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CAS No. 915087-33-1
Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Selleck's Enzalutamide (MDV3100) has been cited by 383 publications
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|Description||Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.|
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)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04335682||Recruiting||Drug: Darolutamide|Drug: Enzalutamide||Metastatic Prostate Cancer|Prostate Cancer Metastatic|Prostate Cancer|Castrate Resistant Prostate Cancer||Alliance Foundation Trials LLC.|Bayer||August 17 2021||Phase 2|
|NCT04655365||Not yet recruiting||Drug: Enzalutamide capsule||Prostate Cancer||CHU de Quebec-Universite Laval|Astellas Pharma Europe Ltd.||January 4 2021||Phase 2|
|NCT04475601||Terminated||Drug: Enzalutamide Pill||COVID-19|Corona Virus Infection||Andreas Josefsson|Umeå University|Sahlgrenska University Hospital Sweden|University Hospital Umeå|Uppsala University Hospital|Skane University Hospital|Jonkoping County Hospital|Sundsvall Hospital|Helsingborgs Hospital|Göteborg University|Astellas Pharma Europe Ltd.|Norrlands University Hospital|Västerbotten County Council||July 15 2020||Phase 2|
|NCT04456049||Not yet recruiting||Drug: Enzalutamide||COVID-19 Infection||Ricardo Pereira Mestre|Oncology Institute of Southern Switzerland|Institute of Oncology Research|Institute for Research in Biomedicine|Ente Ospedaliero Cantonale Bellinzona||July 2020||Phase 2|
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