Enzalutamide

• Enzalutamide is an androgen receptor inhibitor used to treat prostate cancer.
• It works by blocking androgen signaling, which is crucial for prostate cancer cell growth.
• The medication is prescribed for metastatic castration-resistant prostate cancer (mCRPC) and non-metastatic CRPC.
• Common side effects include fatigue and hot flashes, while serious side effects can include seizures.
• Patients should adhere strictly to prescribed dosages and be aware of potential drug interactions.

What is Enzalutamide and How Does It Work?

Enzalutamide is a potent, orally administered androgen receptor inhibitor. It is specifically designed to target the androgen receptor (AR) signaling pathway, which plays a critical role in the development and progression of prostate cancer. Unlike older anti-androgens, Enzalutamide acts at multiple steps in the AR signaling pathway, making it effective even when cancer cells become resistant to traditional hormone therapies.

The mechanism of how Enzalutamide works involves several key actions. It competitively inhibits androgen binding to the androgen receptor, preventing the activation of the receptor. Furthermore, it inhibits nuclear translocation of the activated AR, meaning it stops the receptor from moving into the cell’s nucleus where it would bind to DNA and promote gene expression for cancer cell growth. Lastly, Enzalutamide impairs the association of the AR with DNA, further suppressing the transcription of AR-regulated genes. These combined actions lead to reduced proliferation of prostate cancer cells and increased apoptosis (programmed cell death).

Enzalutamide: Uses, Side Effects, and Important Information

What Enzalutamide is used for primarily involves the treatment of prostate cancer. It is indicated for patients with metastatic castration-resistant prostate cancer (mCRPC), meaning the cancer has spread and is no longer responding to treatments that lower testosterone levels. It is also approved for the treatment of non-metastatic castration-resistant prostate cancer (nmCRPC) in patients at high risk for developing metastatic disease. Clinical studies have demonstrated that Enzalutamide can significantly improve overall survival and delay disease progression in these patient populations.

Regarding Enzalutamide side effects and benefits, patients often experience a range of adverse reactions. Common side effects can include:

• Fatigue
• Hot flashes
• Headache
• Diarrhea
• Hypertension (high blood pressure)
• Musculoskeletal pain

More serious, though less common, side effects can include seizures, posterior reversible encephalopathy syndrome (PRES), and cardiovascular events such as ischemic heart disease. The benefits of Enzalutamide typically outweigh these risks for eligible patients, as it has been shown to extend life and improve quality of life by controlling cancer growth. Regular monitoring by a healthcare professional is crucial to manage side effects and ensure patient safety.

Comprehensive Enzalutamide drug information emphasizes its oral administration and the importance of consistent dosing. It is typically taken once daily, with or without food. Patients should not crush, chew, or break the tablets. Healthcare providers must be informed of all other medications being taken, as Enzalutamide can interact with various drugs, including strong CYP2C8 inhibitors and CYP3A4 inducers, potentially altering its effectiveness or increasing side effects. Special precautions are necessary for patients with a history of seizures or other neurological conditions. Adherence to the prescribed regimen and regular follow-up appointments are vital for optimal treatment outcomes.