
Antiandrogen Comparison Tool
Mechanism: Androgen-receptor antagonist
Approval: 1993
Dosage: 250 mg TID (three times daily)
Side Effects: Liver toxicity, GI upset
Cost: Low ($30/month)
Dosing: Complex (3x daily)
Mechanism: Androgen-receptor antagonist
Approval: 1995
Dosage: 50 mg QD (once daily)
Side Effects: Hot flashes, mild liver impact
Cost: Moderate ($70/month)
Dosing: Simple (Once daily)
Mechanism: Receptor antagonist + nuclear translocation blocker
Approval: 2012
Dosage: 160 mg QD (once daily)
Side Effects: Seizures, fatigue, hypertension
Cost: High ($350/month)
Dosing: Simple (Once daily)
Mechanism: Androgen-receptor antagonist
Approval: 1990 (limited)
Dosage: 300 mg QD (once daily)
Side Effects: Visual disturbances, lung toxicity
Cost: Moderate ($50/month)
Dosing: Simple (Once daily)
Mechanism: Steroidal antagonist + progestin
Approval: 1998 (EU)
Dosage: 100-300 mg QD (once daily)
Side Effects: Weight gain, mood swings, liver risk
Cost: Moderate ($120/month)
Dosing: Simple (Once daily)
Mechanism: Weak androgen antagonist (high dose)
Approval: 1959 (diuretic)
Dosage: 100-200 mg QD (once daily)
Side Effects: Hyperkalemia, gynecomastia
Cost: Very Low ($15/month)
Dosing: Simple (Once daily)
Which Antiandrogen Should You Choose?
Consider these factors when selecting your antiandrogen:
- Clinical Stage: Early-stage disease often uses Flutamide or Bicalutamide; metastatic cases may need Enzalutamide
- Side Effect Tolerance: Avoid Enzalutamide if you have a history of seizures; Bicalutamide is safer for liver concerns
- Dosing Convenience: Once-daily regimens improve adherence; Flutamide's 3x daily schedule can lead to missed doses
- Cost and Insurance: Flutamide is cheapest but requires monitoring; Enzalutamide is expensive but potent
- Drug Interactions: Check with your doctor about CYP3A4 metabolism interactions
If you or a loved one are facing prostate‑related hormone therapy, you’ve probably heard the name Flutamide comparison pop up. Flutamide (brand name Eulexin) has been a go‑to antiandrogen for decades, but newer agents and older cousins often promise fewer side effects, simpler dosing, or better cancer control. This guide lines up the most common alternatives, weighs them on real‑world criteria, and helps you decide which drug fits your health goals.
Key Takeaways
- Flutamide blocks the androgen receptor but requires multiple daily doses and can cause liver toxicity.
- Bicalutamide offers once‑daily dosing with a lower risk of liver issues, making it the most popular first‑line alternative.
- Enzalutamide is the most potent newer antiandrogen but costs significantly more and carries a seizure risk.
- Nilutamide and cyproterone acetate are older options; they work but have limited modern use because of side‑effect profiles.
- Spironolactone, though technically a potassium‑sparing diuretic, also blocks androgen receptors and is sometimes used off‑label for hormonal control.
What Is Flutamide (Eulexin)?
When discussing antiandrogen therapy, Flutamide is a non‑steroidal drug sold under the brand name Eulexin. It blocks the androgen receptor, preventing testosterone and dihydrotestosterone from stimulating prostate cells. First approved by the U.S. Food and Drug Administration (FDA) in the early 1990s, Flutamide became the backbone of combined hormonal therapy for locally advanced prostate cancer. The typical dose is 250mg taken three times daily, which can be a pill burden for many patients.
Key strengths of Flutamide include its well‑documented mechanism and relatively low cost compared with newer agents. However, clinicians watch liver function tests closely because hepatotoxicity occurs in up to 10% of users, sometimes requiring dose reduction or cessation.

Top Antiandrogen Alternatives
The market now offers several alternatives, each with a unique mix of potency, dosing convenience, side‑effect profile, and price. Below is a quick snapshot of the most frequently prescribed options.
Bicalutamide (Casodex)
Bicalutamide is a second‑generation non‑steroidal antiandrogen approved in 1995. It blocks the same androgen receptor as Flutamide but does so with a longer half‑life, allowing a simple once‑daily 50mg dose. Liver toxicity is rarer, and the drug is often the first choice for patients who struggle with Flutamide’s three‑times‑daily schedule.
Enzalutamide (Xtandi)
Enzalutamide is a third‑generation antiandrogen approved in 2012 for metastatic castration‑resistant prostate cancer. It not only blocks the androgen receptor but also prevents its movement into the cell nucleus. The standard dose is 160mg once daily. The drug is more potent than Flutamide or Bicalutamide, but its price tag is steep-often three to four times higher. A rare but serious side effect is the risk of seizures, especially in patients with a history of convulsions.
Nilutamide (Nilandron)
Nilutamide is an older non‑steroidal antiandrogen, structurally similar to Flutamide. It’s taken once daily but has fallen out of favor due to its association with visual disturbances and interstitial lung disease. It remains available in some regions for patients who cannot tolerate newer agents.
Cyproterone acetate
Cyproterone acetate is a steroidal antiandrogen that also has progestogenic activity, giving it a dual effect: it blocks androgen receptors and suppresses luteinizing hormone, lowering testosterone production. It’s commonly used in Europe for prostate cancer and severe hirsutism. Daily doses range from 100mg to 300mg. Side effects include weight gain, mood changes, and a modest risk of liver toxicity.
Spironolactone
Although primarily a potassium‑sparing diuretic, Spironolactone antagonizes androgen receptors at higher doses (100‑200mg daily). It’s sometimes prescribed off‑label for patients needing mild antiandrogen effects, such as those with benign prostatic hyperplasia (BPH) or acne. Its side‑effect profile includes hyperkalemia and gynecomastia, which can limit use in prostate cancer patients.
Side‑by‑Side Comparison
Drug | Mechanism | FDA Approval | Typical Dose | Major Side Effects | Monthly Cost (US$) |
---|---|---|---|---|---|
Flutamide | Androgen‑receptor antagonist | 1993 | 250mg TID | Liver toxicity, GI upset | ≈30 |
Bicalutamide | Androgen‑receptor antagonist | 1995 | 50mg QD | Hot flashes, mild liver impact | ≈70 |
Enzalutamide | Receptor antagonist + nuclear translocation blocker | 2012 | 160mg QD | Seizures, fatigue, hypertension | ≈350 |
Nilutamide | Androgen‑receptor antagonist | 1990 (limited) | 300mg QD | Visual disturbances, lung toxicity | ≈50 |
Cyproterone acetate | Steroidal antagonist + progestin | 1998 (EU) | 100‑300mg QD | Weight gain, mood swings, liver risk | ≈120 |
Spironolactone | Weak androgen antagonist (high dose) | 1959 (diuretic) | 100‑200mg QD | Hyperkalemia, gynecomastia | ≈15 |

How to Choose the Right Antiandrogen
Deciding which drug to use isn’t just a numbers game. Consider these practical lenses:
- Clinical stage: Early‑stage or locally advanced disease often responds well to Flutamide or Bicalutamide. Metastatic castration‑resistant cases usually need the potency of Enzalutamide.
- Side‑effect tolerance: If liver health is a concern, Bicalutamide or Cyproterone acetate may be safer bets. Patients with seizure history should avoid Enzalutamide.
- Dosing convenience: A once‑daily regimen improves adherence. Flutamide’s threetimes‑daily schedule can lead to missed doses.
- Cost and insurance coverage: In Australia, the PBS subsidizes Bicalutamide and Enzalutamide for specific indications, but out‑of‑pocket costs can still vary. Flutamide remains the cheapest, but the cost of monitoring liver enzymes should be factored in.
- Drug interactions: Many antiandrogens are metabolized via CYP3A4. Patients on strong inhibitors (e.g., ketoconazole) may need dose adjustments.
Talking with an oncologist or a specialized pharmacist is essential. They can order baseline labs-ALT/AST for liver, potassium for spironolactone, and MRI for disease monitoring-to personalize the regimen.
Practical Tips & Common Pitfalls
Tip 1 - Schedule liver tests early. For Flutamide and Cyproterone acetate, check ALT/AST at baseline, then at 2weeks, 1month, and every 3months thereafter.
Tip 2 - Align doses with meals. Flutamide is best taken with food to reduce GI irritation, while Enzalutamide should be taken on an empty stomach for optimal absorption.
Pitfall - Ignoring drug‑specific warnings. Enzalutamide’s seizure warning is not optional; if a patient experiences a tonic‑clonic event, discontinue immediately.
Tip 3 - Keep a medication diary. Document side effects, dosing times, and any over‑the‑counter meds. This record helps the care team tweak therapy before problems become severe.
Pitfall - Overreliance on “cheapest” option. Flutamide’s low price can be deceptive if frequent liver monitoring adds hidden costs. Weigh total healthcare expenditure, not just drug price.
Frequently Asked Questions
Is Flutamide still used as first‑line therapy?
In many regions Flutamide has been largely replaced by Bicalutamide because of the simpler once‑daily dosing and lower risk of liver injury. However, it remains a cost‑effective option for patients without liver disease and where insurance coverage limits newer drugs.
Can I switch from Flutamide to Bicalutamide without a washout period?
Generally, clinicians transition directly because both drugs share the same mechanism. A brief 24‑hour overlap is acceptable, but liver function should be re‑checked after the switch.
What monitoring is required for Enzalutamide?
Baseline neurologic assessment, periodic blood pressure checks, and routine labs (CBC, liver enzymes) every 3‑6months. Any new seizure activity mandates immediate discontinuation.
Is Spironolactone a viable antiandrogen for prostate cancer?
It’s considered weak compared with dedicated antiandrogens. Some clinicians use it for mild androgen suppression or symptom control, but it’s not first‑line for cancer‑directed therapy.
How does cost differ between Flutamide and Enzalutamide in Australia?
Flutamide typically costs underAU$30 per month for a 3‑month supply, while Enzalutamide can exceedAU$450 per month. PBS subsidies may reduce the out‑of‑pocket price for eligible patients, but the gap remains large.
Choosing the right antiandrogen is a balance of disease control, side‑effect tolerance, lifestyle, and budget. By comparing the key attributes above, you can have a focused conversation with your healthcare team and land on a therapy that feels both effective and manageable.
Comments
Aman Vaid
While the guide does a solid job outlining the basic pharmacology, I must point out that the liver toxicity data for flutamide are derived from studies conducted over two decades ago, which may not reflect current monitoring practices. Modern labs detect transaminase elevations far earlier, reducing the actual clinical incidence. Moreover, the cost comparison omits the hidden expense of routine LFTs, which can be a non‑trivial burden for patients on a tight budget. The dosing frequency of three times daily is also a significant adherence hurdle, especially for elderly patients who may already be managing polypharmacy. Finally, the table could benefit from a column indicating the half‑life of each agent, as that directly influences the dosing convenience you discuss.
Overall, the information is accurate, but a few additional real‑world considerations would make it truly comprehensive.