Overview
Enzalutamide is a second-generation nonsteroidal antiandrogen (NSAA) developed for the treatment of prostate cancer. It is marketed under the brand name Xtandi and is known for its high efficacy in blocking androgen receptors, which are critical for prostate cancer growth. The drug is particularly effective in metastatic castration-resistant prostate cancer (mCRPC) and non-metastatic castration-resistant prostate cancer (nmCRPC). Enzalutamide was approved by the FDA in 2012 and has since become a cornerstone in prostate cancer therapy. Its development marked a significant advancement over first-generation antiandrogens, offering improved binding affinity and reduced agonist activity.
Physical and Chemical Properties
Enzalutamide is a white to off-white powder with a molecular weight of 464.43 g/mol. It is slightly soluble in water but dissolves well in organic solvents such as dimethyl sulfoxide (DMSO) and ethanol. The compound has a melting point of approximately 200-202°C, indicating its stability under normal storage conditions. The molecular formula of enzalutamide is C21H16F4N4O2S, reflecting its complex structure with fluorine and sulfur atoms. These elements contribute to its high binding affinity for androgen receptors and its resistance to metabolic degradation, enhancing its therapeutic effectiveness.
Main Applications
Enzalutamide is primarily used to treat metastatic castration-resistant prostate cancer (mCRPC) and non-metastatic castration-resistant prostate cancer (nmCRPC). It works by competitively inhibiting androgen binding to androgen receptors and blocking androgen receptor nuclear translocation and interaction with DNA. In clinical trials, enzalutamide has demonstrated significant improvements in overall survival and progression-free survival compared to placebo. It is often prescribed when other treatments, such as chemotherapy or first-generation antiandrogens, have failed. The drug is typically administered orally in capsule form.
Safety and Storage
Enzalutamide should be stored at room temperature (20-25°C) in a dry, dark place, away from moisture and direct sunlight. Proper storage ensures the stability and efficacy of the compound over time. Handling should be done with appropriate personal protective equipment (PPE), including gloves and safety goggles, to avoid accidental exposure. Common side effects of enzalutamide include fatigue, hypertension, hot flashes, and seizures. Patients with a history of seizures or cardiovascular disease should be closely monitored. The drug is contraindicated in women who are pregnant or may become pregnant due to potential fetal harm.
B2B Procurement Guide
When procuring enzalutamide in bulk, it is essential to verify the CAS number (915087-33-1) and purity specifications. Reputable suppliers should provide certificates of analysis (CoA) and compliance with Good Manufacturing Practices (GMP). Bulk purchases may offer cost advantages, but buyers should also consider logistics and storage requirements. Prices for enzalutamide typically range from $8,000 to $10,000 per kilogram, depending on the supplier and order quantity. Buyers should also assess the supplier’s track record, delivery timelines, and customer support to ensure a smooth procurement process.
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