Selumetinib

Selumetinib
Clinical data
Trade names	Koselugo
Other names	AZD6244, ARRY-142886
AHFS/Drugs.com	Monograph
MedlinePlus	a620030
License data	US DailyMed: Selumetinib;
Pregnancy; category	AU: D; Contraindicated;
Routes of; administration	By mouth
Drug class	Protein kinase inhibitor
ATC code	L01EE04 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Metabolism	Liver (probably CYP3A4 and CYP2C19)
Metabolites	N‐desmethyl‐selumetinib (active metabolite)
Elimination half-life	5.3–7.2 hrs
Excretion	Bile duct
Identifiers
	IUPAC name 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide;
CAS Number	606143-52-6; as salt: 943332-08-9;
PubChem CID	10127622;
DrugBank	DB11689; as salt: DBSALT002048;
ChemSpider	8303141 ; as salt: 17342538;
UNII	6UH91I579U; as salt: 807ME4B7IJ;
KEGG	D09666 ; as salt: D10024 ;
ChEBI	CHEBI:90227;
ChEMBL	ChEMBL1614701 ; as salt: ChEMBL2105684;
PDB ligand	3EW (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID3048944 ;
ECHA InfoCard	100.169.311
Chemical and physical data
Formula	C17H15BrClFN4O3
Molar mass	457.68 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO;
	InChI InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26) ; Key:CYOHGALHFOKKQC-UHFFFAOYSA-N ;
	(verify)

Selumetinib (INN), sold under the brand name Koselugo, is a medication for the treatment of children, two years of age and older, with neurofibromatosis type I (NF-1), a genetic disorder of the nervous system causing tumors to grow on nerves. It is taken by mouth.

Common side effects include headache, abdominal pain and other problems of the gastrointestinal tract, fatigue, muscle pain, as well as dry skin and other skin problems.

Selumetinib was approved for medical use in the United States in April 2020, and in the European Union in June 2021. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.