Molecular Weight(MW): 464.44
Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
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|Description||Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.|
Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys).  Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. 
|In vivo||Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. |
AR reporter assay:Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of Enzalutamide is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to Enzalutamide treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of Enzalutamide. After two days of incubation, reporter activities are assayed.
|In vitro||DMSO||92 mg/mL (198.08 mM) warming|
|In vivo||2% DMSO+30% PEG 300+ddH2O||5mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02711956||Not yet recruiting||Metastatic Castration-Resistant Prostate Cancer||Zenith Epigenetics||October 2016||Phase 1|
|NCT02684227||Not yet recruiting||Endometrial Cancer||M.D. Anderson Cancer Center|Astellas Pharma Inc|Medivation, Inc.|National Comprehensive Cancer Network||August 2016||Phase 2|
|NCT02685397||Not yet recruiting||Castration-resistant Prostate Cancer Patients With Oligometastases||Sir Mortimer B. Davis - Jewish General Hospital||August 2016||Phase 2|Phase 3|
|NCT02833883||Not yet recruiting||Prostate Cancer|Castration-resistant Prostate Cancer.||Memorial Sloan Kettering Cancer Center|Celgene Corporation|Thomas Jefferson University|University of Michigan||July 2016||Phase 1|
|NCT02689427||Not yet recruiting||Breast Cancer||M.D. Anderson Cancer Center|Astellas Pharma US, Inc.||June 2016||Phase 2|
|NCT02339168||Recruiting||Prostate Cancer||University of California, Davis|National Cancer Institute (NCI)|Medivation, Inc.|Astellas Pharma Inc||June 2016||Phase 1|
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