Darolutamide is an androgen receptor (AR) inhibitor with a flexible polar-substituted pyrazole structure that binds with high affinity directly to the receptor ligand binding domain.
Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR mediated transcription. A major metabolite, keto-darolutamide, exhibited similar in vitro activity to darolutamide. Darolutamide treatment decreases prostate tumour cell proliferation leading to potent antitumour activity.
NUBEQA is indicated for the treatment of adult men with:
• non-metastatic castration-resistant prostate cancer (nmCRPC) who are at high risk of developing metastatic disease.
• metastatic hormone-sensitive prostate cancer (mHSPC) in combination with docetaxel and androgen deprivation therapy.