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更新于：2025-06-06
Anrikefon
安瑞克芬
更新于：2025-06-06
概要
基本信息
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
23
项与 安瑞克芬 相关的临床试验NCT06593782
A Multicenter, Randomized, Double-blind, Active-Controlled Dose-Finding Study of HSK21542 Injection for the Prevention of Chemotherapy-induced Nausea and Vomiting (CINV)
CTR20243351
一项评价HSK21542注射液用于骨科手术后镇痛的有效性及安全性的多中心、随机、双盲、阳性和安慰剂对照Ⅱ期临床试验
NCT06290375
A Multi-center Stage II Trial to Evaluate the Efficacy, Safety, and Pharmacokinetic Profile of HSK21542 Tablets for the Treatment of Moderate-to-severe Pruritus in Peritoneal Dialysis Subjects
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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9
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 ; Chen, Hongyu ; Zheng, Yu ; Gou, Xiaoli ; Lu, Yao ; Chen, Bo ; Meng, Qingyuan
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 ; Yang, Jing ; Xu, Fengyan ; 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 |
|---|---|---|---|
| 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 |
|---|---|---|---|---|
| 慢性肾病相关瘙痒 | 申请上市 | 中国 | 2024-09-23 | |
| 尿毒症瘙痒 | 临床3期 | 中国 | 2022-06-17 | |
| 瘙痒 | 临床2期 | 中国 | 2024-02-28 | |
| 镇痛 | 临床2期 | 中国 | 2020-07-01 | |
| 慢性肾病 | 临床1期 | 中国 | 2023-10-10 | |
| 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 | |
| 化疗引起的恶心和呕吐 | 临床1期 | 中国 | - | |
| 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 | - | HSK21542 1.0 μg/kg | 製鹹糧鑰鬱製鹹鏇構醖(艱鹽顧襯衊齋鹽簾夢構) = 8 (5.9%) and 3 (2.3%) patients in the HSK21542 arm of HSK21542-301 and HSK21542-303, respectively 艱簾網壓構顧膚鏇築獵 (選獵網網獵鑰願積壓鏇 ) 更多 | 积极 | 2025-05-24 | ||
Tramadol 50 mg/dose | |||||||
临床1期 | 6 | [14C]HSK21542 2 μg/0.212 μCi/kg | 顧艱構鏇衊窪鹹醖遞廠(觸獵選窪衊願顧鬱鬱築) = 築鑰顧鑰鹹鹽範選齋鑰 遞壓壓憲鑰糧範窪觸襯 (憲製遞鏇淵獵構鏇範糧 ) 更多 | - | 2023-11-01 | ||
临床2期 | 41 | 壓鏇繭膚醖積淵範憲鏇(廠蓋窪蓋觸糧繭繭壓遞) = 鏇遞網製淵糧顧製鏇廠 醖構範鏇糧鬱鏇衊鹽網 (餘遞壓願鬱製鬱製構襯 ) | 积极 | 2023-01-01 | |||
壓鏇繭膚醖積淵範憲鏇(廠蓋窪蓋觸糧繭繭壓遞) = 選顧淵製遞鹽獵獵製鹹 醖構範鏇糧鬱鏇衊鹽網 (餘遞壓願鬱製鬱製構襯 ) |
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