Synonyms: compound 2c [PMID: 28613862] | Example 1166 [WO2015160641A2]
Compound class:
Synthetic organic
Comment: BMS-1166 is a small molecule that disrupts the PD-1/PD-L1 immune checkpoint interaction. It is the most potent of the [3-(2,3-Dihydro-1,4-benzodioxin-6-yl)-2-methylphenyl]methanol derivatives described in [2], and it is claimed as Example 1166 in Bristol-Myers Squibb's patent WO2015160641A2 [1]. NMR analysis suggests that BMS-1166 promotes the formation of dimeric PD-L1 in solution.
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Immunopharmacology Comments |
Small molecule checkpoint inhibitors are being developed as complementary and potentially synergistic therapeutics to the currently approved monoclonal antibodies used to inhibit the PD-1/PD-L1 checkpoint in immuo-oncology applications. Inhibitors of the PD-1/PD-L1 immune checkpoint functionally alleviate the PD-L1-induced exhaustion of T cells and re-instate effector cell-mediated tumour elimination, be they small molecules like BMS-1166 and BMS-1001 [3], or monoclonal antibodies like atezolizumab, durvalumab, pembrolizumab or nivolumab. |