Table 4 Anti-tumor performance of epacadostat in preclinical studies

CT26 colon carcinoma

34 % ^a at 30 mg/kg BID

57 % ^a at 100 mg/kg BID

Activity of tumor infiltrating lymphocytes increased

[65]

PAN02 pancreatic adenocarcinoma

37 % ^a at 25 mg/kg BID

57 % ^a at 100 mg/kg BID

-

[79]

CT26 colon carcinoma

47.5 % ^b at 100 mg/kg BID

-

[87]

Lewis lung carcinoma

51 % ^c at 80 mg/kg daily

Intratumoural ratio of CD4 effector T cells to Tregs elevated

[88]

B16F10 melanoma

50 % ^c at 80 mg/kg daily

Intratumoural ratio of CD4 effector T cells to Tregs elevated

[88]

Lewis lung carcinoma

68 % ^d at 60 mg/kg daily

Intratumoural ratio of CD4 effector T cells to Tregs elevated

[89]

CT26 colon carcinoma

23.4 % ^b at 100 mg/kg BID

-

[90]

RIL-175 hepatocellular carcinoma

Significant tumor reduction when combined with anti-PD-1, not significant at 300 mg/kg as single agent

-

[83]

MMTV-Neu breast cancer

Tumor growth inhibition enhanced when combined with lapatinib and BMS777607 (MerTK inhibitor), not significant reduction at 20 mg/kg as single agent

-

[81]

B16F10 melanoma

Significant tumor reduction when combined with agonistic CD40 antibody, not significant reduction at 100 mg/kg as single agent

Percentage of CD8⁺ CD107a⁺ effector T cells in tumor increased

[82]

B16SIY melanoma

Complete responders found when combined with αCTLA-4 (3/16) and αPD-L1 (2/15) ^e

Frequency of tumor-reactive T cells in tumor-draining lymph nodes and spleen not substantially increased

[80]