A Phase 1, Randomized, Double-Blinded, Placebo-Controlled, Single- and Multiple- Dose Escalation Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Oral VVZ-2471 in Healthy Male Volunteers

开始日期2022-11-01

申办/合作机构

Vivozon, Inc.

100 项与 VVZ-2471 相关的临床结果

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100 项与 VVZ-2471 相关的转化医学

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100 项与 VVZ-2471 相关的专利（医药）

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项与 VVZ-2471 相关的文献（医药）

2025-06-01·CNS DRUGS

Evaluation of Safety, Pharmacokinetic, and Pharmacodynamic Characteristics of a Novel Dual mGluR5/5-HT2AR Antagonist (VVZ-2471) in a Randomized, Double-Blind, First-in-Human Study

Article

作者: Lee, Sang Rim ; Cho, Sunyoung ; Kim, Jina ; Song, Inkyung ; Chung, Jae-Yong ; Yu, Kyung-Sang ; Lee, HyunJoon ; Bae, Sungyeun

BACKGROUND:

VVZ-2471 is a dual-target compound that simultaneously inhibits both metabotropic glutamate receptor subtype 5 and serotonin receptor subtype 2A. Preclinical studies have supported VVZ-2471 as a promising candidate for opioid use disorder. This study aimed to evaluate the safety and pharmacokinetic (PK)-pharmacodynamic (PD) characteristics of VVZ-2471 capsules in healthy Korean adults.

METHODS:

A phase I, double blind, placebo controlled, single ascending dose (SAD) and multiple ascending dose (MAD) study was conducted in healthy adult males. In the SAD study, participants received a single oral dose of VVZ-2471 ranging from 25 to 600 mg, including a satellite food-effect group receiving 200 mg. In the MAD study, participants received 200 mg once daily (QD), 200 mg twice daily, and 400 mg QD for 7 days. Plasma and urine samples were collected for the PK analyses. Safety analysis was based on adverse events, clinical laboratory tests, vital signs, physical examinations, 12-lead electrograms, oxygen saturation monitoring, and the Beck Depression Inventory-II test. The potential of VVZ-2471 for treating addiction was explored using a well-established questionnaire on smoking urges (QSU-Brief) consisting of ten items.

RESULTS:

A total of 49 and 24 healthy Korean adult males completed the SAD and MAD study, respectively. The overall demographic characteristics of participants who received VVZ-2471 or placebo in the SAD and MAD studies were generally comparable. Following a single oral dose of VVZ-2471 up to 600 mg, the area under the concentration-time curve (AUC) increased proportionally with the dose. After repeated administration, the accumulation ratio of VVZ-2471 ranged from 1.4 to 2.0. In the fed state, the maximum plasma concentration and AUC of VVZ-2471 decreased to 0.78-fold and 0.61-fold, respectively, compared with the fasting state. Urinary excretion was marginal. The most common adverse events were nausea and dizziness. Among 29 smokers, participants given VVZ-2471 at 200 mg or higher had reduced smoking urges compared with the placebo.

CONCLUSIONS:

VVZ-2471 was well tolerated up to a single oral dose of 600 mg and a daily oral dose of 400 mg for 7 days. While preliminary, a trend of reducing smoking urges was observed in the VVZ-2471 group.

REGISTRATION:

Clinical Research Information Service (CRiS), Republic of Korea (a primary registry in the World Health Organization (WHO) Registry Network) identifier no. KCT000889.

项与 VVZ-2471 相关的新闻（医药）

2025-11-10

·今日头条

镇痛又戒瘾！这款口服新药VVZ-2471获批临床

最近，生物医药圈传来一个重磅好消息——Vivozon公司宣布，其口服非阿片类镇痛候选药物VVZ-2471的IND申请已获得美国FDA批准，即将启动针对吸烟者的1b期临床试验！这可不是一款普通的止痛药，它不仅有望解决难缠的神经理性疼痛，还能顺带抑制成瘾相关行为，相当于给患者送上了“双重福利”。对于被慢性疼痛和成瘾问题困扰的人群来说，这无疑是黑暗中的一抹亮色。今天咱们就来好好聊聊这款“全能型”新药的过人之处。要理解VVZ-2471的价值，咱们得先说说目前医疗领域面临的两大“老大难”问题：神经病理性疼痛的折磨和阿片类药物的成瘾危机。先说说神经病理性疼痛，这可不是普通的“磕碰痛”，而是源于神经系统本身的损伤或病变，就像电线短路后不断发出错误的疼痛信号。它的痛法五花八门，可能是烧灼样、电击样，也可能是针刺样的剧痛，常见于糖尿病神经病变、带状疱疹后遗症、三叉神经痛等疾病。更要命的是，这种疼痛往往反复发作、难以根治，普通的止痛药比如布洛芬根本不管用，严重影响患者的睡眠和情绪，甚至让人陷入“疼痛-焦虑-疼痛加剧”的恶性循环。数据显示，普通人群中这种疼痛的患病率高达7%-10%，相当于每10个人里就可能有1个正在遭受它的折磨。再说说阿片类药物的困境。长期以来，对于严重疼痛，医生们常依赖阿片类药物来缓解，但这类药物的成瘾风险一直是悬在患者头上的“利剑”。像咱们熟悉的复方甘草片，里面就含有阿片粉，长期吃不仅容易成瘾，还会导致低钾血症，让人心慌、四肢无力。更可怕的是，阿片类药物滥用还可能导致用药过量和死亡，美国每年因阿片类药物过量死亡的人数就超过8万，堪称“致命的止痛药” 。而且很多慢性疼痛患者长期用药后会产生耐药性，不得不不断加量，进一步增加了成瘾风险。除此之外，成瘾问题本身也是个大麻烦。就拿吸烟来说，尼古丁会刺激大脑产生多巴胺，让人产生愉悦感，一旦停吸就会出现烦躁、失眠等戒断反应，这就是上瘾的底层逻辑。而很多吸烟者同时还患有神经病理性疼痛，比如糖尿病患者吸烟会加重神经损伤，让疼痛更难控制，这两种问题叠加，简直让患者苦不堪言。更让人无奈的是，目前针对这些问题缺乏完美的解决方案。治疗神经理性疼痛效果有限，而缓解疼痛的药物又可能带来成瘾风险，形成了一个难以打破的“死循环”。就在这时，VVZ-2471的出现，有望打破这个僵局。这款新药的核心亮点在于它的“双重受体拮抗剂”身份，简单说就是它能同时精准“瞄准”并阻断血清素5-HT2A受体和mGluR5受体这两个关键靶点。这两个受体就像是神经系统里的“兴奋开关”，当它们异常活跃时，就会导致神经兴奋性失衡，进而引发疼痛和成瘾行为。 VVZ-2471就像一个“神经调节器”，通过阻断这两个“开关”，能有效调节神经系统的兴奋性，从根源上缓解神经理性疼痛。而且它完全不依赖阿片类成分，从源头上避免了成瘾风险，这可是个巨大的突破！更神奇的是，这种作用机制还能顺带抑制成瘾相关行为，比如吸烟、阿片类药物依赖等，相当于一款药能解决两个核心问题。可能有人会好奇，为什么要选择吸烟者作为1b期临床试验的对象呢？其实这里面大有讲究。一方面，很多吸烟者本身就存在神经理性疼痛的风险，比如长期吸烟会影响血液循环，加重神经损伤；另一方面，吸烟成瘾本身就是典型的成瘾行为，正好能验证VVZ-2471在抑制成瘾方面的潜力。可以说，这个试验人群的选择非常有针对性，能同时考察药物在镇痛和戒瘾两方面的效果。值得一提的是，VVZ-2471的研发进展远不止这一步。目前，它已经在韩国开展针对神经理性疼痛患者的2期临床试验，这意味着它在镇痛方面的效果已经经过了初步验证。更让人振奋的是，今年9月，这款药物还被美国国立卫生研究院（NIH）下属的国家药物滥用研究所（NIDA）选为阿片类药物成瘾（OUD）的治疗开发项目。要知道，NIDA在药物成瘾治疗领域可是权威中的权威，他们的认可充分说明VVZ-2471在戒瘾方面的潜力得到了专业机构的高度重视。要知道，阿片类药物成瘾目前是全球性的公共卫生危机，仅美国监狱中就有大量成瘾患者，而有效的药物治疗能显著降低他们出狱后的复吸率和 overdose 死亡率。VVZ-2471能被NIDA选中，足以证明它在解决成瘾问题上的重要价值。这款新药还有一个很大的优势——口服剂型。对于需要长期用药的慢性疼痛患者来说，口服药比打针、输液方便太多，大大提升了用药依从性。而且作为非阿片类药物，它避免了阿片类药物常见的呼吸抑制、便秘等副作用，安全性更有保障。咱们来畅想一下VVZ-2471未来的应用场景：一位饱受糖尿病神经痛折磨的吸烟者，每天吃一片药，不仅疼痛得到了缓解，吸烟的欲望也慢慢降低；一位阿片类药物成瘾的患者，在它的帮助下，既能摆脱疼痛困扰，又能逐步戒除药瘾，重新回归正常生活。这画面想想就让人激动！当然，我们也得理性看待，VVZ-2471目前还处于临床试验阶段，后续还需要更多的数据来验证它的长期效果和安全性。但不可否认的是，它的出现为疼痛治疗和成瘾干预提供了全新的思路。这种“镇痛+戒瘾”的双重功效，在目前的药物研发中并不多见，一旦成功上市，将有望改写相关疾病的治疗格局。对于患者来说，这意味着他们终于不用在“缓解疼痛”和“避免成瘾”之间做艰难选择；对于医生来说，这将是一款全新的“利器”，能更精准地帮助患者解决问题；对于整个医疗行业来说，VVZ-2471的研发进展也为非阿片类镇痛药物和成瘾治疗药物的发展提供了宝贵的经验。目前，韩国的2期临床试验正在推进中，美国针对吸烟者的1b期临床试验也即将启动。让我们共同期待这些临床试验能取得积极成果，希望VVZ-2471能早日完成研发，获批上市。相信在不久的将来，这款“全能型”新药将走进更多患者的生活，为他们驱散疼痛的阴霾，摆脱成瘾的枷锁，重新拥抱健康快乐的人生！

临床申请

2025-11-09

·药明康德

有望预防癌症的现货型免疫疗法；有望抑制烟瘾的小分子药物获批临床…… | 一周盘点

本期看点 1. 现货型癌症疫苗NOUS-209在林奇综合征（LS）携带者中的1b/2期临床试验数据积极，展现出预防LS相关初发和复发癌症的潜力。 2. 口服非阿片类镇痛候选药物VVZ-2471的IND申请已获得美国FDA批准，该药不仅有望缓解神经病理性疼痛，还具备抑制成瘾相关行为的潜力。 NOUS-209：公布1b/2期临床试验的新数据 Nouscom公司公布了其现货型癌症疫苗NOUS-209在林奇综合征携带者中的1b/2期临床试验新数据。NOUS-209是一种旨在“拦截癌症”于发生前的预防性免疫疗法，利用公司专有的病毒载体平台递送209种在微卫星不稳定性高（MSI-H）肿瘤中广泛存在的共享移码肽（FSP）新抗原，训练免疫系统识别并清除癌前及癌变细胞。LS是最常见的遗传性癌症综合征，显著增加结直肠癌、子宫内膜癌等多种癌症风险，目前缺乏有效的药物预防手段。研究显示，每年一次的NOUS-209重复治疗可安全、有效地增强LS携带者持久的T细胞免疫应答。在临床效果方面，尽管基线时4.7%的受试者存在需切除的高级别腺瘤（按标准治疗已清除），但在治疗后一年随访期内未检出任何新的高级别腺瘤，而该人群预期年发病率约为4%。该结果首次提供了NOUS-209具有癌症预防潜力的临床证据。此外，对原发及异时性MSI肿瘤的分析证实，NOUS-209靶向的大量FSP新抗原持续存在，支持其在预防LS相关初发和复发癌症中的广泛应用前景。 VVZ-2471：IND申请获得FDA许可 Vivozon公司宣布，其口服非阿片类镇痛候选药物VVZ-2471的IND申请已获得美国FDA批准，启动针对吸烟者的1b期临床试验。VVZ-2471是一种双重受体拮抗剂，可同时阻断血清素5-HT2A受体和mGluR5受体，通过调节神经系统兴奋性，不仅有望缓解神经病理性疼痛，还具备抑制成瘾相关行为的潜力。目前，该药物正在韩国开展针对神经病理性疼痛患者的2期临床试验，并已于今年9月被美国国立卫生研究院（NIH）下属的国家药物滥用研究所（NIDA）选为阿片类药物成瘾（OUD）的治疗开发项目。 SPY003：公布1期临床试验的中期数据 Spyre Therapeutics公司公布了其在研长效单克隆抗体SPY003的积极1期临床试验中期数据。SPY003是一种靶向IL-23 p19亚基的延长半衰期抗体，旨在用于治疗炎症性肠病（IBD），包括溃疡性结肠炎和克罗恩病。该药基于Spyre的长效抗体平台开发，具备支持每季度甚至每年两次皮下给药的潜力。此次公布的数据来自一项随机、双盲、安慰剂对照的1期研究，共纳入59名健康成人受试者。SPY003在所有剂量水平下均表现出良好的耐受性，安全性特征与同类抗IL-23药物一致，仅报告两例≥2级治疗相关不良事件（均判定与药物无关），无严重不良事件；最常见的治疗期间不良事件为头痛。关键药代动力学数据显示，SPY003的半衰期约为85天，有望通过单次皮下注射实现每季度或每年两次的维持给药方案。此外，未观察到抗药抗体对药代动力学产生明显影响。参考资料： [1] Vesper Bio announces positive Phase Ib/IIa topline results for lead candidate VES001 for frontotemporal degeneration. Retrieved November 7, 2025, from https://www.prnewswire.com/news-releases/vesper-bio-announces-positive-phase-ibiia-topline-results-for-lead-candidate-ves001-for-frontotemporal-degeneration-302600150.html [2] 비보존, '비마약성 진통제' 1b상 "美 IND 승인". Retrieved November 7, 2025, from https://www.biospectator.com/news/view/26828 [3] Caribou Biosciences Announces Positive Data from ANTLER Phase 1 Trial Demonstrating Efficacy and Durability of Vispa-cel (CB-010), an Allogeneic CAR-T Cell Therapy, on Par with Autologous CAR-T Cell Therapies. Retrieved November 7, 2025, from https://www.globenewswire.com/news-release/2025/11/03/3179104/0/en/Caribou-Biosciences-Announces-Positive-Data-from-ANTLER-Phase-1-Trial-Demonstrating-Efficacy-and-Durability-of-Vispa-cel-CB-010-an-Allogeneic-CAR-T-Cell-Therapy-on-Par-with-Autolog.html [4] Benitec Biopharma Provides Positive Interim Clinical Study Results for BB-301 Phase 1b/2a Clinical Trial and Receives FDA Fast Track Designation for BB-301. 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Retrieved November 7, 2025, from https://ankyratx.com/press-releases/ankyra-announces-publication-of-phase-1-clinical-data-and-will-present-at-the-society-for-immunotherapy-of-cancer-sitc-annual-meeting/ [11] 한미약품, 'UCN2 유사체' 비만 "美1상 IND 승인". Retrieved November 7, 2025, from https://www.biospectator.com/news/view/26883 [12] TREOS Bio Announces Publication of Phase 1b Clinical Trial Results of PolyPEPI1018 Plus TAS-102 in Refractory MSS mCRC in JCO Oncology Advances. Retrieved November 7, 2025, from https://www.globenewswire.com/news-release/2025/11/06/3182356/0/en/TREOS-Bio-Announces-Publication-of-Phase-1b-Clinical-Trial-Results-of-PolyPEPI1018-Plus-TAS-102-in-Refractory-MSS-mCRC-in-JCO-Oncology-Advances.html [13] 4DMT Announces Positive Long-Term Data from Phase 1/2 PRISM Clinical Trial in Wet AMD Supporting 4D-150’s Potential as a Backbone Therapy with Consistent and Durable Benefit over Multiple Years. Retrieved November 7, 2025, from https://www.globenewswire.com/news-release/2025/11/06/3182290/0/en/4DMT-Announces-Positive-Long-Term-Data-from-Phase-1-2-PRISM-Clinical-Trial-in-Wet-AMD-Supporting-4D-150-s-Potential-as-a-Backbone-Therapy-with-Consistent-and-Durable-Benefit-over-M.html [14] Assembly Biosciences Presents Positive Phase 1b Data for Next-Generation Capsid Assembly Modulator ABI-4334 at AASLD The Liver Meeting. Retrieved November 7, 2025, from https://www.globenewswire.com/news-release/2025/11/07/3183614/16259/en/Assembly-Biosciences-Presents-Positive-Phase-1b-Data-for-Next-Generation-Capsid-Assembly-Modulator-ABI-4334-at-AASLD-The-Liver-Meeting.html [15] Immunocore presents Phase 1 data for hepatitis B candidate at AASLD’s The Liver Meeting. Retrieved November 7, 2025, from https://www.globenewswire.com/news-release/2025/11/07/3183593/0/en/Immunocore-presents-Phase-1-data-for-hepatitis-B-candidate-at-AASLD-s-The-Liver-Meeting.html [16] Nouscom Presents New Positive Phase 1/2b data of NOUS-209 at SITC 2025, Supporting Plans to Initiate Registration-Enabling Study for Cancer Interception in Lynch Syndrome Carriers. Retrieved November 7, 2025, from https://www.globenewswire.com/news-release/2025/11/07/3183707/0/en/Nouscom-Presents-New-Positive-Phase-1-2b-data-of-NOUS-209-at-SITC-2025-Supporting-Plans-to-Initiate-Registration-Enabling-Study-for-Cancer-Interception-in-Lynch-Syndrome-Carriers.html 免责声明：本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

临床申请免疫疗法临床1期临床2期疫苗

100 项与 VVZ-2471 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
疼痛	临床2期	韩国	Vivozon, Inc.	-
焦虑症	临床1期	-	Vivozon, Inc.	-
慢性疼痛	临床1期	-	Vivozon, Inc.	-
抑郁症	临床1期	-	Vivozon, Inc.	-
未指明的药物依赖	临床1期	-	Vivozon, Inc.	-
吸烟	临床申请批准	美国	Vivozon, Inc.	2025-11-10