Prasugrel hydrochloride is a novel antiplatelet agent that is a third-generation thienopyridine. Prasugrel produces inhibition of platelet aggregation to 20 μM or 5 μM ADP. Prasugrel hydrochloride binds to P2Y12 receptors and showed greater platelet inhibition and decreased incidence of ischemic events when compared to clopidogrel. In the absence of lansoprazole, the extent of absorption (AUC) of prasugrel free base was about 8-9% lower, while the rate of absorption (Cmax) after administration of prasugrel free base was 20% lower when compared to prasugrel hydrochloride. When lansoprazole was used to raise the pH level in the upper gastro-intestinal tract, AUC was decreased by 25% after administration of prasugrel hydrochloride and by 41% after prasugrel free base. In addition, the peak plasma levels were decreased by 52% and 72%, respectively (geometric means). The relative bioavailability of the prasugrel free base compared to prasugrel hydrochloride, both in the presence and in the absence of the proton pump inhibitor lansoprazole, differs so much that most probably a generic formulation containing prasugrel free base will not be equivalent in all aspects to the originator product.
| Molecular Weight | 409.91 |
| Formula | C20H20FNO3S.HCl |
| CAS Number | 389574-19-0 |
| Solubility (25°C) | DMSO 30 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.
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