Pharmacological Review on Enzalutamide

Abstract

A key therapeutic option in the treatment of prostate cancer, especially metastatic castration-resistant prostate cancer (mCRPC), is enzalutamide, a second-generation anti androgen drug. Enzalutamide was developed and approved by the FDA in 2012 following its discovery by Charles Sawyer and Michael Jung at the University of California, Los Angeles. Its therapeutic value has further cemented with later extensions in indications to include metastatic castration-sensitive prostate cancer and non-metastatic castration-resistant prostate cancer. Enzalutamide’s crystalline structure and restricted water solubility are two of its physical and chemical characteristics that highlight its formulation and pharmacological implications. Enzalutamide pharmacologically inhibits the binding of dihydro testosterone to the androgen receptor in a competitive manner, hence hindering the progression of cancer. It is mostly metabolized in the liver, where it produces active metabolites that are mainly excreted in faces. Its effectiveness in improving overall survival, especially in high-risk patients, has been demonstrated in clinical trials. Although enzalutamide has many therapeutic advantages, it also has several noticeable side effects, such as gynecomastia, exhaustion, and seizures. In addition, there are very few cases of CNS adverse effects, such as posterior reversible encephalopathy syndrome (PRES). As a result, close observation is necessary, particularly in those who already have seizure disorders. All things considered, enzalutamide is a mainstay of the treatment of prostate cancer, providing patients with better results and a higher quality of life at different stages of the disease.