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A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain

耐受性 医学 安慰剂 吗啡 类阿片 麻醉 随机对照试验 不利影响 止痛药 内科学 受体 病理 替代医学
作者
Eugene R. Viscusi,Lynn R. Webster,Michael Kuss,Stephen E. Daniels,James A. Bolognese,Seth Zuckerman,David G. Soergel,Ruth Ann Subach,Emily A. Cook,Franck Skobieranda
出处
期刊:Pain [Lippincott Williams & Wilkins]
卷期号:157 (1): 264-272 被引量:166
标识
DOI:10.1097/j.pain.0000000000000363
摘要

In Brief Efficacy of conventional opioids can be limited by adverse events (AEs). TRV130 is a structurally novel biased ligand of the μ-opioid receptor that activates G protein signaling with little β-arrestin recruitment. In this phase 2, randomized, placebo- and active-controlled study, we investigated the efficacy and tolerability of TRV130 in acute pain after bunionectomy. We used an adaptive study design in which 144 patients experiencing moderate-to-severe acute pain after bunionectomy were randomized to receive double-blind TRV130, placebo, or morphine in a pilot phase. After pilot phase analysis, 195 patients were randomized to receive double-dummy TRV130 0.5, 1, 2, or 3 mg every 3 hours (q3h); placebo; or morphine 4 mg q4h intravenously. The primary end point was the time-weighted average change in numeric rating scale pain intensity over the 48-hour treatment period. Secondary end points included stopwatch and categorical assessments of pain relief. Safety and tolerability were also assessed. TRV130 2 and 3 mg q3h, and morphine 4 mg q4h produced statistically greater mean reductions in pain intensity than placebo over 48 hours (P < 0.005). TRV130 at 2 and 3 mg produced significantly greater categorical pain relief than morphine (P < 0.005) after the first dose, with meaningful pain relief occurring in under 5 minutes. TRV130 produced no serious AEs, with tolerability similar to morphine. These results demonstrate that TRV130 rapidly produces profound analgesia in moderate-to-severe acute pain, suggesting that G-protein-biased μ-opioid receptor activation is a promising target for development of novel analgesics. TRV130, a G-protein-biased μ-opioid receptor ligand with little β-arrestin recruitment, produced analgesia in moderate-to-severe acute pain, suggesting efficacy with similar tolerability vs conventional opioids.

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