selumetinib
Overview
Selumetinib is a selective MEK1/2 inhibitor with FDA approval for neurofibromatosis type 1 (NF1)-associated plexiform neurofibromas in pediatric patients. It is under investigation for other RAS/RAF/MEK-driven malignancies.
Evidence in the corpus
- Selumetinib (MEK inhibitor) was among MAPK-pathway directed therapies evaluated across BRAF fusion-positive tumors (N=241, 52 histologies at MSK); MEK inhibitor monotherapy provided durable benefit particularly in pilocytic astrocytomas (all 6 patients >6 months on therapy, median 8 months across all MEK inhibitor-treated patients), while combination BRAF+MEK inhibition was less durable (median 1 month) PMID:38922339.
- NCI-60 CellMiner pharmacogenomics analysis linked MAPK pathway genomic features to selumetinib sensitivity in colon cancer cell lines PMID:22802077
- In a co-clinical trial in KRAS-mutant LUAD, selumetinib plus docetaxel was tested in parallel in GEM murine models and a human phase II study; the murine arm identified STK11/LKB1 loss as a genetic modifier of response and informed retrospective reanalysis of the human trial PMID:23999436.
- Used as a tool MEK inhibitor alongside dabrafenib and trametinib for in vitro validation of MAP2K2 resistance mutations in BRAF V600E melanoma cell lines PMID:24265153
- MEK inhibitor; proposed as therapeutic candidate for KRAS/NRAS/GNAQ-altered cisplatin-resistant GCT alongside trametinib per Appendix Table A2 of the cisplatin-resistance biomarker study PMID:27646943
Resistance mechanisms
- Not directly characterized in the corpus.
Cancer types (linked)
Sources
This page was processed by crosslinker on 2026-05-09. - PMID:22802077
This page was processed by crosslinker on 2026-05-09. - PMID:23999436
This page was processed by crosslinker on 2026-05-09. - PMID:24265153
This page was processed by crosslinker on 2026-05-09. - PMID:27646943
This page was processed by wiki-cli on 2026-05-14.