AZD3514 is a novel selective androgen receptor down-regulator (SARD) for prostate cancer. AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors. In vivo, oral dosing of AZD3514 (100mg/kg once-daily for 7 days) significantly inhibited testosterone-induced growth of sexual accessory organs in the Hershberger castrated rat assay. AZD3514 treatment also reduced AR protein in LNCaP cells maintained in steroid-depleted conditions; an effect which was evident within 6 - 8h, and maximal at 18 - 24h. Administration of AZD3514 (100 mg/kg/day orally) for 3 days to Copenhagen rats bearing R3327H Dunning prostate tumours, indicates that AZD3514 treatment also reduces tumour AR in vivo. AZD3514 has also been shown to reduce AR protein expression, PSA synthesis and cell growth in vitro in a subclone of cells serially maintained in the presence of bicalutamide (LNCaP-CR).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
Bradbury RH, et al. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1945-8. PMID: 23466225.
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