Table 2.
Summary of pharmacokinetic parameters for the direct-acting antivirals approved by the US Food and Drug Administration and European Medicines Agency
| Drug | tmax (h) | Cmax (ng/mL) | Cmin (ng/mL) | AUC (ng∙h/mL) | Vd/F | t½ (h) | Protein binding (%) | References |
|---|---|---|---|---|---|---|---|---|
| Protease inhibitors | ||||||||
| Glecaprevir | 5.0 | 597 | NR | 4800 | NR | 6–9 | 97 | [6, 20] |
| Grazoprevir | 2 | 165 | 18.0 | 1420 | 1250 | 24 | > 98.8 | [17, 18] |
| Voxilaprevir | 4 | 192 | 47 | 2577 | NR | 33 | > 99 | [8, 21] |
| NS5A inhibitors | ||||||||
| Daclatasvir | 1–2 | 1534 | 232 | 14,122 | 47 | 12–15 | ± 99 | [9, 10] |
| Elbasvir | 3 | 121 | 48.4 | 1920 | 680 | 31 | > 99.9 | [17, 18] |
| Ledipasvir | 4.0 | 323 | NR | 7290 | 47 | > 99.8 | [15, 16] | |
| Pibrentasvir | 5.0 | 110 | NR | 1430 | NR | 23–29 | > 99.9 | [6, 20] |
| Velpatasvir (Epclusa®) | 3 | 259 | 51 | 2970 | NR | 15 | > 99.5 | [7, 19] |
| Velpatasvir (Vosevi®) | 4 | 311 | NR | 4041 | NR | 17 | > 99 | [8, 21] |
| NS5B inhibitors | ||||||||
| Sofosbuvir/GS-331007 (Sovaldi®) | 0.5–2/2 | NR | NR | 1010/7200 | NR | 0.4/27 | 61–65/minimal | [11, 12] |
| Sofosbuvir/GS-331007 (Harvoni®) | ~ 1/4 | 618/707 | NR | 1320/12,000 | NR | 0.5/27 | 61–65/minimal | [15, 16] |
| Sofosbuvir/GS-331007 (Epclusa®) | 0.5–1/3 | 566/868 | NR | 1260/13,970 | NR | 0.5/25 | 61–65/minimal | [7, 19] |
| Sofosbuvir/GS-331007 (Vosevi®) | 2/4 | 678/744 | NR | 1665/12,834 | NR | 0.5/29 | 61–65/minimal | [8, 21] |
Primary data were used from the SmPC and FDA prescribing information concerning HCV-infected patients without cirrhosis
AUC area under the concentration–time curve, Cmax maximal plasma concentration, Cmin minimal plasma concentration, FDA US Food and Drug Administration, NR data were not reported and/or available in the SmPC and FDA prescribing information, SmPC Summary of Product Characteristics, t½ elimination half-life, tmax time to maximal plasma concentration, Vd/F volume of distribution