Ruxolitinib is an anti-tumor drug for the treatment of myeloproliferative neoplasm-associated myelofibrosis, further myeloproliferative neoplasms, polycythemia vera and refractory cancer.
Ruxolitinib (INCB18424) is potent, selective JAK1 and JAK2 inhibitors (IC50 2.7 and 4.5nM, respectively) have potent anti-tumor and immunomodulatory activities. Ruxolitinib inhibited IL-6 signal (IC50 = 281nM) and JAK2V617F Ba/F3 cell proliferation (IC50 = 127nM). Ruxolitinib also inhibited STAT3 phosphorylation in wild-type JAK2 and JAK2 V617F mutant patients. Clinical application it can significantly reduce the level of circulating inflammatory cytokines related. ruxolitinib has a potent effect in rat adjuvant arthritis and multiple Murine Arthritis models.
Ruxolitinib is a kinase inhibitor indicated for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, myelofibrosis after polycythemia vera and myelofibrosis after essential thrombocythemia.
