Product Name

Ruxolitinib Phosphate

CAS Number

1092939-17-7

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Product Name:
Ruxolitinib Phosphate
CAS Number:
1092939-17-7
Indication:
Treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera (post-PV) myelofibrosis and post-essential thrombocythemia (post-ET) myelofibrosis. [Lexicomp] Myeolofibrosis is the proliferation of abnormal bone marrow stem cells which cause fibrosis (the excessive formation of connective tissue).
Mode of Action:

Ruxolitinib is a kinase inhibitor that is selective for the Janus Associated Kinases (JAK) 1 and 2. These kinases are responsible for the mediation of cytokine and growth factor signalling which in turn effect immune function and hematopoiesis. The signalling process involves signal transducers and transcription activators (STAT) which modulate gene expression. Patients with myelofibrosis have abnormal JAK1 and JAK2 activity thus ruxolitinib works to regulate this.

Pharmacodynamics:

The mean half-maximal inhibitory concentration (IC50) for JAK 1 and JAK 2 are 2.8 nmol/L and 3.3 nmol/L respectively. After administration of ruxolitinib, a decrease in levels of phosphorylated STAT (marker for JAK activity) in a dose-dependent manner can be observed. Pharmacodynamic resistance has not been observed.

Metabolism:

Ruxolitinib is metabolized by CYP3A4. Less potent active metabolites forms as a result.

Toxicity:

Thrombocytopenia was the dose-limiting toxicity.

IUPAC:
1H-Pyrazole-1-propanenitrile, beta-cyclopentyl-4-(7H-pyrrolo(2, 3-d)pyrimidin-4-yl)-, (betaR)-, phosphate (1:1)
ATC:
L01XE18
DrugBank:
DB08877
Formula:
C17-H18-N6.H3-O4-P
Molecular Mass:
404.3649
Synonyms:
3R)-3-Cyclopentyl-3-(4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)-1H-pyrazol-1-yl)propanenitrile phosphate (1:1), INCB018424 salt, Jakafi, Jakavi, Ruxolitinib phosphate, UNII-436LRU32H5
SMILES:
C(#N)C[C@H]([C@@H]1CCCC1)n1ncc(c1)c1ncnc2c1cc[nH]2.P(=O)(O)(O)O
AHFS Code:
10:00
InChi:
1S/C17H18N6.H3O4P/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;1-5(2,3)4/h6,8-12,15H,1-5H2,(H,19,20,21);(H3,1,2,3,4)/t15-;/m1./s1
General Reference:
General Reference:

 

  1. Cervantes F, Martinez-Trillos A: Myelofibrosis: an update on current pharmacotherapy and future directions. Expert Opin Pharmacother. 2013 May;14(7):873-84. doi: 10.1517/14656566.2013.783019. Epub 2013 Mar 21. Pubmed
  2. Lexi-Comp, Inc. (Lexi-DrugsTM ). Lexi-Comp, Inc.; July, 2013.
  3. Yang LP, Keating GM: Ruxolitinib: in the treatment of myelofibrosis. Drugs. 2012 Nov 12;72(16):2117-27. doi: 10.2165/11209340-000000000-00000. Pubmed

 

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