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Background and Objectives <p>Tapentadol is a novel, centrally acting, potent analgesic with a dual mechanism of action on µ-opioid receptors and noradrenaline reuptake in the central nervous system. This study was conducted to compare the pharmacokinetics, preliminary pharmacodynamics, and safety of single-dose tapentadol hydrochloride intravenous infusion (IV) with tapentadol hydrochloride oral immediate-release (IR) and tapentadol hydrochloride oral extended-release (ER).</p> Methods <p>In this randomized, open-label, multicenter, active-controlled, parallel-group phase 1 trial, 28 Chinese patients with moderate noncancer pain were randomly assigned in a 1:1:1 ratio to receive a single dose of either tapentadol IV (0.5&#xa0;mg/kg), tapentadol IR (100&#xa0;mg), or tapentadol ER (100&#xa0;mg). Adverse events were monitored, serum samples were collected for pharmacokinetic analysis, and 11-point numeric rating scale (NRS) scores were recorded for preliminary pharmacodynamic evaluation during the study.</p> Results <p>The geometric mean (geomean) absolute bioavailability of tapentadol IR and ER after a single-dose administration under fasting conditions was 44.3% (90% confidence interval [CI] 37.5–52.3) and 34.0% (90% CI 27.1–52.3), respectively. The NRS scores demonstrated a decreasing trend across all three groups. Treatment-related adverse event (TRAE) occurred in 50.0% (tapentadol IV), 70% (tapentadol IR), and 50.0% (tapentadol ER) of patients. No events led to dose adjustment or interruption or necessitated additional concomitant medication, and there were no serious adverse events (SAEs), withdrawals, or deaths.</p> Conclusions <p>Tapentadol IV exhibits precise pharmacokinetics, promising pharmacodynamic properties, and a favorable safety profile compared with IR and ER routes for patients with moderate noncancer pain, supporting further clinical research and development of tapentadol injection.</p> Trial Registration <p><a href="http://www.chinadrugtrials.org.cn/">http://www.chinadrugtrials.org.cn/</a>; CTR20212327 2021-09-27.</p>

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A Multicenter, Randomized, Open-Label, Active-Controlled, Parallel-Group Study Evaluating the Pharmacokinetics of Single-Dose Tapentadol Hydrochloride Intravenous Infusion and Tapentadol Hydrochloride Oral Tablets in Patients with Pain

  • 期刊论文

  • 发表日期：

    2025年10月9日

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  • Zhiqin Hu,
  • Tenghua Wang,
  • Xiaoqiang Li,
  • Ying Luo,
  • Xiaole Wang,
  • Chen Li,
  • Zhixin Zhang,
  • Xuan Wang,
  • Jin He,
  • Yaoxuan Zhan,
  • Xintong Liang,
  • Sichao Zheng,
  • Yongmei Li,
  • Yindong Zong,
  • Lizhong Liu,
  • Jinlian Bi,
  • Yongdong Zhang,
  • Na Zhou,
  • Haiyan Liu,
  • Li Ban,
  • Dajiang Qin,
  • Yi Fang

摘要

Background and Objectives

Tapentadol is a novel, centrally acting, potent analgesic with a dual mechanism of action on µ-opioid receptors and noradrenaline reuptake in the central nervous system. This study was conducted to compare the pharmacokinetics, preliminary pharmacodynamics, and safety of single-dose tapentadol hydrochloride intravenous infusion (IV) with tapentadol hydrochloride oral immediate-release (IR) and tapentadol hydrochloride oral extended-release (ER).

Methods

In this randomized, open-label, multicenter, active-controlled, parallel-group phase 1 trial, 28 Chinese patients with moderate noncancer pain were randomly assigned in a 1:1:1 ratio to receive a single dose of either tapentadol IV (0.5 mg/kg), tapentadol IR (100 mg), or tapentadol ER (100 mg). Adverse events were monitored, serum samples were collected for pharmacokinetic analysis, and 11-point numeric rating scale (NRS) scores were recorded for preliminary pharmacodynamic evaluation during the study.

Results

The geometric mean (geomean) absolute bioavailability of tapentadol IR and ER after a single-dose administration under fasting conditions was 44.3% (90% confidence interval [CI] 37.5–52.3) and 34.0% (90% CI 27.1–52.3), respectively. The NRS scores demonstrated a decreasing trend across all three groups. Treatment-related adverse event (TRAE) occurred in 50.0% (tapentadol IV), 70% (tapentadol IR), and 50.0% (tapentadol ER) of patients. No events led to dose adjustment or interruption or necessitated additional concomitant medication, and there were no serious adverse events (SAEs), withdrawals, or deaths.

Conclusions

Tapentadol IV exhibits precise pharmacokinetics, promising pharmacodynamic properties, and a favorable safety profile compared with IR and ER routes for patients with moderate noncancer pain, supporting further clinical research and development of tapentadol injection.

Trial Registration

http://www.chinadrugtrials.org.cn/; CTR20212327 2021-09-27.