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[摘要]：Ruxolitinib (INCB-018424) is a selective tyrosine-protein kinase JAK1 and JAK2 inhibitor that acts by blocking the JAK/STAT pathway, which plays a key role in the signaling of many cytokines and growth factors involved in cellular proliferation, growth and hematopoiesis. Ruxolitinib is being developed as an oral formulation for the treatment of several diseases, showing a good safety profile without off-target toxicities. The compound showed promising results in early clinical studies in myeloproliferative neoplasms and is currently in phase III clinical development for the treatment of myelofibrosis, either primary or secondary to polycythemia or essential thrombocythemia. Ruxolitinib is also being evaluated in phase clinical trials for the treatment of polycythemia vera, essential thrombocythemia and secondary, post-myeloproliferative disorder acute myeloid leukemia. Its potential efficacy is being tested in other leukemias, as well as in prostate cancer and multiple myeloma. This novel JAK1/2 inhibitor is also being used topically for the treatment of psoriasis in phase II studies, and it was studied for the treatment of rheumatoid arthritis but development in this indication has been discontinued. |
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