Glenza® (Enzalutamide) — Next-Generation Androgen Receptor Inhibitor for Prostate Cancer

The Most Broadly Approved ARSI — Proven Survival Benefit Across the Full Prostate Cancer Continuum

Glenza® (Enzalutamide) is a potent next-generation androgen receptor signalling inhibitor (ARSI) that inhibits multiple critical steps in the androgen receptor (AR) signalling pathway — competitively blocking androgen binding to AR, inhibiting AR nuclear translocation, and preventing AR-DNA binding and transcriptional activation. Unlike first-generation antiandrogens (Bicalutamide, Flutamide) which act only as competitive AR antagonists and can exhibit partial agonist activity in castration-resistant settings, Enzalutamide provides comprehensive AR pathway inhibition across all three key AR signalling steps — delivering more complete androgen receptor blockade with no reported agonist activity.

Glenza is approved for the broadest range of prostate cancer settings of any ARSI — metastatic castration-resistant prostate cancer (mCRPC) in both chemotherapy-naive and post-Docetaxel settings, metastatic hormone-sensitive prostate cancer (mHSPC) in combination with ADT, and non-metastatic castration-resistant prostate cancer (nmCRPC) with high PSA doubling time — making it the most versatile androgen receptor inhibitor available and an essential medicine across the entire prostate cancer treatment continuum.

A.K. Pharma is a trusted medicine distributor in Delhi supplying genuine Glenza (Enzalutamide) in both 40mg and 160mg capsule strengths to hospitals, oncology centres, urology clinics, and pharmacies across India. Glenza contains Enzalutamide — the same active ingredient as the originator Xtandi — available at accessible pricing for Indian patients requiring ARSI therapy.

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What is Glenza (Enzalutamide)?

Glenza contains Enzalutamide — a diarylthiohydantoin small molecule that acts as a pure androgen receptor antagonist with inhibitory activity at multiple points in the AR signalling cascade.

Why AR Signalling Inhibition Beyond Simple Competitive Blockade Is Critical:

In hormone-sensitive prostate cancer, testosterone drives AR activation → prostate cancer cell growth. Standard ADT (castration) reduces testosterone to castration levels — initially controlling disease. However, prostate cancer cells develop mechanisms to reactivate AR signalling despite castration:

• AR gene amplification — more AR protein expressed → more sensitive to low testosterone levels
• AR ligand-binding domain mutations — altered AR can be activated by weak androgens or even antiandrogens (first-generation ARSI agonism)
• Intratumoral androgen synthesis — tumour cells synthesise their own androgens from adrenal precursors — driving AR activation independently of systemic testosterone
• AR splice variants (AR-V7) — constitutively active AR variants that lack the ligand-binding domain and are independent of ligand

Enzalutamide was specifically engineered to overcome these resistance mechanisms — with 5-8x greater AR binding affinity than Bicalutamide, no agonist activity, and inhibition of downstream AR signalling steps beyond simple competitive binding.

Enzalutamide’s Three-Step AR Inhibition:

1. Androgen binding inhibition — Enzalutamide binds to the AR ligand-binding domain with high affinity — competitively blocking testosterone and DHT binding — preventing AR activation
2. Nuclear translocation inhibition — Enzalutamide-bound AR cannot translocate from cytoplasm to nucleus — blocking AR’s transcriptional activity
3. DNA binding inhibition — even if some AR reaches the nucleus, Enzalutamide prevents AR from binding to androgen response elements (AREs) in DNA — blocking transcription of AR target genes driving cell proliferation and survival

Full prescribing information is available at the FDA label for Enzalutamide.

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Clinical Studies and Evidence

AFFIRM Trial (Enzalutamide Post-Docetaxel mCRPC) Published in the New England Journal of Medicine (2012), the landmark AFFIRM trial enrolled 1,199 patients with mCRPC who had progressed after Docetaxel chemotherapy — comparing Enzalutamide vs placebo. Key results:

• Overall survival — median OS 18.4 months (Enzalutamide) vs 13.6 months (placebo) — HR 0.63 — significantly improved — 37% reduction in risk of death
• PSA response (≥50% decline) — 54% vs 2%
• Objective response rate — 29% vs 4%
• Time to PSA progression — 8.3 months vs 3.0 months
• Radiographic PFS — 8.3 months vs 2.9 months
• Established Enzalutamide as a new standard of care in post-chemotherapy mCRPC — one of the most impactful prostate cancer trials ever conducted

PREVAIL Trial (Enzalutamide Chemotherapy-Naive mCRPC) Published in the New England Journal of Medicine (2014), the PREVAIL trial enrolled 1,717 asymptomatic or mildly symptomatic chemotherapy-naive mCRPC patients — comparing Enzalutamide vs placebo. Key results at updated analysis:

• Overall survival — median OS 32.4 months (Enzalutamide) vs 30.2 months (placebo) — HR 0.71 — significantly improved
• Radiographic PFS — median not reached (Enzalutamide) vs 3.9 months (placebo) — HR 0.19 — dramatically superior
• PSA response — 78% vs 3%
• Time to chemotherapy initiation — significantly delayed — 28.0 months vs 10.8 months
• Established Enzalutamide in pre-chemotherapy mCRPC — significantly delaying disease progression and chemotherapy initiation

ARCHES Trial (Enzalutamide + ADT in Metastatic Hormone-Sensitive Prostate Cancer) Published in the Journal of Clinical Oncology (2019) with updated OS data, the ARCHES trial enrolled 1,150 patients with mHSPC — comparing Enzalutamide + ADT vs placebo + ADT. Key results at OS analysis:

• Overall survival — significantly improved with Enzalutamide + ADT — HR 0.66 — 34% reduction in risk of death
• Radiographic PFS — median not reached (Enzalutamide + ADT) vs 19.0 months (ADT alone) — HR 0.39 — significantly superior
• PSA undetectable (<0.2 ng/mL) — 70% vs 15%
• Established Enzalutamide + ADT as a standard of care for mHSPC — one of the most effective regimens in hormone-sensitive prostate cancer

ENZAMET Trial (Enzalutamide + ADT in mHSPC — Including Docetaxel-Eligible) Published in the New England Journal of Medicine (2019) with OS update published in The Lancet Oncology (2023), the ENZAMET trial demonstrated:

• Overall survival — significantly improved with Enzalutamide + ADT — HR 0.70 — benefit maintained at 5-year follow-up with 5-year OS 57% vs 45%
• Demonstrated durable long-term OS benefit even in patients who also received Docetaxel — confirming Enzalutamide’s additive benefit beyond chemotherapy

PROSPER Trial (Enzalutamide in Non-Metastatic CRPC) Published in the New England Journal of Medicine (2018), the PROSPER trial enrolled 1,401 patients with nmCRPC and PSA doubling time ≤10 months — comparing Enzalutamide vs placebo + ongoing ADT. Key results:

• Metastasis-free survival (MFS) — median MFS 36.6 months (Enzalutamide) vs 14.7 months (placebo) — HR 0.29 — dramatically superior — 21.9-month improvement in MFS
• Overall survival — significantly improved — HR 0.73
• Established Enzalutamide as the standard of care for high-risk nmCRPC with PSA doubling time ≤10 months — preventing or significantly delaying metastatic progression

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Available Strengths

Glenza is available in the following presentations:

Standard dose: 160mg orally once daily — with or without food.

Both strengths are available from A.K. Pharma — the 160mg capsule provides a convenient single-capsule daily dose while the 40mg capsules provide flexibility for dose reductions (120mg = three 40mg capsules; 80mg = two 40mg capsules).

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Indications — What Glenza is Used For

Metastatic Castration-Resistant Prostate Cancer (mCRPC):

• In patients who have received prior Docetaxel chemotherapy (AFFIRM trial)
• In chemotherapy-naive patients (PREVAIL trial)
• Always in combination with ongoing castration (ADT or bilateral orchiectomy)

Metastatic Hormone-Sensitive Prostate Cancer (mHSPC):

• In combination with ADT for newly diagnosed metastatic HSPC (ARCHES and ENZAMET trials)
• One of the standard of care options for mHSPC alongside Abiraterone + Prednisone and Docetaxel

Non-Metastatic Castration-Resistant Prostate Cancer (nmCRPC):

• For patients with nmCRPC and PSA doubling time ≤10 months — the high-risk subset most likely to develop metastases rapidly
• Significantly delays metastatic progression — median MFS improvement of nearly 22 months vs placebo

For detailed indication information refer to MedlinePlus Enzalutamide.

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Key Benefits of Glenza

Three-Step AR Pathway Inhibition — No Partial Agonism Unlike first-generation antiandrogens that can exhibit partial agonist activity in the CRPC setting (driving tumour growth rather than inhibiting it), Enzalutamide is a pure antagonist at all AR signalling steps — no agonism even in the context of AR amplification, AR mutations, or low androgen environments. This pure antagonist profile is essential in the CRPC setting where first-generation antiandrogens fail.

Proven OS Benefit Across Three Major Prostate Cancer Settings Enzalutamide demonstrates significant overall survival benefit in mCRPC post-chemotherapy (AFFIRM), chemotherapy-naive mCRPC (PREVAIL), mHSPC (ARCHES/ENZAMET), and nmCRPC (PROSPER) — OS benefit across four major prostate cancer trial settings is unique among ARSIs.

Dramatic Metastasis-Free Survival Improvement in nmCRPC The PROSPER trial demonstrates a 21.9-month improvement in median MFS in nmCRPC — nearly tripling the MFS from 14.7 to 36.6 months. For patients with rising PSA on ADT without visible metastases, Enzalutamide provides the most robust delay in metastatic progression of any approved therapy.

No Corticosteroid Requirement Unlike Abirapro (Abiraterone) which requires mandatory Prednisone co-administration to prevent mineralocorticoid excess, Enzalutamide does not require routine corticosteroid co-administration — simplifying treatment, reducing polypharmacy, and avoiding corticosteroid-related side effects.

No Food Restriction Enzalutamide can be taken with or without food — eliminating the strict empty stomach requirement of Abiraterone and reducing the risk of dosing errors.

Convenient Once-Daily Oral Dosing Once-daily oral capsule therapy — 1 capsule (160mg) or 4 capsules (4 × 40mg) per day — maintains patient independence and quality of life without the need for regular clinical visits for parenteral therapy.

Single-Capsule 160mg Formulation Available The 160mg single capsule formulation provides the complete daily dose in one capsule — dramatically improving convenience and adherence compared to the four-capsule 40mg dosing.

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How Glenza Works — Androgen Receptor Signalling in Prostate Cancer

Normal AR Signalling in Prostate Cells:

1. Testosterone and DHT diffuse into prostate cell cytoplasm
2. Androgens bind to AR in cytoplasm → conformational change → AR activation
3. AR-androgen complex dimerises → translocates to nucleus
4. AR dimers bind to androgen response elements (AREs) in DNA
5. Coactivators recruited → transcription of AR target genes (PSA, TMPRSS2, SLC45A3, etc.)
6. AR target genes drive cell proliferation, survival, and differentiation

CRPC — How Prostate Cancer Escapes ADT:

• ADT reduces testosterone to castration levels — but AR signalling is reactivated through amplification, mutations, intratumoral synthesis, splice variants
• First-generation antiandrogens competitively block AR at step 2 (androgen binding) — but partial agonism and insufficient AR binding affinity allow escape
• Enzalutamide overcomes these mechanisms through superior binding affinity and multi-step inhibition

Enzalutamide’s Mechanism:

Step 1 — Competitive AR Binding: Enzalutamide binds to the androgen-binding domain of AR with 5-8x higher affinity than Bicalutamide — competitively blocking testosterone and DHT from binding. Pure antagonist — no partial agonism even in the context of AR amplification or overexpression.

Step 2 — Nuclear Translocation Inhibition: Enzalutamide-bound AR cannot undergo the conformational changes required for nuclear localisation signal exposure — AR remains sequestered in the cytoplasm by heat shock proteins — preventing nuclear entry and transcriptional activity.

Step 3 — DNA Binding Inhibition: If any AR reaches the nucleus despite step 2 inhibition — Enzalutamide prevents AR from binding to androgen response elements — blocking transcription of AR target genes driving proliferation and survival.

Step 4 — Downstream Effects: Without AR-driven transcription:

• PSA production falls → PSA response
• Cell cycle progression genes (cyclin D1, etc.) are not activated → cell cycle arrest
• Survival genes (BCL-2, etc.) are not upregulated → increased apoptosis sensitivity
• TMPRSS2-ERG fusion oncogene expression reduced in fusion-positive tumours

For detailed mechanism overview refer to EAU Prostate Cancer Guidelines and NCCN Prostate Cancer Guidelines.

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Glenza vs Abirapro — Key Comparison in Prostate Cancer

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Dosage and Administration

All Indications — Standard Dose:

• 160mg orally once daily — with or without food
• Take at approximately the same time each day
• Swallow capsules whole — do not open, dissolve, or chew
• Continue ongoing ADT (GnRH agonist/antagonist or surgical castration) throughout Glenza treatment

Dose Reduction for Toxicity:

• First reduction: 120mg once daily (three 40mg capsules)
• Second reduction: 80mg once daily (two 40mg capsules)
• If 80mg not tolerated — consider discontinuation

Duration:

• mCRPC: Until disease progression or unacceptable toxicity
• mHSPC: Until disease progression or unacceptable toxicity
• nmCRPC: Until disease progression or unacceptable toxicity

Missed Dose:

• If a dose is missed — take it as soon as possible on the same day. Return to normal dosing schedule the next day. Do not take two doses on the same day

Monitoring:

• Seizure assessment at baseline — assess risk factors before starting
• Blood pressure — ADT + ARSI combination increases cardiovascular risk
• Fasting blood glucose and HbA1c — metabolic monitoring throughout
• PSA — every 3 months to assess treatment response
• Bone mineral density — DEXA scan at baseline and annually (long-term ADT + ARSI causes bone loss)
• Cardiovascular risk factor assessment throughout

Full dosing guidelines available at Drugs.com Enzalutamide Dosage.

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Treatment Sequencing — Glenza in the Prostate Cancer Treatment Algorithm

Newly Diagnosed mHSPC (High-Risk or High-Volume):

• Glenza + ADT — standard of care (ARCHES/ENZAMET)
• Alternative: Abirapro + Prednisone + ADT (LATITUDE)
• Note: Glenza + Abirapro combination not recommended — overlapping AR pathway inhibition without proven additive benefit and increased toxicity

nmCRPC (Rising PSA on ADT, PSA DT ≤10 months, No Metastases on Imaging):

• Glenza is the preferred ARSI for nmCRPC — dramatic MFS benefit (PROSPER)
• Continue until metastases detected → transition to mCRPC algorithm

mCRPC (First-Line — Pre-Chemotherapy):

• Glenza monotherapy (PREVAIL) — if not previously used in mHSPC
• If Glenza was used in mHSPC and progressed → Abirapro (Abiraterone) has limited cross-resistance activity; Pivikto (Lutetium-177 PSMA) is emerging as preferred subsequent therapy in PSMA-positive patients

mCRPC (Post-Docetaxel):

• Glenza (AFFIRM) — standard option post-chemotherapy if not previously used as ARSI

After Glenza Progression in mCRPC:

• Pivikto (Lutetium-177 PSMA) — VISION trial — for PSMA-positive mCRPC after prior ARSI and chemotherapy — preferred subsequent therapy
• Abirapro (Abiraterone) — reduced but some activity after Enzalutamide progression
• Docetaxel or Cabazitaxel chemotherapy

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Who Should Use Glenza

Glenza is prescribed for:

• Men with mCRPC — pre and post-Docetaxel — who have not previously received Enzalutamide
• Men with newly diagnosed mHSPC — in combination with ADT — particularly high-volume or high-risk disease
• Men with nmCRPC and PSA doubling time ≤10 months — high-risk of rapid metastatic progression
• Patients where corticosteroid avoidance is preferred (vs Abiraterone)
• Patients where simplified oral dosing without food restrictions is preferred

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

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Possible Side Effects

Common side effects include fatigue (51%), back pain (29%), decreased appetite (19%), constipation (23%), arthralgia (20%), diarrhoea (17%), hot flushes (20%), upper respiratory tract infection (11%), hypertension (14%), and peripheral oedema (15%).

Serious side effects include:

Seizures: Seizures occurred in 0.9% of patients in AFFIRM — Enzalutamide lowers the seizure threshold. Do not use in patients with history of seizure, predisposing factors for seizure, or concomitant medications that lower seizure threshold. Permanently discontinue if seizure occurs during treatment.

Posterior Reversible Encephalopathy Syndrome (PRES): Rare cases reported — confirm with MRI if suspected; permanently discontinue.

Cardiovascular Events: Ischaemic heart disease and ischaemic cerebrovascular events — monitor cardiovascular risk factors throughout treatment. ADT + ARSI combination increases overall cardiovascular risk.

Falls and Fractures: Increased risk of falls (4.6%) and fractures (8.8%) — particularly in elderly patients and those with pre-existing bone loss from long-term ADT. Monitor bone mineral density and consider bone-protective therapy.

Embryo-Foetal Toxicity: Enzalutamide can cause foetal harm — relevant for male patients with female partners of reproductive potential — effective contraception required.

Full side effect information available at FDA Enzalutamide Safety Information.

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Precautions

• Seizure risk — contraindicated in patients with history of seizures or significant predisposing factors; permanently discontinue if seizure occurs during treatment
• CYP2C8 inhibitors — strong CYP2C8 inhibitors (e.g. gemfibrozil) significantly increase Enzalutamide exposure — avoid or reduce dose to 80mg daily if unavoidable
• Strong CYP3A4 and CYP2C8 inducers — rifampicin significantly reduces Enzalutamide levels; avoid concomitant use
• Enzalutamide is a strong CYP3A4 inducer — reduces plasma levels of many co-administered drugs including warfarin, statins, immunosuppressants — review all concomitant medications
• QT prolongation — Enzalutamide may cause QT prolongation — use with caution with other QT-prolonging medicines
• Bone protection — long-term ADT + ARSI causes bone mineral density loss — DEXA scan monitoring and consider Denosumab (Prolia/Xgeva) or bisphosphonate
• Falls prevention — particularly important in elderly patients
• Metabolic monitoring — ADT-related metabolic syndrome; monitor glucose, lipids, blood pressure
• Refer to EAU Prostate Cancer Guidelines for complete management context

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Storage and Handling

• Store at room temperature below 30°C
• Keep in original packaging — protect from moisture and light
• Keep out of reach of children
• No special temperature requirements — straightforward oral capsule formulation

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

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Manufacturer Information

Glenza (Enzalutamide) contains the same active ingredient as the originator Xtandi — originally developed by Medivation Inc (now Pfizer) and Astellas Pharma. Enzalutamide received FDA approval in August 2012 for post-chemotherapy mCRPC — with subsequent approvals for pre-chemotherapy mCRPC (2014), nmCRPC (2018), and mHSPC (2019). A.K. Pharma supplies only genuine Glenza sourced from authorised distributors.

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Related Prostate Cancer Medicines Available at A.K. Pharma

• Abirapro (Abiraterone Acetate) — CYP17 inhibitor for mCRPC and mHSPC
• Firmagon (Degarelix) — GnRH antagonist ADT — no testosterone flare
• Zoladex (Goserelin) — GnRH agonist ADT
• Pivikto (Lutetium-177 PSMA) — PSMA radioligand therapy for mCRPC post-ARSI
• Browse all Cancer Medicines available at A.K. Pharma

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Frequently Asked Questions

Q. What is Glenza used for? Glenza (Enzalutamide) is used to treat metastatic castration-resistant prostate cancer (mCRPC) — both pre and post-chemotherapy — metastatic hormone-sensitive prostate cancer (mHSPC) in combination with ADT, and non-metastatic castration-resistant prostate cancer (nmCRPC) with high PSA doubling time risk. More information available at MedlinePlus.

Q. What is the generic name of Glenza? The generic name of Glenza is Enzalutamide. It is a next-generation androgen receptor signalling inhibitor (ARSI) — the same active ingredient as the originator Xtandi.

Q. How is Glenza different from Abirapro (Abiraterone)? Glenza (Enzalutamide) inhibits the androgen receptor — blocking AR at three steps. Abirapro (Abiraterone) inhibits CYP17A1 — blocking androgen synthesis. Key practical differences: Glenza does not require corticosteroids or food restrictions while Abiraterone requires mandatory Prednisone and empty stomach dosing. Both have similar OS efficacy in mCRPC and mHSPC. Glenza is additionally approved for nmCRPC.

Q. What strengths of Glenza are available? A.K. Pharma supplies both 40mg and 160mg capsule strengths. The standard daily dose is 160mg — one 160mg capsule or four 40mg capsules once daily. The 40mg capsules enable dose reductions to 120mg (three capsules) or 80mg (two capsules) for toxicity management.

Q. Does Glenza cause seizures? Enzalutamide has been associated with seizures in approximately 0.9% of patients — it lowers the seizure threshold. Glenza is contraindicated in patients with a history of seizures or significant predisposing factors. Permanently discontinue if a seizure occurs during treatment. Careful benefit-risk assessment is required in patients at risk.

Q. Can Glenza be used for hormone-sensitive prostate cancer? Yes — Glenza + ADT is approved for metastatic hormone-sensitive prostate cancer based on the ARCHES and ENZAMET trials which demonstrated significant OS benefit — 34% reduction in risk of death. It is one of the standard of care options for mHSPC alongside Abiraterone + Prednisone + ADT.

Q. Is Glenza available in India? Glenza 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 Glenza in India? Glenza price in India varies by strength 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 Glenza 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 Glenza in bulk? Yes. A.K. Pharma supplies Glenza 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 Glenza from A.K. Pharma?

• Licensed medicine distributor in Delhi with all required drug licenses
• 100% genuine Glenza sourced from authorised distributors
• Both 40mg and 160mg capsule strengths available — complete dose management
• Available alongside the full prostate cancer medicine portfolio — Abirapro, Firmagon, Zoladex, Pivikto
• Bulk supply available for hospitals and oncology 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 Glenza Supply 📍 E-2/257A, 2nd Floor, Shastri Nagar, New Delhi 110052 📞 011 4172 6999 📱 WhatsApp: +91 9810034827 🌐 akpharma.in