Description:
IC50 Value: 5.1±1.2 nM (EC50, HCMV-AD169 strain, CPE reduction assay) [1]
AIC246 is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors. AIC246 exhibits outstanding anti-HCMV activity in vitro and in vivo and currently is undergoing a clinical phase IIb trial.
in vitro: AIC246 blocks viral replication without inhibiting the synthesis of progeny HCMV DNA or viral proteins. Marker transfer analyses confirmed that these mutations were sufficient to mediate AIC246 resistance. The mapping of drug resistance to open reading frame UL56 suggests that viral DNA processing and/or packaging is targeted by AIC246. In line with this, we demonstrate that AIC246 affects the formation of proper unit-length genomes from viral DNA concatemers and interferes with virion maturation [2]. he anti-HCMV activity of AIC246 was evaluated in vitro and in vivo using various c