Momelotinib (International Nonproprietary Name, INN, formerly GS-0387, CYT-387) is an Janus kinase inhibitor, inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50, IC
50 values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC
50 = 0.16 ''μ''M).
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 (solid and liquid tumors) and inflammatory conditions.
As of 2016, momelotinib is being investigated for primary myelofibrosis or post-polycythemia vera or post-Essential thrombocytosis, essential thrombocythemia myelofibrosis (post-PV/ET MF), as well as a treatment for relapsed or refractory metastatic Pancreatic cancer, pancreatic ductal adenocarcinoma (in combination with capecitabine and oxaliplatin).
Discovery
The drug was originally discovered by Australian drug discovery company Cytopia, then developed by YM Biosciences, YM BioSciences Inc. (since acquired by Gilead Sciences as of 2013).
References
External links
www.ymbiosciences.com* https://oncologytube.com/video/41076/momelotinib-a-jak-inhibitor-vs-danazol-in-myelofibrosis?channelName=EHA
Benzamides
4-Morpholinyl compunds
Nitriles
Non-receptor tyrosine kinase inhibitors
Protein kinase inhibitors
Aminopyrimidines
Experimental cancer drugs
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