HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials

Abstract HSK21542, a peripherally restricted kappa opioid receptor agonist, was evaluated for efficacy and safety in patients with postoperative pain following abdominal surgery. This was assessed in two phase 3, multicentre, randomized, double-blind, controlled trials (HSK21542-301 [ClinicalTrials....

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Main Authors: Yinbo Zhong, Younian Xu, Qian Lei, Mengchang Yang, Saiying Wang, Xiaoling Hu, Haihui Xie, Yalan Li, Zhong Qin, Zhengfeng Gu, Jiaqiang Zhang, Yuexin Wang, Jinglei Wu, Haiying Wang, Yue Ming, Zhongyuan Xia, Haoyu Zhai, Ke Jiang, Peng Zhang, Zhiping Wang, Liangrong Wang, Lin Li, Zhigang Cheng, Huayong Jiang, Guonian Wang, Jingli Chen, Zhibin Zhao, Xiangdong Chen, Min Yan
Format: Article
Language:English
Published: Nature Portfolio 2025-05-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-025-60013-y
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author Yinbo Zhong
Younian Xu
Qian Lei
Mengchang Yang
Saiying Wang
Xiaoling Hu
Haihui Xie
Yalan Li
Zhong Qin
Zhengfeng Gu
Jiaqiang Zhang
Yuexin Wang
Jinglei Wu
Haiying Wang
Yue Ming
Zhongyuan Xia
Haoyu Zhai
Ke Jiang
Peng Zhang
Zhiping Wang
Liangrong Wang
Lin Li
Zhigang Cheng
Huayong Jiang
Guonian Wang
Jingli Chen
Zhibin Zhao
Xiangdong Chen
Min Yan
author_facet Yinbo Zhong
Younian Xu
Qian Lei
Mengchang Yang
Saiying Wang
Xiaoling Hu
Haihui Xie
Yalan Li
Zhong Qin
Zhengfeng Gu
Jiaqiang Zhang
Yuexin Wang
Jinglei Wu
Haiying Wang
Yue Ming
Zhongyuan Xia
Haoyu Zhai
Ke Jiang
Peng Zhang
Zhiping Wang
Liangrong Wang
Lin Li
Zhigang Cheng
Huayong Jiang
Guonian Wang
Jingli Chen
Zhibin Zhao
Xiangdong Chen
Min Yan
author_sort Yinbo Zhong
collection DOAJ
description Abstract HSK21542, a peripherally restricted kappa opioid receptor agonist, was evaluated for efficacy and safety in patients with postoperative pain following abdominal surgery. This was assessed in two phase 3, multicentre, randomized, double-blind, controlled trials (HSK21542-301 [ClinicalTrials.gov identifier, NCT04738357] and HSK21542-303 [ClinicalTrials.gov identifier, NCT05390905]) in China. HSK21542-301 was a dual-arm study comparing HSK21542 1.0 μg/kg with placebo, while HSK21542-303 involved three arms comparing HSK21542 1.0 μg/kg with tramadol 50 mg/dose and placebo. All treatments were administered intravenously. The primary endpoint was the time-weighted summed pain intensity differences over 24 h (SPID0-24 h). Both HSK21542-301 (least squares [LS] mean [± standard error], −39.1 [1.88] vs −27.4 [1.89]; P < 0.001) and HSK21542-303 (−64.0 [2.25] vs −45.9 [2.25]; P < 0.001) demonstrated superiority of HSK21542 over placebo in terms of SPID0-24 h, while HSK21542-303 showed non-inferiority to tramadol (LS mean difference, −1.1; 95% confidence interval, −7.4 to 5.1; P < 0.001). Furthermore, HSK21542 had a comparable safety profile to placebo, inducing fewer gastrointestinal adverse events compared with tramadol. Grade ≥3 treatment-emergent adverse events occurred in eight (5.9%) and three (2.3%) patients in the HSK21542 arm of HSK21542-301 and HSK21542-303, respectively. In conclusion, HSK21542 showed potent analgesic effect and was well tolerated in patients who underwent abdominal surgery and experienced postoperative pain.
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spelling doaj-art-59d12aa3c42c46dab6f862676aed69ce2025-08-20T03:48:18ZengNature PortfolioNature Communications2041-17232025-05-0116111310.1038/s41467-025-60013-yHSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trialsYinbo Zhong0Younian Xu1Qian Lei2Mengchang Yang3Saiying Wang4Xiaoling Hu5Haihui Xie6Yalan Li7Zhong Qin8Zhengfeng Gu9Jiaqiang Zhang10Yuexin Wang11Jinglei Wu12Haiying Wang13Yue Ming14Zhongyuan Xia15Haoyu Zhai16Ke Jiang17Peng Zhang18Zhiping Wang19Liangrong Wang20Lin Li21Zhigang Cheng22Huayong Jiang23Guonian Wang24Jingli Chen25Zhibin Zhao26Xiangdong Chen27Min Yan28Department of Anesthesiology, Second Affiliated Hospital of Zhejiang University School of MedicineDepartment of Anesthesiology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China; Key Laboratory of Anesthesiology and Resuscitation (Huazhong University of Science and Technology), Ministry of Education, China; Institute of Anesthesia and Critical Care Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and TechnologyDepartment of Anesthesiology, Sichuan Provincial People’s Hospital, School of Medicine, University of Electronic Science and Technology of ChinaDepartment of Anesthesiology, The Third People’s Hospital of ChengduThe Third Xiangya Hospital of Central South UniversityThe First Affiliated Hospital of University of South ChinaDongguan People’s Hospital (The Tenth Affiliated Hospital of Southern Medical University)The First Affiliated Hospital of Jinan University (Guangzhou Overseas Chinese Hospital, The First Clinical Medical College of Jinan University)Wuxi People’s HospitalWuxi People’s HospitalHenan Provincial People’s HospitalDepartment of Anesthesiology, Cangzhou People’s HospitalDepartment of Anesthesiology, Liuzhou People’s Hospital Affiliated to Guangxi Medical UniversityDepartment of Anesthesiology, Second Affiliated Hospital of Zhejiang University School of MedicineDepartment of Anesthesiology, Second Affiliated Hospital of Zhejiang University School of MedicineRenmin Hospital of Wuhan UniversityThe First People’s Hospital of GuangyuanThe Affiliated Hospital of Guizhou Medical UniversityYibin Second People’s HospitalAffiliated Hospital of Xuzhou Medical UniversityThe First Affiliated Hospital of Wenzhou Medical UniversityGeneral Hospital of the Northern Theater Command of Chinese PLAXiangya Hospital Central South UniversityShaoxing People’s HospitalThe Fourth Hospital of Harbin Medical UniversityDepartment of Anesthesiology, The Central Hospital of Wuhan, Tongji Medical College, Huazhong University of Science and TechnologyThe First People’s Hospital of LianyungangDepartment of Anesthesiology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China; Key Laboratory of Anesthesiology and Resuscitation (Huazhong University of Science and Technology), Ministry of Education, China; Institute of Anesthesia and Critical Care Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and TechnologyDepartment of Anesthesiology, Second Affiliated Hospital of Zhejiang University School of MedicineAbstract HSK21542, a peripherally restricted kappa opioid receptor agonist, was evaluated for efficacy and safety in patients with postoperative pain following abdominal surgery. This was assessed in two phase 3, multicentre, randomized, double-blind, controlled trials (HSK21542-301 [ClinicalTrials.gov identifier, NCT04738357] and HSK21542-303 [ClinicalTrials.gov identifier, NCT05390905]) in China. HSK21542-301 was a dual-arm study comparing HSK21542 1.0 μg/kg with placebo, while HSK21542-303 involved three arms comparing HSK21542 1.0 μg/kg with tramadol 50 mg/dose and placebo. All treatments were administered intravenously. The primary endpoint was the time-weighted summed pain intensity differences over 24 h (SPID0-24 h). Both HSK21542-301 (least squares [LS] mean [± standard error], −39.1 [1.88] vs −27.4 [1.89]; P < 0.001) and HSK21542-303 (−64.0 [2.25] vs −45.9 [2.25]; P < 0.001) demonstrated superiority of HSK21542 over placebo in terms of SPID0-24 h, while HSK21542-303 showed non-inferiority to tramadol (LS mean difference, −1.1; 95% confidence interval, −7.4 to 5.1; P < 0.001). Furthermore, HSK21542 had a comparable safety profile to placebo, inducing fewer gastrointestinal adverse events compared with tramadol. Grade ≥3 treatment-emergent adverse events occurred in eight (5.9%) and three (2.3%) patients in the HSK21542 arm of HSK21542-301 and HSK21542-303, respectively. In conclusion, HSK21542 showed potent analgesic effect and was well tolerated in patients who underwent abdominal surgery and experienced postoperative pain.https://doi.org/10.1038/s41467-025-60013-y
spellingShingle Yinbo Zhong
Younian Xu
Qian Lei
Mengchang Yang
Saiying Wang
Xiaoling Hu
Haihui Xie
Yalan Li
Zhong Qin
Zhengfeng Gu
Jiaqiang Zhang
Yuexin Wang
Jinglei Wu
Haiying Wang
Yue Ming
Zhongyuan Xia
Haoyu Zhai
Ke Jiang
Peng Zhang
Zhiping Wang
Liangrong Wang
Lin Li
Zhigang Cheng
Huayong Jiang
Guonian Wang
Jingli Chen
Zhibin Zhao
Xiangdong Chen
Min Yan
HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials
Nature Communications
title HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials
title_full HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials
title_fullStr HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials
title_full_unstemmed HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials
title_short HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials
title_sort hsk21542 in patients with postoperative pain two phase 3 multicentre double blind randomized controlled trials
url https://doi.org/10.1038/s41467-025-60013-y
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