摘要

隨著鴉片類止痛藥相關依賴與過量風險成為公共衛生問題，臨床對於更安全且無成癮風險的非鴉片類止痛藥需求漸增。本文回顧suzetrigine，一種於2025年1月獲得美國食品藥物管理局核准用於成人中度至重度急性疼痛治療的選擇性電位依賴性鈉離子通道1.8 亞型 (voltage-gated sodium channel 1.8, Nav1.8) 抑制劑，探討其療效與安全性。Suzetrigine 為口服小分子藥物，能降低周邊神經興奮性與疼痛訊號傳遞，且無成癮風險。建議起始劑量為100 mg，之後每12 小時給予50 mg，療程不宜超過14 天。兩項3 期臨床試驗顯示，suzetrigine 相較安慰劑可顯著降低疼痛強度，並具較快起效時間（數字疼痛評估量表 [Numeric Pain Rating Scale, NPRS] 從基線下降 ≥ 2 分的中位數時間：NAVIGATE 1 為240 分鐘，NAVIGATE 2 為119 分鐘）。事後分析亦支持其合併ibuprofen 時止痛效果進一步提升，顯示其於多模式止痛策略中具應用潛力。目前實證資料來自術後疼痛模型，其他急性疼痛情境尚待驗證。Suzetrigine 整體耐受性良好， 嚴重不良事件罕見， 常見不良事件包括噁心 (8.2%–19%)、便祕 (3.5%–10.5%) 與頭痛 (4.2%–4.9%)，發生率多低於對照組。雖止痛效果未優於hydrocodone/acetaminophen，惟其良好的安全性與非鴉片特性，使其成為中重度術後急性疼痛的替代方案。期望未來有更多關於不同疼痛型態、長期安全性與成本效益等面向的研究，以確立suzetrigine 在臨床實務上的效益。

 

ABSTRACT

As opioid analgesic dependence and overdose become growing public health concerns, clinical demand is increasing for safer, non-addictive non-opioid analgesics. This article reviews suzetrigine, a selective voltage-gated sodium channel 1.8 (Nav1.8) inhibitor approved by the U.S. Food and Drug Administration in January 2025 for the treatment of moderate to severe acute pain in adults, evaluating its efficacy and safety. Suzetrigine is an oral small-molecule drug reducing peripheral neuronal excitability and pain transmission, without addiction risk. The recommended initial dose is 100 mg, followed by 50 mg every 12 hours, with treatment duration not exceeding 14 days. Two phase III clinical trials demonstrated significant pain reduction compared to placebo, with rapid onset of analgesia (median time to achieve a ≥ 2-point reduction on the Numeric Pain Rating Scale (NPRS), NAVIGATE 1: 240 minutes; NAVIGATE 2: 119 minutes). Post hoc analyses showed combining suzetrigine with ibuprofen enhanced analgesic effects, supporting its role in multimodal analgesia. Current evidence is based on postoperative pain models; further studies in other acute pain settings are warranted. Overall tolerability was favorable, with serious adverse events rare. Common adverse events included nausea (8.2%–19%), constipation (3.5%–10.5%), and headache (4.2%–4.9%), mostly occurring less frequently than in comparators. Although analgesic efficacy was not superior to hydrocodone/ acetaminophen, suzetrigine’s favorable safety profile and non-opioid mechanism make it an alternative in moderate-to-severe postoperative acute pain. Future studies on various pain types, long-term safety, cost-effectiveness, and other aspects are needed to ensure suzetrigine’s effectiveness in real-world practice.

 

 

Submitted for publication: 2025.05.04; Accepted for publication: 2025.07.05