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darolutamide
- Development stage
- Approved
- Lead developer
- Bayer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Darolutamide is a nonsteroidal androgen receptor antagonist used to treat prostate cancer. It is indicated for non-metastatic castration-resistant prostate cancer (nmCRPC) and, in combination with docetaxel, for metastatic hormone-sensitive prostate cancer (mHSPC). Darolutamide works by competitively inhibiting androgens from binding to the androgen receptor, thereby blocking androgen receptor nuclear translocation and transcriptional activity. This results in decreased proliferation of prostate cancer cells and tumor size. Its main metabolite, keto-darolutamide, has similar pharmacological activity. Darolutamide was developed by Bayer HealthCare Pharmaceuticals and was first approved by the FDA in July 2019[1][2][4][7].
- Brand names
- Nubeqa
- Other names
- darolutamidaODM201ODM-201ODM 201BAY1841788BAY-1841788BAY 1841788
02
Targets
AR (Adrenergic receptors)PR (Progesterone receptor)
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