Topical Bicalutamide for Hair Loss: Androgen (DHT) Receptor Blocker

Bicalutamide is a medication that belongs to a class of drugs called antiandrogens. It is used in the treatment of prostate cancer. Prostate cancer growth is often driven by the male hormone testosterone, which is an androgen. Bicalutamide works by blocking the action of androgens, specifically by binding to the androgen receptors on prostate cancer cells. This helps to slow down the growth and spread of prostate cancer.

Androgen receptors are proteins located inside cells, including cells in the prostate gland, hair follicles, and skin. They each have a ‘binding site’ that allows them to interact with androgens like DHT.

When DHT is present in the bloodstream, it diffuses into target cells where androgen receptors are located. DHT enters the cell and binds to the androgen receptor.

When DHT binds to the androgen receptor, it causes a conformational change in the receptor’s structure. This change allows the androgen receptor complex to move into the cell nucleus and interact with DNA.

Once inside the nucleus, the DHT-bound androgen receptor complex interacts with specific regions of DNA called androgen response elements. This interaction regulates the expression of various genes involved in male sexual development, growth of prostate cells, increase in body hair growth and other androgen-related functions. It also seems to lead to hair loss in the scalps of some men.

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The problem with existing drugs like Finasteride is they reduce DHT within the body. But DHT is needed for many other things. In reality we only want to reduce the amount of DHT that gets inside the hair follicles and modifies the gene expression.

We can do this by blocking the access to the androgen receptors using a drug like Bicalutamide.

While Bicalutamide’s structure is similar to DHT, it is different enough that it does not activate the androgen receptor like DHT does. Therefore it binds to the receptors but doesn’t cause the hair loss.

When Bicalutamide binds to the androgen receptor, it occupies the binding site and prevents the natural androgens from attaching. This effectively blocks the androgen receptor from being activated by these hormones.

By binding to the androgen receptor without activating it, Bicalutamide prevents the androgen receptor from transmitting signals that would normally lead to the cellular effects of androgens.

Is topical Bicalutamide safe to use?

I’m unaware of any saefty issues of using topical Bicalutamide. However, since it’s an antiandrogen, as it enters the body a small proportion of it will enter the blood stream and travel to other parts of the body where it will have mild anti-androgen effects. Is this a problem? I don’t see it being a problem, but as with all of these things you should consult with a medical professional before trying it. It’s possible that a medication like this will have side effects in some people that we’re currently unaware of.

What are the possible side effects?

From researching the web, I can see these are the possible side effects:

Hot Flashes: Many individuals experience hot flashes, which are sudden feelings of warmth, flushing, and sweating.

Breast Tenderness or Enlargement: Bicalutamide can lead to changes in breast tissue, resulting in tenderness or enlargement (gynecomastia) in some men.

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Fatigue: Some people may experience increased fatigue or tiredness.

Decreased Libido: Bicalutamide can affect sexual desire and function.

Nausea: Nausea is a potential side effect, though it is generally mild.

Diarrhea: Some individuals may experience diarrhea as a side effect.

Liver Function Changes: Bicalutamide can affect liver function, leading to changes in liver enzyme levels. Regular monitoring of liver function is important during treatment.

Muscle and Joint Pain: Some people may experience muscle or joint discomfort.

Skin Rash: Skin rash is another possible side effect, though it is generally not common.

Changes in Blood Sugar Levels: Bicalutamide can affect blood sugar levels and may require monitoring, especially in individuals with diabetes.

Bicalutamide is a commonly used oral drug for the treatment of prostate cancer. It’s known to be safe to use but must be prescribed by a doctor.

Are there any studies on the use of topical Bicalutamide for treating hair loss?

From what I can see Bicalutamide has only been studied for use in female hair loss caused by androgens. Some women experience higher than normal DHT hormone levels, which can cause hair loss and facial hair growth. Here’s an extract from a study that used topical Bicalutamide to treat female hair loss caused by androgens:

Six premenopausal women, with a mean age of 35.7 years and clinical diagnosis of Olsen Grade II or III female androgenetic alopecia accompanied by significant seborrhea were treated with 1 ml bicalutamide 0.5% mesotherapy. Three monthly sessions were performed. A subtle improvement in hair density was described after the third session. The overall satisfaction of the patients with the treatment was 6.3, on a scale of 1–1
Source: National Library of Medicine

I’ve also noticed a company has filed a patent for the use of topical Bicalutamide for treating hair loss and other conditions — such as acne — that are caused by androgens binding to receptors.

It looks as though it may be a safe and promising treatment.

There are some amateur scientists self-experimeting with this treatment and reporting positive results with no side effects.

Will I be trying it?

I must admit I am tempted to give this a try, but for now I’ll research its application further and will report back with updates here.

How much Bicalutamide do you need to apply to the scalp for treating hair loss?

In the study referenced above 1ml was used.