Hybutimibe, an innovative cholesterol absorption inhibitor for lipid-lowering therapy: current evidence and future perspectives.

Authors

Sha Li, Hui-Hui Liu, Jian-Jun Li

Published in

Frontiers in pharmacology. Volume 17. Pages 1936459. Epub Oct 05, 2026.

Abstract

Achievement of low-density lipoprotein cholesterol (LDL-C) targets is crucial for the prevention of atherosclerotic cardiovascular disease (ASCVD). As first-line lipid-lowering drugs, statins often fail to achieve adequate LDL-C control rates in clinical practice due to individual variations in efficacy, safety concerns, and poor long-term adherence. Cholesterol absorption inhibition mediated by the Niemann-Pick C1-like 1 (NPC1L1) pathway provides a complementary approach to statin-based lipid lowering regimens. Hybutimibe is an oral NPC1L1 inhibitor approved in China and has reported pharmacokinetic characteristics that differ from those of ezetimibe; however, the clinical relevance of these differences has not been established in direct comparative studies. Evidence from Phase I-III clinical trials and post-marketing real-world studies indicates that hybutimibe monotherapy or combination therapy with statins can achieve significant and sustained LDL-C reduction; in patients with inadequate response to statin monotherapy, combination with hybutimibe exhibits superior lipid-lowering efficacy compared to statin dose escalation, with favorable overall safety. However, available studies have primarily evaluated LDL-C and other lipid parameters as surrogate endpoints. No dedicated cardiovascular outcome trial has established whether hybutimibe reduces major adverse cardiovascular events, cardiovascular mortality, or all-cause mortality. This article systematically reviews the research and development background, pharmacological properties, mechanism of action, clinical efficacy, safety, and post-marketing real-world evidence of hybutimibe, exploring its application value as an adjuvant therapy in optimizing clinical LDL-C management.

PMID:
42898767
Bibliographic data and abstract were imported from PubMed on 20 Oct 2026.

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