Table 1.
Comparative pharmacology of statins
| Increasing lipophilicity |
|||||||
|---|---|---|---|---|---|---|---|
| Lovastatin | Simvastatin | Atorvastatin | Pitavastatin | Fluvastatin | Rosuvastatin | Pravastatin | |
| IC50 HMG-CoA reductase (nM) | 2–4 | 1–2 (active metabolite) | 1.16 | 0.1 | 3–10 | 0.16 | 4 |
| Oral absorption (%) | 30 | 60–85 | 30 | 80 | 98 | 50 | 35 |
| Bioavailability (%) | 5 | <5 | 12 | 60 | 30 | 20 | 18 |
| Protein binding (%) | >98 | >95 | >98 | 96 | >98 | 90 | 50 |
| Half life (h) | 2–5 | 2–5 | 7–20 | 10–13 | 1–3 | 20 | 1–3 |
| Metabolism by CYP450 | 3A4 (?2C8) | 3A4 (2C8, 2D6) | 3A4 (2C8) | (2C9) | 2C9 | 2C9 (2C19) | (3A4) |
| Cellular transporter | OATP1B1 | (MRP2) | OATP1B1 | OATP1B1 (MRP2) | OATP1B1 | OATP1B1 | OATP1B1 (MRP2) |
| Daily dose (mg) | 10–40 | 10–40 | 10–80 | 1–4 | 80 (retard formulation) | 5–40 | 10–40 |
Adapted from Sirtori.10
Figures in parentheses indicate a minor metabolic pathway or transporter.
CYP450, cytochrome P450; IC50, 50% inhibitory concentration; HMG-CoA, 3-hydroxy-3-methylglutaryl coenzyme A; MRP2, multidrug resistance-associated protein 2; OATP1B1, Organic Anion Transporting Polypeptide 1B1.