依度沙班吸收快速[43]，可以直接与FXa活性位点结合且抑制活性不需监

Edoxaban absorbs quickly [43], can directly bind to the FXa active site and does not need to monitor the coagulation index for its inhibitory activity, its selectivity for thrombin (factor IIa) is 10,000 times lower than for FXa, and for other serine proteases There is no interaction. Edoxaban is a substrate of CYP3A4, not an inhibitor and inducer of CYP1A2, CYP3A4 and P-gp transporter [31]. The absolute bioavailability of edoxaban orally is 67%, the peak plasma concentration time is 1 to 5 hours after oral administration, the plasma elimination half-life is 6 to 11 hours, and 35% is excreted by the kidney [31-32, 35-36]. Studies on the structure-activity relationship of edoxaban indicate that [32-38]: a rigid naphthenic diamine structure in the edoxaban molecule not only improves the biological activity of such structures, but also greatly improves its pharmacokinetics nature. In the structure, 5-chloro 2-aminopyridine is connected to the parent nucleocycloalkane diamine with a dicarbonyl group, which improves its pharmacodynamic activity, and makes it fit well with the P1 pocket, while ensuring that the methylpiperazine part is compatible with P4 Pockets are well bonded

In the form of rapid absorption of the electron saban, can be directly bound with the FXa active site and inhibited activity does not need to monitor the clotting index, its selective ratio of coagulation enzyme (IIa factor) is 10000 times lower than the FXa, and does not interact with other serine proteases. Ido saban is the substrate of CYP3A4 and is not an inhibitor and inducer of CYP1A2, CYP3A4 and P-gp transport proteins. Indo-saban oral absolute bioavailability of 67%, plasma peak concentration of 1 to 5h after oral, plasma elimination half-life of 6 to 11h, 35% by the kidneys excreted . The study of the structure-effect relationship between Edo Saban and the study of the structure of a rigid cyclaline diamine structure in the Ydu Saban molecule not only improves the bioactivity of the structure, but also greatly improves the pharmacokinetic properties of the intake. Structure 5-chlorine 2-aminopyridine is connected to the parent nuclear cyclaline diamine with diuretic base, which improves its efficacy activity and makes it fit well with the P1 pocket, while ensuring that the methylzine part fits well with the P4 pocket.

Edaxaban has a rapid absorption [43], it can directly bind to the FXa active site, and its inhibitory activity does not need to monitor coagulation indicators. Its selectivity to thrombin (IIA factor) is 10000 times lower than that of FXa, and it has no interaction with other serine proteases. Edoxaban is the substrate of CYP3A4, not the inhibitor and inducer of CYP1A2, CYP3A4 and P-gp transporter [31]. The absolute bioavailability of etoxaban was 67%, the peak concentration time of plasma was 1-5h after oral administration, the half-life of plasma elimination was 6-11h, and 35% of it was excreted by kidney [31-32, 35-36]. The structure-activity relationship of edaxaban showed that [32-38]: a rigid cycloalkylenediamine structure in edaxaban not only improved the biological activity of this kind of structure, but also greatly improved its pharmacokinetic properties. In the structure, 5-chloro-2-aminopyridine is connected to the parent naphthenic diamine with dicarbonyl group, which improves its activity and makes it fit well with P1 pocket, and ensures that the methylpiperazine part is well bonded with P4 pocket<br>