momelotinib

Momelotinib is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC₅₀ values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3. As of 2011, momelotinib is being developed as a drug for myelofibrosis and currently undergoes Phase I/II clinical trials. Additional potential treatment indications for momelotinib include other myeloproliferative neoplasms, cancer and inflammatory conditions. As of 2016, momelotinib is being investigated for primary myelofibrosis or post-polycythemia vera or post-essential thrombocythemia myelofibrosis, as well as a treatment for relapsed or refractory metastatic pancreatic ductal adenocarcinoma.