{"meta":{"totalResults":2,"from":0},"results":[{"aliases":[{"type":"CodeName","name":"HC-1119"},{"type":"Synonym","name":"enzalutamide deuterated"},{"type":"CodeName","name":"HC1119"},{"type":"CodeName","name":"HC 1119"},{"type":"Synonym","name":"N-trideuteromethyl enzalutamide"},{"type":"Synonym","name":"D3-ENT"}],"definition":{"html":"A deuterated form of enzalutamide, an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Upon administration, deuterated enzalutamide competitively binds to and inhibits the activity of ARs expressed on prostate cancer cells, which impairs nuclear translocation and DNA binding, resulting in apoptosis of prostate cancer cells. This results in a reduction in prostate cancer cell growth. AR overexpression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance. Deuterium incorporation, by replacing the hydrogen atoms of the N-CH3 moiety with deuterium atoms, decreases enzalutamide's metabolism and allows for an increased pharmacokinetic profile, thereby enhancing its anti-tumor efficacy compared to non-deuterated enzalutamide. As the deuterated form can’t cross the blood-brain barrier (BBB), the deuterated form also reduces the unwanted brain-related side effects of enzalutamide and improves its safety profile.\n","text":"A deuterated form of enzalutamide, an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Upon administration, deuterated enzalutamide competitively binds to and inhibits the activity of ARs expressed on prostate cancer cells, which impairs nuclear translocation and DNA binding, resulting in apoptosis of prostate cancer cells. This results in a reduction in prostate cancer cell growth. AR overexpression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance. Deuterium incorporation, by replacing the hydrogen atoms of the N-CH3 moiety with deuterium atoms, decreases enzalutamide's metabolism and allows for an increased pharmacokinetic profile, thereby enhancing its anti-tumor efficacy compared to non-deuterated enzalutamide. As the deuterated form can’t cross the blood-brain barrier (BBB), the deuterated form also reduces the unwanted brain-related side effects of enzalutamide and improves its safety profile.\n"},"drugInfoSummaryLink":null,"nciConceptId":"C158096","nciConceptName":"Deutenzalutamide","termId":797006,"name":"deuterated enzalutamide","firstLetter":"d","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"deutenzalutamide"},{"aliases":[{"type":"CodeName","name":"MDV3100"},{"type":"Synonym","name":"selective androgen receptor modulator MDV3100"},{"type":"USBrandName","name":"Xtandi"},{"type":"CodeName","name":"ASP9785"},{"type":"ChemicalStructureName","name":"benzamide, 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-methyl-"},{"type":"NSCNumber","name":"766085"}],"definition":{"html":"An orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Through a mechanism that is reported to be different from other approved AR antagonists, enzalutamide inhibits the activity of prostate cancer cell ARs, which may result in a reduction in prostate cancer cell proliferation and, correspondingly, a reduction in the serum prostate specific antigen (PSA) level. AR over-expression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance.","text":"An orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Through a mechanism that is reported to be different from other approved AR antagonists, enzalutamide inhibits the activity of prostate cancer cell ARs, which may result in a reduction in prostate cancer cell proliferation and, correspondingly, a reduction in the serum prostate specific antigen (PSA) level. AR over-expression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/enzalutamide","text":"Enzalutamide"},"nciConceptId":"C71744","nciConceptName":"Enzalutamide","termId":560774,"name":"enzalutamide","firstLetter":"e","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"enzalutamide"}],"links":null}