Ruxolitinib

Ruxolitinib is the first clinically applied, potent, and selective JAK1/2 inhibitor for the treatment of myeloproliferative disorders. As a selective JAK1/2 inhibitor, Ruxolitinib suppresses erythroid progenitor colony formation in polycythemia vera patients with the constitutively active JAK2 V617F mutation and reduces malignant cell proliferation. The compound also decreases interleukin 6 and TNF‑α signaling in JAK2 V617F‑driven mouse models. Ruxolitinib is FDA‑approved for intermediate or high‑risk myelofibrosis and polycythemia vera when there has been an inadequate response to or intolerance of hydroxyurea. As a high‑purity reference standard, Ruxolitinib is indispensable for analytical method development, impurity profiling, quality control testing, and ANDA filings for generic ruxolitinib manufacturers. Additionally, Ruxolitinib serves as a critical tool compound for studying JAK‑STAT signaling pathways and developing novel JAK inhibitor therapies.

 

 Product Parameters

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Parameter	Specification
Product Name	Ruxolitinib
CAS Number	941678-49-5
Molecular Formula	C₁₇H₁₈N₆
Molecular Weight	306.37 g/mol
Appearance	White to offwhite solid
Melting Point	90-100°C
Density	1.4
Storage Condition	−20°C for longterm storage

 

Pharmacological Action

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Myelofibrosis (MF) is a rare myelodysplastic disorder characterized by the replacement of bone marrow tissue with scar tissue, leading to hematopoiesis in organs such as the liver and spleen. Its clinical manifestations include splenomegaly, anemia, leukopenia and thrombocytopenia, as well as varying degrees of bone sclerosis. Symptoms may also encompass fatigue, abdominal discomfort, subcostal pain, musculoskeletal pain, pruritus, and night sweats.

 

Ruxolitinib is the first oral medication approved by the U.S. Food and Drug Administration (FDA) for the treatment of myelofibrosis. It is a tyrosine kinase inhibitor, specifically a small-molecule inhibitor targeting protein kinases JAK1 and JAK2, indicated for intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thromostosis myelofibrosis.

 

On August 29,2012, the European Union approved ruxolitinib, the first drug approved for the treatment of myelofibrosis. Ruxolitinib is indicated for intermediate-or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-thrombocythemia primary myelofibrosis. Currently, ruxolitinib has been approved in more than 50 countries worldwide, including the European Union, Canada, and several countries in Asia, Latin America, and South America.

 

Novartis Pharmaceuticals in the United States has obtained authorization from Incyte to develop and commercialize ruxolitinib outside the U.S. Both the European Commission and the FDA have granted ruxolitinib orphan drug status for the treatment of myelofibrosis. Currently, Incyte sells ruxolitinib in the United States under the brand name Jakafi for the treatment of intermediate or high-risk myelofibrosis.

 

Current Application Status

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Ruxolitinib (also known as LUX) is a kinase inhibitor indicated for the treatment of intermediate-or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia myelofibrosis, and post-thrombocytosis myelofibrosis. Ruxolitinib (Jakavi) is an oral JAK1 and JAK2 tyrosine kinase inhibitor approved by the European Union in August 2012 for the management of intermediate-or high-risk myelofibrosis.

Currently, ruxolitinib Jakavi has been approved in over 50 countries worldwide, including the European Union, Canada, and several countries in Asia, Latin America, and South America. Novartis has licensed the development and commercialization rights for ruxolitinib outside the United States from Incyte. Both the European Commission and the FDA have granted ruxolitinib orphan drug status for the treatment of myelofibrosis. In the United States, Incyte currently sells ruxolitinib under the brand name Jakafi for the treatment of intermediate or high-risk myelofibrosis.

Bioactivity

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Ruxolitinib (INCB18424) is a potent, selective inhibitor of JAK1 and JAK2 (IC50 values of 2.7 nM and 4.5 nM, respectively), exhibiting strong antitumor and immunomodulatory activities. Ruxolitinib inhibits IL-6 signaling (IC50 = 281 nM) and the proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM). It also suppresses STAT3 phosphorylation in patients with wild-type JAK2 or JAK2V617F mutations. Its clinical efficacy is attributed to its significant reduction of circulating inflammatory cytokine levels. Ruxolitinib demonstrates therapeutic effects in rat models of adjuvant-induced arthritis and polyarticular arthritis.

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