Prostate cancer is the most common non-skin type of cancer that affects American men, and it occurs when the cells in the prostate grow out of control. The prostate is a gland present in men’s reproductive system, which is shaped and sized like a walnut and located below the bladder, near the rectum and around the urethra. The main function of the prostate is to produce a fluid that protects and nourishes sperm cells in semen, making the semen more liquid. Due to the location of the gland, prostate cancer affects both the urinary and reproductive systems.

There are many treatment options for prostate cancer, including watchful waiting, surgery, radiation therapy, cryotherapy, hormone therapychemotherapy, vaccine treatment, and bone-directed treatment. Hormone therapy is based on the reduction of the levels of the male hormones androgens, in order to stop the cancer growth. There are different approaches classified as hormone therapy including surgical castration, luteinizing hormone-releasing hormone (LHRH) analogs, and anti-androgens like flutamide (Eulexin®), bicalutamide (Casodex®), nilutamide (Nilandron®), Enzalutamide (Xtandi®), Estrogens (female hormones), and Ketoconazole (Nizoral®).

How Enzalutamide Works

Enzalutamide is a hormone therapy designed for men who suffer from advanced prostate cancer. The hormones in the body are the trigger for the growth of cancer, particularly androgens. Therefore, this approach is meant to disturb the action of androgens. Enzalutamide is an androgen receptor antagonist, which means that it works by blocking the male hormones from signaling the cancer cell to grow. The treatment is expected to stop the growth of the tumor, and in some cases it might even shrink it.

“Enzalutamide (formerly known as MDV3100) is a rationally designed, targeted androgen-receptor inhibitor that competitively binds to the ligand-binding domain of the androgen receptor and inhibits androgen-receptor translocation to the cell nucleus, recruitment of androgen-receptor cofactors, and androgen-receptor binding to DNA,” demonstrated the authors of the study “Enzalutamide in Metastatic Prostate Cancer before Chemotherapy.” “In a phase 1–2 trial, enzalutamide was found to have encouraging antitumor activity in men with castration-resistant prostate cancer, with data suggesting a greater benefit in men who had not yet received chemotherapy.”

Enzalutamide to Treat Prostate Cancer

The compound, which was called MDV3100 while under investigation, was approved by the US Food and Drug Administration (FDA) on August 31, 2012. Developed by Medivation, Inc., and Astellas Pharma US, Inc., enzalutamide is commercialized in the country under the brand name Xtandi® Capsules and it is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel. The approval was based on a study with 1199 patients who were randomly assigned enzalutamide 160 mg orally once daily or placebo.

Patients who received enzalutamide had a median survival of 18.4 months, while the survival rate for the placebo group was 13.6 months, which demonstrated the primary efficacy endpoint of the study. In addition, the research also revealed that at least five percent of the patients experienced adverse reactions like asthenia or fatigue, back pain, diarrhea, arthralgia, hot flush, peripheral edema, musculoskeletal pain, headache, upper respiratory infection, muscular weakness, dizziness, insomnia, lower respiratory infection, spinal cord compression and cauda equina syndrome, hematuria, paresthesia, anxiety, and hypertension.

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