Table 1.
Pharmaticokinetic variables of marketed statins
| Variable | Pitavastatin | Atorvastatin | Fluvastatin | Lovastatin | Pravastatin | Rosuvastatin | Simvastatin |
|---|---|---|---|---|---|---|---|
| Prodrug | No | No | No | Yes | No | No | Yes |
| Lipophilcity (log P) | 1.49 | 4.06 | 3.24 | 4.30 | −0.23 | 0.13 | 4.68 |
| Tmax | 0.5–0.8 | 1.0–2.0 | <1.0 | 2.0–4.0 | 1.0–1.5 | 3.0–5.0 | 4.0 |
| T 1/2 (h) | 11 | 14 | <3 | 2 | 2 | 19 | 1.4–3.0 |
| Absorption (%) | 80 | 30 | 98 | 30 | 3.4 | 40–60 | 60–80 |
| Bioavailability (%) | 60 | 14 | 24 | <5 | 17 | 20 | <5 |
| Protein binding (%) | 96 | >98 | 98 | >95 | 50 | 88 | 95 |
| Major P450 metabolic enzyme | CYP2C9 | CYP3A4 | CYP2C9 (minor) | CYP3A4 | None | CPY2C (minor) | CPY3A4 |
| Systemic active metabolites (n) | No | Yes (2) | No | Yes (4) | No | Minimal | Yes (3) |
| Renal excretion (%) | 2 | <2 | <6 | 10 | 20 | 10 | 13 |
Note: This table lists the most important pharmacokinetic variables for all available statins including pitavastatin. The noteworthy difference which often effects drug selection is the metabolic pathway, especially utilizing the CYP system, leading to drug–drug competition for metabolism and subsequent interactions. Log P or the logarithm of partial coefficient of statins relates to lipophilicity (the higher the log P the more lipid soluble).