Andocur® (Cyproterone Acetate) — Steroidal Antiandrogen for Prostate Cancer and Androgen-Dependent Conditions

The Original Antiandrogen — Six Decades of Clinical Use in Prostate Cancer Hormonal Management

Andocur® (Cyproterone Acetate) is a steroidal antiandrogen and progestogen — a synthetic derivative of 17α-hydroxyprogesterone — with potent androgen receptor (AR) antagonist activity, significant progestogenic activity, and mild glucocorticoid activity. Cyproterone Acetate competitively blocks androgen binding to the androgen receptor in prostate cancer cells and other androgen-sensitive tissues — inhibiting androgen-driven cell growth in hormone-sensitive prostate cancer — and suppresses LH and FSH secretion through its progestogenic activity on the hypothalamic-pituitary axis, providing a dual antiandrogen mechanism combining peripheral AR blockade with central gonadotrophin suppression.

Andocur is used across multiple clinical scenarios in prostate oncology and androgen-related medicine — as monotherapy for advanced prostate cancer, as antiandrogen flare prophylaxis during GnRH agonist initiation, as management of hot flushes in men receiving GnRH agonist therapy, and for severe hypersexuality and sexual deviation. In prostate cancer, Cyproterone Acetate remains clinically relevant as a cost-effective oral antiandrogen with decades of real-world evidence — particularly in the Indian oncology setting where access to newer generation ARSIs may be limited for some patient populations.

A.K. Pharma is a trusted medicine distributor in Delhi supplying genuine Andocur (Cyproterone Acetate) in both 50mg and 100mg tablet strengths to hospitals, oncology centres, urology clinics, and pharmacies across India. Manufactured by Bayer, Andocur has been used in prostate cancer management for over six decades — one of the longest-established antiandrogen therapies in urology and oncology.

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What is Andocur (Cyproterone Acetate)?

Andocur contains Cyproterone Acetate — a steroidal compound with three distinct pharmacological activities that collectively contribute to its clinical utility in prostate cancer and androgen-dependent conditions:

Activity 1 — Androgen Receptor Antagonism (Primary Antiandrogen Mechanism): Cyproterone Acetate competitively binds to the androgen receptor (AR) — the intracellular receptor that mediates the biological effects of testosterone and dihydrotestosterone (DHT) in prostate cells. By occupying the AR ligand-binding domain, CPA prevents testosterone and DHT from activating AR → AR-driven gene transcription is suppressed → prostate cancer cell proliferation and survival signals are blocked.

However — critically different from next-generation ARSIs (Enzalutamide/Glenza, Apalutamide, Darolutamide) — Cyproterone Acetate is a partial agonist at the AR in some contexts, particularly with AR overexpression or AR mutations (as occur in castration-resistant prostate cancer). This partial agonism is why CPA is used predominantly in hormone-sensitive rather than castration-resistant settings, and why it has been superseded by next-generation AR antagonists (Glenza/Enzalutamide) in the CRPC setting.

Activity 2 — Progestogenic Activity (Central Gonadotrophin Suppression): Cyproterone Acetate is a potent progestogen — binding to progesterone receptors in the hypothalamus and pituitary with high affinity. This progestogenic activity:

• Suppresses hypothalamic GnRH release
• Suppresses pituitary LH and FSH secretion
• Reduces testicular testosterone production — providing a dual mechanism combining central (testosterone suppression) and peripheral (AR blockade) antiandrogen activity
• This central suppression makes CPA different from non-steroidal antiandrogens (Bicalutamide, Flutamide) which have no progestogenic activity and can cause LH/FSH elevation (and reflex testosterone rise) when used as monotherapy

Activity 3 — Mild Glucocorticoid Activity: Weak glucocorticoid receptor binding — relevant for the management of hot flushes (through central thermoregulatory mechanisms) and potentially contributing to the suppression of adrenal androgen production at higher doses.

Full prescribing information is available at the European Medicines Agency Cyproterone Acetate information.

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Clinical Studies and Evidence

Cyproterone Acetate vs Flutamide in Advanced Prostate Cancer Published in the European Urology (2000), a Phase 3 randomised controlled trial comparing Cyproterone Acetate 250mg/day vs Flutamide 750mg/day in 310 patients with metastatic prostate cancer demonstrated comparable progression-free survival and overall survival between the two antiandrogens — with Cyproterone Acetate showing significantly better tolerability in terms of diarrhoea and liver toxicity compared to Flutamide.

Cyproterone Acetate in Maximum Androgen Blockade (MAB) Multiple trials have evaluated Cyproterone Acetate as part of combined androgen blockade (CAB) — CPA + GnRH agonist vs GnRH agonist alone — demonstrating additive benefit from peripheral AR blockade on top of central testosterone suppression in metastatic hormone-sensitive prostate cancer, consistent with the MAB concept.

Hot Flush Management in GnRH Agonist-Treated Prostate Cancer Multiple randomised crossover studies have demonstrated Cyproterone Acetate 100mg/day significantly reduces hot flush frequency and severity in men receiving GnRH agonist therapy (Zoladex/Goserelin, Lucrin/Leuprolide) compared to placebo — with response rates of 70-80%. This represents one of the most clinically important and under-recognised indications for Andocur in the Indian oncology setting, where hot flushes are a major quality of life concern for men on long-term ADT.

Antiandrogen Flare Prevention — Cyproterone Acetate Before GnRH Agonist Initiation: Randomised studies demonstrate CPA 200-300mg/day started 3 days before first GnRH agonist injection and continued for 4 weeks effectively prevents the testosterone flare — with no clinically significant testosterone rises observed during the CPA cover period. This is now a standard recommendation in European and Indian urology guidelines for GnRH agonist initiation in men with bone metastases, spinal involvement, or urinary obstruction — where testosterone flare could cause serious clinical deterioration.

Cyproterone Acetate Monotherapy in Locally Advanced and Metastatic Prostate Cancer: A landmark randomised controlled trial published in the British Journal of Urology (1999) compared CPA monotherapy (300mg/day) vs orchiectomy in locally advanced and metastatic prostate cancer — demonstrating comparable disease-specific survival in locally advanced disease, though inferior OS in metastatic disease vs surgical castration. This established CPA monotherapy as an option in locally advanced prostate cancer (as an alternative to castration in suitable patients) but confirmed GnRH agonist/antagonist + antiandrogen as the preferred approach in metastatic disease.

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Available Strengths

Andocur is available in the following tablet strengths:

Both strengths are available from A.K. Pharma — enabling flexible dosing across all clinical indications.

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Indications — What Andocur is Used For

Prostate Cancer — Locally Advanced and Metastatic:

• Monotherapy for locally advanced (T3-T4) or metastatic hormone-sensitive prostate cancer — particularly in patients where GnRH agonist is not preferred
• As antiandrogen cover during GnRH agonist initiation — to prevent testosterone flare (standard of care in patients with bone metastases, spinal disease, or urinary obstruction)
• Combined androgen blockade — Andocur + GnRH agonist (Zoladex/Firmagon) for maximum androgen deprivation

Hot Flushes in GnRH Agonist-Treated Prostate Cancer:

• Management of vasomotor symptoms (hot flushes) in men receiving GnRH agonist therapy — one of the most common quality-of-life complications of ADT, occurring in 50-80% of men on long-term GnRH agonist therapy
• 100mg/day Cyproterone Acetate is highly effective for hot flush control

Severe Hypersexuality and Sexual Deviation:

• Reduction of sexual drive in men with paraphilias or severe hypersexuality unresponsive to psychological therapy

For detailed indication information refer to Drugs.com Cyproterone Acetate.

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Key Benefits of Andocur

Dual Antiandrogen Mechanism — Peripheral AR Blockade + Central Gonadotrophin Suppression Unlike non-steroidal antiandrogens (Bicalutamide, Flutamide) which only block peripheral AR — Andocur combines peripheral AR antagonism with central hypothalamic-pituitary suppression (through progestogenic activity). This dual mechanism makes CPA uniquely effective as monotherapy — it reduces both testosterone levels and AR-driven signalling simultaneously, without the reflex LH/FSH elevation seen with non-steroidal antiandrogens.

Standard of Care for GnRH Agonist Flare Prevention Andocur is the recommended antiandrogen for covering the testosterone flare when initiating GnRH agonist therapy — Bicalutamide is the alternative. The EAU Prostate Cancer Guidelines and Indian Urological Association guidelines both recommend antiandrogen cover (CPA or Bicalutamide) for 4 weeks when starting GnRH agonists in at-risk patients. Andocur is well-established in this role with decades of evidence.

Highly Effective Hot Flush Management CPA 100mg/day achieves 70-80% reduction in hot flush frequency and severity in ADT-treated men — significantly higher response rates than many alternative approaches (megestrol acetate, SSRIs, gabapentin). Hot flushes are one of the most distressing ADT side effects and significantly impair quality of life — Andocur provides evidence-based and effective symptom control.

Six Decades of Clinical Evidence Andocur has been in clinical use since the 1960s — providing the most extensive long-term safety and efficacy database of any antiandrogen in prostate cancer. This historical evidence base provides confidence in long-term safety for patients requiring years of therapy.

Oral Once/Twice-Daily Dosing — Outpatient Management Simple oral tablet dosing — once or twice daily depending on indication — allows complete outpatient management with periodic monitoring. No injections or clinical attendance for drug administration required.

Cost-Effective Antiandrogen Option Andocur is significantly more cost-effective than next-generation ARSIs (Enzalutamide, Apalutamide, Darolutamide) — providing clinically meaningful androgen blockade at accessible pricing for the broad Indian prostate cancer patient population who may not have access to newer agents.

Both Strengths Available — Flexible Dosing Across Indications A.K. Pharma supplies both 50mg and 100mg Andocur — enabling dosing from 100mg/day (hot flushes) to 300mg/day (monotherapy) across all clinical scenarios.

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How Andocur Works — Steroidal Antiandrogen Mechanism

The HPG Axis and Prostate Cancer:

Prostate cancer cells — like normal prostate epithelial cells — express androgen receptors (AR) and depend on androgen (testosterone, DHT) signalling for growth, survival, and function. The hypothalamic-pituitary-gonadal (HPG) axis controls testosterone production:

Hypothalamic GnRH (pulsatile) → Pituitary LH/FSH secretion → Testicular Leydig cell testosterone production → Peripheral DHT conversion (via 5α-reductase) → Prostate cancer cell AR activation → AR-driven transcription → Cancer cell proliferation

Andocur’s Dual Mechanism:

Peripheral Mechanism — AR Antagonism:

1. Cyproterone Acetate is absorbed and distributed to prostate cancer cells
2. CPA competes with testosterone and DHT for binding to the AR ligand-binding domain — binding with high affinity
3. CPA-bound AR cannot undergo the conformational changes required for transcriptional coactivator recruitment
4. AR-driven gene transcription is suppressed — genes driving prostate cancer cell proliferation (PSA, TMPRSS2, cell cycle regulators) are not activated
5. Prostate cancer cell growth and survival are inhibited

Central Mechanism — Gonadotrophin Suppression:

1. Cyproterone Acetate binds progesterone receptors in the hypothalamus → reduces GnRH pulse frequency and amplitude
2. Reduced GnRH → reduced pituitary LH and FSH secretion
3. Reduced LH → reduced Leydig cell testosterone synthesis → plasma testosterone falls
4. This central testosterone suppression adds to peripheral AR blockade — providing more complete androgen deprivation than peripheral AR blockade alone (as with non-steroidal antiandrogens)

Why This Dual Mechanism Enables Effective Monotherapy: Non-steroidal antiandrogens (Bicalutamide) block AR at the periphery — but the resulting loss of androgen negative feedback on the hypothalamus and pituitary → reflex LH and FSH surge → compensatory testosterone elevation → partial overcoming of the peripheral AR block. In contrast, CPA’s central progestogenic suppression prevents this reflex testosterone rise — maintaining testosterone suppression while simultaneously blocking peripheral AR → effective monotherapy without the testosterone surge that limits non-steroidal antiandrogen monotherapy efficacy.

For detailed mechanism overview refer to EAU Prostate Cancer Guidelines.

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Andocur in the Prostate Cancer Treatment Algorithm

1. Antiandrogen Flare Cover (Most Common Current Use in Indian Practice): When starting Zoladex (Goserelin) or other GnRH agonists:

• Start Andocur 100mg three times daily (300mg/day) or 100mg twice daily (200mg/day) — 3 days BEFORE first GnRH agonist injection
• Continue for 4 weeks total — covering the entire testosterone flare period
• Then discontinue Andocur — continue GnRH agonist alone or with other antiandrogen combination
• Mandatory in patients with bone metastases, spinal cord compromise, or urinary tract obstruction where testosterone surge could cause serious harm

2. Hot Flush Management: For men experiencing troublesome hot flushes on GnRH agonist therapy:

• Andocur 50mg twice daily (100mg/day) — continuous
• Assess response at 4 weeks
• Highly effective — 70-80% reduction in hot flush frequency and severity

3. Combined Androgen Blockade (CAB/MAB):

• Andocur 50mg twice daily + ongoing GnRH agonist (Zoladex or Firmagon)
• Adds peripheral AR blockade to central testosterone suppression
• Note: In mHSPC, next-generation ARSIs (Glenza/Enzalutamide, Abirapro/Abiraterone) have demonstrated superior OS benefit vs CPA-based CAB and are preferred where accessible

4. Monotherapy (Locally Advanced Prostate Cancer):

• Andocur 200-300mg/day (100mg twice or three times daily)
• For locally advanced (T3-T4) prostate cancer where castration is declined or contraindicated
• Inferior to GnRH agonist in metastatic disease — not recommended for M1 disease as monotherapy

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Dosage and Administration

Antiandrogen Flare Cover (GnRH Agonist Initiation):

• 100mg three times daily (300mg/day) — starting 3 days before first GnRH agonist injection
• Continue for 4 weeks total
• Then discontinue

Hot Flush Management:

• 50mg twice daily (100mg/day) — continuous while on GnRH agonist therapy
• Assess response at 4 weeks
• Adjust dose to 50mg once daily if adequate response at lower dose

Combined Androgen Blockade:

• 50mg twice daily (100mg/day) — in combination with GnRH agonist
• Ongoing throughout GnRH agonist treatment

Prostate Cancer Monotherapy (Locally Advanced):

• 200-300mg/day (100mg twice or three times daily) — as monotherapy
• Continue until disease progression

Administration:

• Take after meals — food improves tolerability
• Swallow tablets whole with water
• Take at approximately the same time each day

Monitoring:

• LFTs — baseline and regularly throughout treatment (hepatotoxicity risk with high-dose CPA)
• PSA — every 3 months to assess treatment response
• Testosterone — baseline and periodically
• Haematocrit — monitor for polycythaemia (rare at antiandrogen doses)
• Cardiovascular assessment — ADT increases cardiovascular risk

Full dosing guidelines available at Drugs.com Cyproterone Acetate.

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Who Should Use Andocur

Andocur is prescribed for:

Prostate Cancer:

• All men starting GnRH agonist therapy who require antiandrogen flare protection — particularly those with bone metastases, spinal involvement, or urinary obstruction
• Men on long-term ADT with significant hot flushes reducing quality of life — hot flush management
• Men with locally advanced prostate cancer requiring hormonal therapy where monotherapy is preferred
• Combined androgen blockade with GnRH agonist — in settings where next-generation ARSIs are not accessible

Severe Hypersexuality:

• Men with severe paraphilias or hypersexuality unresponsive to psychological therapy — where androgen suppression is clinically indicated

Andocur is prescribed by urologists, medical oncologists, and radiation oncologists. A.K. Pharma supplies Andocur to hospitals, oncology centres, urology clinics, and pharmacies across Delhi and India.

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Possible Side Effects

Common side effects in men include gynaecomastia and breast tenderness (most common — from peripheral oestrogen excess relative to androgens), hot flushes (paradoxically, though less severe than with GnRH agonists alone), decreased libido, erectile dysfunction, fatigue, and weight gain.

Serious side effects include:

Hepatotoxicity — Black Box Warning in Most Countries: Dose-dependent hepatotoxicity is the most important serious adverse effect — occurring predominantly at high doses (>200mg/day). Liver enzyme elevation, cholestatic jaundice, hepatitis, and rarely fatal hepatic necrosis have been reported — primarily with doses used in hypersexuality treatment rather than oncology doses. At lower doses (100mg/day for hot flushes, 100-200mg/day for flare cover), the hepatotoxicity risk is significantly lower but still requires monitoring. LFT monitoring at baseline and every 3 months is mandatory.

Cardiovascular Effects: Venous thromboembolic events (DVT, PE) — particularly at high doses. Combined with ADT-related cardiovascular risk — monitor cardiovascular risk factors throughout. Andocur is contraindicated in patients with prior VTE.

Adrenal Cortical Suppression: At high doses, mild glucocorticoid activity may suppress adrenal cortical function — patients undergoing significant physiological stress (surgery, major illness) may require temporary corticosteroid supplementation.

Meningioma: Long-term use of Cyproterone Acetate (typically at high doses in women for other indications) has been associated with increased risk of intracranial meningioma. Regulatory agencies in Europe have required updated labelling for this risk at high doses — less relevant at the doses used in prostate cancer flare prophylaxis and hot flush management but important for long-term high-dose monotherapy.

Full side effect information available through EMA Cyproterone Acetate Safety Information.

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Precautions

• Hepatotoxicity monitoring — mandatory LFTs at baseline and every 3 months; do not initiate if significant liver disease; discontinue if jaundice or LFT elevation >3× ULN
• VTE risk — contraindicated in patients with prior VTE; monitor for DVT/PE symptoms throughout treatment
• Meningioma — regular neurological review for long-term high-dose therapy; MRI if neurological symptoms develop; discontinue if meningioma diagnosed
• Cardiovascular monitoring — ADT increases cardiovascular risk; monitor blood pressure, blood glucose, lipids
• Not for use in women (in this oncology context) — Andocur is also used in women for other indications but with different dosing and different risk-benefit profile
• Diabetes mellitus — Andocur may affect carbohydrate metabolism; monitor blood glucose
• Adrenal stress precaution — patients on high-dose CPA undergoing surgery or major illness may need corticosteroid supplementation
• Refer to EAU Prostate Cancer Guidelines for complete management context

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Storage and Handling

• Store at room temperature below 25°C
• Keep in original packaging — protect from moisture and light
• Keep out of reach of children
• No cold chain required — straightforward oral tablet formulation

As a responsible medicine distributor in Delhi, A.K. Pharma stores all medicines including Andocur under manufacturer-recommended conditions ensuring product integrity for every supply.

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Manufacturer Information

Andocur (Cyproterone Acetate) is manufactured by Bayer AG, a global pharmaceutical and life sciences company. Cyproterone Acetate was developed by Bayer in the 1960s — one of the earliest antiandrogens synthesised and the first to enter clinical use. A.K. Pharma supplies only genuine Andocur sourced from authorized Bayer distributors.

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Related Prostate Cancer Medicines Available at A.K. Pharma

• Zoladex (Goserelin) — GnRH agonist — used with Andocur for flare cover and combined androgen blockade
• Firmagon (Degarelix) — GnRH antagonist — no testosterone flare; does not require antiandrogen cover
• Abirapro (Abiraterone) — CYP17 inhibitor — superior to CPA in mHSPC (LATITUDE trial)
• Glenza 160mg (Enzalutamide) — next-generation ARSI — superior to CPA in mCRPC and mHSPC
• Browse all Cancer Medicines available at A.K. Pharma

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Frequently Asked Questions

Q. What is Andocur used for? Andocur (Cyproterone Acetate) is used in prostate cancer for antiandrogen flare prophylaxis during GnRH agonist initiation, management of hot flushes in men receiving ADT, combined androgen blockade with GnRH agonists, and as monotherapy for locally advanced prostate cancer. It is also used for severe hypersexuality. More information available at Drugs.com.

Q. What is the generic name of Andocur? The generic name of Andocur is Cyproterone Acetate. It is a steroidal antiandrogen and progestogen — manufactured by Bayer — one of the oldest and most established antiandrogen medicines in prostate cancer management.

Q. What is testosterone flare and how does Andocur prevent it? When a GnRH agonist (such as Zoladex/Goserelin) is first administered, it causes a temporary surge in testosterone lasting 1-2 weeks before testosterone suppression occurs — this is called the testosterone flare. In patients with bone metastases, spinal cord involvement, or urinary obstruction, this testosterone surge can cause serious clinical deterioration. Andocur, started 3 days before the first GnRH agonist injection and continued for 4 weeks, blocks the androgen receptor at the tissue level — preventing the biological effects of the testosterone surge while the GnRH agonist establishes suppression.

Q. How effective is Andocur for hot flushes from ADT? Andocur 100mg/day (50mg twice daily) achieves 70-80% reduction in hot flush frequency and severity — making it one of the most effective pharmacological treatments for ADT-related hot flushes. Hot flushes affect 50-80% of men on long-term GnRH agonist therapy and significantly impair quality of life. Andocur provides evidence-based, highly effective symptom relief.

Q. How is Andocur different from newer antiandrogens like Enzalutamide (Glenza)? Andocur (Cyproterone Acetate) is a first-generation steroidal antiandrogen that partially blocks AR and also suppresses testosterone through central mechanisms. Glenza (Enzalutamide) is a next-generation ARSI that blocks AR at three levels with no agonist activity and significantly superior OS benefit in mCRPC and mHSPC. Andocur remains clinically valuable for flare prophylaxis, hot flush management, and in settings where next-generation ARSIs are not accessible, but Enzalutamide/Abiraterone have replaced CPA as the preferred combination partners in metastatic prostate cancer where OS benefit is the priority.

Q. Why does Andocur require liver function monitoring? Cyproterone Acetate — particularly at high doses — can cause dose-dependent hepatotoxicity including elevated liver enzymes, cholestatic hepatitis, and rarely fatal hepatic necrosis. Mandatory baseline LFTs and monitoring every 3 months throughout treatment are required. Patients should be advised to report any symptoms of liver disease (jaundice, dark urine, abdominal pain, nausea) immediately.

Q. Is Andocur available in India? Andocur can be supplied to hospitals, oncology centres, and pharmacies across India through licensed pharmaceutical distributors. Contact A.K. Pharma — medicine distributor in Delhi — for availability and pricing.

Q. What is the price of Andocur in India? Andocur price in India varies by strength (50mg or 100mg) and pack size. Contact A.K. Pharma at 011 4172 6999 or WhatsApp +91 9810034827 for current pricing and bulk supply rates.

Q. How to order Andocur from A.K. Pharma? You can request a quote directly from this page, call us at 011 4172 6999, or WhatsApp us at +91 9810034827 with your requirements and we will respond promptly.

Q. Does A.K. Pharma supply Andocur in bulk? Yes. A.K. Pharma supplies Andocur in bulk to oncology centres, urology clinics, hospitals, and pharmacies across Delhi and India. Contact us for bulk pricing and availability.

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Why Order Andocur from A.K. Pharma?

• Licensed medicine distributor in Delhi with all required drug licenses
• 100% genuine Andocur sourced from authorized Bayer distributors
• Both 50mg and 100mg tablet strengths available — complete dosing flexibility
• Available alongside companion prostate cancer medicines — Zoladex, Firmagon, Abirapro, Glenza
• Bulk supply available for hospitals and urology centres
• Prompt response to all quote requests
• Serving urologists and oncologists across Delhi NCR and India

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Contact A.K. Pharma for Andocur Supply 📍 E-2/257A, 2nd Floor, Shastri Nagar, New Delhi 110052 📞 011 4172 6999 📱 WhatsApp: +91 9810034827 🌐 akpharma.in