主要研究目的： 1) 定量分析男性健康受试者给药[14C]YZJ-4729酒石酸盐后排泄物中的总放射性，获得人体放射性排泄率数据和主要排泄途径； 2) 定量分析受试者单次给药[14C]YZJ-4729酒石酸盐后人血浆、尿液和粪便的放射性代谢物谱，鉴定主要代谢产物，确定受试物在人体内的代谢途径及消除途径； 3) 定量分析受试者单次给药[14C]YZJ-4729酒石酸盐后全血和血浆中的总放射性，获得血浆总放射性的药代动力学参数，并考察全血和血浆中总放射性的分配情况。次要研究目的： 1) 采用已验证的LC-MS/MS方法定量分析血浆中YZJ-4729酒石酸盐及其代谢产物（如适用）的浓度，获得血浆中YZJ-4729及其代谢产物（如适用）的药动学参数。 2) 观察[14C]YZJ-4729酒石酸盐单次给药后中国成年男性健康受试者的安全性。

[Translation]

Main study objectives: 1) To quantitatively analyze the total radioactivity in the excreta of male healthy subjects after administration of [14C]YZJ-4729 tartrate, and obtain the data on human radioactive excretion rate and main excretion pathways; 2) To quantitatively analyze the radioactive metabolite profiles in human plasma, urine and feces after a single administration of [14C]YZJ-4729 tartrate to identify the main metabolites, and determine the metabolic pathways and elimination pathways of the test substance in the human body; 3) To quantitatively analyze the total radioactivity in whole blood and plasma after a single administration of [14C]YZJ-4729 tartrate to obtain the pharmacokinetic parameters of total plasma radioactivity, and investigate the distribution of total radioactivity in whole blood and plasma. Secondary study objectives: 1) To quantitatively analyze the concentration of YZJ-4729 tartrate and its metabolites (if applicable) in plasma using a validated LC-MS/MS method, and obtain the pharmacokinetic parameters of YZJ-4729 and its metabolites (if applicable) in plasma. 2) To observe the safety of [14C]YZJ-4729 tartrate in healthy Chinese adult male subjects after a single administration.

Start Date01 Apr 2024

Sponsor / Collaborator

Shanghai Haiyan Pharmaceutical Technology Co Ltd

NCT06680466 / Active, not recruitingPhase 2

A Multicenter, Ramdomized, Double-Blind, Dose-Regimen Finding, Placebo and Active-Controlled Phase Ⅱ Study to Evaluate the Efficacy and Safety of YZJ-4729 in Patients With Moderate to Severe Acute Pain After Abdominal Surgery

Primary Objective： To explore the analgesic efficacy of YZJ-4729 compared with placebo in patients with acute postoperative pain following abdominal surgery.
Secondary Objective： To explore the analgesic efficacy and safety of YZJ-4729 compared with placebo and morphine in patients with acute postoperative pain following abdominal surgery.

Start Date26 Dec 2023

Sponsor / Collaborator

Shanghai Haiyan Pharmaceutical Technology Co Ltd

CTR20232827 / Active, not recruitingPhase 2

YZJ-4729酒石酸盐注射液用于腹部手术术后镇痛有效性及安全性的多中心、随机、双盲、剂量探索、安慰剂及阳性药平行对照的Ⅱ期临床试验

[Translation] A multicenter, randomized, double-blind, dose-finding, placebo- and active drug-controlled phase II clinical trial on the efficacy and safety of YZJ-4729 tartrate injection for postoperative analgesia in abdominal surgery

初步探索与安慰剂相比，YZJ-4729 酒石酸盐注射液用于腹部手术术后镇痛的有效性；探索与安慰剂、吗啡相比，YZJ-4729 酒石酸盐注射液用于腹部手术术后镇痛的安全性。

[Translation]

To preliminarily explore the effectiveness of YZJ-4729 tartrate injection for postoperative analgesia in abdominal surgery compared with placebo; to explore the safety of YZJ-4729 tartrate injection for postoperative analgesia in abdominal surgery compared with placebo and morphine.

Start Date26 Dec 2023

Sponsor / Collaborator

Shanghai Haiyan Pharmaceutical Technology Co Ltd

100 Clinical Results associated with YZJ-4729

100 Translational Medicine associated with YZJ-4729

100 Patents (Medical) associated with YZJ-4729

Literatures (Medical) associated with YZJ-4729

Frontiers in Pharmacology

Pharmacokinetics, metabolite profiling, safety and tolerability of YZJ-4729 tartrate, a novel G protein-biased μ-opioid receptor agonist, in healthy Chinese subjects

Article

Author: Ni, Yufeng ; Ouyang, Wen ; Ding, Li ; Gao, Huaye ; Cheng, Minlu ; Yang, Guoping

Objective:YZJ-4729 is a novel G protein-biased μ-opioid receptor agonist for the treatment of acute pain in adult patients who require intravenous opioid analgesic therapy. The aim of this study was to assess the pharmacokinetics, metabolite profiling, safety and tolerability of YZJ-4729 in healthy Chinese subjects following the single intravenous doses ranged from 0.2 mg to 6 mg.Methods:This single-center, randomized, double-blind, placebo-controlled clinical study was conducted in 54 healthy male and female Chinese subjects after single ascending doses of YZJ-4729 tartrate (0.2, 0.5, 1.5, 3, 4.5, and 6 mg). Subjects in each cohort were assigned randomly to receive a single intravenous dose of YZJ-4729 tartrate injection or placebo at a ratio of 4:1. Pharmacokinetic characteristics, metabolite profiling, safety and tolerability profiles of the study drug were evaluated.Results:Overall, YZJ-4729 was safe and well tolerated in healthy Chinese subjects. The study drug reached peak plasma concentrations nearly at the end of the infusion. After administration, YZJ-4729 was eliminated rapidly with a terminal elimination half-life of 0.862–2.50 h, and excreted little in human excreta. The maximum drug concentration and area under the plasma concentration-time curve increased with dose escalation across the entire dose range. YZJ-4729 experienced extensive metabolism in human body. A total of 19 metabolites were identified and the characteristic metabolic pathways involved hydroxylation, ketone formation, N-dealkylation and glucuronide conjugation. Metabolite M10 was the most abundant circulating metabolite, and represented over 10% of total drug-related systemic exposure. Further PK and safety evaluation of M10 was necessary.Conclusion:The clinical study results laid a foundation for the further clinical studies of YZJ-4729 in patients.Clinical Trial Registration:http://www.chinadrugtrials.org.cn, identifier CTR20222574.

100 Deals associated with YZJ-4729

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Pain	Phase 2	CN	Shanghai Haiyan Pharmaceutical Technology Co Ltd	26 Dec 2023
Analgesia	Phase 2	CN	Shanghai Haiyan Pharmaceutical Technology Co Ltd	26 Dec 2023
Pain, Postoperative	Phase 1	CN	Shanghai Haiyan Pharmaceutical Technology Co Ltd	12 Oct 2022

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