The pharmacodynamic effects of PCSK9 inhibitor evolocumab are rapid, with maximum suppression within 4 hours, according to a recent review of the clinical pharmacokinetics and pharmacodynamics. The review also found:
- Evolocumab exhibits nonlinear kinetics and a half-life of 11 to 17 days.
- With maximal suppression of PCSK9 occurring within 4 hours, peak reduction of LDL-C, ranging from 55 to 75%, occurs ~1-2 weeks after a dose of evolocumab.
- Patient-specific factors do not have a clinically meaningful effect on the pharmacodynamic effects of evolocumab; thus, no dose adjustment is necessary based on patient-specific factors of concomitant medication use.
- When combined with a statin, evolocumab can result in additional lowering of LDL-C.
Kasichayanula S, Grover A, Emery MG, et al. Clinical pharmacokinetics and pharmacodynamics of evolocumab, a PCSK9 inhibitor. [Published online ahead of print January 20, 2018]. Clin Pharmacokinet. doi:10.1007/s40262-017-0620-7.
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