Preferred Label : Carbon C 14 Vemurafenib;
NCIt synonyms : 14 C-labeled Vemurafenib;
NCIt definition : A radioconjugate composed of vemurafenib, an ATP-competitive, small-molecule inhibitor
of BRAF(V600E) kinase, labeled with the radioisotope carbon C 14, with potential use
for evaluating the pharmacokinetic profile of vemurafenib. Vemurafenib selectively
binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which
may result in both an inhibition of an over-activated MAPK signaling pathway in BRAF(V600E)
kinase-expressing tumor cells and a reduction in tumor cell proliferation. Labeling
of vemurafenib with the radioactive tracer carbon C 14 allows for the evaluation of
vemurafenib's pharmacokinetic profile, including its absorption, distribution, metabolism,
and excretion (ADME). The BRAF(V600E) gene mutation in which valine is substituted
for glutamic acid at residue 600 (V600E), is found in many cancer cell types and plays
a key role in the over-activation of the MAPK signaling pathway.;
Origin ID : C121958;
UMLS CUI : C4055272;
Semantic type(s)
- concept_is_in_subset
