Bicalutamide (Oral)

Used in partnership with another drug, Bicalutamide controls the progression of Stage 2 metastatic prostate cancer.


Bicalutamide is an oral medication that is given to male patients with Stage 2 metastatic prostate cancer. It is supplied to patients in the form of a tablet and is used in partnership with another drug to control the disease and prevent it from spreading further and to other parts of the body. It is also marketed and sold under the brand name Casalex in the United States.

Stage 2 metastatic prostate cancer is a form of prostate cancer where the disease has begun in the prostate and spread to other parts of the body. It is therefore not curable, however it can be controlled with medications. Bicalutamide is part of a family of drugs called the antiandrogens, which work by limiting and blocking the impact of the male hormone testosterone. Blocking the production of this hormone helps to prevent the growth of cancer cells, instead limiting the progression of the disease.

Bicalutamide is always prescribed to cancer patients along with another type of drug called a luteinizing hormone releasing hormone (LHRH), such as leuprolide or goserelin.

Administration of Bicalutamide will always be closely monitored by a trained doctor or healthcare professional. This is to monitor whether the drug is lowering and controlling the level of cancer cells being produced by the body. Patients that respond well to Bicalutamide can go on taking it as a long-term treatment for the condition, which can in some cases enable the patient to live a normal life. Regular monitoring is required as, if or when the drug starts to lose its effectiveness, the patient can be transferred to an alternative drug that works in the same way.

Bicalutamide can be taken for a number of purposes relating to prostate cancer. It can be taken on its own along with an LHRH, after radiotherapy has taken place, before you have hormone treatments, or after you have had your prostate removed by operation. This drug needs to be taken before you begin other hormone treatments. This is because bicalutamide takes several weeks to reduce the level of testosterone in your body, in many cases. While you are waiting for the testosterone levels to decrease, the drugs can make your symptoms feel worse. Bicalutamide can also be taken to treat flare reactions; in this case you need to take it for several days before you begin to use a hormone blocker. You will then need to continue taking the drug for between four to six weeks.

Conditions treated

  • Stage D2 metastatic prostate cancer (cancer that has spread)

Type of medicine

  • antiandrogen

Side effects

Bicalutamide comes with the risk of various side effects for patients. Patients should therefore be monitored closely by their doctors and book appointments for regular check-ups. Many side effects experienced are normal as the body adapts to the medication, so are not a cause for concern. However, patients should be mindful of side effects as Bicalutamide is a strong drug, and the body's response to producing less of the male hormone can lead to other health complications. If you are worried about any side effects you may be experiencing as a result of taking Bicalutamide, you should contact your doctor for advice straight away. If Bicalutamide is considered to be dangerous or detrimental to your health, there are other medications that you can instead be prescribed.

Common side effects are:

  • headache
  • hot flushes
  • pain or swelling in the breast / chest
  • pain in the back
  • dizziness
  • weakness
  • upset stomach or stomach cramp
  • diarrhea
  • vomiting or nausea
  • change in weight - either an increase or decrease
  • loss of appetite
  • dizziness
  • pain in the pelvis area
  • joint and muscle pain
  • abdominal pain
  • diarrhea
  • gassy feeling - trapped wind
  • pain or tingling sensation in the feet or hands
  • difficulty sleeping (insomnia)
  • uneasy or agitated feeling
  • rashes or spots on any part of the body
  • excess sweating
  • inability to create or maintain an erection
  • loss of sex drive
  • blood in the urine
  • need to urinate frequently, particularly at night time
  • painful or difficult urination
  • difficulty reaching an empty bladder

Some of the more serious side effects include the below. It is very rare to experience these, but patients that do report these may need to transfer to another medication:


  • jaundice (skin yellowing)
  • yellowness in the eyes
  • excessive tiredness, even after little or no exertion
  • bleeding or bruising
  • flu type symptoms
  • lack of appetite
  • pain in upper right hand side of the stomach
  • little or no energy
  • chest pain
  • abdominal pain or upset stomach


The dosage of bicalutamide will be dependent on a number of factors, but it is generally the same for all adult males. The usual dose for treating prostate cancer is either 50 mg or 150 mg tablets, which should be taken once per day at the same time of day.

Patients should always follow the instructions on the label and should not attempt to alter the dose - do not take more or less than what has been prescribed to you.

Major drug interactions

Before you start a course of Bicalutamide, you should tell your doctor if you are taking any other medication - whether it is a prescription drug or an over the counter medication. This is because there are some drugs that cause a reaction when taken at the same time as Bicalutamide. The effects of taking some drugs together can lead to unpleasant or dangerous symptoms and can also cause the Bicalutamide to be less effective. There are 235 drugs that have been found to have a reaction on some level with Bicalutamide (645 generic and brand names combined). Of these, 10 have been found to have a major reaction (20 including their generic and brand names), meaning that they are not safe to take together. These major reactions are:

  • bendroflumethiazide, nadolol
  • Arava (leflunomide)
  • Aubagio (teriflunomide)
  • cisapride
  • Halfan (halofantrine)
  • halofantrine
  • Juxtapid (lomitapide)
  • Kynamro (mipomersen)
  • leflunomide
  • levomethadyl acetate
  • lomitapide
  • mipomersen
  • Orap (pimozide)
  • Orlaam (levomethadyl acetate)
  • pimozide
  • Propulsid (cisapride)
  • pseudoephedrine / terfenadine
  • Seldane (terfenadine)
  • Seldane-D (pseudoephedrine / terfenadine)
  • terfenadine
  • teriflunomide



There have been several cases of death reported that has been caused by liver failure. This failure is thought to have been contributed to by the patient taking Bicalutamide. This hepatotoxicity usually took place within the first four months of the course of treatment.

Doctors should take the patient's serum transaminase levels before treatment starts, and at regular intervals throughout the first four months. Tests should then be carried out periodically to check for signs of liver disease. Signs to look out for include fatigue, vomiting, nausea, flu symptoms, jaundice, dark urine and abdominal pain.

Upon noticing any of the above symptoms of liver disease, the doctor should take the patient's ALT levels. If these levels have risen to double the normal level, the patient should stop taking bicalutamide immediately to prevent any further impact. Liver checks should be carried out regularly after that.


Patients taking bicalutamide may experience a reduced glucose tolerance. This can, in severe cases, lead to diabetes if left untreated. Patients should be closely monitored for a change in glucose levels throughout the treatment cycle.

Fertility and family planning

You should not attempt to father a child when taking this medication. This is because the medication can impact on the development of the fetus and therefore could lead to abnormalities at birth. If you are planning to start a family, you should wait until a few months after the end of your treatment.

Women and pregnancy

Bicalutamide should not be used to treat women. It is intended for male use only. The drug can also cause harm to a fetus if consumed by a pregnant woman.


There is no data to suggest any adverse impact on children. Due to the nature of the conditions that bicalutamide treats, it is generally not prescribed to children.

Other conditions

Patients should always tell their doctors if they are suffering from any other conditions. This is because there are some conditions that will not be compatible with bicalutamide - and the drug may end up making these conditions worse. It could also be dangerous for patients to take this drug when suffering from certain conditions. For example, those with diabetes could see their glucose tolerance decreasing to dangerously low levels. And those with liver problems could also be at a greater risk of developing liver failure. Keep a list of all conditions and other medications that you have, or have had in the past. Your doctor will be able to make a judgement on whether the drug is right for you.


There are no special instructions for storage of this medication. However, it should always be stored out of the reach of children. Consumption by children or by those for whom the medication was not prescribed can be highly dangerous. More than 60,000 children in the United States are admitted to emergency rooms per year as a result of taking medication that was not meant for them. Always keep medication in the box it was supplied in and preferably in a locked cupboard.

Keep the medication at room temperature and keep it away from direct light sources and damp conditions.


Always dispose of medication that has gone out of date. Do not take medication that has passed its expiry date. Instead, you should dispose of it safely. Do not attempt to ground tablets or flush them down the sink or toilet. Instead, take them out of the packet, put them into a plastic bag that can be sealed tightly shut, and then mix them with a substance such as cat litter, used coffee beans or soil or dirt. Then tightly close the bag and put it in your trash can.

Alternatively, the best way to dispose of your unwanted or unused medication is to find a local take-back scheme in your area. These schemes are set up by the FDA to safely dispose of medicines and prevent them getting into the wrong hands, or harming the environment. You can find out what schemes are available in your area, and then easily arrange for the quick pick-up of your drugs.


If you take too much bicalutimide, get help immediately. Call your local poison control center at 1-800-222-1222. Always stick to the amount of intake that is prescribed by your doctor - dosages should not be increased without consultation. You should not attempt to take increased doses.


Bicalutamide is a highly effective treatment for controlling stage 2 prostate cancer. It will always be prescribed with their medication and is only suitable to be taken by men, to reduce their levels of testosterone. Bicalutamide is a very strong drug that can cause some fairly strong side effects in a number of patients. More than half of those that take it are likely to experience hot flushes, and this is considered to be normal in the majority of cases. However, there are risks of more severe side effects, so patients should always consult a doctor if experiencing anything unusual or persistent. Medical studies and registers have been conducted to find out the impact of the drug for patients, and it has been found to cause serious liver damage and even failure that can result in death. Upon any signs of liver failure, the drug should be stopped immediately and the patient should be closely monitored.

Patients can help to reduce their chances of developing side effects by being upfront about any other drugs, or supplements they are taking. Patients should also tell their doctors about any other conditions they could be suffering from. Again, this is because they could impact on the effectiveness of the drug in treating stage 2 prostate cancer.

Overall, if all usage instructions are followed and the patient is closely monitored by a doctor throughout the treatment, the drug can be a safe and effective treatment that suppresses stage 2 prostate cancer and stops the disease progressing to other parts of the body. Regular tests should be taken to monitor for signs of liver disease, and to see how the body is responding to the drug.

There are various medical studies available that confirm the safety and effectiveness of this drug, and it continues to be a widely used treatment - potentially life saving to those with prostate cancer that has spread to other parts of the body. It is one of the most popular and widely-prescribed treatments and is easy for patients to maintain throughout the treatment course. It is effective as a medium for long term treatment for many patients suffering from stage 2 prostate cancer.

Last Reviewed:
December 23, 2017
Last Updated:
April 04, 2018
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