Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors.

@article{Koblish2010HydroxyamidineIO,
  title={Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors.},
  author={Holly Kurzawa Koblish and Michael J. Hansbury and Kevin J. Bowman and Gengjie Yang and Claire L. Neilan and Patrick J. Haley and Timothy C. Burn and Paul Waeltz and Richard B. Sparks and Eddy W. Yue and Andrew P. Combs and Peggy A. Scherle and Kris Vaddi and Jordan S. Fridman},
  journal={Molecular cancer therapeutics},
  year={2010},
  volume={9 2},
  pages={489-98}
}
Malignant tumors arise, in part, because the immune system does not adequately recognize and destroy them. Expression of indoleamine-2,3-dioxygenase (IDO; IDO1), a rate-limiting enzyme in the catabolism of tryptophan into kynurenine, contributes to this immune evasion. Here we describe the effects of systemic IDO inhibition using orally active hydroxyamidine small molecule inhibitors. A single dose of INCB023843 or INCB024360 results in efficient and durable suppression of Ido1 activity in the… CONTINUE READING