Ruxolitinib phosphateProduct ingredient forRuxolitinib

Ruxolitinib, formerly known as INCB018424 or INC424, is an anticancer drug and a Janus kinase (JAK) inhibitor. It is a potent and selective inhibitor of JAK1 and JAK2,³which are tyrosine kinases involved in cytokine signalling and hematopoiesis.²骨髓增殖性肿瘤,如myelofibrosis and polycythemia vera, are often characterized by aberrant activation of the JAK-STAT pathway, leading to abnormal blood cell counts and thrombotic complications. By inhibiting JAK1 and JAK2, ruxolitinib works to block the dysregulated cell signalling pathways and prevents abnormal blood cell proliferation.⁵Due to a large number of patients with myeloproliferative neoplasms who have JAK2 mutations, ruxolitinib was the first ATP-competitive inhibitor of JAK1 and JAK2 ever developed.¹⁵

Ruxolitinib was first approved for the treatment of adult patients with myelofibrosis by the FDA in 2011, followed by EMA's approval in 2012.⁵In 2014, it was approved for the treatment of polycythemia vera in adults who have an inadequate response to or are intolerant ofhydroxyureaand in 2019, ruxolitinib was approved for use in steroid-refractory acute graft-versus-host disease in adults and children.¹⁹The topical formulation of ruxolitinib is used to treat atopic dermatitis and vitiligo.²³It is being investigated for other inflammatory skin conditions.¹²

Ruxolitinib has been investigated to treat patients with coronavirus disease 2019 (COVID-19) accompanied by severe systemic hyperinflammation. In phase II clinical trials, ruxolitinib improved chest computed tomography and improved recovery in patients with lymphopenia.^6,7However, phase III clinical trials later determined that ruxolitinib was inadequate in meeting its primary endpoint of reducing the number of hospitalized COVID-19 patients who experienced severe complications²⁰thus the drug was not approved as a treatment for COVID-19.

PubChem Compound

25127112

ChemSpider

26286920

ChEBI

66917

ChEMBL

CHEMBL1795071

Wikipedia

Ruxolitinib