Delving into the Latest Updates on Opiranjerin hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Opiranjerin, Vvz-149 free base, VVZ-000149

+ [3]

Target

5-HT2A receptor x GlyT2

Action

antagonists, inhibitors

Mechanism

5-HT2A receptor antagonists(Serotonin 2a (5-HT2a) receptor antagonists), GlyT2 inhibitors(Glycine transporter 2 inhibitors)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Pain, Postoperative

Inactive Indication

Acute Pain

Originator Organization

Vivozon, Inc.

Active Organization

Vivozon Pharmaceutical Co., Ltd.

Inactive Organization

Vivozon, Inc.

Drug Highest PhaseApproved

First Approval Date

South Korea (12 Dec 2024),

Pain, Postoperative

Regulation-

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Structure/Sequence

Molecular FormulaC21H35ClN2O5

InChIKeyGSCGQHXDHYVKOL-UHFFFAOYSA-N

CAS Registry1440796-75-7

VVZ-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.

DESIGN:

Randomized, parallel group, double-blind, Phase 3 clinical trial (Trial no. NCT05764525).

SETTING:

5 tertiary referral centers in South Korea.

PATIENTS:

284 patients undergoing laparoscopic colectomy.

INTERVENTIONS:

A continuous 10-h intravenous infusion of VVZ-149 (n = 141) or placebo (n = 143) administered after emergence from anesthesia.

MEASUREMENTS:

Pain 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 RESULTS:

Pain 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.

CONCLUSIONS:

When 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 NUMBER:

Trial Number NCT05764525.

01 Feb 2022·Journal of clinical anesthesiaQ2 · MEDICINE

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

Q2 · MEDICINE

Article

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

STUDY OBJECTIVE:

VVZ-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.

DESIGN:

Randomized, parallel group, double-blind Phase 2 clinical trial (NCT02489526).

SETTING:

3 academic institutions in the United States.

PATIENTS:

60 patients undergoing laparoscopic colorectal surgery.

INTERVENTIONS:

A continuous 8-h intravenous infusion of VVZ-149 Injections (n = 40) or placebo (n = 20) administered after emergence from anesthesia.

MEASUREMENTS:

The 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 RESULTS:

Postoperative 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.

CONCLUSIONS:

VVZ-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.

08 Sep 2021·Pain medicine (Malden, Mass.)Q3 · MEDICINE

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

Q3 · MEDICINE

Article

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

Abstract:

Objective:

VVZ-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.

Methods:

Sixty 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).

Results:

Pain 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.

Conclusions:

VVZ-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.

1

News (Medical) associated with Opiranjerin hydrochloride

18 Feb 2025

·www.prnewswire.com

VIVOZON Pharmaceutical Obtains MFDS Approval for UNAFRA Inj.: A Breakthrough Non-Opioid analgesic

SEOUL, South Korea, Feb. 18, 2025 /PRNewswire/ -- On February 17, VIVOZON Pharmaceutical announced that its non-opioid analgesic, UNAFRA Inj., was approved on December 12, 2024. (Active ingredient: Opiranserin HCl) has received approval from the Ministry of Food and Drug Safety (MFDS). With this milestone, UNAFRA Inj. has become the 38th innovative drug in Korea. Continue Reading CI UNAFRA Inj., discovered by using the company's proprietary multi-target drug development platform, is the world's first non-opioid, non-NSAIDS analgesic. It induces analgesic effect by simultaneously inhibiting Glycine Transporter Type 2 (GlyT2) and Serotonin Receptor 2a (5HT2a), thereby blocking pain signals and transmission synergistically across both the central and peripheral nervous systems. Previously, VIVOZON Pharmaceutical confirmed the safety and tolerance of the drug and secured statistical significance for efficacy in a domestic Phase 3 clinical trial and applied for new drug application (NDA) from MFDS in November 2023. The efficacy of the drug was confirmed through the primary endpoint Sum of Pain Intensity Difference over 12 Hours (SPID 12), and secondary endpoints including number of Patient-Controlled Analgesia (PCA) requests and opioid consumption over 12 Hours. This approval marks a breakthrough in the treatment landscape for moderate to severe pain, addressing the high unmet medical needs in a market that previously lacked alternatives to opioid analgesics. UNAFRA Inj. has been hailed as a game changer by the medical community, showing rapid pain relief with fewer side effects and zero risk of addiction compared to existing opioids with severe addiction. The company emphasized that UNAFRA Inj. stands apart from earlier domestically developed drugs, which were primarily "Best-in-Class" or "Me-Too" drugs mimicking existing treatments. In contrast, UNAFRA Inj. is Korea's first "First-in-Class" innovative new drug, demonstrating significant advancements in drug development complexity and originality. Spokesperson from the company states, "We are thrilled to share this groundbreaking approval with our shareholders and investors who have supported us over the years. This milestone will accelerate our plans for product launch and marketing activities." Logo - WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalPhase 3NDA

100 Deals associated with Opiranjerin hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Opiranjerin hydrochloride	-	DB16271

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Pain, Postoperative	South Korea	Vivozon Pharmaceutical Co., Ltd.	12 Dec 2024

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Pain	Phase 3	United States	Vivozon Pharmaceutical Co., Ltd.	19 Jul 2021
Pain	Phase 1	-	Vivozon, Inc.	01 Jul 2014

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05764525 (CTgov)	Phase 3	Acute Pain \| Pain, Postoperative	285	VVZ-149 Injections (VVZ-149 Injections)	bvmsdremev(ihnlzzafaw) = myduaefttk nniifgwhny (ducrhsagir, 1.73) View more	-	20 Feb 2025
				Placebo (Placebo)	bvmsdremev(ihnlzzafaw) = wgtqscrajv nniifgwhny (ducrhsagir, 1.72) View more
NCT05764525 (Pubmed) Manual	Phase 3	Pain, Postoperative	284	VVZ-149	jgxgvtqpbo(orwppwldtu) = 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. iddhpmqptq (jlbwluljip ) View more	Positive	19 Dec 2024
				Placebo
NCT02489526 (Pubmed) Manual	Phase 2	Pain, Postoperative	60	VVZ-149	svzdjtcavi(aybrbuqiyg) = non-significantly lower in patients receiving VVZ-149 compared to those receiving placebo hqbjfnzokk (vnyjcfsgiz ) View more	Positive	15 Nov 2021
				Placebo
NCT02844725 (Pubmed) Manual	Phase 2	Pain, Postoperative	59	VVZ-149	mwvrakyykv(zluirfmtkz) = reaching statistical significance at 4 hours post-emergence gslxbibwfy (lsbyuxevvf ) View more	Positive	08 Sep 2021
				Placebo