Preferred Label : Carbon C 14 Idasanutlin;
NCIt synonyms : C14 Idasanutlin; [14C]-radiolabeled Idasanutlin;
NCIt definition : A radiopharmaceutical agent composed of an orally available, small-molecule antagonist
of MDM2 (mouse double minute 2; Mdm2 p53 binding protein homolog), and labeled with
the radioisotope carbon C 14, with potential use for evaluating the pharmacokinetics
of idasanutlin. Upon oral administration, idasanutlin binds to MDM2 blocking the interaction
between the MDM2 protein and the transcriptional activation domain of the tumor suppressor
protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded
and the transcriptional activity of p53 is restored. This may lead to p53-mediated
induction of tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and
negative regulator of the p53 pathway, is often overexpressed in cancer cells and
has been implicated in cancer cell proliferation and survival. . Labeling of idasanutlin
with the radioactive tracer carbon C 14 permits the evaluation of idasanutlin's pharmacokinetic
profile, including its absorption, distribution, metabolism, and excretion (ADME).;
NCI Metathesaurus CUI : CL514081;
Origin ID : C130024;
UMLS CUI : C4329618;
Semantic type(s)
- concept_is_in_subset
