MedKoo product information:

Ruxolitinib

Deacription of Ruxolitinib: Ruxolitinib phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies. In November 2011, Ruxolitinib was approved by the U.S. Food and Drug Administration for the treatment of intermediate or high-risk myelofibrosis based on results of the COMFORT-I and COMFORT-II Trials. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Ruxolitinib, an oral drug taken twice daily, inhibits JAK1 and 2. It is the first JAK inhibitor to be approved FDA in November, 2011.

Current developer:   Incyte Corp and Novartis AG

Ruxolitinib is a drug being investigated for the treatment of myeloproliferative diseases, plaque psoriasis, and various types of cancer. It is a Janus kinase inhibitor with selectivity for subtypes 1 and 2 of this enzyme.  Roxolitinib is being marketed by Incyte Pharmaceuticals and Novartis under the trade name Jakafi. Results from Phase II clinical trials suggest that the drug can substantially improve symptoms and reduce spleen size in myelofibrosis patients, but it has not been shown to produce remission.[4] As of February 2011, it is undergoing Phase III trials studying myelofibrosis  and polycythemia vera. In June 2011, it was announced that both phase III trials of ruxolitinib in the treatment of myelofibrosis (COMFORT-I and -II) met their primary endpoints of a significant increase in number of patients experiencing at least 35% reduction of spleen volume. In November 2011, Ruxolitinib was approved by the U.S. Food and Drug Administration for the treatment of intermediate or high-risk myelofibrosis based on results of the COMFORT-I and COMFORT-II Trials. (source: http://en.wikipedia.org/wiki/Ruxolitinib).

1: Ostojic A, Vrhovac R, Verstovsek S. Ruxolitinib for the treatment of myelofibrosis. Drugs Today (Barc). 2011 Nov;47(11):817-27. PubMed PMID: 22146225.

2: Tefferi A, Pardanani A. Serious adverse events during ruxolitinib treatment discontinuation in patients with myelofibrosis. Mayo Clin Proc. 2011 Dec;86(12):1188-91. Epub 2011 Oct 27. PubMed PMID: 22034658; PubMed Central PMCID: PMC3228619.

3: Tefferi A, Litzow MR, Pardanani A. Long-term outcome of treatment with ruxolitinib in myelofibrosis. N Engl J Med. 2011 Oct 13;365(15):1455-7. PubMed PMID: 21995409.

4: Ostojic A, Vrhovac R, Verstovsek S. Ruxolitinib: a new JAK1/2 inhibitor that offers promising options for treatment of myelofibrosis. Future Oncol. 2011 Sep;7(9):1035-43. PubMed PMID: 21919691.

5: Naqvi K, Verstovsek S, Kantarjian H, Ravandi F. A potential role of ruxolitinib in leukemia. Expert Opin Investig Drugs. 2011 Aug;20(8):1159-66. doi: 10.1517/13543784.2011.589383. Epub 2011 Jun 3. Review. PubMed PMID: 21635221.

6: Shi JG, Chen X, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, McKeever EG Jr, Punwani NG, Williams WV, Yeleswaram S. The Effect of CYP3A4 Inhibition or Induction on the Pharmacokinetics and Pharmacodynamics of Orally Administered Ruxolitinib (INCB018424 Phosphate) in Healthy Volunteers. J Clin Pharmacol. 2011 May 20. [Epub ahead of print] PubMed PMID: 21602517.

7: Mesa RA. Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis. IDrugs. 2010 Jun;13(6):394-403. PubMed PMID: 20506062.