Elucidating the structure and cytochrome P450-mediated mechanism for novel metabolites of GDC-0575 in rats

Chenghong Zhang, Sungjoon Cho, José G. Napolitano, David Russell, Christine Gu, Alan Deese, Chong Han, Yuan Chen & Shuguang Ma
1. GDC-0575 is an ATP-competitive small-molecule inhibitor of ChK1 that is being developed by Genentech for the treatment of various human malignancies. 2. In a radiolabeled mass balance study of GDC-0575 in rats, two novel metabolites, named M12 (-71 Da,) and M17 (+288 Da), were detected as abundant circulating metabolites. 3. Subsequent mass spectrometry and nuclear magnetic resonance analysis showed that M12 was a cyclized metabolite of GDC-0575, whereas M17 was its heterodimer to the...
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