“海”选新星｜“安全镇痛卫士”安瑞克芬的自述

思舒静®（安瑞克芬注射液）是全球首个获得镇痛适应症的高选择性外周K受体激动剂，于2025年5月获批上市。其通过精准激动外周κ阿片受体发挥高效镇痛及抗瘙痒作用，不易透过血脑屏障，有效避免了呼吸抑制、成瘾等中枢神经系统不良事件。目前已获批用于治疗腹部手术后的轻、中度疼痛，以及维持性血液透析的慢性肾脏疾病相关中重度瘙痒成人患者。今年5月，“治疗术后疼痛”新适应症上市许可申请获受理。

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2.Yuan JJ, Bian YC, Ma S, Chen W, Zhang FY, Zhang H, Miao LY. Pharmacokinetics, Mass Balance and Metabolism of [14C]HSK21542, a Novel Kappa Opioid Receptor Agonist, in Humans. Eur J Drug Metab Pharmacokinet. 2023 Nov;48(6):723-731. doi: 10.1007/s13318-023-00858-0. Epub 2023 Oct 13. PMID: 37833493.

3.     Pan M, Wang G, Zhou L, Xu Y, Yao L, Wu C, Mei C, Zhao Z, Sun D, Guan T, Chen Q, Shi M, Xu H, Zeng W, Li F, Yan R, Liu BC. Safety and effectiveness of HSK21542 for hemodialysis patients: a multiple ascending dose study. Front Pharmacol. 2023 Oct 9;14:1203642. doi: 10.3389/fphar.2023.1203642. PMID: 37876731; PMCID: PMC10590914.

4.     Zhang M, Lei Z, Yao X, Zhang L, Yan P, Wu N, Chen M, Zhang F, Liu D. Model informed drug development: HSK21542 PBPK model supporting dose decisions in specific populations. Eur J Pharm Sci. 2024 May 1;196:106763. doi: 10.1016/j.ejps.2024.106763. Epub 2024 Apr 8. PMID: 38599505.

5.     Gou X, Chen Y, Ye Q, Meng Q, Jia Y, Li P, Wang Q, Wang J, Zhang C, Wang J, Dong Y. Preclinical evaluation of abuse potential of the peripherally-restricted kappa opioid receptor agonist HSK21542. Regul Toxicol Pharmacol. 2024 Dec;154:105731. doi: 10.1016/j.yrtph.2024.105731. Epub 2024 Oct 23. PMID: 39455048.

6.     Xu Y, Zhang T, Huang X, Tuerhong S, Chen X. Efficacy and safety of anrikefon injection for postoperative analgesia in specific patient groups (elderly, liver damage, renal damage) after abdominal surgery. J Anesth Transl Med. 2024 Dec 27;3(4):202-208. doi: 10.1016/j.jatmed.2024.11.002. PMID: 41929422; PMCID: PMC13001774.

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8.     Shao R, Wang HY, Ruan ZR, Jiang B, Yang DD, Hu Y, Xu YC, Yang JT, Gao W, Zhao WY, Yan M, Lou H. Phase I clinical trial evaluating the safety, tolerance, pharmacokinetics and pharmacodynamics of HSK21542 injection in healthy volunteers. Basic Clin Pharmacol Toxicol. 2024 Dec;135(6):743-754. doi: 10.1111/bcpt.14094. Epub 2024 Oct 13. PMID: 39397291.

9.     Gou X, Ye Q, Chen B, Zheng Y, Chen H, Fan L, Meng Q, Zhang C, Lu Y, Wang J. Reproductive and developmental toxicity assessment of HSK21542, a novel peripherally-restricted kappa opioid receptor agonist in rats and rabbits. Regul Toxicol Pharmacol. 2025 Jun;159:105811. doi: 10.1016/j.yrtph.2025.105811. Epub 2025 Mar 18. PMID: 40113157.

10.  Zhong Y, Xu Y, Lei Q, Yang M, Wang S, Hu X, Xie H, Li Y, Qin Z, Gu Z, Zhang J, Wang Y, Wu J, Wang H, Ming Y, Xia Z, Zhai H, Jiang K, Zhang P, Wang Z, Wang L, Li L, Cheng Z, Jiang H, Wang G, Chen J, Zhao Z, Chen X, Yan M. HSK21542 in patients with postoperative pain: two phase 3, multicentre, double-blind, randomized, controlled trials. Nat Commun. 2025 May 24;16(1):4830. doi: 10.1038/s41467-025-60013-y. PMID: 40413233; PMCID: PMC12103582.

11.  Zhong Y, Wang H, Yan M, Yang M, Zhang J, Nan L, Wang Z, Yang J, Wu J, Guo Q, Hu X, Xu H, Xu Q, Wang D. Efficacy and safety of peripherally-restricted κ-opioid receptor agonist-HSK21542 for postoperative analgesia in patients undergoing laparoscopic abdominal surgery: a randomized, placebo-controlled phase 2 trial. Front Med (Lausanne). 2025 Jul 24;12:1604790. doi: 10.3389/fmed.2025.1604790. PMID: 40776930; PMCID: PMC12328421.

12.  Gou X, Ye Q, Chen B, Zheng Y, Chen H, Fan L, Meng Q, Zhang C, Lu Y, Wang J. Reproductive and developmental toxicity assessment of HSK21542, a novel peripherally-restricted kappa opioid receptor agonist in rats and rabbits. Regul Toxicol Pharmacol. 2025 Jun;159:105811. doi: 10.1016/j.yrtph.2025.105811. Epub 2025 Mar 18. PMID: 40113157.

13.  李子媛,苏文杰,王美容,李军,夏道林,陈元良,黄桂明,董良,邓佳,段开明.安瑞克芬与泰吉利定对全身麻醉腹部手术后中重度疼痛患者镇痛效果的比较[J].中华麻醉学杂志,2025,45(10):1291-1297.DOI:10.3760/cma.j.cn131073-20250731-01012.

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15.  Yu S, Zou L, Dong S, Wu J, Huang X, Zhong Y, Wang H, Yao Y, Yan M. HSK21542 for Postoperative Analgesia in Gynecological Surgery: A Pooled Post-Hoc Analysis of Two Phase III Randomized Controlled Trials. Anesth Analg. 2026 Mar 23. doi: 10.1213/ANE.0000000000008004. Epub ahead of print. PMID: 41874970.

16.  Liu BC, Li ZL, Zhang P, Zhong AM, Bai YL, Xu Y, Gao BH, Li YL, Wang Y, Zhou LH, Yao L, Wang JX, Yan R, Wang L, Liao B, Xie DQ, Yi XM, Guan TJ, Wang CL, Li GS, Li FQ, Chen JH; Anrikefon-302 study collaborator group. Efficacy and safety of anrikefon in patients with pruritus undergoing haemodialysis: multicentre, double blind, randomised placebo controlled phase 3 trial. BMJ. 2025 Aug 19;390:e085208. doi: 10.1136/bmj-2025-085208. PMID: 40829896; PMCID: PMC12362199.

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18.  Pan M, Wang G, Zhou L, Xu Y, Yao L, Wu C, Mei C, Zhao Z, Sun D, Guan T, Chen Q, Shi M, Xu H, Zeng W, Li F, Yan R and Liu B-C (2023) Safety and effectiveness of HSK21542 for hemodialysis patients: a multiple ascending dose study. Front. Pharmacol. 14:1203642. doi: 10.3389/fphar.2023.1203642

1. Chen XY, et al. Quantification of crisugabalin (HSK16149) in biological matrix by LC-MS/MS method: An application to rat pharmacokinetic and tissue distribution studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2025;2.8(IF).

2. Gou XL, et al. Pharmacology and mechanism of action of HSK16149, a selective ligand of the α2δ subunit of voltage-gated calcium channels with analgesic activity in animal models of chronic pain. J Pharmacol Exp Ther. 2021;3.1(IF).

3. Gou XL, et al. Crisugabalin, a ligand for the α2δ subunit of voltage-gated calcium channels, exhibits no obvious abuse potential in rodents. Pharmacol Biochem Behav. 2025;2.5(IF).

4. Liu YM, et al. A phase I study to evaluate the safety, tolerability, and pharmacokinetics of a novel, potent GABA analog HSK16149 in healthy Chinese subjects. Front Pharmacol. 2023;4.4(IF).

5. Wu QQ, et al. Effect of a high-fat and high-calorie meal on the pharmacokinetics of a novel potent GABA analog HSK16149 in healthy subjects. Pharmacol Res Perspect. 2023;2.9(IF).

6. Miao J, et al. Safety and pharmacokinetics of a novel potent GABA analog crisugabalin in Chinese subjects with varying degrees of renal impairment. Br J Clin Pharmacol. 2026;2.4(IF).

7. Chen ZQ, et al. Structural and Computational Insights into the Mechanism of the Superior Pharmacological Activity of Crisugabalin: A Third-Generation Cavα2δ1 Ligand. J Chem Inf Model. 2026;5.3(IF).

8. Guo XH, et al. GABA analogue HSK16149 in Chinese patients with diabetic peripheral neuropathic pain: a phase 3 randomized clinical trial. JAMA Netw Open. 2024;10.5(IF).

9. Lu QJ, et al. Efficacy and safety of crisugabalin (HSK16149) in adults with postherpetic neuralgia: a phase 3 randomized clinical trial. JAMA Dermatol. 2024;11.5(IF).

10. Guo XH, et al. Rapid onset of crisugabalin in patients with diabetic peripheral neuropathic pain: a secondary analysis of a multicenter randomized double-blind controlled study. Pain Ther. 2025;4.1(IF).

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12. Jiang HW, et al. Crisugabalin combined with acetyl-L-carnitine for diabetic peripheral neuropathic pain: a phase 2 randomized controlled trial. J Pain Res. 2026;2.5(IF).

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1．中国成人术后镇痛指南成人术后疼痛管理临床实践指南（2024版）

2．腹部手术围手术期疼痛管理指南（2025版）

3．安瑞克芬临床应用专家推荐意见

1. 数据统计截至2026年5月10日。

2.本资讯旨在提供前沿医学信息与研究进展，仅供医疗卫生专业人士参考，不属于产品推广和广告用途。文中内容不能取代专业的医疗指导，也不应视为诊疗建议。医疗卫生专业人士在对文中涉及到的任何药品进行处方时，请严格遵循产品最新详细处方资料。

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