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Aromatase inhibitors tend to cause fewer serious side effects than tamoxifen, such as blood clots, stroke, and endometrial cancer. But aromatase inhibitors can cause more heart problems , more bone loss ( osteoporosis ), and more broken bones than tamoxifen, at least for the first few years of treatment. If you and your doctor are considering an aromatase inhibitor as part of your treatment plan, you may want to ask your doctor about having a bone density test to see if a bone strengthening medicine might be necessary while you're taking the aromatase inhibitor.
ARN-509 (< 10 μM) inhibits androgen-mediated induction or repression of mRNA expression levels for 13 endogenous genes including PSA and TMPRSS2 in the LNCaP/AR prostate cancer cell line. ARN-509 (< 10 μM) inhibits the proliferative effect of R1881 (30 pM) in the LNCaP/AR prostate cancer cell line. ARN-509 (10 μM) impairs AR nuclear localization and thus reduces the concentration of AR available to bind androgen response elements (ARE) in LNCaP cells expressing AR-EYFP. ARN-509 (10 μM) is able to effectively compete with R1881 (1 nM) and prevent AR from binding to promoter regions. ARN-509 inhibits R1881-induced VP16-AR–mediated transcription with IC50 of μM in Hep-G2 cells expressing a VP16-AR fusion protein and an ARE-driven luciferase reporter.