BMS-986094 is an orally available prodrug of nucleotide analogue 2′-C-methylguanosine that potently inhibits Hepatitis C virus (HCV) replication. It is a guanosine nucleotide inhibitor of HCV RNA-dependent RNA polymerase NS5b.
guanosine nucleotide inhibitor of HCV RNA-dependent RNA polymerase NS5b
β-D-2'-C-Methyl-2,6-diaminopurine ribonucleoside (2'-C-Me-DAPN) phosphoramidate prodrug (DAPN-PD) is a selective hepatitis C virus inhibitor that is metabolized intracellularly into two active metabolites: 2'-C-Methyl-DAPN triphosphate (2'-C-Me-DAPN-TP) and 2'-C-methyl-guanosine 5'-triphosphate (2'-C-Me-GTP). BMS-986094 and IDX-184 are also bioconverted to 2'-C-Me-GTP. A phase IIb clinical
Antimicrobial agents and chemotherapy, 55(5), 1843-1851 (2011-03-02)
INX-08189 is an aryl-phosphoramidate of 6-O-methyl-2'-C-methyl guanosine. INX-08189 was highly potent in replicon assays, with a 50% effective concentration of 10±6 nM against hepatitis C genotype 1b at 72 h. The inhibitory effect on viral replication was rapid, with a
Toxicological sciences : an official journal of the Society of Toxicology, 153(2), 396-408 (2016-07-29)
BMS-986094, the prodrug of a guanosine nucleotide analogue (2'-C-methylguanosine), was withdrawn from clinical trials due to serious safety issues. Nonclinical investigative studies were conducted as a follow up to evaluate the potential for BMS-986094-related mitochondrial-toxicity. In vitro, BMS-986094 was applied
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