Basic Information
ID DDInter1659
Drug Type small molecule
Molecular Formula C17H15BrClFN4O3
Molecular Weight 457.680
CAS Number 606143-52-6
Description Activation of the Raf-MEK-ERK signaling pathway is known to be implemented in several types of malignancies, thus, mitogen-activated protein kinase kinase (MEK) inhibitors such as selumetinib are important tools that can target the problematic overactivity of this pathway.[A193611] Results from clinical trials investigating earlier developed MEK inhibitors were underwhelming.[A193611] However, selumetinib demonstrated impressive efficacy and tolerability in Phase I trials, leading to its continued investigation for the treatment of various types of tumors in Phase II trials.[A193611] Currently, the novel MEK 1 / 2 inhibitor, selumetinib, is approved solely for the treatment of Neurofibromatosis type 1 (NF-1) in a limited age group. NF-1 is considered rare with an estimated incidence of 1/3000 individuals.[A193608] It is a genetic, autosomal dominant condition resulting from mutations of the NF1 gene, which can lead to various complications including the development of multiple tumors in the nervous system.[A193533,A193608] Some patients with this disorder develop plexiform neurofibromas (PN); however, this is considered to be relatively uncommon compared to other variants of NF-1.[A193608] Luckily, the use of selumetinib in patients with NF-1 has shown efficacy in shrinking associated tumors and is linked to other positive clinical outcomes.[A193533]
ATC Classification L01EE04
IUPAC Name 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-1,3-benzodiazole-6-carboxamide
InChI CYOHGALHFOKKQC-UHFFFAOYSA-N
Canonical SMILES CN1C=NC2=C(F)C(NC3=C(Cl)C=C(Br)C=C3)=C(C=C12)C(=O)NOCCO
Useful Links DrugBank ChEBI PubChem Substance KEGG Drug ChemSpider BindingDB PharmGKB Wikipedia ChEMBL ZINC
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