Preferred Label : Deutenzalutamide;
NCIt synonyms : D3-ENT; N-trideuteromethyl Enzalutamide; Enzalutamide Deuterated; Deuterated Enzalutamide;
NCIt definition : A deuterated form of enzalutamide, an orally bioavailable, organic, non-steroidal
small molecule targeting the androgen receptor (AR) with potential antineoplastic
activity. Upon administration, deutenzalutamide 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 deutenzalutamide form
also reduces the unwanted brain-related side effects of enzalutamide and improves
its safety profile.;
UNII : 3OKI556HC2;
CAS number : 1443331-82-5;
Molecule name : HC 1119; HC-1119;
NCI Metathesaurus CUI : CL937681;
Origin ID : C158096;
UMLS CUI : C5544347;
Currated CISMeF NLP mapping
- Semantic type(s)
- concept_is_in_subset
- has_target
