Understanding the Mechanism of Action: How Enzalutamide Targets mCRPC Cells 

Introduction:

Prostate cancer is a prominent contributor to cancer-related mortality in men globally, frequently advancing to metastatic castration-resistant prostate cancer (mCRPC), which presents substantial therapeutic hurdles. Nevertheless, recent strides in treatment, notably with medications like enzalutamide, have transformed the approach to managing this formidable type of prostate cancer. This blog explores enzalutamide’s detailed mechanism of action and its crucial role in addressing mCRPC cells.

What is mCRPC:

Metastatic castration-resistant prostate cancer (mCRPC) represents an advanced stage of prostate cancer, marked by tumor progression beyond the prostate gland and resistance to hormone therapy. Unlike localized prostate cancer, which responds to androgen deprivation therapy (ADT), mCRPC exhibits aggressive growth and metastasis despite low testosterone levels. 

Symptoms include urinary difficulties, fatigue, weight loss, and bone pain. Treatment options for mCRPC include chemotherapy, immunotherapy, and novel drugs like enzalutamide and abiraterone acetate, which have shown promising outcomes in terms of overall survival and quality of life.

Mechanism of Action of Enzalutamide: 

Enzalutamide works by blocking the androgen receptor on cancer cells, thereby inhibiting the ability of androgens to fuel prostate cancer growth. Enzalutamide binds to the androgen receptor with 5 to 8-fold greater affinity than first-generation antiandrogens such as bicalutamide. 

It is a competitive androgen receptor (AR) inhibitor that has a threefold inhibition on the androgen signaling. It inhibits androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with chromosomal DNA to upregulate oncogenes. Enzalutamide is primarily eliminated by hepatic metabolism. The drug is metabolized by CYP2C8 and CYP3A4, and its active metabolite is primarily formed by CYP2C8. 

Enzalutamide is indicated for the treatment of castration-resistant prostate cancer, metastatic castration-sensitive prostate cancer (mCSPC), and non-metastatic castration-sensitive prostate cancer (nmCSPC) with biochemical recurrence at high risk for metastasis. Enzalutamide has shown positive outcomes in terms of overall survival and quality of life for patients with mCRPC. 

Side Effects Of Enzalutamide

Side effects of enzalutamide can include fatigue, hot flashes, hypertension, diarrhea, nausea, and musculoskeletal pain. Other potential adverse effects may include headache, dizziness, decreased appetite, and weight loss. Additionally, enzalutamide can lead to liver function abnormalities, seizures, and an increased risk of falls. Patients need to discuss any concerning symptoms with their healthcare provider while undergoing treatment with enzalutamide.

Conclusion:

Enzalutamide marks a significant shift in managing metastatic castration-resistant prostate cancer (mCRPC), offering a targeted approach to interrupt androgen receptor signaling and halt tumor growth. As our understanding of mCRPC progresses, enzalutamide remains at the forefront of therapeutic innovation, providing hope for patients battling this aggressive form of prostate cancer. To check availability of enzalutamide in India(the generic version), interested individuals can contact the Patient Support Team at (+91) 9315705373 or via email at help@sansfro.com.