In this study, we compared the anti-tumor effects of YH29407, the best-in-class IDO1 inhibitor with improved pharmacodynamics and pharmacokinetics, with first and second-generation IDO1 inhibitors (epacadostat and BMS-986205, respectively). Our results suggest that an IDO1 inhibitor, YH29407, has enhanced PK/PD compared to previous IDO1 inhibitors by causing a change in the population of CD8 T cells including infiltrating T cells into the tumor. Ultimately, YH29407 overcame the limitations of the competing drugs and displayed potential as an immunotherapy strategy in combination with aPD-1.

almost 2 years ago

Journal • PD(L)-1 Biomarker • IO biomarker

MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • CD8 (cluster of differentiation 8) • B2M (Beta-2-microglobulin) • LCK (LCK Proto-Oncogene, Src Family Tyrosine Kinase)

linrodostat (BMS-986205) • epacadostat (INCB024360) • YH29407

over2years

Combination therapy with anti-PD-1 and YH29407, a novel IDO1 inhibitor, enhances T cell-mediated antitumor immunity in MC38 tumor-bearing mice (AACR 2022)

Taken together, we suggest that YH29407 is the best combination partner with immune checkpoint inhibitors for solid tumor.

over 2 years ago

Preclinical • Combination therapy

CD8 (cluster of differentiation 8)

linrodostat (BMS-986205) • YH29407

over3years

[VIRTUAL] YH29407, a novel IDO1 inhibitor, enhances the anti-tumor effects through increased tumor-reactive T cell functions in solid tumor (AACR 2021)

The novel IDO1 inhibitor, YH29407, with improved pharmacokinetic and pharmacodynamic profiles, showed antitumor inflammatory reprogramming leading to enhanced antitumor efficacy.

over 3 years ago

IO biomarker

IFNG (Interferon, gamma) • FASLG (Fas ligand) • MMP2 (Matrix metallopeptidase 2) • GZMB (Granzyme B)

IDO1 expression

linrodostat (BMS-986205) • epacadostat (INCB024360) • YH29407