Evolocumab
Evolocumab, a biologic. Fully human IgG2 mAb binding PCSK9. Same mechanism as alirocumab. FOURIER trial 2017 established CV event… Subcutaneous half-life 14 d.
Fully human IgG2 mAb binding PCSK9. Same mechanism as alirocumab. FOURIER trial 2017 established CV event reduction. Glagov trial showed atherosclerosis regression on IVUS.
PK: ABSORPTION RATE AUTHORED FROM A VERBATIM PEAK TIME. This row carried no ka, so the solver substituted 1.0/h and the modelled peak landed at 6.2 h — for a slowly-absorbed subcutaneous product that is wrong by design, not by a little. Source: "Cmax (tmax) was 4.0 days" — a stated point value after a single subcutaneous dose. With the stored half-life fixing ke, Tmax solves uniquely for ka by inverting the model own definition, ln(ka/ke)/(ka-ke) = Tmax — ARITHMETIC, NOT AN ESTIMATE — giving 0.02992/h, which reproduces 96 h on substitution. EXPOSURE IS UNCHANGED: the absorption rate cancels out of AUC entirely, so only the shape moves.
Pharmacokinetics
- Subcutaneous — t½ 14.0 d · F 72% · ka 0.02992 h⁻¹ · Vd 2.66 L
Related compounds
- Alirocumab — synergistic
Sources: PMID:28304224, PMID:32729822