Prostate cancer is a malignant disease of the male reproductive system that occurs when the cells of the prostate start to grow out of control. The prostate is a gland present below men’s bladder, near the rectum and around the urethra. When it is affected by cancer, both the reproductive and urinary system are damaged, and patients experience symptoms such as urinary problems, including a slow or weak urinary stream or the need to urinate more often especially at night, blood in the urine, erectile dysfunction, pain in the hips, back, chest, or other areas from cancer spread to bones and weakness or numbness in the legs or feet.

Hormone therapy is one of the treatment options for patients who suffer from prostate cancer. These work at the hormonal level to suppress tumor growth and ease the symptoms of the disease. One of the types of hormone therapy is focused on reducing androgen production by the testicles, which can be achieved with an orchiectomy, with drugs called luteinizing hormone-releasing hormone (LH-RH) agonists or with estrogen. In addition, hormone therapy to block the action of androgens in the body are known as anti-androgens, and hormone therapy that blocks the production of androgens throughout the body include drugs that prevent the production of androgens by the adrenal glands, prostate cancer cells, and testicles.

How does leuprolide acetate work?

Leuprolide acetate is classified as a luteinizing hormone-releasing hormone (LH-RH) agonist, which means that it inhibits the secretion of gonadotropin. The chronic administration of leuprolide acetate suppresses ovarian or testicular steroidogenesis, depending on the patient’s gender. Testosterone and dihydrotestosterone (DHT) are both male sex hormones from the class of androgens. These hormones control the development and maintenance of male characteristics and are responsible for the growth of both healthy and cancerous prostate cells.

In the case of prostate cancer, tumor growth is also promoted by androgens. Therefore, the compound acts by reducing the production of testosterone to a level known as chemical castration and it may also inhibit androgen receptor-positive tumor progression. Leuprolide acetate works as continuous therapy and its effects may be reversible when the therapy is discontinued.

“The acetate salt of a synthetic nonapeptide analog of gonadotropin-releasing hormone. Leuprolide binds to and activates gonadotropin-releasing hormone (GnRH) receptors,” notes the National Cancer Institute (NCI) Drug Dictionary. “Continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.”

Leuprolide acetate to treat prostate cancer

Leuprolide acetate was approved by the US Food and Drug Administrated (FDA) in January 2002, following a request by Atria Laboratories. It is commercialized under the brand names Eligard, Lupron, or Viadur, and it is indicated as a palliative treatment for patients with advanced prostate cancer. Leuprolide acetate is designed to be administered as a subcutaneous injection and deliver 7.5 mg of the compound at a controlled rate over a one-month therapeutic period. It is injected into the body as a liquid, but it solidifies and continuously released the product for continued therapy.

According to the FDA approval, long-term studies demonstrated that continued therapy with leuprolide acetate is able to keep testosterone levels below castration for up to seven years. Due to the lower levels of testosterone, tumor growth rate is also decreased and patients with prostate cancer are expected to experience fewer symptoms. However, there are also adverse events associated with the treatment with leuprolide acetate, including malaise, fatigue, dizziness, hot flashes or sweats, gastroenteritis, and colitis. Sanofi Synthelabo is a marketing partner of Atrix for Eligard and the companies are currently working on additional products to release leuprolide acetate for a period of three and four months.


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