TABLE 6.
Relative rate of incorporation of the active triphosphate metabolite GS-443902 by human mitochondrial DNA and RNA polymerases
| Clinical compound | Nucleotide triphosphate | Rate of incorporation (% of natural dNTP or NTP)a |
|
|---|---|---|---|
| DNA polymerase γ | mtRNA polymerase | ||
| RDV | GS-443902 | 0% | 5.8% ± 1.4% |
| Decitabine | 5-aza-2′-dCTP | 79% ± 8% | ND |
| BMS-986094 | 2’CMe-GTP | ND | 92% ± 33% |
| Balapiravir/RG1626 | 4’CN-CTP | ND | 112% ± 10% |
a
The rate of single nucleotide incorporation was measured in the presence of 50 μM nucleotide analog for DNA Pol γ and 500 μM for POLRMT and expressed as the % of the natural dNTP or NTP incorporation at the same concentration. Data are presented as the average ± SD from three or more independent experiments. ND, not done.