Drug intelligence / Profile preview

Y-320

Development stage
Discontinued
Lead developer
Mitsubishi Tanabe Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Y-320 is an orally active, small-molecule immunomodulator originally developed by Mitsubishi Tanabe Pharma for the treatment of rheumatoid arthritis. It was initially identified as a potent inhibitor of interleukin-17 (IL-17) production in T cells stimulated with interleukin-15 (IL-15). More recent research has revealed that Y-320 acts as an allosteric inhibitor of the stimulator of interferon genes (STING) protein, binding to its transmembrane domain to block Golgi translocation and downstream interferon signaling. Additionally, Y-320 has been shown to function as a potent pan-sialylation inhibitor by directly binding and inhibiting key sialyltransferases (such as ST3Gal1, ST3Gal2, and ST6GalNAc2), which suppresses tumor-specific sialic acid levels and enhances antitumor immunity in models of pancreatic ductal adenocarcinoma. Y-320 also acts as a substrate and inhibitor of P-glycoprotein (P-gp), reversing multidrug resistance in cancer cells.

Other names
1-(4-chlorophenyl)-N-[3-cyano-4-[4-(4-morpholinyl)-1-piperidinyl]phenyl]-5-methyl-1H-pyrazole-4-carboxamide1-(4-chlorophenyl)-N-[3-cyano-4-(4-morpholin-4-ylpiperidin-1-yl)phenyl]-5-methylpyrazole-4-carboxamide
02

Targets

Glycosylation (Glycosylation enzymes)ST (ST8 alpha-N-acetyl-neuraminide alpha-2,8-sialyltransferase 4)STING (Stimulator of interferon genes protein)

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