Alirocumab
Alirocumab, a biologic. Fully human IgG1 monoclonal antibody binding circulating PCSK9 → prevents PCSK9-mediated hepatic LDLR degradation… Subcutaneous half-life 17 d.
Fully human IgG1 monoclonal antibody binding circulating PCSK9 → prevents PCSK9-mediated hepatic LDLR degradation → 2-fold increase in LDLR surface expression → 50–60% LDL reduction on top of statin. ODYSSEY Outcomes trial (2018) demonstrated MACE reduction.
PK: ABSORPTION RATE AUTHORED FROM THE PRALUENT LABEL. This row carried no ka, so the solver substituted 1.0/h and put the peak at 6.4 h. Source, verbatim from the current FDA label (DailyMed setid 446f6b5c-0dd4-44ff-9bc2-c2b41f2806b4): "After subcutaneous administration of 75 mg to 300 mg alirocumab, median times to maximum serum concentrations (t max ) were 3-7 days." RANGE: the shorter endpoint is taken. PUBMED HAS THIS NOWHERE — 27 targeted searches across two passes returned four usable peak times for this whole class, because Tmax is a label figure that rarely reaches an abstract. A regulatory label is already a first-class source in this schema. 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 0.04815/h, which reproduces 72 h on substitution. EXPOSURE IS UNCHANGED: the absorption rate cancels out of AUC, so only the shape moves.
Pharmacokinetics
- Subcutaneous — t½ 17.0 d · F 86% · ka 0.04815 h⁻¹ · Vd 4.9 L
Related compounds
- Evolocumab — synergistic
- Inclisiran — synergistic
Sources: PMID:30403574