Table 3.
| Drug | Prodrug | Solubility | Bioavailability (%) | Metabolism by Cytochrome P450 Enzymes | OATP Transport | Substrates of P-glycoprotein | Metabolites | Protein Binding | T1/2 (h) |
|---|---|---|---|---|---|---|---|---|---|
| Type I—fungal derived statins | |||||||||
| lovastatin | Yes | Lipophilic | <5 | CYP3A4 | OATP1B1 | Yes | Active metabolites | >96% | 2–4 |
| pravastatin | No | Hydrophilic | 17 | Sulfation | OATP1B1 OATP1B3 OATP2B1 |
No | Not active metabolites | 50% | 1–3 |
| simvastatin | Yes | Lipophilic | <5 | CYP3A4 | OATP1B1 | Yes | Active metabolites | >95% | 2–3 |
| Type II—synthetically derived statins | |||||||||
| fluvastatin | No | Lipophilic | 24 | CYP2C9 | OATP1B1 OATP1B3 OATP2B1 |
No | Not active metabolites | >98% | 0.5–3 |
| atorvastatin | No | Lipophilic | ~12 | CYP3A4 | OATP1B1 OATP2B1 |
Yes | Active metabolites | >98% | 15–30 |
| cerivastatin | No | Lipophilic | 60 | CYP3A4 CYP2C8 |
OATP1B1 | No | Active metabolites | >99% | 2–3 |
| pitavastatin | No | Lipophilic | ~60 | Main: lactonization/glucuronidation Minimal: CYP2C8 CYP2C9 |
OATP1B1 OATP1A2 OATP1B3 |
Yes | Minimally metabolized | 96% | 10–12 |
| rosuvastatin | No | Hydrophilic | 20 | Minimal: CYP2C9 CYP2C19 |
OATP1B1 OATP1A2 OATP1B3 OATP2B1 |
No | Minimally metabolized | 88% | 19–20 |
CYP—cytochrome P450 enzyme; OATP—Organic anion transporting polypeptide.