Ruxolitinib

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Ruxolitinib, sold under the brand name Jakafi among others, is a medication used for the treatment of intermediate or high-risk myelofibrosis,[5] a type of myeloproliferative neoplasm that affects the bone marrow;[10][11] polycythemia vera, when there has been an inadequate response to or intolerance of hydroxyurea;[5][12] and steroid-refractory acute graft-versus-host disease.[5] Ruxolitinib is a Janus kinase inhibitor.[5] It was developed and marketed by Incyte Corp in the US under the brand name Jakafi,[5] and by Novartis elsewhere in the world, under the brand name Jakavi.[13]

Quick facts: Clinical data, Trade names, Other names, AHFS...
Ruxolitinib
Ruxolitinib_Structural_formula_V1.svg
Clinical data
Trade namesJakafi, Jakavi, Opzelura
Other namesINCB018424, INC424
AHFS/Drugs.comMonograph
MedlinePlusa612006
License data
Pregnancy
category
Routes of
administration
By mouth, topical
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability95%[9]
Protein binding97%[9]
MetabolismLiver (mainly CYP3A4-mediated)[9]
Elimination half-life2.8-3 hours[9]
ExcretionUrine (74%), faeces (22%)[9]
Identifiers
  • (3R)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H18N6
Molar mass306.373 g·mol−1
3D model (JSmol)
  • N#CCC(C1CCCC1)n1cc(-c2ncnc3[nH]ccc23)cn1
  • 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 checkY
  • Key:HFNKQEVNSGCOJV-OAHLLOKOSA-N checkY
 ☒NcheckY (what is this?)  (verify)
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It was approved for medical use in the United States in 2011,[14] and in the European Union in 2012.[7] Ruxolitinib is the first FDA-approved pharmacologic treatment to address repigmentation in vitiligo patients.[15]