Preferred Label : Iodine I 124 Icapamespib;
NCIt synonyms : 124I-PU-AD; [124I]-PU-AD; Iodine I 124 PU-AD;
NCIt related terms : ICAPAMESPIB I-124;
NCIt definition : A radioconjugate composed of icapamespib, a synthetic purine-scaffold inhibitor of
the molecular chaperone heat shock protein 90 (Hsp90), conjugated to the radioisotope
iodine I 124, with potential imaging activity upon positron emission tomography (PET).
Upon administration of iodine I 124 icapamespib, the icapamespib moiety selectively
binds to cancer cells expressing stress-induced Hsp90 (stress Hsp90). Upon PET, Hsp90-overexpressing
cancer cells can be visualized and patients who may benefit from icapamespib therapy
can be identified. This radioconjugate may also be used to determine the pharmacokinetics
of icapamespib. Icapamespib is able to cross the blood-brain-barrier (BBB) and specifically
targets stress Hsp90, as seen in certain conditions, such as cancer and neurodegenerative
diseases, while normal housekeeping Hsp90 complexes are not targeted by icapamespib
at dose levels administered for imaging. Additionally, housekeeping Hsp90 complexes
are only targeted at doses that are much larger than that are needed to exert an anticancer
effect.;
UNII : Q1J3TQ99O2;
CAS number : 1450804-65-5;
NCI Metathesaurus CUI : CL507947;
Origin ID : C128487;
UMLS CUI : C5667153;
Semantic type(s)
- concept_is_in_subset
- has_target
