预约演示
更新于：2026-02-06
Anrikefon
安瑞克芬
更新于：2026-02-06
概要
基本信息
药物类型 小分子化药 |
别名 HSK 21542、HSK-21542、HSK21542 + [1] |
作用方式 激动剂 |
作用机制 κ opioid receptor激动剂(κ-阿片受体激动剂) |
在研适应症 |
原研机构 |
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2025-05-13), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C39H57N7O5 |
InChIKeyVWXDZAZSCZVCPV-YFRBGRBWSA-N |
CAS号2269511-95-5 |
Sequence Code 319389768
关联
35
项与 安瑞克芬 相关的临床试验NCT07380113
An Exploratory Study Comparing Anrikefon With Nalfurafine in Improving Sleep Quality Among CKD-aP Patients Undergoing Hemodialysis: An Open-Label Randomized Controlled Clinical Trial
ChiCTR2600117976
The efficacy and safety of Anrikofen injection for acute pain after abdominal laparoscopic gynecological surgery: a single center, randomized, double-blind, controlled clinical study
NCT07353983
Pharmacokinetic Evaluation of Anrikefon Injection in the Geriatric Population With the Management of Acute Pain Following Abdominal Laparoscopy
100 项与 安瑞克芬 相关的临床结果
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100 项与 安瑞克芬 相关的转化医学
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100 项与 安瑞克芬 相关的专利（医药）
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14
项与 安瑞克芬 相关的文献（医药）2025-06-01REGULATORY TOXICOLOGY AND PHARMACOLOGY
Reproductive and developmental toxicity assessment of HSK21542, a novel peripherally-restricted kappa opioid receptor agonist in rats and rabbits
Article
作者: Ye, Qidi ; Fan, Litong ; Wang, Ju ; Zhang, Chen ; Zheng, Yu ; Chen, Hongyu ; Gou, Xiaoli ; Lu, Yao ; Meng, Qingyuan ; Chen, Bo
HSK21542, a potent and peripherally-restricted kappa opioid receptor (KOR) agonist, is currently being developed to treat postoperative pain and pruritus. Given that conventional opioids (MOR agonists) are widely recognized for their toxicological impacts on the reproductive system and embryonic development, we evaluated the effects of HSK21542 accordingly. The results showed that HSK21542 did not influence male and female fertility or early embryonic development in rats. HSK21542 also did not show significant manifestations of pre- and post-natal development toxicity in rats. In the embryo-fetal developmental study, even though there was a 3.5 % increase in incidence of fetuses with incomplete ossification of thoracic vertebral centrum in the 4 mg/kg/day group, the plasma exposure of HSK21542 in rats at the no observed adverse effect level (NOAEL) was 82.3 times higher than that of human exposure at 1 μg/kg. On the other hand, exposure to HSK21542 during pregnancy in rabbits did not show any teratogenic risk, only causing a minor impact on bone ossification in fetuses. In conclusion, HSK21542 has a favorable safety profile with only minor effects on the embryo-fetal developmental outcomes.
2025-02-01Expert Review of Clinical Pharmacology
Population pharmacokinetic modeling and exposure-response analysis of anrikefon: insights and implications in clinical analgesia
Article
作者: Chen, Meixia ; Xu, Fengyan ; Yang, Jing ; Wang, Yongrui ; Liu, Xiao ; Sun, Zhongyi ; Zhang, Fengyi ; Zhao, Wanyun ; Wang, Kun ; Liu, Lu
BACKGROUND:
Anrikefon (HSK21542), a potent and selective peripheral kappa opioid receptor (KOR) agonist developed by Haisco, effectively blocks pain and itch signals.
AIM:
To develop a population pharmacokinetic (PK) model for anrikefon and conduct exposure-response (E-R) analysis for safety and efficacy in postoperative pain patients.
METHOD:
The Population PK analysis uses NONMEM software with data from six trials. E-R relationships were assessed using safety and efficacy data from three trials. Covariate screening and Bayesian post-hoc simulations identified relevant factors and compared exposure metrics. The fixed dosing regimen was evaluated by simulation. Safety and efficacy endpoints were evaluated using logistic regression and Emax models.
RESULTS:
A three-compartment model with linear elimination accurately described anrikefon's PK, incorporating weight through allometric scaling. Significant covariates affecting clearance included creatinine clearance, total bilirubin, albumin, aspartate transaminase, and age. Fixed and weight-based dosing showed similar exposures. No apparent E-R trend was observed for safety endpoints. The Emax model indicated that most of subjects achieved over 90% of the maximum effect for SPID0-24 h at 1.0 μg/kg. Safety analysis confirmed this dose was well tolerated with no safety issues.
CONCLUSION:
This study provides valuable insights into dose selection, PK variability, and safety and efficacy endpoints.
2024-12-01BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
Phase I clinical trial evaluating the safety, tolerance, pharmacokinetics and pharmacodynamics of HSK21542 injection in healthy volunteers
Article
作者: Yang, Dan‐dan ; Jiang, Bo ; Shao, Rong ; Xu, Yi‐chao ; Hu, Yin ; Gao, Wei ; Lou, Honggang ; Ruan, Zou‐rong ; Yan, Min ; Wang, Hai‐ying ; Zhao, Wan‐yun ; Yang, Jin‐ting
Abstract:
HSK21542 injection is a new peripheral kappa opioid receptor (KOR) agonist. To evaluate its safety, tolerability, pharmacokinetics and pharmacodynamics, this study was conducted in healthy volunteers, consisting of two parts: a single ascending dose (0.2–3.375 μg/kg, 15‐min infusion) and different infusion durations (0.2 and 1 μg/kg, 2‐ or 15‐min infusion). The area under the plasma concentration‐time curve (AUC) and peak concentration (Cmax) of HSK21542 were dose‐linear among 0.2–3.375 μg/kg. After intravenous injection, HSK21542 was rapidly eliminated with a half‐life (t1/2) of 1.5 h, and the majority (48.02%) of the dose was excreted unchanged in urine. Pharmacodynamic results showed that HSK21542 increased prolactin release and reached a peak at 1–2 h after administration but had no significant effect on vasopressin levels. There was a brief increase in urine volume within the initial 2 h after administration. HSK21542 was well tolerated; most of the adverse effects (AEs) in the trial group were grade 1, and only 2 cases (4.0%) were grade 2. The main AE was paresthesia, which appeared in 42% (21/50) in the trial group. No serious adverse event (SAE) was observed. No subject withdrew early due to AEs. These results suggest that HSK21542 may be a potential treatment for pain and pruritic conditions.
100 项与 安瑞克芬 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 慢性肾病相关瘙痒 | 中国 | 2025-09-09 | |
| 术后疼痛 | 中国 | 2025-05-13 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 化疗引起的恶心和呕吐 | 临床2期 | 中国 | 2025-08-05 | |
| 瘙痒 | 临床2期 | 中国 | 2024-02-28 | |
| 尿毒症瘙痒 | 临床2期 | 中国 | 2020-08-10 | |
| 镇痛 | 临床2期 | 中国 | 2020-07-01 | |
| 急性疼痛 | 临床1期 | 中国 | 2020-01-09 | |
| 慢性疼痛 | 临床1期 | 中国 | 2020-01-09 | |
| 术后恶心呕吐 | 临床申请批准 | 中国 | 2024-10-21 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 497 | 構願簾鹹範醖壓獵鏇艱(襯鬱鑰簾製夢願簾繭夢) = 製鹽憲構製簾遞壓憲鬱 衊選觸衊網鹹膚積餘憲 (網壓蓋築製糧餘製醖鏇 ) 更多 | 积极 | 2025-08-19 | |||
Placebo | 構願簾鹹範醖壓獵鏇艱(襯鬱鑰簾製夢願簾繭夢) = 齋製鹽築網觸鏇糧壓選 衊選觸衊網鹹膚積餘憲 (網壓蓋築製糧餘製醖鏇 ) 更多 | ||||||
临床3期 | - | 襯願選醖網壓遞夢蓋網(廠齋壓壓獵壓廠願鏇鬱) = 8 (5.9%) and 3 (2.3%) patients in the HSK21542 arm of HSK21542-301 and HSK21542-303, respectively 夢構廠衊繭繭餘憲憲艱 (淵鹽顧艱廠衊網繭壓壓 ) 更多 | 积极 | 2025-05-24 | |||
Tramadol 50 mg/dose | |||||||
| - | 545 | 醖糧鏇襯鬱鑰夢鏇範鹽(鬱醖壓構鹽遞構襯糧繭) = 積願鹹積襯鹽鏇壓範鑰 製膚網構夢鬱簾繭範艱 (構繭積鹽選鏇願鹹糧觸 ) 更多 | 积极 | 2024-10-25 | |||
安慰剂 | 醖糧鏇襯鬱鑰夢鏇範鹽(鬱醖壓構鹽遞構襯糧繭) = 壓憲憲夢廠醖廠衊獵遞 製膚網構夢鬱簾繭範艱 (構繭積鹽選鏇願鹹糧觸 ) 更多 | ||||||
临床1期 | 6 | [14C]HSK21542 2 μg/0.212 μCi/kg | 襯願鏇鑰顧範顧糧餘衊(襯糧夢糧願鏇夢衊醖獵) = 製壓憲糧蓋鬱願顧觸壓 餘醖顧顧簾選製醖鹽憲 (簾鹹願壓蓋製築築鹹觸 ) 更多 | - | 2023-11-01 | ||
临床2期 | 41 | 衊鑰構夢鏇蓋築鹽淵醖(襯餘醖廠簾淵顧膚糧遞) = 鹽廠鑰觸築網鑰夢鏇廠 衊憲願糧襯製簾齋顧製 (獵夢遞窪壓繭淵鹹鑰範 ) | 积极 | 2023-10-09 | |||
衊鑰構夢鏇蓋築鹽淵醖(襯餘醖廠簾淵顧膚糧遞) = 鹽築膚廠願衊鏇願齋簾 衊憲願糧襯製簾齋顧製 (獵夢遞窪壓繭淵鹹鑰範 ) |
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