Enzalutamide 99% Purity Anti-Prostate Cancer API Androgen Receptor Antagonist CAS 915087-33-1 Pharmaceutical Grade for Prostate Cancer Treatment

Product Overview

Enzalutamide is a potent, non-steroidal androgen receptor (AR) antagonist used for the treatment of prostate cancer. It was the first second-generation anti-androgen approved for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Enzalutamide works by competitively inhibiting androgen binding to the androgen receptor, preventing AR nuclear translocation, and inhibiting AR-mediated transcription, thereby blocking androgen-driven tumor growth.

Chemically, enzalutamide is 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluoro-N-methylbenzamide with the molecular formula C₂₁H₁₆F₄N₄O₂S and a molecular weight of 464.44 g/mol. It is a white to off-white crystalline powder with low aqueous solubility and good oral bioavailability.

Mechanism of Action

Enzalutamide exerts its anti-tumor effects through multiple mechanisms targeting the androgen receptor pathway:

• Competitive AR Antagonism: Competes with androgens for binding to the ligand-binding domain of the AR

• Inhibition of AR Nuclear Translocation: Prevents the AR from translocating to the cell nucleus

• Inhibition of DNA Binding: Blocks AR binding to DNA and subsequent gene transcription

• No Partial Agonist Activity: Unlike first-generation anti-androgens like bicalutamide, enzalutamide has no known agonist activity

Enzalutamide has demonstrated significant improvements in both overall survival and progression-free survival in multiple Phase III clinical trials across different stages of prostate cancer, including mCRPC and non-metastatic CRPC.

Clinical Indications & Market Position

Enzalutamide is indicated for:

• Metastatic Castration-Resistant Prostate Cancer (mCRPC): First-line and second-line treatment

• Non-Metastatic Castration-Resistant Prostate Cancer (nmCRPC): High-risk disease

• Metastatic Hormone-Sensitive Prostate Cancer (mHSPC): In combination with androgen deprivation therapy

As a second-generation anti-androgen, enzalutamide has become a standard of care in advanced prostate cancer. The global enzalutamide market continues to grow due to the increasing incidence of prostate cancer worldwide and the expansion of indications to earlier disease stages.

Quality Specifications

Our enzalutamide API meets strict pharmaceutical quality standards:

• Purity: ≥99.0% by HPLC

• Related substances: Total impurities ≤1.0%, single impurity ≤0.15%

• Enantiomeric purity: ≥99.5%

• Residual solvents: Meet ICH Q3C guidelines

• Heavy metals: ≤10 ppm

• Loss on drying: ≤0.5%

• Residue on ignition: ≤0.1%

• Particle size: Customizable (D90 ≤ 50μm standard)

• Each batch released with full Certificate of Analysis (COA)

• GMP manufacturing with complete quality documentation

Packaging & Storage

• Packaging options: 25kg fiber drums with double PE liners, 5kg aluminum tins, 1kg aluminum foil bags

• Custom packaging: Available upon request for special requirements

• Storage conditions: Store in tightly sealed containers in a cool, dry place, protected from light

• Shelf life: 36 months under proper storage conditions

• Supply capacity: Kilograms to tons available, ensuring reliable supply

• Regulatory support: Technical documentation available to support customer product development and registration