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Abiraterone

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Abiraterone is an androgen biosynthesis inhibitor used to treat prostate cancer. It works by decreasing the production of testosterone and other androgens that can stimulate tumor growth. It is primarily indicated for adults as part of a comprehensive oncology management plan to improve outcomes.


Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Abiraterone Acetate
Reference Brand
Zytiga
Manufacturer
Janssen-Cilag
Product Form
Tablet
Regulatory Classification
Rx
Primary Category
Cancer Treatment
Product Category
Antineoplastic Agents, Endocrine Therapy
Pharmacological Class
CYP17 Inhibitor, Androgen Synthesis Inhibitor
Manufacturer Description
Abiraterone is a hormonal therapy used to treat specific types of prostate cancer, usually in combination with prednisone or prednisolone.
Mechanism of Action
Abiraterone works by blocking the enzyme CYP17, which is required for the body to produce androgens (male hormones). By reducing androgen levels, it helps slow the growth of prostate cancer cells that rely on these hormones to divide.
Route of Administration
Oral
Onset Time
Varies (days to weeks for hormonal changes)
Duration
24 hours
Contraindications
Severe liver impairment, Pregnancy, Hypersensitivity to abiraterone
Severe Adverse Events
Heart failure, Liver toxicity, Adrenal insufficiency
Common Side Effects
Joint swelling, Hot flushes, Diarrhoea
Uncommon Side Effects
High blood pressure, Low blood potassium, Fluid retention
Drug Interactions
Rifampicin, Phenytoin, St John's wort, Ketoconazole
Pregnancy Safety Warnings
Not for use in women; may cause birth defects if exposed.
Age Restrictions
Adults only
Storage Guidelines
Store at room temperature away from moisture.
Related Products
Zytiga, Yonsa

Abiraterone FAQ

Can I take Abiraterone with other prostate cancer drugs like enzalutamide?

Abiraterone and enzalutamide both target androgen signalling but work through different mechanisms. Combining them is not recommended because it substantially increases the risk of liver toxicity and hypertension. Any combination therapy should only be pursued in a clinical trial setting or under specialist supervision.

Do I need to stop taking Abiraterone before surgery?

There is no routine requirement to discontinue abiraterone before elective surgery, but the surgical team should be informed of the medication due to its effects on blood pressure, electrolytes, and wound healing. Adjustments to glucocorticoid dosing may be necessary peri-operatively.

How does food affect the absorption of Abiraterone?

A high-fat meal can double the drug’s absorption, potentially raising the incidence of side effects. For consistent exposure, take the tablet on an empty stomach, at least one hour before or two hours after any food.

Can Abiraterone cause weight gain?

Fluid retention associated with mineralocorticoid excess may lead to a modest increase in body weight. This is usually reversible with diuretics, blood-pressure control, and appropriate glucocorticoid cover.

Is a blood test required before each dose of Abiraterone?

Routine full-dose laboratory monitoring is not needed before every single dose, but regular checks of liver enzymes, potassium, and blood pressure are essential-typically every 2-4 weeks early in therapy and then at longer intervals if stable.

Will Abiraterone affect my cholesterol levels?

Some patients experience modest changes in lipid profiles, particularly increases in LDL cholesterol. Lipid panels should be performed periodically, and statin therapy may be considered if levels become elevated.

Can I travel internationally with Abiraterone tablets?

Yes, but keep the medication in its original labelled container, carry a copy of the prescription, and be prepared to show the prescription at customs if asked. For flights longer than 8 hours, bring a small cooler pack if ambient temperatures may exceed 30 °C.

What should I do if I miss a dose while on a strict schedule?

If you remember within 12 hours, take the missed tablet; otherwise, skip it and continue with the next scheduled dose. Doubling up is unnecessary and may increase side-effect risk.

Are there any special considerations for men with a history of heart disease?

Because abiraterone can raise blood pressure and cause fluid overload, patients with pre-existing cardiac conditions require more intensive monitoring and may need antihypertensive or diuretic therapy. Cardiologists should be involved in the care plan where appropriate.

Is there a generic version of Abiraterone available in the UK?

Abiraterone acetate is the generic name, and the 250 mg tablet is marketed under the brand name Zytiga in the UK. Generic equivalents may become available after patent expiry; they contain the same active ingredient and dosage strength.

What is Abiraterone?

Abiraterone is a medication used in the treatment of advanced prostate cancer. The active ingredient in Abiraterone is abiraterone acetate, an oral androgen biosynthesis inhibitor. In the United Kingdom it is available as a 250 mg pill (tablet) and is prescribed by specialist oncologists under the supervision of the Medicines and Healthcare products Regulatory Agency (MHRA). It is marketed in the UK under the brand name Zytiga.

Abiraterone belongs to the therapeutic class often described as oncology support agents because it is used alongside other cancer-directed therapies to control disease progression. The medication is supplied only by prescription (Rx) and requires careful monitoring of hormonal and metabolic parameters.

How Abiraterone Works in the Body

Abiraterone acetate is a pro-drug that is rapidly converted in the gut and liver to abiraterone, the active metabolite. Abiraterone blocks the enzyme CYP17A1 (17α-hydroxylase/17,20-lyase), which is essential for the production of androgens (testosterone, dihydrotestosterone) in the adrenal glands, testes, and prostate tumour tissue.

By inhibiting CYP17A1, abiraterone dramatically reduces circulating androgen levels, depriving prostate cancer cells of the hormones they need to grow. The drug’s effect is systemic rather than limited to the testes, which explains its efficacy in castration-resistant disease where tumours have adapted to low testosterone environments.

Key pharmacological points:

  • Onset of action: Hormonal suppression begins within days of the first dose.
  • Peak effect: Maximum reduction in androgen concentrations is typically seen after 1 - 2 weeks of continuous therapy.
  • Duration: As long as the daily pill is taken, the enzyme inhibition persists; there is no clinically relevant drug accumulation.
  • Metabolism: Abiraterone is further metabolised mainly by CYP3A4 and excreted in the feces.
  • Pharmacokinetics: Oral bioavailability is modest; food can increase absorption, so the medication is usually taken on an empty stomach (at least one hour before or two hours after meals).

Conditions Treated by Abiraterone

Abiraterone is approved in the United Kingdom for the following indications, as detailed in the MHRA product licence and NICE technology appraisal guidance:

  • Metastatic castration-resistant prostate cancer (mCRPC) in patients who have previously received a chemotherapy regimen containing docetaxel.
  • Metastatic castration-resistant prostate cancer in patients who have not received prior chemotherapy, when combined with prednisone (or prednisolone) to mitigate mineralocorticoid-related side effects.

In both settings, abiraterone is prescribed alongside ongoing continuous androgen-deprivation therapy (ADT), usually in the form of a luteinising hormone-releasing hormone (LHRH) agonist or antagonist, to maintain castrate levels of testosterone.

Off-Label and Investigational Applications

Current peer-reviewed literature does not support routine off-label use of abiraterone for conditions other than prostate cancer. Investigational studies have explored its role in:

  • Hormone-sensitive breast cancer (as a steroidogenesis inhibitor).
  • Castration-resistant ovarian cancer (early-phase trials).

These uses remain experimental, are not approved by the UK regulatory agencies, and would require enrolment in a clinical trial or a specialist’s compassionate-use prescription.

Disclaimer: Off-label use of abiraterone must be undertaken only under the direct supervision of a qualified oncologist, with a clear risk-benefit assessment and appropriate monitoring.

Who Should (Not) Use Abiraterone?

Absolute Contraindications

  • Known hypersensitivity to abiraterone acetate, prednisone, or any tablet excipients.
  • Severe active liver disease (Child-Pugh class C) or persistent hepatic transaminase elevations (>5 × upper limit of normal).
  • Uncontrolled hypertension or significant cardiovascular disease (e.g., recent myocardial infarction, unstable angina).
  • Concurrent use of strong CYP3A4 inducers (e.g., rifampicin, carbamazepine) that could markedly reduce abiraterone plasma concentrations.

Relative Contraindications and Cautions

  • Mild to moderate hepatic impairment (Child-Pugh A or B): dose adjustments are not recommended, but close liver function monitoring is essential.
  • Renal impairment: No dose reduction is required, yet patients with end-stage renal disease should be observed for fluid-related side effects.
  • Pregnancy & lactation: Abiraterone is contraindicated; it may cause fetal harm. Male patients should be advised that the drug is not a contraceptive and that partners of women of child-bearing potential should use reliable contraception.
  • Elderly patients (≥ 75 years): Increased susceptibility to hypertension, hypokalaemia, and cardiac events; start at the standard dose but monitor closely.

Special Populations

  • Patients with adrenal insufficiency: Must receive concomitant glucocorticoid replacement (prednisone 5 mg twice daily) to prevent adrenal crisis.
  • Patients on chronic steroids: Dose of prednisone may need adjustment; coordinate with the prescribing oncologist.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Fluid retention / peripheral oedema - often managed with diuretics or dose interruption.
  • Hypertension - requires regular blood pressure monitoring; antihypertensive therapy may be initiated.
  • Hypokalaemia - electrolyte checks every 2-4 weeks; potassium supplements if needed.
  • Fatigue - generally mild to moderate, improves with disease control.
  • Gastrointestinal discomfort (nausea, abdominal pain) - take the tablet on an empty stomach to minimise.

Serious Adverse Events

  • Hepatic toxicity - transaminases may rise sharply; discontinue if > 5 × ULN.
  • Severe hypertension or hypertensive crisis - immediate medical attention required.
  • Adrenal insufficiency - signs include severe fatigue, hypotension, and electrolyte disturbances; must be treated with glucocorticoids.
  • Cardiovascular events (e.g., myocardial infarction, arrhythmia) - risk is heightened in patients with pre-existing cardiac disease.

Drug Interactions

  • CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, erythromycin) - may increase abiraterone exposure; dose modification is generally not recommended but monitor for toxicity.
  • CYP3A4 inducers (e.g., rifampicin, phenytoin, St John’s wort) - reduce abiraterone levels, potentially compromising efficacy; avoid concomitant use.
  • Strong acid-reducing agents (e.g., proton-pump inhibitors) - can modestly decrease absorption; spacing the dose by at least 2 hours is advisable.
  • Warfarin - no direct interaction, but liver function changes may affect INR; monitor more frequently.

Food and Lifestyle Interactions

  • Food: High-fat meals increase abiraterone absorption by up to 2-fold, which may raise the risk of adverse effects. Take the tablet at least one hour before or two hours after meals.
  • Alcohol: Excessive intake can exacerbate liver toxicity and hypertension; limit consumption.
  • Driving / machinery: No direct impairment, but severe fatigue or dizziness from hypotension warrants caution.

If a patient is unsure about any medication, supplement, or herb they are taking, they should disclose all products to their healthcare professional before starting abiraterone.

How to Take Abiraterone

  • Standard dose: One 250 mg tablet once daily, taken on an empty stomach (as described above).
  • Glucocorticoid co-therapy: Prednisone 5 mg twice daily (or equivalent dose of prednisolone) must be taken with food to reduce mineralocorticoid-related side effects.
  • Missed dose: Take the missed tablet as soon as remembered if it is still within 12 hours of the scheduled time; otherwise skip and resume the regular schedule. Do not double the dose.
  • Overdose: Symptoms may include severe hypertension, electrolyte disturbances, or hepatic dysfunction. Seek emergency medical care; supportive measures and correction of electrolyte abnormalities are the mainstays of treatment.
  • Discontinuation: Abrupt cessation is generally safe if glucocorticoid cover is maintained. However, in patients with adrenal insufficiency, tapering of the steroid component may be required under medical supervision.

No dose adjustments are required for age, weight, or renal function, but the liver function must be within acceptable limits before initiation and monitored throughout therapy.

Monitoring and Follow-Up

Effective and safe use of abiraterone relies on regular clinical and laboratory assessment:

  • Baseline investigations: Full liver function panel (ALT, AST, bilirubin), serum potassium, blood pressure, and ECG if cardiac disease is suspected.
  • During treatment:
  • Liver enzymes and potassium every 2-4 weeks for the first three months, then every 3 months if stable.
  • Blood pressure at each oncology visit (typically monthly).
  • PSA (prostate-specific antigen) levels every 4-6 weeks to gauge disease response.
  • Imaging: Periodic CT or bone scans per oncologist’s protocol (often every 12 weeks) to assess tumour burden.
  • Adverse-event assessment: Prompt evaluation of any new hypertension, oedema, or signs of liver injury.

Patients should be instructed to contact their healthcare team immediately if they experience symptoms such as severe abdominal pain, sudden weight gain, persistent vomiting, or visual changes.

Storage and Handling

  • Keep tablets at room temperature (15 °C - 30 °C), away from direct sunlight and moisture.
  • Store the medication in the original container with the child-proof lid intact.
  • Do not refrigerate or freeze.
  • Dispose of unused tablets according to the NHS “Medicines Return Programme” or follow local pharmacy take-back schemes.

Medication-Specific Glossary

CYP17A1 inhibition
The process by which abiraterone blocks the enzyme 17α-hydroxylase/17,20-lyase, halting androgen production.
Mineralocorticoid excess
An adverse effect of abiraterone characterised by hypertension, hypokalaemia, and fluid retention, mitigated by concurrent glucocorticoid therapy.
Adrenal insufficiency
Inadequate production of cortisol and aldosterone; abiraterone can precipitate this condition if glucocorticoid cover is insufficient.

Medical Disclaimer

This article provides educational information about Abiraterone and is not a substitute for professional medical advice. Treatment decisions, including the use of unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Abiraterone is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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