Synonyms: BMS-986205 | BMS986205 | Compound 2 [PMID: 29531094] | Example 19 [US20160137652A1]
Compound class:
Synthetic organic
Comment: Linrodostat (BMS-986205) is a potent and selective, orally available indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor [3], being investigated as an immuno-therapeutic for various malignancies. The INN for linrodostat specifies the (R) stereoisomer. The chemical structure is claimed as example 19 in Flexus Bioscience's patent US2016137652 [1] and the compound is being taken through clinical development by Bristol-Myers Squibb. Mechanistically, linrodostat competes with the heme cofactor for binding to the apo-form of the enzyme, and once bound prevents heme from rebinding [3].
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Immunopharmacology Comments |
BMS-986205 is an immuno-therapy clinical candidate that targets IDO1, an enzyme that is an important drug target in cancer therapeutic development [2]. IDO1 inhibition restores and promotes the proliferation and activation of various immune cells, thereby circumventing the IDO1-induced immunosuppression in the tumour micorenvironment that facilitates tumour cell immune evasion. |