Ruxolitinib
(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile,
| CAS number | 941678-49-5 |
|---|
Incyte Corporation (Nasdaq: INCY) announced today that several analyses from clinical studies of Jakafi® (ruxolitinib) will be presented at the 2012 American Society of Hematology (ASH) Annual Meeting from Dec. 8 to 11 , 2012 at the Georgia World Congress Center in Atlanta. Jakafi, an oral Janus kinase (JAK) inhibitor, is FDA-approved for the treatment of patients with intermediate or high-risk myelofibrosis (MF).
Ruxolitinib (trade names Jakafi and Jakavi, by Incyte Pharmaceuticals and Novartis) is a drug for the treatment of intermediate or high-risk myelofibrosis, a type of bone marrow cancer.[2] It is also being investigated for the treatment of other types of cancer (such as lymphomas and pancreatic cancer),[3] for polycythemia vera,[3] and for plaque psoriasis.
The phase III Controlled Myelofibrosis Study with Oral JAK Inhibitor-I (COMFORT-I) and COMFORT-II trials showed significant benefits by reducing spleen size, relieving debilitating symptoms, and improving overall survival.[4][5][6][7]
Ruxolitinib is a Janus kinase inhibitor with selectivity for subtypes 1 and 2 of this enzyme.[8][9]
In November 2011, ruxolitinib was approved by the USFDA for the treatment of intermediate or high-risk myelofibrosis based on results of the COMFORT-I and COMFORT-II Trials.[10]
Some analysts believe this to be a potential blockbuster drug.[3] As of the end of March 2012, and according to an Incyte spokesman, approximately 1000 physicians had prescribed the drug in the United States, out of a total 6500 hematologists and oncologists nationwide.[3]
References
- Shilling, A. D.; Nedza, F. M.; Emm, T.; Diamond, S.; McKeever, E.; Punwani, N.; Williams, W.; Arvanitis, A. et al. (2010). “Metabolism, Excretion, and Pharmacokinetics of [14C]INCB018424, a Selective Janus Tyrosine Kinase 1/2 Inhibitor, in Humans”. Drug Metabolism and Disposition 38 (11): 2023. doi:10.1124/dmd.110.033787. PMID 20699411. edit
- Mesa, Ruben A.; Yasothan, Uma; Kirkpatrick, Peter (2012). “Ruxolitinib”. Nature Reviews Drug Discovery 11 (2): 103–4. doi:10.1038/nrd3652. PMID 22293561.
- Natoli, Cori Anne (May 5, 2012), “Incyte looks to ride on drug's success”, The News Journal, http://www.delawareonline.com/article/20120506/BUSINESS/205060304/Incyte-looks-to-ride-on-drug-s-success, retrieved May 6, 2012
- Harrison, C.; Kiladjian, J. J.; Al-Ali, H. K.; Gisslinger, H.; Waltzman, R.; Stalbovskaya, V.; McQuitty, M.; Hunter, D. S. et al. (2012). “JAK Inhibition with Ruxolitinib versus Best Available Therapy for Myelofibrosis”. New England Journal of Medicine 366 (9): 787–798. doi:10.1056/NEJMoa1110556. PMID 22375970. edit
- Verstovsek, S.; Mesa, R. A.; Gotlib, J.; Levy, R. S.; Gupta, V.; Dipersio, J. F.; Catalano, J. V.; Deininger, M. et al. (2012). “A Double-Blind, Placebo-Controlled Trial of Ruxolitinib for Myelofibrosis”. New England Journal of Medicine 366 (9): 799–807. doi:10.1056/NEJMoa1110557. PMID 22375971. edit
- Tefferi, A. (2012). “Challenges Facing JAK Inhibitor Therapy for Myeloproliferative Neoplasms”. New England Journal of Medicine 366 (9): 844–846. doi:10.1056/NEJMe1115119. PMID 22375977. edit
- ASCO Annual Meeting 2011: JAK Inhibitor Ruxolitinib Demonstrates Significant Clinical Benefit in Myelofibrosis
- Mesa, RA (2010). “Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis”. IDrugs : the investigational drugs journal 13 (6): 394–403. PMID 20506062. edit
- Pardanani, A.; Tefferi, A. (2011). “Targeting myeloproliferative neoplasms with JAK inhibitors”. Current Opinion in Hematology 18 (2): 1. doi:10.1097/MOH.0b013e3283439964. PMID 21245760. edit
- “FDA Approves Incyte's Jakafi(TM) (ruxolitinib) for Patients with Myelofibrosis” (Press release). Incyte. http://investor.incyte.com/phoenix.zhtml?c=69764&p=irol-newsArticle&ID=1631201&highlight=. Retrieved 2012-01-02.
