1. Clinical & Scientific Overview
Enzalutamide (TIP-MED-000568, Reference Code [ONC-19]) is classified under
Oncology & Antineoplastic Medicines as a Hormonal Oncology Therapy (Antiandrogen) • Second-Generation Non-Steroidal Androgen Receptor Signalling Inhibitor (ARSI).
Within the Indian regulatory and compendial framework, it is governed under Schedule H (Prescription Only — Specialist Oncology Supervision).
Xtandi (Astellas Pharma India), Bdenza (BDR Pharmaceuticals), Enzamide (Cipla Ltd)
Soft Capsule / Film-Coated Tablet: 40 mg, 80 mg
Oncology Specialisation & Cytotoxic Safety Protocol
Hormonal Oncology Therapy (Antiandrogen)
Antineoplastic Hormonal Agent
Standard Regimen & Cycle Context: 160 mg (four 40 mg capsules or two 80 mg tablets) orally once daily with or without food (continue concurrent GnRH analogue or bilateral orchidectomy).
Signature Dose-Limiting Toxicities & Organ Monitoring: Profound central fatigue/asthenia, hypertension, falls and fractures, ischaemic heart disease, and central GABA-A antagonism triggering generalized seizures (0.5–2% — higher in patients with brain metastases, prior stroke, or seizure threshold-lowering medications); potent CYP3A4, CYP2C9, and CYP2C19 inducer.
Extravasation, Premedication & Safe Cytotoxic Handling: Screen for seizure history and conduct comprehensive drug interaction reconciliation (enzalutamide strongly induces CYP3A4 and CYP2C9, slashing plasma levels of apixaban, rivaroxaban, warfarin, and fentanyl).
3. Mechanism of Action & Pharmacodynamics
Triple-stage androgen receptor blockade: competitively inhibits androgen binding to the AR, blocks nuclear translocation of the activated AR complex, and prevents AR binding to DNA androgen response elements.
4. Therapeutic Indications & Evidence-Supported Uses
- Metastatic Castration-Sensitive (mCSPC), Non-Metastatic Castration-Resistant (nmCRPC), and Metastatic Castration-Resistant Prostate Cancer (mCRPC)
🇮🇳 Jurisdiction & Indication Note: Indications and schedules reflect Indian compendial and regulatory records (CDSCO / Indian Pharmacopoeia & NFI / NLEM 2022). Where international reference labels (US FDA DailyMed / NCBI StatPearls) are cited for pharmacokinetic or mechanistic parameters, international approvals do not automatically imply CDSCO approval in India.
5. Educational Dosage Context, Formulations & Administration
Educational Dosing & Regimen Summary: Educational Oncology Regimen Context (Specialist Reference Only): 160 mg (four 40 mg capsules or two 80 mg tablets) orally once daily with or without food (continue concurrent GnRH analogue or bilateral orchidectomy).
Administration & Meal Timing: 160 mg (four 40 mg capsules or two 80 mg tablets) orally once daily with or without food (continue concurrent GnRH analogue or bilateral orchidectomy).
6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment
Specialist oncology pharmacokinetic profile; dosing depends on Body Surface Area (BSA in m2), Calvert GFR formula, or flat targeted dosing with strict organ-function adjustments.
Hepatic enzymatic activation/inactivation or proteolytic degradation (for monoclonal antibodies); see specific polymorphism and interaction notes.
Verify serum creatinine and eGFR before every cycle; see drug-specific renal dosing and uroprotection rules.
Check total bilirubin, AST, and ALT prior to each cycle; taxanes, anthracyclines, and TKIs require strict hepatic dose modification.
7. Contraindications, Precautions & High-Risk Warnings
- Severe hypersensitivity to Enzalutamide or formulation vehicle
- Pregnancy and lactation (potent teratogen/embryotoxic class warning unless explicitly evaluated by oncology specialist)
- Severe unrecovered bone marrow aplasia or decompensated organ failure per protocol thresholds
Key Clinical Precautions: Profound central fatigue/asthenia, hypertension, falls and fractures, ischaemic heart disease, and central GABA-A antagonism triggering generalized seizures (0.5–2% — higher in patients with brain metastases, prior stroke, or seizure threshold-lowering medications); potent CYP3A4, CYP2C9, and CYP2C19 inducer.
8. Adverse Effects Profile
- Profound central fatigue/asthenia, hypertension, falls and fractures, ischaemic heart disease, and central GABA-A antagonism triggering generalized seizures (0.5–2% — higher in patients with brain metastases, prior stroke, or seizure threshold-lowering medications); potent CYP3A4, CYP2C9, and CYP2C19 inducer.
- Profound central fatigue/asthenia, hypertension, falls and fractures, ischaemic heart disease, and central GABA-A antagonism triggering generalized seizures (0.5–2% — higher in patients with brain metastases, prior stroke, or seizure threshold-lowering medications); potent CYP3A4, CYP2C9, and CYP2C19 inducer.
9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions
- Profound central fatigue/asthenia, hypertension, falls and fractures, ischaemic heart disease, and central GABA-A antagonism triggering generalized seizures (0.5–2% — higher in patients with brain metastases, prior stroke, or seizure threshold-lowering medications); potent CYP3A4, CYP2C9, and CYP2C19 inducer.
- Avoid live-attenuated vaccines during immunosuppressive chemotherapy; verify CYP3A4, UGT1A1, DPD, and QTc interactions before each cycle.
10. Clinical Monitoring, Patient Counselling & Storage
Clinical & Laboratory Monitoring: Screen for seizure history and conduct comprehensive drug interaction reconciliation (enzalutamide strongly induces CYP3A4 and CYP2C9, slashing plasma levels of apixaban, rivaroxaban, warfarin, and fentanyl).
Pharmacist Patient Counselling Points:
- Screen for seizure history and conduct comprehensive drug interaction reconciliation (enzalutamide strongly induces CYP3A4 and CYP2C9, slashing plasma levels of apixaban, rivaroxaban, warfarin, and fentanyl).
- Report fever >=38.0°C (100.4°F) immediately (medical emergency: possible febrile neutropenia).
- Follow strict reproductive contraception and safe cytotoxic oral handling instructions.
Storage, Stability & Dispensing Safeguards: Screen for seizure history and conduct comprehensive drug interaction reconciliation (enzalutamide strongly induces CYP3A4 and CYP2C9, slashing plasma levels of apixaban, rivaroxaban, warfarin, and fentanyl).
11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)
12. Authoritative References, Regulatory Sources & Editorial Disclaimer
Primary Compendial & Guideline Reference: National Cancer Grid (NCG) India Consensus Guidelines; NLEM 2022 Antineoplastic Section; Indian Pharmacopoeia (IP) & CDSCO Approved Oncology Prescribing Information.
Official Verification Portals: National Cancer Grid (NCG) India — Evidence-Based Oncology Guidelines • CDSCO — Central Drugs Standard Control Organization Approved Drug Data • Indian Pharmacopoeia Commission (IPC)
Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: VERIFIED_EDUCATIONAL_CONTENT
Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.
13. Related Reference Monographs, Educational Guides & Visual Concept
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