What does the drug bicalutamide do?

Bicalutamide is an anti-androgen medication that is primarily used to treat prostate cancer. It is typically used together with a gonadotropin-releasing hormone (GnRH) analog or surgical removal of the testicles to treat advanced prostate cancer. To a lesser extent, it is used for early prostate cancer at a higher dosage as monotherapy without castration. Bicalutamide is also used to treat excessive hair growth and scalp hair loss in women, as a component of feminizing hormone therapy for transgender women, to treat early puberty in boys, and to prevent overly long-lasting erections in men.

Comparison of bicalutamide with other antiandrogens

The side effect profile of bicalutamide in men and women differs from that of other antiandrogens and is considered favorable in comparison. Relative to GnRH analogs and the steroidal antiandrogen (SAA) cyproterone acetate (CPA), bicalutamide monotherapy has a much lower incidence and severity of hot flashes and sexual dysfunction. In addition, unlike GnRH analogs and CPA, bicalutamide monotherapy is not associated with decreased bone mineral density or osteoporosis. Conversely, bicalutamide monotherapy is associated with much higher rates of breast tenderness, gynecomastia, and feminization in men than GnRH analogs and CPA. However, gynecomastia with bicalutamide is rarely severe and discontinuation rates due to this side effect are fairly low. These differences in side effects between bicalutamide monotherapy, GnRH analogs, and CPA are attributed to the fact that whereas GnRH analogs and CPA suppress estrogen production, bicalutamide monotherapy does not lower estrogen levels and in fact, actually increases them.

Bicalutamide does not share the risk of neuropsychiatric side effects like depression and fatigue as well as cardiovascular side effects like coagulation changes, blood clots, fluid retention, ischemic cardiomyopathy, and adverse serum lipid changes that CPA has been associated with. It has a much lower risk of hepatotoxicity than flutamide and CPA and of interstitial pneumonitis than nilutamide. The drug also does not share the unique risks of diarrhea with flutamide and nausea, vomiting, visual disturbances, and alcohol intolerance with nilutamide. Unlike enzalutamide, bicalutamide is not associated with seizures or related central side effects like anxiety and insomnia. However, although the risk of adverse liver changes with bicalutamide is low, enzalutamide differs from bicalutamide in having no known risk of elevated liver enzymes or hepatotoxicity. In contrast to the SAA spironolactone, bicalutamide does not have antimineralocorticoid effects and hence is not associated with hyperkalemia, urinary frequency, dehydration, hypotension, or other related side effects. In women, unlike CPA and spironolactone, bicalutamide does not produce menstrual irregularity or amenorrhea and does not interfere with ovulation or fertility.

Medical use of bicalutamide

Bicalutamide is approved for and mainly used in the following indications:

Metastatic prostate cancer (MPC) in men in combination with a gonadotropin-releasing hormone (GnRH) analog or surgical castration at 50 mg/day

Locally advanced prostate cancer (LAPC) in men as monotherapy at 150 mg/day (not approved for this use in the United States)

In Japan, bicalutamide is uniquely used at a dosage of 80 mg/day both in combination with castration and as a monotherapy in the treatment of prostate cancer.

Bicalutamide is also employed for the following off-label (non-approved) indications:

To reduce the effects of the testosterone flare at the initiation of GnRH agonist therapy in men

Androgen-dependent skin and hair conditions such as acne, seborrhea, excessive hair growth, and scalp hair loss in women as well as high testosterone levels due to polycystic ovary syndrome (PCOS) in women, at 25 to 50 mg/day generally in combination with a birth control pill

Feminizing hormone therapy for transgender women in combination with estrogen usually at 50 mg/day

Peripheral precocious puberty in boys at 12.5 to 100 mg/day in combination with an aromatase inhibitor like anastrozole, especially for familial male-limited precocious puberty (testotoxicosis)

Overly long-lasting erections in men at 50 mg per week to 50 mg every other day

The medication has been suggested but has uncertain effectiveness in the following indication:

Hypersexuality and paraphilias, particularly in combination with chemical castration

For more information on these uses, see the medical uses of bicalutamide article.

How to use Bicalutamide

Read the Patient Information Leaflet if available from your pharmacist before you start taking bicalutamide and each time you get a refill. If you have any questions, ask your doctor or pharmacist.

Take this medication by mouth with or without food as directed by your doctor, usually once a day.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.

Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.

Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

The company can provide related products. If you are interested, please contact us in time

Sales specialist:(Allen)

E mail：allen@faithfulbio.com

WhatsApp/Skype/Telegram: +86 13137770562

Sales specialist:(Tina)

E mail：sales2@faithfulbio.com

WhatsApp/Skype/Telegram: +86 177 8986 8285

Sales specialist:(sunny)

E mail：sunny@faithfulbio.com

WhatsApp/Skype/Telegram: +86 13262001053