Momelotinib (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
, formerly GS-0387, CYT-387) 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 (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 thrombocythemia myelofibrosis (post-PV/ET MF), as well as a treatment for relapsed or refractory metastatic
pancreatic ductal adenocarcinoma (in combination with
capecitabine and
oxaliplatin
Oxaliplatin, sold under the brand name Eloxatin among others, is a cancer medication (platinum-based antineoplastic class) used to treat colorectal cancer. It is given by injection into a vein.
Common side effects include numbness, feeling ti ...
).
Discovery
The drug was originally discovered by
Australia
Australia, officially the Commonwealth of Australia, is a Sovereign state, sovereign country comprising the mainland of the Australia (continent), Australian continent, the island of Tasmania, and numerous List of islands of Australia, sma ...
n drug discovery company Cytopia, then developed by
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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