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BMS-986251 (Bristol Myers Squibb)
- Development stage
- Discontinued
- Lead developer
- Bristol Myers Squibb
- Modality
- Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous
01
Overview
BMS-986251 (formerly IONIS-IDO1Rx) is an antisense oligonucleotide (ASO) designed to selectively inhibit the expression of indoleamine 2,3-dioxygenase 1 (IDO1). IDO1 is an enzyme that catalyzes the rate-limiting step of tryptophan degradation along the kynurenine pathway. In the tumor microenvironment, overexpressed IDO1 depletes tryptophan and produces kynurenine metabolites, which suppress T-cell and natural killer (NK) cell activity while promoting the differentiation of regulatory T cells (Tregs), thereby facilitating immune evasion. By binding to IDO1 mRNA and inducing its degradation via an RNase H-dependent mechanism, BMS-986251 aims to restore anti-tumor immune responses. It was developed by Ionis Pharmaceuticals in collaboration with Bristol Myers Squibb and has been investigated in clinical trials for advanced solid tumors, often in combination with checkpoint inhibitors like nivolumab.
- Other names
- indoleamine 2,3-dioxygenase 1 antisense oligonucleotidesIDO1 ASOIDO-1 ASOIDO 1 ASOIDO1 antisense oligonucleotideIDO-1 antisense oligonucleotideIDO 1 antisense oligonucleotide
02
Targets
RORγt
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