Preferred Label : Luxdegalutamide;
NCIt synonyms : AR Degrader ARV-766; Androgen Receptor PROTAC Degrader ARV-766; AR PROTAC ARV-766; AR-targeted PROTAC Protein Degrader ARV-766; Androgen Receptor Degrader ARV-766;
NCIt definition : An orally bioavailable androgen receptor (AR)-targeted protein degrader, composed
of an AR ligand attached to an E3 ligase recognition moiety and utilizing the proteolysis
targeting chimera (PROTAC) technology, with potential antineoplastic activity. Upon
oral administration, luxdegalutamide targets and binds to the AR ligand binding domain
on the AR. E3 ligase is then recruited to the AR by the E3 ligase recognition moiety
of luxdegalutamide and the AR is tagged by ubiquitin. This causes ubiquitination and
degradation of AR by the proteasome, and prevents the expression of AR target genes
and halts AR-mediated signaling. This inhibits the proliferation of AR-overexpressing
tumor cells. In addition, the degradation of the AR releases luxdegalutamide, allowing
it to bind to additional AR. AR plays a key role in the proliferation of castration-resistant
prostate cancer cells (CRPC). Luxdegalutamide may degrade resistance-driving point
mutations of AR, including the L702H mutation associated with treatments including
abiraterone.;
UNII : 5BD7R933PV;
CAS number : 2750830-09-0;
Molecule name : ARV-766; ARV 766;
NCI Metathesaurus CUI : CL1771378;
Origin ID : C183151;
UMLS CUI : C5666903;
Semantic type(s)
- concept_is_in_subset
- has_target
