Enzalutamide is a pivotal pharmaceutical API and analytical reference standard in the treatment of prostate cancer, functioning as a potent androgen receptor antagonist with a unique mechanism of action. Unlike earlier antiandrogens, Enzalutamide inhibits AR nuclear translocation and DNA binding in addition to blocking coactivator recruitment. Enzalutamide is marketed under the brand name XTANDI® for the treatment of castration-resistant prostate cancer (CRPC), metastatic castration-sensitive prostate cancer (mCSPC), and non-metastatic castration-sensitive prostate cancer (nmCSPC) with biochemical recurrence at high risk for metastasis. Enzalutamide demonstrates an IC₅₀ value of 36 nM for AR inhibition in LNCaP prostate cells and induces significant tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. Enzalutamide is supplied with detailed characterization data and serves as both the API for commercial production and a reference standard for analytical method development and quality control applications.
|
Parameter |
Specification |
|
Product Name |
Enzalutamide |
|
CAS Number |
915087-33-1 |
|
Molecular Formula |
C₂₁H₁₆F₄N₄O₂S |
|
Molecular Weight |
464.44 g/mol |
|
Appearance |
White solid |
|
Melting Point |
|
|
Storage Condition |
–20 °C |
|
Density |
1.49 |
|
pKa |
13.88 ± 0.46 |
Enzalutamide can now be applied to almost all stages of prostate cancer. For example, for patients with advanced disease before chemotherapy, it can significantly delay the time when patients start chemotherapy. In addition, for post-chemotherapy CRPC and mCRPC, it can significantly improve the overall survival time and progression-free survival time of patients.
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM.
The main side effects of Enzalutamide (XTANDI) are hypertension and fatigue. The most common adverse reactions (≥5%) are asthenia/fatigue, back pain, diarrhea, arthralgia, hot flashes, peripheral blood edema, musculoskeletal pain, headache, upper respiratory tract infection, muscle weakness, dizziness, insomnia, lower respiratory tract infection, spinal cord compression and cauda equina syndrome, hematuria, paresthesia, anxiety and hypertension.
Looking for Enzalutamide for your prostate cancer API program, impurity reference standard needs, or androgen receptor research? Cosperpharm is here to support your project. Reach out to our team today for a quote, technical documentation, or to discuss your specific requirements—we're ready to partner with you.
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