Olezarsen: A Next-Generation Antisense Therapy for Hypertriglyceridemia and Familial Chylomicronemia Syndrome

Olezarsen:一种用于治疗高甘油三酯血症和家族性乳糜微粒血症综合征的新一代反义疗法

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Abstract

Olezarsen (Tryngolza) is a next-generation, N-acetylgalactosamine (GalNAc)-conjugated antisense oligonucleotide that selectively inhibits hepatic ApoC-III, a key regulator of triglyceride metabolism. By inhibiting ApoC-III, olezarsen increases triglyceride clearance through both lipoprotein lipase (LPL)-dependent and -independent pathways. In the Phase 3 BALANCE trial, olezarsen reduced fasting triglycerides by approximately 60% at 12 months in patients with familial chylomicronemia syndrome (FCS), with a marked decrease in pancreatitis events versus placebo. Consistent triglyceride reductions (around 50%) were also observed in moderate and severe hypertriglyceridemia, along with improvements in ApoB-containing lipoproteins and high-density lipoprotein (HDL) profiles. In completed trials, olezarsen demonstrated a favorable safety profile, with most adverse events limited to mild injection-site reactions and no clinically significant thrombocytopenia. Ongoing Phase 3 trials (ESSENCE, CORE, and CORE2) will further define its role in cardiovascular risk reduction and pancreatitis prevention in broader hypertriglyceridemic populations. Olezarsen represents a precision medicine advance, offering effective triglyceride lowering with improved tolerability compared with earlier antisense therapies.

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