Table 3. Drug interference summary: ex vivo test panel.
| Nominal Concentration of Evolocumab (ng/mL) |
Evolocumab (nM) | PCSK9 (nM) | Molar Ratio [drug: ligand] |
%Inhibition |
|---|---|---|---|---|
| 1,000,000 | 6667 | 2.5 | 2667 | 100 |
| 100,000 | 667 | 2.5 | 267 | 100 |
| 10,000 | 66.7 | 2.5 | 26.7 | 100 |
| 1,875 | 12.5 | 2.5 | 5.00 | 100 |
| 938 | 6.25 | 2.5 | 2.50 | 100 |
| 469 | 3.125 | 2.5 | 1.25 | 100 |
| 234 | 1.563 | 2.5 | 0.625 | 91 |
| 117 | 0.781 | 2.5 | 0.313 | 48 |
| 58.6 | 0.391 | 2.5 | 0.156 | 29 |
| 29.3 | 0.195 | 2.5 | 0.078 | 14 |
| 14.6 | 0.098 | 2.5 | 0.039 | 6 |
| 7.3 | 0.049 | 2.5 | 0.020 | 2 |
| 3.7 | 0.024 | 2.5 | 0.010 | 2 |
| 1.8 | 0.012 | 2.5 | 0.005 | -5 |
| 0.0 | 0 | 2.5 | 0 | 0 |
%Inhibition: (concentration measured-nominal/nominal) × 100; Nominal is defined as the endogenous PCSK9 measured in the serum pool; Highlighted cells represent the targeted [drug: ligand] molar ratios for samples that would be used in the ex vivo challenge experiments.