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Generic Bicalutamide
Bicalutamide is a non‑steroidal antiandrogen indicated for the treatment of advanced prostate cancer in combination with a luteinizing hormone‑releasing hormone (LHRH) agonist (medical castration) or after surgical orchiectomy. Bicalutamide competitively binds to androgen receptors on prostate tumour cells, blocking the action of circulating testosterone and dihydrotestosterone. By inhibiting androgen‑mediated cell growth and differentiation, it slows disease progression. Bicalutamide is not a chemotherapeutic agent and must be used together with continuous androgen deprivation therapy; it does not lower serum testosterone and should never be given as monotherapy for advanced disease except in selected patients under specialist supervision.
Usual adult dose: The recommended dose is one 50 mg tablet taken orally once daily, at approximately the same time each day. Treatment with bicalutamide is started concomitantly with an LHRH agonist (e.g., leuprolide, goserelin) or following bilateral orchiectomy. The tablet may be taken with or without food. No dose adjustment is required for elderly patients or those with mild renal impairment. In patients with moderate‑to‑severe hepatic impairment, bicalutamide is not recommended because of extensive hepatic metabolism and the risk of accumulation. If a dose is missed, it should be taken as soon as remembered, but two doses must not be taken on the same day. Treatment is continued as long as clinical benefit is maintained and unacceptable toxicity does not occur.
Dosage form: Film‑coated tablets: 50 mg (white to off‑white, round, biconvex). Available in blister packs of 28 or 30 tablets.
Onset of action: Once steady‑state plasma levels are reached (approximately 4 weeks after starting once‑daily dosing), the antiandrogenic effect is fully established. Clinical benefit, reflected by a decline in prostate‑specific antigen (PSA) levels and delay in disease progression, is typically assessed after 3 to 6 months of combined therapy.
Duration of action: The elimination half‑life of the active (R)‑enantiomer of bicalutamide is approximately 6 days, which supports once‑daily dosing and maintains continuous androgen receptor blockade throughout the dosing interval. Upon discontinuation, the drug is slowly cleared over several weeks.
Alcohol recommendation: There is no known direct interaction between bicalutamide and alcohol. However, bicalutamide is extensively metabolized by the liver and can cause hepatotoxicity. Heavy alcohol consumption may further impair liver function and increase the risk of liver injury. Patients should limit alcohol intake and undergo regular liver function testing as recommended by their oncologist.
Most common side effects: Due to the associated LHRH agonist or surgical castration, the most frequent adverse effects are hot flashes, loss of libido, and impotence. Bicalutamide itself commonly causes breast tenderness and gynecomastia (breast enlargement), which may be severe; prophylactic breast irradiation or tamoxifen may be considered. Gastrointestinal effects include nausea, diarrhea, and abdominal pain. Hepatotoxicity, ranging from reversible transaminase elevations to severe hepatitis and rare cases of fatal hepatic failure, is a serious risk; liver function must be monitored at baseline, regularly during the first few months of therapy, and whenever symptoms suggestive of hepatitis develop. If jaundice or marked transaminase elevations occur, the drug should be interrupted or discontinued. Bicalutamide is a CYP3A4 substrate and may interact with strong CYP3A4 inhibitors. As a component of androgen deprivation therapy, bicalutamide may contribute to metabolic changes, osteoporosis, and cardiovascular risk. Women of child‑bearing potential must not handle broken tablets or use bicalutamide; if a female partner is or could become pregnant, barrier contraception is essential. Bicalutamide must be prescribed and supervised by a healthcare professional experienced in oncology.
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What is Bicalutamide?
Bicalutamide is a hormone therapy that helps hold prostate cancer in check. It belongs to a group of drugs called non-steroidal anti-androgens. Prostate cancer cells need testosterone to grow and spread. Bicalutamide doesn't stop the body from making testosterone, but it blocks the docking stations, the androgen receptors, on the surface of the cancer cells. Without an open docking station, testosterone can't deliver its signal to divide. The cancer slows its growth, and in many men, it shrinks or remains stable for years.
This drug is almost always paired with an LHRH agonist, a separate injection that tells the testicles to stop producing testosterone. Together, they form a complete androgen blockade. Bicalutamide is also used on its own in specific situations, sometimes at a higher dose, but the 50 mg tablet is the standard partner in combination therapy. You take it once a day, every day, as part of a long-term strategy to keep the cancer dormant. It doesn't cure prostate cancer, but it pushes the disease back from the edge, preserving quality of life and extending survival.
Mechanism and Pharmacology
Bicalutamide is a pure antagonist of the androgen receptor. It has a shape that fits the receptor perfectly, locking into place without activating it. Think of it as a wrong key that gets stuck in a lock. The right key, testosterone or dihydrotestosterone, can't enter because the lock is already jammed. Inside the cancer cell, the receptor normally travels to the nucleus and flips on growth genes. Bicalutamide prevents that entire journey. It holds the receptor in the cytoplasm, inert. The 50 mg dose is enough to block the receptors completely when testosterone levels are already low from LHRH therapy.
After you swallow the tablet, it absorbs slowly, reaching steady levels in your blood after about a month due to its long half-life of roughly 6 days. It's processed by the liver, mainly through the CYP3A4 enzyme, and then eliminated gradually in urine and feces. Because it lingers in the body, missing a single dose doesn't immediately undo the blockade, but consistent daily intake keeps the shield up. The liver's central role in clearing the drug means that liver function must be monitored regularly. Bicalutamide can irritate the liver in a small number of men, sometimes severely, so blood tests are non-negotiable.
How to Use Bicalutamide
Take one 50 mg tablet each day, at the same time, with a glass of water. You can take it with or without food. The most important thing is to take it daily and to keep getting your LHRH injections on schedule. Your oncologist will typically start the bicalutamide a few days before the first LHRH injection to prevent a temporary flare of testosterone that can worsen bone pain or urinary symptoms. After that, you continue both treatments long-term.
If you forget a dose, take it as soon as you remember. If it's already the next day, skip the missed dose and resume your usual routine. Don't double up. If you miss several doses, call your doctor before restarting. You'll need regular PSA tests to track the cancer's activity, and liver function tests every few months to catch any signs of inflammation early. Do not stop taking bicalutamide abruptly, even if you feel fine. The cancer is being suppressed. Stopping can allow it to wake up and progress.
Side Effects of Bicalutamide
The side effects are mostly the consequence of shutting down the male hormone axis. Hot flashes are very common, sudden waves of heat and sweating that come out of nowhere. They can be disruptive to sleep but often become less intense over time. Breast tenderness and enlargement (gynecomastia) occur because the small amount of estrogen that the male body produces is now unopposed. The breast tissue can become sore and swollen, and in some men, this is significant enough to need treatment. Radiation to the breast area or a short course of tamoxifen can help.
Fatigue is another frequent companion. A bone-deep tiredness that rest doesn't always fix. Muscle loss and a gradual drop in physical strength can occur over months and years. Some men experience diarrhea, nausea, or a reduced appetite. A rash or itching is less common. The most serious risk is liver toxicity. This can happen quietly, with no symptoms at first, which is why blood tests are so important. But if you notice yellowing of your skin or eyes, dark urine, severe nausea, vomiting, or pain in the upper right side of your belly, stop taking the drug and get medical help immediately. These signs of liver injury are rare but require urgent attention. Lung inflammation is an even rarer but serious reaction, causing shortness of breath and cough.
High-Risk Groups (Elderly, Pregnancy)
Bicalutamide is not for women. It is strictly a prostate cancer drug. If a pregnant woman is exposed to the tablets or powder, it can harm the developing baby, especially a male fetus. Women who are pregnant or may become pregnant should not handle broken tablets. The drug has no use in breastfeeding.
Elderly men, who are the main group receiving this therapy, do not need a different dose. However, they are more likely to have other health issues. Liver function and the list of other medications need careful review. Falls from muscle weakness are a real concern. Men with moderate to severe liver disease should not take bicalutamide, or should use a reduced dose with very close monitoring. Kidney problems do not require a dose change, as the drug is cleared mostly by the liver. Men with significant heart disease or a history of arrhythmias should be monitored, though bicalutamide itself has minimal direct cardiac effects.
Interaction With Activities (Driving, Alcohol)
Bicalutamide does not directly make you drowsy, but the fatigue it often brings can slow your reactions and make driving unsafe. If you feel tired, don't get behind the wheel. Alcohol is not strictly forbidden, but it can add to the liver's workload and worsen the fatigue. Heavy drinking while on this medication is a gamble you shouldn't take. If you drink, keep it minimal and always tell your oncologist the truth about your intake.
Drug Interactions
The liver enzyme CYP3A4 processes bicalutamide. Drugs that strongly block this enzyme, like the antifungals ketoconazole and itraconazole, or certain antibiotics like clarithromycin, can raise bicalutamide levels and increase the risk of side effects. Drugs that strongly rev up the enzyme, like rifampin or phenytoin, can lower bicalutamide levels and might reduce its anti-cancer effect. Your oncologist needs to know every medication, supplement, and herbal product you take. The blood thinner warfarin deserves special attention. Bicalutamide can bump warfarin off its protein binding sites, making it more potent and raising the risk of bleeding. If you're on warfarin, your INR will need frequent checks and your warfarin dose will likely be adjusted.
Alternative Options
Bicalutamide is one of several anti-androgens. The older drug flutamide has a higher risk of severe liver problems and is rarely used. Nilutamide is another older option with its own set of side effects, including difficulty adjusting to darkness. The newer androgen receptor blockers, enzalutamide (Xtandi), apalutamide (Erleada), and darolutamide (Nubeqa), are more powerful and are often used when the cancer becomes resistant to bicalutamide. For initial hormone therapy, bicalutamide combined with an LHRH agonist remains a standard, well-tolerated choice for many men. The decision of which anti-androgen to use depends on the cancer's specific features, your overall health, and the side effect profile you can best manage.
INN, Brand Names, and Classification in Canada
INN (International Nonproprietary Name): Bicalutamide
Available brand names in Canada: Casodex, and generic bicalutamide
ATC code: L02BB03
Forms and strengths: Tablets 50 mg
Manufacturers: AstraZeneca Canada Inc. (Casodex), Apotex Inc., Teva Canada Limited, Sandoz Canada Inc., and other generic manufacturers.
Registration status in Canada: Registered
Classification: Prescription (Rx)
Frequently Asked Questions
Does bicalutamide lower my testosterone?
No. It blocks the receptor that testosterone uses, but your blood testosterone level may actually rise slightly when taken alone. In combination with an LHRH agonist, the LHRH agonist does the lowering, and bicalutamide blocks whatever is left.
How long will I need to take bicalutamide?
Usually, for as long as the cancer stays hormone-sensitive and you can tolerate the side effects. This can be several years. If your PSA begins to rise despite treatment, the cancer may have become resistant, and your oncologist will discuss next steps.
Can bicalutamide make my breasts grow?
Yes, breast tenderness and some growth (gynecomastia) is a common side effect. It's caused by the shift in the balance between androgens and estrogens. If it becomes painful, let your doctor know. There are ways to manage it, including radiation or medication.
What if my liver tests come back abnormal?
Your oncologist will assess the severity. Mild elevations might mean more frequent monitoring. A significant rise usually means pausing the drug, and if the liver recovers, possibly restarting at a lower dose. Severe reactions mean stopping bicalutamide permanently and switching to another therapy.
Delivery Information Across Canada
We ship Bicalutamide to all provinces and territories. Delivery times vary depending on how remote your location is:
- Ontario (Toronto, Ottawa, Mississauga): 5 to 7 days
- Quebec (Montreal, Quebec City, Laval): 5 to 7 days
- British Columbia (Vancouver, Victoria, Burnaby): 5 to 9 days
- Alberta (Calgary, Edmonton, Red Deer): 5 to 9 days
- Manitoba (Winnipeg, Brandon): 5 to 9 days
- Saskatchewan (Saskatoon, Regina): 5 to 9 days
- Nova Scotia (Halifax, Sydney): 5 to 9 days
- New Brunswick (Moncton, Fredericton): 5 to 9 days
- Newfoundland and Labrador (St. John's, Corner Brook): 7 to 14 days
- Prince Edward Island (Charlottetown): 7 to 14 days
- Yukon, Northwest Territories, Nunavut: 7 to 14 days
All shipments are packed discreetly with no branding or indication of contents on the outside.
| Shipping method | Delivery time | Price | |
Delivery |
14-21 days | 14.95$ | Tracking# available in 4 days |
Delivery |
9-14 days | 30$ | Tracking# available in 2 days |
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