Hybutimibe, an innovative cholesterol absorption inhibitor for lipid-lowering therapy: current evidence and future perspectives.
- 1Cardiometabolic Center, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing, China.
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.
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BibTeX
@article{li2026hybutimibe,
title = {{Hybutimibe, an innovative cholesterol absorption inhibitor for lipid-lowering therapy: current evidence and future perspectives.}},
author = {Sha Li and Hui-Hui Liu and Jian-Jun Li},
journal = {Frontiers in pharmacology},
year = {2026},
month = oct,
doi = {10.3389/fphar.2026.1936459},
url = {https://europepmc.org/article/MED/42898767},
note = {CC BY},
}
RIS
TY - JOUR
TI - Hybutimibe, an innovative cholesterol absorption inhibitor for lipid-lowering therapy: current evidence and future perspectives.
AU - Sha Li
AU - Hui-Hui Liu
AU - Jian-Jun Li
PY - 2026
DA - 2026/10/05
JO - Frontiers in pharmacology
DO - 10.3389/fphar.2026.1936459
UR - https://europepmc.org/article/MED/42898767
AB - 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.
SN - 1663-9812
ER -