Selumetinib,
activating mutations in the BRAF V600E, are
associated with poorer outcomes in patients with papillary thyroid
cancer. MAPK kinase (MEK), immediately downstream
of BRAF, is a promising target for MAPK/ERK pathway inhibition. In
addition to thyroid cancer, BRAF-activating mutations are prevalent in
melanoma (–59%), colorectal cancer (5–22%), serous ovarian cancer
(–30%), and several other tumor types. Four lines bearing V600E BRAF
mutations were all sensitive to selumetinib, with GI50 values ranging
from 14 to 50 nM. A positive control BRAF mutant melanoma line, SKMel28,
exhibited a similar GI50 of 23 nM. A Phase II clinical trial about
selumetinib in cancers with BRAF mutations is ongoing.
Tyrosine Kinase Inhibitors. Ингибиторы тирозинкиназ с точки зрения медицинского химика.
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