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Pivastatin calcium (Livalo) is a new member of the statin group. Like other statins, it is an inhibitor of hmG-COA reductase, an enzyme that catalyzes the first step in cholesterol synthesis. Most statins are metabolized in part by one or more liver cytochrome P450 enzymes, leading to an increased likelihood of complex interactions and problems with certain foods, such as grapefruit juice. Pivastatin appears to be a substrate for CYP2C9, rather than CYP3A4(a common source of interactions with other statins).
Pak J Pharm Sci. 2016 May;29(3 Suppl):1043-51.
Chromatographic resolution of drug analogues: 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors (statins)
Pitavastatin Calcium purchased from AbMole
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Source | Pak J Pharm Sci (2016). Figure 1. Pitavastatin calcium (Abmole Bioscience) |
| Method | HPLC chromatogram | |
| Cell Lines | ||
| Concentrations | 80μg/ml | |
| Incubation Time | ||
| Results | The results summarized in (table 1) obtained for pravastatin, rosuvastatin, pitavastatin, atorvastatin, fluvastatin, lovastatin and simvastatin were comparable with the corresponding labeled amounts. |
| Molecular Weight | 880.98 |
| Formula | C50H46CaF2N2O8 |
| CAS Number | 147526-32-7 |
| Solubility (25°C) | DMSO 49 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Paul Chan, et al. An evaluation of pitavastatin for the treatment of hypercholesterolemia
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