Bicalustad (Bicalutamide)

What Is Bicalustad and What Is It Used For?

Quick Answer: Bicalustad (bicalutamide) is a non-steroidal antiandrogen medication prescribed for the treatment of prostate cancer. It blocks the action of male hormones (androgens) on prostate tissue, inhibiting the growth of androgen-dependent cancer cells. It is available as 50 mg and 150 mg film-coated tablets taken once daily.

Bicalustad belongs to a class of medications known as non-steroidal antiandrogens. The active substance, bicalutamide, works by competitively binding to androgen receptors in the prostate gland. This blocks the stimulatory effects of dihydrotestosterone (DHT) and testosterone on prostate cancer cells, effectively inhibiting their growth and proliferation. Unlike steroidal antiandrogens, bicalutamide does not have progestational or glucocorticoid activity, which means it has a more targeted mechanism of action with fewer hormonal side effects unrelated to androgen blockade.

The clinical use of bicalutamide depends on the dose and the stage of prostate cancer being treated. At a dose of 50 mg once daily, bicalutamide is used as part of combined androgen blockade (CAB) for the treatment of advanced prostate cancer. In this setting, it is taken together with an LHRH (luteinising hormone-releasing hormone) agonist — such as goserelin, leuprorelin, or triptorelin — or following surgical removal of the testes (bilateral orchiectomy). The rationale for this combined approach is that while LHRH agonists or orchiectomy reduce testicular androgen production, bicalutamide blocks the residual androgens produced by the adrenal glands from stimulating prostate cancer cells.

At the higher dose of 150 mg once daily, bicalutamide is indicated for patients with locally advanced prostate cancer who are at substantial risk of disease progression. In this context, it may be prescribed as a standalone treatment (monotherapy) or as adjuvant therapy following radical prostatectomy (complete surgical removal of the prostate) or radiotherapy. The Early Prostate Cancer (EPC) programme, a large-scale international clinical trial programme, demonstrated that bicalutamide 150 mg as adjuvant therapy significantly reduced the risk of disease progression in patients with locally advanced prostate cancer.

Prostate cancer is the most commonly diagnosed cancer in men worldwide, and androgen deprivation therapy (ADT) — of which bicalutamide is a key component — remains a cornerstone of treatment. According to the European Association of Urology (EAU) and the National Comprehensive Cancer Network (NCCN), antiandrogen therapy plays a vital role across multiple stages of the disease, from locally advanced to metastatic settings. Bicalutamide has been widely prescribed since its first approval in the 1990s and is available as a generic medication under numerous brand names, including Bicalutamid Sandoz, Bicalutamide Teva, Bicalutamide Orion, Bicalutamide Accord, and Bicalutamide Bluefish.

How Does Bicalutamide Work?

Bicalutamide exerts its anticancer effects through competitive inhibition of the androgen receptor. In normal prostate physiology, testosterone and its more potent metabolite DHT bind to androgen receptors in prostate cells, stimulating cell growth and survival. In prostate cancer, this androgen-driven signalling pathway becomes dysregulated, driving tumour proliferation. Bicalutamide competes with these androgens for binding to the receptor, effectively blocking the growth-promoting signals. The drug has a long elimination half-life of approximately 6 days at steady state, which supports its convenient once-daily dosing schedule.

After oral administration, bicalutamide is well absorbed from the gastrointestinal tract. Food does not significantly affect its absorption, so it can be taken with or without meals. The drug is extensively metabolised in the liver and excreted in both urine and faeces. Importantly, it is the (R)-enantiomer of bicalutamide that is pharmacologically active, with the (S)-enantiomer being rapidly cleared and considered inactive.

What Should You Know Before Taking Bicalustad?

Quick Answer: Before starting bicalutamide, your doctor must assess your liver function, cardiac health, and current medications. The drug is contraindicated in women, children, and patients with prior bicalutamide-induced liver injury. It must not be combined with terfenadine, astemizole, or cisapride.

Contraindications

There are several important situations in which bicalutamide must not be used. You should not take Bicalustad if you are allergic to bicalutamide or any of the other ingredients in the formulation (see the ingredients section below). Additionally, bicalutamide is strictly contraindicated if you have previously experienced liver problems while taking this medication. Rechallenge after hepatotoxicity carries a significant risk of recurrence and potentially more severe liver damage.

Bicalutamide must not be taken together with the following medications due to the risk of serious cardiac arrhythmias:

• Terfenadine (an antihistamine previously used for hay fever)
• Astemizole (an antihistamine previously used for allergies)
• Cisapride (a gastrointestinal prokinetic agent)

Bicalustad is indicated exclusively for adult males. It must not be used by women, children, or adolescents. The drug has no role in the treatment of any condition in female patients, and exposure during pregnancy could cause harm to a developing male foetus.

Warnings and Precautions

Before starting treatment with bicalutamide, discuss the following conditions with your doctor, as they may affect whether this medication is appropriate for you or require additional monitoring:

• Liver impairment: If you have moderate to severe liver disease, bicalutamide should only be used after careful consideration of the potential benefits and risks by your doctor. If prescribed, regular monitoring of liver function tests (bilirubin, transaminases, alkaline phosphatase) is essential. The European Medicines Agency (EMA) recommends liver function testing before treatment initiation, at regular intervals during the first 4 months, and periodically thereafter. Treatment must be discontinued immediately if severe hepatic abnormalities develop.
• Severe kidney impairment: Bicalutamide should only be prescribed after careful medical evaluation in patients with severely reduced kidney function.
• Cardiovascular disease: Patients with existing heart conditions, including cardiac arrhythmias (irregular heartbeats), should be closely monitored. Bicalutamide may increase the risk of QT prolongation and cardiac rhythm disturbances. If you are taking medications for heart rhythm problems, inform your doctor before starting bicalutamide.
• Diabetes mellitus: Patients with diabetes who are already receiving LHRH agonist therapy may experience worsened glycaemic control. Close monitoring of blood glucose levels is recommended.

Androgen deprivation therapy, including bicalutamide, has been associated with an increased risk of cardiovascular events. A meta-analysis published in the Journal of Clinical Oncology found that combined androgen blockade may modestly increase cardiovascular morbidity, particularly in men with pre-existing heart disease. The FDA and EMA have both issued guidance recommending cardiovascular risk assessment before initiating antiandrogen therapy.

Pregnancy and Breastfeeding

Bicalutamide is contraindicated in women and must never be given to pregnant or breastfeeding women. The drug's antiandrogen mechanism could potentially interfere with normal development of a male foetus. Male patients taking bicalutamide should use effective contraception if their partner is of childbearing potential, as the effects of bicalutamide on male fertility and potential transfer through seminal fluid have not been fully characterised.

Driving and Operating Machinery

Bicalutamide may cause dizziness or drowsiness in some patients. If you experience these effects, you should not drive a vehicle or operate heavy machinery. This is particularly relevant during the initial weeks of treatment when the body is adjusting to the medication.

Excipients

Bicalustad tablets contain lactose monohydrate. If you have been told by your doctor that you have an intolerance to certain sugars, consult your doctor before taking this medication. The tablets also contain less than 1 mmol (23 mg) of sodium per tablet, meaning they are essentially sodium-free.

How Does Bicalustad Interact with Other Drugs?

Quick Answer: Bicalutamide interacts with several medications through the cytochrome P450 enzyme system, particularly CYP3A4. It is strictly contraindicated with terfenadine, astemizole, and cisapride. It also interacts with warfarin, ciclosporin, cimetidine, ketoconazole, calcium channel blockers, and midazolam.

Bicalutamide is primarily metabolised in the liver through oxidation and glucuronidation. The pharmacologically active (R)-enantiomer is predominantly cleared by CYP3A4, while the inactive (S)-enantiomer is mainly glucuronidated. Bicalutamide also has the potential to inhibit CYP3A4-mediated metabolism of other drugs, which underlies several of its clinically significant drug interactions. Understanding these interactions is essential for safe prescribing, particularly given that many patients with prostate cancer are elderly and may be taking multiple medications concurrently.

Major Interactions (Contraindicated)

The following drug combinations are strictly contraindicated due to the risk of potentially life-threatening cardiac arrhythmias:

Moderate Interactions (Use with Caution)

The following medications may interact with bicalutamide, potentially altering the effectiveness or safety of one or both drugs. Your doctor may need to adjust doses or increase monitoring:

QT-Prolonging Drugs

Bicalutamide may affect certain medications used to treat cardiac arrhythmias and can increase the risk of heart rhythm disturbances when taken alongside other QT-prolonging agents. These include:

• Antiarrhythmics: quinidine, procainamide, amiodarone, sotalol
• Methadone (used for pain management and opioid dependence treatment)
• Moxifloxacin (fluoroquinolone antibiotic)
• Antipsychotics (used for serious psychiatric conditions)

If you are taking any of these medications, your doctor should assess the cardiac risks before prescribing bicalutamide and may recommend regular ECG monitoring throughout treatment. The risk of QT prolongation is cumulative, meaning that the combination of multiple QT-prolonging drugs significantly increases the probability of dangerous arrhythmias.

What Is the Correct Dosage of Bicalustad?

Quick Answer: The recommended dose of bicalutamide is either 50 mg once daily (in combination with LHRH agonist or surgical castration) or 150 mg once daily (as monotherapy or adjuvant therapy). Tablets should be swallowed whole with water, at approximately the same time each day.

Always take bicalutamide exactly as prescribed by your doctor. The correct dose depends on your specific clinical situation, the stage of your prostate cancer, and whether you are receiving other hormonal treatments simultaneously. Do not change your dose or stop taking the medication without first consulting your doctor.

Adults

Children and Adolescents

Bicalutamide is not indicated for use in children or adolescents. There are no paediatric indications for this medication. It should never be administered to anyone under 18 years of age.

Elderly Patients

No dose adjustment is required for elderly patients based on age alone. However, given that the majority of patients treated with bicalutamide are older men, clinicians should consider age-related factors such as reduced liver function, cardiovascular comorbidities, and polypharmacy when prescribing. The European Society for Medical Oncology (ESMO) recommends comprehensive geriatric assessment for older patients receiving cancer treatment to optimise outcomes and minimise toxicity.

Missed Dose

If you forget to take your daily dose of bicalutamide, skip the missed dose and wait until it is time for your next scheduled dose. Do not take a double dose to make up for a forgotten one. Try to take your medication at approximately the same time each day to establish a routine. Setting a daily alarm or using a pill organiser can help you remember.

Overdose

If you take more bicalutamide than prescribed, or if a child accidentally ingests the medication, contact your doctor, go to a hospital emergency department, or call your local poison control centre immediately. There is no specific antidote for bicalutamide overdose. Treatment is supportive and symptomatic. Bring the remaining tablets and the medication packaging with you so that healthcare professionals can identify what you have taken.

Stopping Treatment

Do not stop taking bicalutamide without consulting your doctor first, even if you feel well. Prostate cancer treatment typically requires long-term medication adherence, and stopping prematurely may allow the disease to progress. If you experience side effects that concern you, speak with your doctor about the best course of action rather than discontinuing treatment on your own. In some cases, your doctor may adjust the dose or switch to an alternative medication.

What Are the Side Effects of Bicalustad?

Quick Answer: Like all medications, bicalutamide can cause side effects. The most common include breast tenderness/enlargement, hot flushes, weakness, sexual dysfunction, and gastrointestinal symptoms. Serious but less common effects include liver damage, interstitial lung disease, and cardiovascular events. Seek immediate medical attention if you notice yellowing of the skin or eyes, severe breathing difficulties, or signs of allergic reaction.

Side effects of bicalutamide are largely a consequence of its antiandrogen mechanism of action. Many of the most common effects — such as hot flushes, gynaecomastia (breast enlargement), and sexual dysfunction — result from the reduction in androgen signalling. Understanding the frequency and nature of potential side effects helps patients and healthcare providers make informed treatment decisions and enables early recognition of serious adverse events.

Liver-Related Side Effects

Hepatotoxicity is one of the most clinically significant adverse effects of bicalutamide. Liver problems can range from mild, asymptomatic elevations in liver enzymes to severe hepatitis and, very rarely, fulminant liver failure. The risk appears to be highest during the first few months of treatment. Signs of liver problems include yellowing of the skin or eyes (jaundice), dark urine, persistent fatigue, abdominal pain (particularly in the upper right area), and unexplained loss of appetite. Your doctor should perform liver function tests before starting treatment and at regular intervals, especially during the first 4 months.

Cardiovascular Side Effects

Androgen deprivation therapy, including bicalutamide, has been associated with cardiovascular side effects. These include an increased risk of myocardial infarction (heart attack), heart failure, and QT interval prolongation on ECG. A comprehensive review published by the American Heart Association highlighted that men receiving ADT should undergo cardiovascular risk assessment and receive appropriate preventive measures, including management of traditional risk factors such as hypertension, hyperlipidaemia, diabetes, and obesity. Regular cardiac monitoring is recommended, particularly in patients with pre-existing cardiovascular disease.

Gynaecomastia and Breast Pain

Breast tenderness and enlargement (gynaecomastia) are among the most frequently reported side effects, particularly with the 150 mg monotherapy dose, where they may affect up to 70-80% of patients. This occurs because blocking androgen receptors shifts the oestrogen-to-androgen balance, allowing oestrogen effects to predominate in breast tissue. While not dangerous, gynaecomastia can significantly affect quality of life. Strategies to manage this include prophylactic low-dose radiotherapy to the breast area or treatment with tamoxifen. Discuss these options with your oncologist if breast symptoms are troublesome.

How Should You Store Bicalustad?

Quick Answer: Store Bicalustad at room temperature with no special storage conditions required. Keep out of the sight and reach of children. Do not use after the expiry date printed on the packaging.

Bicalustad does not require any special storage conditions. It should be stored at room temperature, away from excessive heat and humidity. Keep the medication in its original packaging (blister pack) to protect it from moisture and light until you are ready to take a dose.

As with all medications, keep Bicalustad out of the sight and reach of children. Do not use this medicine after the expiry date stated on the carton or blister pack after "EXP." The expiry date refers to the last day of the stated month.

Do not dispose of medications via wastewater or household waste. Ask your pharmacist how to dispose of medicines that are no longer needed. These measures help to protect the environment, as pharmaceutical compounds can contaminate water sources if not disposed of properly.

What Does Bicalustad Contain?

Quick Answer: Each Bicalustad tablet contains bicalutamide as the active ingredient (50 mg or 150 mg). Inactive ingredients include lactose monohydrate, sodium starch glycolate, povidone K30, magnesium stearate, and a film coating of titanium dioxide, hypromellose, and macrogol 400.

Active Ingredient

Each film-coated tablet contains either 50 mg or 150 mg of bicalutamide.

Inactive Ingredients (Excipients)

Tablet core:

• Lactose monohydrate (a sugar-based filler)
• Sodium starch glycolate (Type A) (a disintegrant to help the tablet break down)
• Povidone K30 (a binder that holds the tablet together)
• Magnesium stearate (a lubricant used in tablet manufacturing)

Film coating:

• Titanium dioxide (E171) (a white pigment)
• Hypromellose (a coating agent)
• Macrogol 400 (a plasticiser for the film coat)

Appearance and Pack Sizes

Bicalustad 50 mg tablets are white, round, and biconvex film-coated tablets. They are packaged in blister packs made of plastic and aluminium foil. Available pack sizes include 7, 10, 14, 15, 28, 30, 50, 56, 60, 84, 90, and 100 film-coated tablets. Not all pack sizes may be marketed in every country.

Bicalustad is manufactured by STADA Arzneimittel AG, based in Bad Vilbel, Germany, with additional manufacturing sites in Ireland, Austria, and Belgium. It is distributed internationally under various generic brand names.