Ruxolitinib

Ruxolitinib
Clinical data
Trade names	Jakafi, Jakavi, Opzelura
Other names	INCB018424, INC424
AHFS/Drugs.com	Monograph
MedlinePlus	a612006
License data	US DailyMed: Ruxolitinib;
Pregnancy; category	AU: C;
Routes of; administration	By mouth, topical
ATC code	L01EJ01 (WHO) D11AH09 (WHO);
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	95%
Protein binding	97%
Metabolism	Liver (mainly CYP3A4-mediated)
Elimination half-life	2.8-3 hours
Excretion	Urine (74%), faeces (22%)
Identifiers
	IUPAC name (3R)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile;
CAS Number	941678-49-5 ;
PubChem CID	25126798;
IUPHAR/BPS	5688;
DrugBank	DB08877 ;
ChemSpider	25027389 ;
UNII	82S8X8XX8H;
KEGG	D09959 ; as salt: D09960 ;
ChEMBL	ChEMBL1789941 ;
PDB ligand	RXT (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID10240930 ;
Chemical and physical data
Formula	C17H18N6
Molar mass	306.373 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES N#CCC(C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1;
	InChI InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1 ; Key:HFNKQEVNSGCOJV-OAHLLOKOSA-N ;
	(what is this?) (verify)

Ruxolitinib (sold under the brand names Jakafi and Jakavi among others, and as Opzelura in cream form) is a medication used for the treatment of intermediate or high-risk myelofibrosis, a type of myeloproliferative neoplasm that affects the bone marrow; polycythemia vera, when there has been an inadequate response to or intolerance of hydroxyurea; and steroid-refractory acute graft-versus-host disease. Ruxolitinib is a Janus kinase inhibitor. It was developed and marketed by Incyte Corp in the US under the brand name Jakafi, and by Novartis elsewhere in the world, under the brand name Jakavi.

It was approved for medical use in the United States in 2011, and in the European Union in 2012. Ruxolitinib is the first FDA-approved pharmacologic treatment to address repigmentation in vitiligo patients.

The crystal structure of ruxolitinib and of its dihydrate form are known.