Epacadostat
Chemical compound
From Wikipedia, the free encyclopedia
Epacadostat (previously INCB24360) is an investigational drug for cancer.[1] Epacadostat is an inhibitor of indoleamine 2,3-dioxygenase-1 (IDO1).[1][2][3] Epacadostat inhibits IDO1 by competitively blocking it, without interfering with IDO2 or tryptophan 2,3-dioxygenase (TDO). It has antitumor activity in some models, though is most effective when combined with other immunotherapy agents.[4]
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| Formula | C11H13BrFN7O4S |
| Molar mass | 438.23 g·mol−1 |
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History and clinical trials
As of 2017, the combination of epacadostat with pembrolizumab (Keytruda) was being investigated by Incyte and Merck & Co. in several cancers, as was the combination of epacadostat with nivolumab (Opdivo) by Incyte and Bristol Myers Squibb.[5]
In April 2018, Incyte announced they were halting the Phase III ECHO-301/KEYNOTE-252 (NCT02752074) trial of epacadostat with pembrolizumab for melanoma as the combination therapy missed the first primary endpoint of improving progression-free survival vs. pembrolizumab alone.[6][7] The second primary endpoint of overall survival is not yet determined.[6]