<"And our recently acquired JAK 1, 2 inhibitor Momelotinib has been successfully reformulated and we’re currently in discussions with regulatory authorities regarding the specifics of the myelofibrosis Phase 3 program."
reformulated - - what up with that?>
Momelotinib or Cyt-387 is N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl) phenyl] amino]-4-pyrimidinyl] benzamide; N-(cyanopyrimidin-4-yl) benzamide, according to my sleuthing on the JAK1/2 inhibitor space. It has a CAS # as follows: 1056634-68-4.
Note that the following statements are my opinion and I may be wrong on certain points.
This compound is orange in color, and although Cytopia did not present data on its initial formulation in the clinic, I would bet that it was delivered to patients in a capsule to allow for the initial clinical studies to be adequately blinded. I do not know the metabolic stream or whether it is passed in the urine as a colored substance. ( I have had past experience with colored compound(s) and they are a pain in the axx for clinical trial blinding, especially if they excreted via the kidney as the unmetabolized drug substance, obviously.) I suspect Cytopia was most interested in Ph2 proof of concept and did not have the pharmaceutical sciences expertise to deal with formulating the compound in a pill form.
Obviously GILD has mucho experience in formulation and tableting of drug substances. They would want to have close to the final drug substance, if not the final form - presumably as a tablet, for the Ph3 program. So, that may be the "what up with that."
Here is some other info on momelotinib, including a PhD thesis on this compound on mutated forms of JAK2 and the effects of various JAK inhibitors on the wild type and mutant forms.
ht tp://mpnforum.com/the-senyak-report-june-2013/
tspace.library.utoronto.ca.?
I am not sure the above will open as the link provided, but if you google CYT-387 you should come up with the Michael Marit PhD thesis from the University of Toronto. |
