linrodostat

Linrodostat (BMS-986205) is an orally bioavailable, potent, and selective small molecule inhibitor of the enzyme indoleamine 2,3-dioxygenase 1 (IDO1). Developed by Bristol Myers Squibb following its acquisition of Flexus Biosciences, linrodostat is designed to reverse tumor-mediated immunosuppression. IDO1 is a key enzyme that catalyzes the degradation of the essential amino acid tryptophan into kynurenine; tumors often overexpress IDO1 to create a tryptophan-depleted and kynurenine-rich microenvironment that inhibits T-cell function and promotes immune evasion. By selectively inhibiting IDO1, linrodostat restores T-cell activity and enhances the anti-tumor immune response. It has been extensively evaluated in Phase 1 and Phase 2 clinical trials, primarily in combination with immune checkpoint inhibitors such as nivolumab (anti-PD-1) and ipilimumab (anti-CTLA-4), for the treatment of various advanced solid tumors, including melanoma, non-small cell lung cancer, and bladder cancer.

Brand names

linrodostat

Other names

linrodostat mesylate