks of continuous therapy. This protracted down-regulation of
GnRH receptor activity is the key objective of Leuprorelin therapy and ultimately results in
decreased LH and FSH secretion, leading to Hypogonadism and thus a dramatic reduction in
estradiol and testosterone levels regardless of sex. while treating prostate cancer, the initial
increase in testosterone levels can be associated with Leuprorelin therapy is
counterproductive to treatment goals.
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