Display options
Cite
Yue EW, Sparks R, Polam P, et al. INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology. ACS Med Chem Lett. 2017;8(5):486-491doi: 10.1021/acsmedchemlett.6b00391.
Yue, E. W., Sparks, R., Polam, P., Modi, D., Douty, B., Wayland, B., Glass, B., Takvorian, A., Glenn, J., Zhu, W., Bower, M., Liu, X., Leffet, L., Wang, Q., Bowman, K. J., Hansbury, M. J., Wei, M., Li, Y., Wynn, R., Burn, T. C., Koblish, H. K., Fridman, J. S., Emm, T., Scherle, P. A., Metcalf, B., & Combs, A. P. (2017). INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology. ACS medicinal chemistry letters, 8(5), 486-491. https://doi.org/10.1021/acsmedchemlett.6b00391
Yue, Eddy W, et al. "INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology." ACS medicinal chemistry letters vol. 8,5 (2017): 486-491. doi: https://doi.org/10.1021/acsmedchemlett.6b00391
Yue EW, Sparks R, Polam P, Modi D, Douty B, Wayland B, Glass B, Takvorian A, Glenn J, Zhu W, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Emm T, Scherle PA, Metcalf B, Combs AP. INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology. ACS Med Chem Lett. 2017 Mar 06;8(5):486-491. doi: 10.1021/acsmedchemlett.6b00391. eCollection 2017 May 11. PMID: 28523098; PMCID: PMC5430407.
Copy Download .nbib Format: NLM
Share it on

ACS Med Chem Lett. 2017 Mar 06;8(5):486-491. doi: 10.1021/acsmedchemlett.6b00391. eCollection 2017 May 11.

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.

ACS medicinal chemistry letters

Eddy W Yue, Richard Sparks, Padmaja Polam, Dilip Modi, Brent Douty, Brian Wayland, Brian Glass, Amy Takvorian, Joseph Glenn, Wenyu Zhu, Michael Bower, Xiangdong Liu, Lynn Leffet, Qian Wang, Kevin J Bowman, Michael J Hansbury, Min Wei, Yanlong Li, Richard Wynn, Timothy C Burn, Holly K Koblish, Jordan S Fridman, Tom Emm, Peggy A Scherle, Brian Metcalf, Andrew P Combs

Affiliations

  1. Incyte Corporation, 1801 Augustine Cut-Off, Wilmington, Delaware 19803, United States.

PMID: 28523098 PMCID: PMC5430407 DOI: 10.1021/acsmedchemlett.6b00391

Abstract

A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor

Keywords: Epacadostat; IDO1; INCB24360; data-centric medicinal chemistry; immuno-oncology

References

  1. Nat Rev Cancer. 2015 Aug;15(8):457-72 - PubMed
  2. Mol Cancer Ther. 2010 Feb;9(2):489-98 - PubMed
  3. Nat Med. 2003 Oct;9(10):1269-74 - PubMed
  4. J Clin Invest. 2007 May;117(5):1147-54 - PubMed
  5. Science. 1998 Aug 21;281(5380):1191-3 - PubMed
  6. Amino Acids. 2013 Dec;45(6):1319-29 - PubMed
  7. Cancer Immunol Immunother. 2010 Nov;59(11):1655-63 - PubMed
  8. J Exp Med. 2013 Jul 1;210(7):1389-402 - PubMed
  9. ChemMedChem. 2016 Jul 19;11(14):1576 - PubMed
  10. Curr Drug Metab. 2008 Jan;9(1):39-45 - PubMed
  11. N Engl J Med. 2010 Aug 19;363(8):711-23 - PubMed
  12. Trends Mol Med. 2004 Jan;10(1):15-8 - PubMed
  13. Curr Cancer Drug Targets. 2009 Dec;9(8):938-52 - PubMed
  14. Nat Rev Drug Discov. 2015 Sep;14 (9):603-22 - PubMed
  15. J Med Chem. 2002 Jun 6;45(12):2615-23 - PubMed
  16. Biochem Biophys Res Commun. 2005 Dec 9;338(1):12-9 - PubMed
  17. Cancer Res. 2007 Jan 15;67(2):792-801 - PubMed
  18. N Engl J Med. 2015 Jun 25;372(26):2521-32 - PubMed
  19. Int J Biochem Cell Biol. 2009 Mar;41(3):467-71 - PubMed
  20. Nat Rev Drug Discov. 2014 Feb;13(2):105-21 - PubMed
  21. J Med Chem. 2009 Dec 10;52(23):7364-7 - PubMed
  22. J Immunother Cancer. 2014 Feb 18;2:3 - PubMed
  23. Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502 - PubMed
  24. J Pharmacol Exp Ther. 1997 Oct;283(1):46-58 - PubMed
  25. Adv Drug Deliv Rev. 2001 Mar 1;46(1-3):3-26 - PubMed
  26. Clin Cancer Res. 2014 Dec 15;20(24):6258-68 - PubMed
  27. J Reprod Immunol. 2004 Apr;61(2):67-77 - PubMed
  28. N Engl J Med. 2015 Jul 2;373(1):23-34 - PubMed
  29. J Immunol. 2006 Oct 15;177(8):5639-46 - PubMed
  30. Blood. 2010 Apr 29;115(17):3520-30 - PubMed
  31. Cancer Res. 2007 Aug 1;67(15):7082-7 - PubMed
  32. Xenobiotica. 2005 Jan;35(1):17-25 - PubMed
  33. Front Immunol. 2014 Nov 20;5:585 - PubMed

Publication Types