Enzalutamide (Xtandi®): A Comprehensive Clinical and Pharmacological Monograph

Section 1: Introduction and Overview

Executive Summary

Enzalutamide is a pivotal second-generation, nonsteroidal antiandrogen (NSAA) that has fundamentally altered the therapeutic paradigm for patients with advanced prostate cancer.[1] As a potent and highly specific androgen receptor (AR) signaling inhibitor, its mechanism of action is multifaceted, involving the blockade of androgen binding, prevention of AR nuclear translocation, and impairment of AR-DNA interaction.[1] This comprehensive inhibition of the primary oncogenic driver in prostate cancer has translated into remarkable clinical efficacy across a broad spectrum of disease states. Enzalutamide has demonstrated significant improvements in survival and delayed disease progression in metastatic and non-metastatic settings, as well as in both castration-sensitive and castration-resistant prostate cancer.[1] Marketed under the brand name Xtandi®, it is recognized as a cornerstone therapy, typically administered orally once daily in conjunction with androgen deprivation therapy (ADT).[1] Its clinical utility is, however, balanced by a distinct and significant safety profile characterized by fatigue, cardiovascular events, and an increased risk of falls and fractures, which necessitates proactive and vigilant clinical management.[5]

Classification and Significance