Darolutamide

General Information

Darolutamide Impurities and Darolutamide 

Daicel Pharma synthesizes high-quality Darolutamide impurity, KetoDarolutamide, which is crucial in the analysis of the quality, stability, and biological safety of the active pharmaceutical ingredient Darolutamide. Moreover, Daicel Pharma offers custom synthesis of Darolutamide impurities and delivers them globally.

Darolutamide [CAS: 1297538-32-9] is a medicine that functions as an androgen receptor antagonist and has potential anti-cancer properties. It treats non-metastatic prostate cancer that has become resistant to hormone therapy.

Darolutamide: Use and Commercial Availability  

Nubeqa is a brand name for Darolutamide for treating adult males with non-metastatic castration-resistant prostate cancer (nmCRPC) at risk of metastasis. It binds to the receptor (target) of androgens, such as testosterone, and blocks them from stimulating prostate cancer cells from growing.

Darolutamide Structure and Mechanism of Action

The chemical name of Darolutamide is N-[(1S)-2-[3-(3-Chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide. Its chemical formula is C₁₉H₁₉ClN₆O₂, and its molecular weight is approximately 398.8 g/mol.

Darolutamide inhibits androgen binding, androgen receptor nuclear translocation, and Androgen receptor-mediated transcription.

Darolutamide Impurities and Synthesis

During the synthetic process¹, Darolutamide impurities form that affect the quality and safety of the drug. These impurities must be monitored and controlled to ensure the drug is safe and effective for patients. It requires a thorough understanding of the potential impurities, their preparation, and appropriate measures to limit them.

Daicel provides a Certificate of Analysis (CoA) for the Darolutamide impurity standard, KetoDarolutamide. The CoA is issued from a cGMP-compliant analytical facility and contains complete characterization data, such as 1H NMR, 13C NMR, IR, MASS, and HPLC purity². Additional characterization data, such as 13C-DEPT and CHN, can be provided upon request. Daicel can also prepare any unknown Darolutamide impurity or degradation product and offer labeled compounds to quantify the efficacy of Darolutamide. Daicel offers Darolutamide-D4, a deuterium-labeled Darolutamide standard used in bio-analytical research such as BA/BE studies. We give a complete characterization