Pharmacokinetics and pharmacogenetics of the MEK1/2 inhibitor, selumetinib, in Asian and Western healthy subjects: a pooled analysis
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Clinical Pharmacology"
DOI: 10.1007/s00228-017-2217-3
Abstract: PurposeEmerging data on selumetinib, a MEK1/2 inhibitor in clinical development, suggest a possible difference in pharmacokinetics (PK) between Japanese and Western patients. This pooled analysis sought to assess the effect of ethnicity on selumetinib exposure… read more here.
Keywords: selumetinib; analysis; mek1 inhibitor; asian subjects ... See more keywords
Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02192
Abstract: Mutations in MEK1/2 have been described as a resistance mechanism to BRAF/MEK inhibitor treatment. We report the discovery of a novel ATP-competitive MEK1/2 inhibitor with efficacy in wildtype (WT) and mutant MEK12 models. Starting from… read more here.
Keywords: selective mek1; inhibitor; mek1 inhibitor; atp competitive ... See more keywords
LGG-44. A PHASE I DOSE ESCALATION TRIAL OF THE MEK1/2 INHIBITOR MEK162 (BINIMETINIB) IN CHILDREN WITH LOW-GRADE GLIOMAS AND OTHER RAS/RAF PATHWAY-ACTIVATED TUMORS
Sign Up to like & getrecommendations! Published in 2018 at "Neuro-oncology"
DOI: 10.1093/neuonc/noy059.385
Abstract: BACKGROUND Ras/Raf/MEK/ERK pathway activation is the primary driver of most pediatric low-grade gliomas (LGG). MEK162 is an orally bioavailable MEK1/2 inhibitor. read more here.
Keywords: grade gliomas; low grade; ras raf; mek1 inhibitor ... See more keywords
P42 Use of trametinib, a MEK1 inhibitor, to treat Erdheim Chester disease (ECD)
Sign Up to like & getrecommendations! Published in 2020 at "Rheumatology"
DOI: 10.1093/rheumatology/keaa111.041
Abstract: Erdheim Chester disease (non-Langerhan’s cell histocytosis) is a poorly recognised rare multisystem disorder. Alfa interferon (αINF) is recommended as initial therapy. BRAFV600E and MAP2K1 mutations have been identified in this condition, for which targeted biologic… read more here.
Keywords: erdheim chester; ecd; mek1 inhibitor; chester disease ... See more keywords
Establishment of a novel method to assess MEK1/2 inhibition in PBMCs for clinical drug development
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Cell and Developmental Biology"
DOI: 10.3389/fcell.2022.1063692
Abstract: The Raf/MEK/ERK signaling pathway plays a key role in regulating cellular proliferation, differentiation, apoptosis, cytokine production, and immune responses. However, it is also involved in diseases such as cancer, and numerous viruses rely on an… read more here.
Keywords: mek1; mek1 inhibition; mek1 inhibitor; mek1 activation ... See more keywords