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Standard assays have failed to detect significant anti-HIV activity of entecavir at clinically meaningful concentrations. However, selection for the HIV M184V mutation and reduction in HIV viral load have been reported with this drug in patients who were coinfected with hepatitis B virus (HBV) and HIV. To provide insight, pharmaceutical-industry researchers examined the in vitro anti-HIV activity of entecavir under a variety of conditions and compared the results of several assays.
Entecavir had weak activity against HIV under standard assay conditions. However, in contrast to drugs used to treat HIV, it showed significantly increased antiviral activity under conditions of low viral inoculum. The M184V mutation lowered the susceptibility of …