Description
Product details
Enzalutamide 40 mg capsules represent a breakthrough in targeted therapy for advanced prostate cancer, particularly in metastatic castration-resistant prostate cancer (mCRPC) and metastatic castration-sensitive prostate cancer (mCSPC). This second-generation androgen receptor inhibitor works by disrupting multiple steps in the androgen signaling pathway, offering patients a chance to slow disease progression, reduce tumor burden, and extend survival even after other treatments fail. Administered as a once-daily oral capsule, enzalutamide 40 mg provides four capsules per day (total 160 mg), making it convenient for long-term use in clinical settings where hormone therapy alone proves insufficient. Patients often turn to enzalutamide when facing rising PSA levels despite androgen deprivation therapy (ADT), experiencing bone pain, or dealing with cancer spread to lymph nodes or distant sites. Its high affinity for androgen receptors—5-8 times stronger than first-generation antiandrogens like bicalutamide—ensures potent blockade without agonist activity, translating to real-world benefits like delayed chemotherapy needs and improved quality of life during treatment. Product Use and Indications Enzalutamide 40 mg primarily treats metastatic castration-resistant prostate cancer (mCRPC) in patients previously treated with docetaxel or progressing despite ADT. The FDA and EMA approvals extend to non-metastatic CRPC (nmCRPC) with high-risk biochemical recurrence and metastatic castration-sensitive prostate cancer (mCSPC) alongside ADT, based on landmark trials like AFFIRM, PREVAIL, PROSPER, and ARCHES. Key uses include: Slowing tumor growth in hormone-refractory stages by inhibiting androgen-driven proliferation. Reducing skeletal-related events like fractures or spinal cord compression in bone metastases. Delaying progression to chemotherapy in pre-chemotherapy mCRPC, with PREVAIL showing 17-month median radiographic progression-free survival (rPFS) versus 4 months for placebo. In mCSPC, ARCHES trial data demonstrated 61% risk reduction in progression or death when combined with ADT. Clinicians monitor PSA response (≥50% decline in 70-80% of patients) and imaging every 3 months to assess efficacy. Mechanism of Action Enzalutamide 40 mg exerts a threefold blockade on androgen receptor (AR) signaling: it competitively inhibits androgen binding to AR (with affinity rivaling dihydrotestosterone), prevents nuclear translocation of the ligand-receptor complex, and disrupts DNA binding and coactivator recruitment at androgen response elements. This comprehensive inhibition downregulates oncogenes like TMPRSS2-ERG fusion genes common in prostate cancer, inducing apoptosis and halting cell proliferation without lowering systemic testosterone levels. Unlike earlier antiandrogens, enzalutamide avoids partial agonist effects, ensuring pure antagonism even in AR-overexpressing tumors. Its active metabolite, N-desmethyl enzalutamide (via CYP2C8), contributes 30% to activity, with steady-state levels achieved in 4 weeks. Key Benefits Extended Progression-Free Survival: In PREVAIL (pre-chemo mCRPC), median overall survival reached 32.4 months versus 30.2 for placebo; PROSPER (nmCRPC) delayed metastasis by 22 months. PSA Response and Tumor Shrinkage: 78% PSA90 response rate; radiographic responses in 29% with measurable disease. Quality of Life Preservation: Delays pain progression (hazard ratio 0.40) and chemotherapy (by 17 months), maintaining daily function. Bone Protection: Reduces fractures by 30% in high-risk patients via AR inhibition in osteoblasts. Combination Synergy: Enhances ADT efficacy in mCSPC, cutting death risk by 33% per ARCHES. These benefits position enzalutamide 40 mg as a cornerstone in modern prostate cancer protocols, especially for fit patients tolerating oral therapy. Side Effects Enzalutamide 40 mg carries a manageable profile, with most effects dose-related and reversible upon discontinuation. Common Side Effects Fatigue/Asthenia (34-50%): Often mild, peaking in first months; rest and nutrition help. Arthralgia/Myalgia (14-21%): Joint/muscle pain managed with NSAIDs. Hot Flashes (20%): Androgen blockade mimic; hydration aids. Headache/Dizziness (12-19%): Transient; avoid driving if severe. Hypertension (6-13%): Monitor BP monthly; antihypertensives as needed. GI Issues (diarrhea 12%, nausea 11%): Antiemetics support compliance. Serious Side Effects Seizures (0.9%): Highest risk in epileptics or brain mets; EEG baseline, avoid triggers. Posterior Reversible Encephalopathy (PRES): Rare (<0.1%); headache, confusion—MRI confirms. Falls/Fractures (15% increased risk): Due to weakness/falls; DEXA scans recommended. Cardiac Events (2-5%): MI/arrhythmias; ECG monitoring in CVD history. Hepatic Injury (1%): ALT/AST elevation; monthly labs first 3 months. Discontinuation occurs in 8-10%; supportive care mitigates most. Dosage and Administration Standard dose: 160 mg (four 40 mg capsules) once daily, with or without food. Swallow intact; no crushing. Adjust for CYP2A4 inducers (e.g., rifampin—increase to 240 mg) or strong inhibitors (reduce to 80 mg). Continue until progression/toxicity; no dose interruptions beyond 28 days without reassessment. Precautions and Monitoring Contraindicated in pregnancy (teratogenic; absolute contraception for men/ partners). Screen for seizure history; CYP2C8/3A4 interactions (e.g., ketoconazole). Baseline LFTs, PSA, testosterone; imaging q8-12 weeks. Elderly (>75) monitor falls. Conclusion Enzalutamide 40 mg stands as a transformative therapy, empowering prostate cancer patients with prolonged control over aggressive disease through precise AR inhibition. Balancing robust efficacy—evidenced by landmark trials delaying metastasis and death—with proactive side effect management, it enhances survival and daily living. Patients achieve meaningful milestones, from family events to travel, underscoring its role in personalized oncology. Consult oncologists for integration into care plans, ensuring optimal outcomes in this challenging journey. Email: info@sterispharma.com / contact@sterispharma.com Call/WhatsApp: 7877551268, 7849827488
