Opiranserin(Opiranserin) - 药物靶点：5-HT2A receptor x GlyT2_在研适应症：急性疼痛，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

Vvz-149 free base

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. (Old)

非在研机构

Vivozon, Inc.

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C21H34N2O5

InChIKeyJQUVQWMHZSYCRQ-UHFFFAOYSA-N

CAS号1441000-45-8

关联

18

项与 Opiranserin 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 Opiranserin 相关的临床结果

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100 项与 Opiranserin 相关的转化医学

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100 项与 Opiranserin 相关的专利（医药）

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4

项与 Opiranserin 相关的文献（医药）

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 ; Nedeljkovic, Srdjan S ; Kim, Jina ; 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.

2018-01-01·The Journal of Clinical Pharmacology

Safety, Tolerability, and Pharmacokinetic Characteristics of a Novel Nonopioid Analgesic, VVZ‐149 Injections in Healthy Volunteers: A First‐in‐Class, First‐in‐Human Study

Article

作者: Jang, Kyungho ; Yoon, Jangsoo ; Chung, Jae‐Yong ; Lee, Sang Rim ; Cho, Sunyoung ; Yu, Kyung‐Sang ; Kim, Anhye ; Lee, SeungHwan ; Lee, Doo H. ; Oh, Jaeseong

AbstractVVZ‐149, a dual antagonist of GlyT2 and 5HT2A receptors, is an investigational analgesic with a novel mechanism of action that is currently under early‐stage clinical development as an injectable agent for the treatment of postoperative pain. Here, the safety, tolerability, and pharmacokinetics of VVZ‐149 injections in healthy male volunteers were explored in a randomized, double‐blind, single‐ and multiple‐ascending‐dose (SAD and MAD, respectively), placebo‐controlled clinical study. Subjects randomly received a 4‐hour intravenous infusion of 0.25‐8 mg/kg VVZ‐149 or placebo in the SAD study (n = 46) or a 4‐hour intravenous infusion of 4–7 mg/kg VVZ‐149 or placebo twice daily for 3 days in the MAD study (n = 20). Serial blood and urine samples were collected for the pharmacokinetic analysis of VVZ‐149 and its active metabolite (VVZ‐368). Noncompartmental and compartmental pharmacokinetic analyses were performed. Various dosing scenarios were simulated to identify the adequate dosing regimen for the subsequent trials. Plasma exposure to VVZ‐149 and VVZ‐368 showed a dose‐proportional increase. VVZ‐149 did not accumulate in the plasma, whereas the plasma concentration of VVZ‐368 increased by 1.23‐ to 2.49‐fold after the fifth and sixth doses, respectively, in the MAD trial. Among the simulated dosing regimens, a loading dose followed by a maintenance dose was found to be an optimal dosing regimen, yielding the effective concentration estimated from animal studies in rat models of neuropathic or inflammatory pain. Single‐ or multiple‐dose administration of VVZ‐149 was generally well tolerated. These results showed that 0.5–8 mg/kg VVZ‐149 exhibited linear pharmacokinetic characteristics and can be safely administered in further clinical studies.

100 项与 Opiranserin 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Opiranserin	-	DB16271

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
术后疼痛	申请上市	美国	Vivozon, Inc.	2019-05-23
早期胃癌	申请上市	韩国	Vivozon, Inc.	2015-08-01
疼痛	申请上市	-	Vivozon, Inc.	2014-07-01
急性疼痛	临床3期	韩国	Vivozon Pharmaceutical Co., Ltd. (Old)	2021-07-19