EnzalutamideEdit
Enzalutamide is a modern, oral antiandrogen used in the treatment of prostate cancer. Sold under the brand name Xtandi, it is a member of the second generation of androgen receptor pathway inhibitors. By binding to the androgen receptor with high affinity, enzalutamide interferes with signaling that drives the growth of many prostate cancers. In clinical practice, it is most commonly employed for metastatic castration-resistant prostate cancer (mCRPC) after progression on androgen deprivation therapy, and it is also approved for non-metastatic castration-resistant disease in several jurisdictions. In some settings, it is used in combination with androgen deprivation therapy for certain metastatic hormone-sensitive cases. Prostate cancer Androgen receptor Androgen deprivation therapy Xtandi
Enzalutamide’s mechanism of action centers on the androgen receptor (AR) signaling axis, which remains a key driver of prostate cancer biology even after traditional hormonal approaches. Unlike earlier antiandrogens, enzalutamide binds AR with greater affinity and prevents several steps in the signaling cascade: it blocks AR translocation into the nucleus, inhibits binding to DNA at androgen response elements, and reduces recruitment of transcriptional coactivators. The net effect is a substantial suppression of AR-driven gene expression, which translates into slowed tumor growth and, in many cases, clinical benefit in patients whose disease has progressed on conventional therapies. Androgen receptor Prostate cancer treatment Hormone therapy AR signaling
Medical uses and clinical context - Metastatic castration-resistant prostate cancer (mCRPC): Enzalutamide is widely used in patients whose disease has progressed following androgen deprivation therapy and, in many guidelines, after prior chemotherapy options. It is one of several AR-directed therapies that aim to delay disease progression and improve symptoms. Prostate cancer mCRPC - Non-metastatic castration-resistant prostate cancer: In appropriate patients, enzalutamide provides another line of defense against disease progression in the absence of detectable metastases. Non-metastatic CRPC - Metastatic hormone-sensitive disease: In some healthcare settings, enzalutamide is employed in combination with androgen deprivation therapy for selected patients with newly diagnosed metastatic disease, reflecting a broader strategy to curb AR signaling early in the disease course. Hormone-sensitive prostate cancer AR-targeted therapy
Administration, pharmacology, and interactions Enzalutamide is an oral medication with a relatively long half-life, allowing for daily dosing in most regimens. It is metabolized primarily in the liver, notably via cytochrome P450 enzymes, and it can influence the metabolism of other drugs that share these pathways. Clinicians pay particular attention to potential drug–drug interactions, as enzalutamide can induce several metabolic enzymes and may alter the blood levels of concurrent medications. Patients receiving anticoagulants, anticonvulsants, or other drugs that rely on hepatic metabolism require careful monitoring and, where appropriate, dose adjustments. Pharmacology Cytochrome P450 Drug interactions Anticoagulants
Side effects, safety, and risk profile Common adverse effects associated with enzalutamide include fatigue, dizziness, hot flashes, back pain, and hypertension. Some patients experience falls or edema, while others report reduced appetite or weight changes. A notable safety consideration is the risk of seizures, which has led to boxed warnings in regulatory documents and careful patient selection in clinical practice. Liver test abnormalities and rare hepatotoxicity have also been observed in some individuals. As with other cancer therapies, the safety profile must be weighed against expected benefits on a patient-by-patient basis. Seizure Adverse effects Hepatotoxicity Prostate cancer treatment
Economic and access considerations The cost of novel oncology drugs, including enzalutamide, is a central issue in healthcare policy and patient access. Supporters of market-based pricing argue that competition, private insurance coverage, and value-based assessments help ensure innovative therapies reach patients who can benefit, while encouraging ongoing research and development. Critics emphasize affordability, potential budget impact on health systems, and the importance of cost-effectiveness analyses to guide allocation of limited resources. Access programs, patient assistance plans, and generics (where applicable) influence real-world availability and adherence. Healthcare economics Drug pricing Access to medicines Xtandi
Controversies and debates - Pricing and value: The price of new cancer drugs often triggers public and political debate about whether the benefits justify the cost, and how best to balance patient access with incentives for innovation. Proponents contend that AR-targeted therapies have transformed outcomes for a subset of men with advanced disease, while opponents call for greater transparency, value-based pricing, and broader affordability measures. - Sequencing and combination strategies: In a landscape with multiple AR-directed agents (including apalutamide and abiraterone), questions arise about optimal sequencing, combination regimens, and sequencing with chemotherapy. Advocates for flexible strategies argue that personalizing therapy to patient risk, comorbidity, and preferences yields better real-world outcomes, while critics worry about escalating costs and complexity of care. - Safety and quality of life: As with other potent systemic therapies, managing side effects and preserving quality of life is a central concern. Critics of aggressive treatment approaches emphasize patient-centered goals and balanced risk management, while supporters argue that delaying progression and extending life are appropriate objectives when carefully monitored. The seizure risk, in particular, frames careful patient selection and counseling as essential components of responsible use. Quality of life Seizure
See also - Prostate cancer - Androgen receptor - Androgen deprivation therapy - Xtandi - Apalutamide - Abiraterone - Chemotherapy