Opiranjerin hydrochloride(Opiranjerin hydrochloride) - 药物靶点：5-HT2A receptor x GlyT2_在研适应症：术后疼痛_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Opiranjerin、Vvz-149 free base

+ [3]

靶点

5-HT2A receptor x GlyT2

作用机制

5-HT2A receptor拮抗剂(5-羟色胺2A受体拮抗剂)、GlyT2抑制剂(甘氨酸转运体2抑制剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Vivozon Pharmaceutical Co., Ltd.

非在研机构

Vivozon, Inc.

最高研发阶段批准上市

首次获批日期

韩国 (2024-12-12),

术后疼痛

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C21H35ClN2O5

InChIKeyGSCGQHXDHYVKOL-UHFFFAOYSA-N

CAS号1440796-75-7

关联

18

项与 Opiranjerin hydrochloride 相关的临床试验

KCT0009038

/ Completed临床1期

A Phase 1, Open, Single-Dose Study to Compare the Exposure level in CSF and Plasma of VVZ-149 Injections in Healthy Male Volunteers

开始日期2023-09-11

申办/合作机构

Vivozon, Inc.

KCT0007704

/ Completed临床2期

A Randomized, Double-Blind, Parallel Group, Placebo-Controlled Study to Evaluate Analgesic Efficacy and Safety of Opiranserin Cream for Myofascial pain syndrome

开始日期2022-06-07

申办/合作机构

Vivozon, Inc.

KCT0007551

/ Completed临床3期

A Phase 3, Multicenter, Randomized, Double-Blind, Parallel Group, Placebo-Controlled Study to Evaluate the Efficacy and Safety of VVZ-149 Injections for the Treatment of Postoperative Pain following Laparoscopic Colectomy

开始日期2021-07-20

申办/合作机构

Vivozon, Inc.

100 项与 Opiranjerin hydrochloride 相关的临床结果

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100 项与 Opiranjerin hydrochloride 相关的转化医学

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100 项与 Opiranjerin hydrochloride 相关的专利（医药）

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5

项与 Opiranjerin hydrochloride 相关的文献（医药）

2025-02-01·Journal of Clinical Anesthesia

Reduction of postoperative pain and opioid consumption by VVZ-149, first-in-class analgesic molecule: A confirmatory phase 3 trial of laparoscopic colectomy

Article

作者: Cho, Sunyoung ; Lee, Sang Rim ; Sim, Ji-Yeon ; Yoon, Seung Zhoo ; Nedeljkovic, Srdjan S ; Kim, Duk Kyung ; Lee, Ho-Jin ; Bahk, Jae-Hyon ; Kim, Jina ; Park, MiHye ; Park, Insun ; Moon, Young-Jin ; Song, Inkyung ; Oh, Ah-Young

STUDY OBJECTIVEVVZ-149 is a small molecule that inhibits the glycine transporter type 2 and the serotonin receptor 5-hydroxytryptamine 2 A. In this Phase 3 study, we investigated the efficacy and safety of VVZ-149 as a single-use injectable analgesic for treating moderate to severe postoperative pain after laparoscopic colectomy.DESIGNRandomized, parallel group, double-blind, Phase 3 clinical trial (Trial no. NCT05764525).SETTING5 tertiary referral centers in South Korea.PATIENTS284 patients undergoing laparoscopic colectomy.INTERVENTIONSA continuous 10-h intravenous infusion of VVZ-149 (n = 141) or placebo (n = 143) administered after emergence from anesthesia.MEASUREMENTSPain intensity was assessed using a numeric rating scale (NRS) from the start of infusion for 48 h. The primary efficacy measure was the Sum of Pain Intensity Difference (SPID) for the first 12 h after the start of drug infusion. Other efficacy measures included SPID at other time points, opioid consumption via on-demand patient-controlled analgesia (PCA) and rescue medication, and proportion of patients who did not require rescue opioids for 48 h post-dose.MAIN RESULTSPain relief as measured by SPID was significantly improved by 35 % in the VVZ-149 group compared to the placebo group at 6 h (p = 0.0193) and 12 h (p = 0.0047) after the start of infusion. Significantly lower pain intensity scores were observed between 4-10 h in the VVZ-149 group compared to the placebo group (p = 0.0007), reaching mild pain (mean NRS <4) at 8 h. VVZ-149 alleviated pain during the first 12 h post-dose with 30.8 % less opioid consumption and 60.2 % fewer PCA requests when compared with placebo. A higher proportion of patients receiving VVZ-149 were rescue opioid-free during 2-6 h (p = 0.0026) and 6-12 h (p = 0.0024) compared with the placebo group. VVZ-149 administration in post-colectomy patients was generally safe and well tolerated.CONCLUSIONSWhen compared to placebo, VVZ-149 infusion demonstrated a significant reduction of pain within the first 12 h after surgery with a substantial decrease in opioid use. VVZ-149 rapidly lowers the pain intensity starting at as early as 4 h post-dose, allowing subjects to experience mild pain levels from 8 h through 48 h. Therefore, the analgesic effect of VVZ-149 was shown to effectively relieve pain and reduce opioid use for treating moderate to severe pain in the early postoperative care setting.REGISTRATION NUMBERTrial Number NCT05764525.

2022-02-01·Journal of Clinical Anesthesia2区 · 医学

Exploratory study of VVZ-149, a novel analgesic molecule, in the affective component of acute postoperative pain after laparoscopic colorectal surgery

2区 · 医学

Article

作者: Bao, Xiaodong ; Zeballos, Jose L ; Lee, Sang Rim ; Ledley, Johanna S ; Bai, Xiang ; Cho, Sunyoung ; Nedeljkovic, Srdjan S ; Zhang, Yi ; Song, Inkyung ; Correll, Darin J ; Bhandari, Ashish

STUDY OBJECTIVEVVZ-149 is a small molecule that inhibits the glycine transporter type 2 and the serotonin receptor 5-hydroxytryptamine 2A. In the present study, we investigated the efficacy and safety of VVZ-149 as a single-use injectable analgesic for treating moderate to severe postoperative pain after colorectal surgery.DESIGNRandomized, parallel group, double-blind Phase 2 clinical trial (NCT02489526).SETTING3 academic institutions in the United States.PATIENTS60 patients undergoing laparoscopic colorectal surgery.INTERVENTIONSA continuous 8-h intravenous infusion of VVZ-149 Injections (n = 40) or placebo (n = 20) administered after emergence from anesthesia.MEASUREMENTSThe outcome measures included pain intensity (PI), opioid consumption via patient-controlled analgesia (PCA), and rescue dosing provided "as needed". Early rescue dosing with opioids postoperatively was associated with preoperative negative affect (anxiety, depression, and pain catastrophizing), enabling it to be used as an indirect measure of the affective component of pain. Efficacy outcomes were compared between treatment groups based on preoperative negative affect and early rescue dosing of opioids.MAIN RESULTSPostoperative PI was non-significantly lower in patients receiving VVZ-149 compared to those receiving placebo. The VVZ-149 group had a 34.2% reduction in opioid consumption for 24 h post-dose, along with fewer PCA demands. Somnolence and headache was higher in the intervention group. For patients characterized by high levels of preoperative negative affect, the VVZ-149 group experienced a significant pain reduction and 40% less opioid use compared to the placebo group.CONCLUSIONSVVZ-149 resulted in a non-significant reduction of postoperative pain during the first 8 h after surgery. Post hoc analysis indicates that VVZ-149 may benefit patients with negative affect who otherwise have higher postoperative opioid use. REGISTRATION NUMBER: www.clinicaltrials.gov, ID: NCT02489526.

2021-09-08·Pain Medicine3区 · 医学

Role of VVZ-149, a Novel Analgesic Molecule, in the Affective Component of Pain: Results from an Exploratory Proof-of-Concept Study of Postoperative Pain following Laparoscopic and Robotic-Laparoscopic Gastrectomy

3区 · 医学

Article

作者: Lee, Chaewon ; Kim, Jina ; Nedeljkovic, Srdjan S ; Song, Inkyung ; Bai, Sun Joon ; Lee, Sang Rim ; Cho, Sunyoung

AbstractObjectiveVVZ-149 is a small molecule that both inhibits the glycine transporter type 2 and the serotonin receptor 5 hydroxytryptamine 2 A. In a randomized, parallel-group, and double-blind trial (NCT02844725), we investigated the analgesic efficacy and safety of VVZ-149 Injections, which is under clinical development as a single-use injectable product for treating moderate to severe postoperative pain.MethodsSixty patients undergoing laparoscopic and robotic-laparoscopic gastrectomy were randomly assigned to receive a 10-hour intravenous infusion of VVZ-149 Injections or placebo, initiated approximately 1 hour before completion of surgical suturing. Major outcomes included pain intensity and opioid consumption via patient-controlled analgesia and rescue analgesia provided “as needed.” The treatment efficacy of VVZ-149 was further examined in a subpopulation requiring early rescue medication, previously associated with the presence of high levels of preoperative negative affect in a prior Phase 2 study (NCT02489526).ResultsPain intensity was lower in the VVZ-149 (n = 30) than the placebo group (n = 29), reaching statistical significance at 4 hours post-emergence (P < .05), with a 29.5% reduction in opioid consumption for 24 hours and fewer demands for patient-controlled analgesia. In the rescued subgroup, VVZ-149 further reduced pain intensity (P < .05) with 32.6% less opioid consumption for 24 hours compared to placebo patients.ConclusionsVVZ-149 demonstrated effective analgesia with reduced postoperative pain and opioid requirements. Consistent with the results from the previous Phase 2 study, patients with early rescue requirement had greater benefit from VVZ-149, supporting the hypothesis that VVZ-149 may alleviate the affective component of pain and mitigate excessive use of opioids postoperatively.

100 项与 Opiranjerin hydrochloride 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Opiranjerin hydrochloride	-	DB16271

研发状态

批准上市

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适应症	国家/地区	公司	日期
术后疼痛	韩国	Vivozon Pharmaceutical Co., Ltd.	2024-12-12

未上市

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适应症	最高研发状态	国家/地区	公司	日期
急性疼痛	临床前	韩国	Vivozon Pharmaceutical Co., Ltd.	2021-07-19
术后疼痛	临床前	美国	Vivozon, Inc.	2019-05-23
疼痛	临床前	-	Vivozon, Inc.	2014-07-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05764525 (Pubmed) 人工标引	临床3期	术后疼痛	284	VVZ-149	(繭選窪選鹽醖齋衊鬱鏇) = significantly improved by 35 % in the VVZ-149 group compared to the placebo group at 6 h (p = 0.0193) and 12 h (p = 0.0047) after the start of infusion. 鹽鹹夢選鹽觸構齋襯鬱 (壓獵築齋選鬱醖憲願鬱 ) 更多	积极	2024-12-19
				Placebo
NCT02489526 (Pubmed) 人工标引	临床2期	术后疼痛	60	VVZ-149	(觸鹽襯蓋構鏇齋夢壓鹹) = non-significantly lower in patients receiving VVZ-149 compared to those receiving placebo 鹹顧夢鬱築鬱衊壓廠蓋 (顧餘觸積艱鹽襯繭憲蓋 ) 更多	积极	2021-11-15
				Placebo
NCT02844725 (Pubmed) 人工标引	临床2期	术后疼痛	59	VVZ-149	(積簾願憲願齋築選鏇蓋) = reaching statistical significance at 4 hours post-emergence 餘憲構鑰窪鹹憲鑰窪網 (製顧獵範餘窪廠廠廠鏇 ) 更多	积极	2021-09-08
				Placebo