Ezetimibe
Ezetimibe. Inhibits Niemann-Pick C1-like 1 (NPC1L1) at the intestinal brush border → blocks dietary cholesterol + phytosterol absorption.… Oral half-life 24 h.
Inhibits Niemann-Pick C1-like 1 (NPC1L1) at the intestinal brush border → blocks dietary cholesterol + phytosterol absorption. Non-statin mechanism → additive LDL reduction when combined with statin. IMPROVE-IT trial established CV benefit of ezetimibe-statin combination.
PK models TOTAL EZETIMIBE, parent plus its active glucuronide, which is what the cited figure describes: verbatim "elimination half-life (t(1/2)) 24.32 +/- 13.27 and 18.90 +/- 9.66 h" for total and free drug respectively. The stored 24.3 was a rounding of the total; the parent alone is 18.90 h. CAVEAT ON THE MODEL ITSELF: ezetimibe recirculates through bile and shows "multiple peaks, indicating enterohepatic recycling" (PMID:11901097), which a monotonic one-compartment curve cannot represent at any half-life, and the model has no state for the glucuronide that carries most of the circulating exposure. ka 2.5 /h, V 100 L and F 0.5 dropped: the abstract states none of them.
Pharmacokinetics
- Oral — t½ 24.3 h
Related compounds
- Atorvastatin / statins — synergistic
Sources: PMID:15871634, PMID:11901097