Enzalutamide
未知生产厂商
Enzalutamide is a second-generation androgen receptor inhibitor used to treat castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer.
Enzalutamide is a second-generation androgen receptor inhibitor used to treat castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer.
Enzalutamide is a competitive androgen receptor (AR) inhibitor that has a threefold inhibition on the androgen signaling pathway without significant AR agonist activity. It inhibits androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with chromosomal DNA to upregulate oncogenes. Enzalutamide binds to the AR with 5 to 8-fold greater affinity than first-generation antiandrogens such as bicalutamide and only 2-3 fold reduced affinity than the natural ligand dihydrotestosterone. Molecular docking showed that enzalutamide binds to the ligand binding domain of the AR distinctive from that of bicalutamide.
Enzalutamide is indicated for the treatment of castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer (mCRPC). It is also used in combination with talazoparib for the treatment of adult patients with HRR gene-mutated mCRPC.
共 3 项相关疾病
