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更新于：2026-04-02

Iloperidone

伊潘立酮

更新于：2026-04-02

概要

基本信息

药物类型

小分子化药

别名

1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone、4'-(3-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino)propoxy)-3'-methoxyacetophenone、Fanaptum

+ [10]

靶点

5-HT2A receptor x D2 receptor

作用方式

拮抗剂

作用机制

5-HT2A receptor拮抗剂(5-羟色胺2A受体拮抗剂)、D2 receptor拮抗剂(多巴胺D2受体拮抗剂)

治疗领域

其他疾病神经系统疾病

在研适应症

躁郁症1型躁狂精神分裂症

非在研适应症

急性精神分裂症情绪易怒原发性肥大性骨关节病+ [3]

原研机构

Novartis Pharma AG

在研机构

Probiomed SA de CV

Vanda Pharmaceuticals, Inc.

Novartis AG

非在研机构

Novartis Pharmaceuticals Corp.

权益机构

Novartis AG

Vanda Pharmaceuticals, Inc.Aventis SA

+ [1]

最高研发阶段批准上市

首次获批日期

美国 (2009-05-06),

精神分裂症

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C24H27FN2O4

InChIKeyXMXHEBAFVSFQEX-UHFFFAOYSA-N

CAS号133454-47-4

关联

项与伊潘立酮相关的临床试验

NCT07090161

/ Recruiting临床2期

A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Iloperidone for the Treatment of Participants With Uncontrolled Hypertension

A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Iloperidone for the Treatment of Participants with Uncontrolled Hypertension

开始日期2025-09-15

申办/合作机构

Vanda Pharmaceuticals, Inc.

NCT06961968

/ Recruiting临床3期

A Multicenter, Double-Blind, Randomized Withdrawal Study in Patients With Schizophrenia Receiving Either Iloperidone Long-Acting Injection (LAI) or Placebo Injection

The purpose of this research is to evaluate the efficacy of dosing iloperidone long-acting injection (LAI) compared to placebo in preventing the exacerbation of symptoms in patients with schizophrenia.

开始日期2025-05-14

申办/合作机构

Vanda Pharmaceuticals, Inc.

NCT06494397

/ Completed临床1期

Crossover Bioequivalence Study of 12 mg VHX-896 and Iloperidone Tablets Under Steady-State Conditions

Study to compare the pharmacokinetics and pharmacodynamics of VHX-896 and iloperidone and evaluate the safety and tolerability of VHX-896 and iloperidone in patients with schizophrenia or bipolar I disorder under steady state conditions.

开始日期2024-07-11

申办/合作机构

Vanda Pharmaceuticals, Inc.

100 项与伊潘立酮相关的临床结果

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100 项与伊潘立酮相关的转化医学

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100 项与伊潘立酮相关的专利（医药）

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324

项与伊潘立酮相关的文献（医药）

2025-11-02·Expert Opinion On Drug Safety

Drug-induced erectile dysfunction: a real-world pharmacovigilance study using the FDA adverse event reporting system database

Article

作者: Zhang, Rui ; Li, Dongxuan ; Du, Qian ; Zhu, Jun ; Wang, Yalan ; Dai, Liyang ; Liu, Songqing ; Wu, Fan ; Zhang, Tongyan

BACKGROUND:

The comprehensive quantitative and comparative risk data of drug-induced erectile dysfunction (ED) are still lacking, and this study aims to supplement this information.

RESEARCH DESIGN AND METHODS:

We reviewed all the ED reports in the FDA Adverse Event Reporting System (FAERS) database from 2004 to 2023 and summarized a potential ED culprit-drug list and its corresponding reporting frequency. The reporting odds ratio (ROR) method was used to conduct disproportionality analysis.

RESULTS:

A total of 20,098 ED reports were retrieved from the FAERS database, which recorded 734 different ED culprit-drugs, involving 74 drug classes. Finasteride was the drug with the highest reporting frequency, and urologicals was the drug class with the highest reporting frequency. In disproportionality analysis, 209 drugs with positive signals showed a close relationship with ED occurrence, among which finasteride was the drug with the highest signal strength. Among 209 drugs with positive signals, 27 were compound preparations, and the risk level of compound preparations was usually higher than their single active ingredient.

CONCLUSIONS:

Our study integrated quantitative and comparative ED risk data of 734 drugs by using the FAERS database, which can provide reference information for regulators, medical personnel, and others involved in drug management and use.

2025-11-01·JOURNAL OF CLINICAL PHARMACOLOGY

Evaluation of Characteristics and Ethnic Sensitivity for FDA‐Approved Drugs with Racial and Ethnic Differences in Pharmacokinetics, Safety, and Efficacy

Article

作者: Muto, Chieko ; Kawai, Norisuke ; Fukuhara, Kei ; Tanetsugu, Yusuke ; Wada, Shinsuke

Abstract:

Racial and ethnic differences in drug disposition and response may have a significant impact on its risk‐benefit balance. Therefore, it is important to examine whether an investigational drug has characteristics that make the pharmacokinetics (PK), safety, and efficacy likely to be affected by intrinsic and extrinsic ethnic factors based on ethnic sensitivity assessment. This assessment is recommended by the latest Japanese guideline (issued in December 2023) for Japanese phase 1 studies before participation in multi‐regional clinical trials (MRCTs). To comprehensively understand characteristics and ethnic sensitivity of drugs that seem to have racial/ethnic differences in its disposition and response, we investigated 620 new molecular entities (NMEs) approved by the United States Food and Drug Administration (FDA) between 2008 and 2023. Of those, only 6.5% (40 NMEs) reported racial/ethnic differences in the PK (5.0%), safety (1.6%), and/or efficacy (0.6%) in the FDA drug labeling, with only one NME (0.16%) having a clinically significant PK difference which requires a reduced starting dose in East Asian patients. Additionally, 4.4% of 620 NMEs reported differences in the pharmacogenetics for drug‐metabolizing enzymes. The comprehensive evaluation of characteristics and ethnic sensitivity of 40 NMEs with racial/ethnic differences in the PK, safety, and/or efficacy indicated two key findings. First, participation in MRCTs from various regions as early as possible is much more important than conduct of an additional phase 1 study in a specific region/country. Second, more attention and deeper evaluation of Asian PK would be needed for drugs with low bioavailability in the overall drug development.

2025-10-01·CNS DRUGS

Antipsychotic-Related Prolactin Changes: A Systematic Review and Dose–Response Meta-analysis

Review

作者: Wu, Hui ; Correll, Christoph U ; Leucht, Stefan ; Qin, Mengchang ; Lin, Xiao ; Siafis, Spyridon ; Schneider-Thoma, Johannes ; Tian, Jing

BACKGROUND:

Prolactin increase is a common and potentially problematic adverse event of antipsychotics. We aimed to discover the relationship between antipsychotic doses and changes in prolactin levels.

OBJECTIVE:

To examine the relationship between antipsychotic doses and changes in prolactin levels in adults with acutely exacerbated schizophrenia.

METHODS:

We searched the Cochrane Schizophrenia Group register (last search 26 July 2024) and previous reviews for fixed-dose, randomized controlled trials (RCTs) that investigated monotherapy of 21 antipsychotics in adults with acutely exacerbated schizophrenia. The primary outcome was mean prolactin change from baseline to study endpoint adopting mean differences (MD) in ng/mL as the effect size measure. The dose-response curves were estimated by conducting random-effects dose-response meta-analyses using the restricted cubic spline method.

RESULTS:

Among 165 eligible studies, 68 studies with 238 dose arms (23,128 participants, 35% female) reported on prolactin and were meta-analyzed. Of these, 94% lasted ≤ 3 months, and 90% of the studies used oral formulations. Participants in one study experienced their first episode, while all other studies also included multiepisode participants. The dose-response curves indicated that with aripiprazole, higher doses were significantly associated with lower prolactin levels than lower doses. Brexpiprazole, cariprazine, lumateperone, and quetiapine carried negligible risks for prolactin increase across examined doses. During treatment with most other antipsychotics, i.e., asenapine, haloperidol, iloperidone, lurasidone, olanzapine, paliperidone, risperidone, and ziprasidone, prolactin levels rose with increasing doses and then continued to increase or plateaued. The shape of the dose-response curves was similar in males and females, with generally larger amplitudes of the curves in females.

CONCLUSIONS:

The prolactin-increasing property varies among antipsychotics, is dose-related, and is greater in females. These findings in adults with acutely exacerbated schizophrenia can help clinicians titrate and adapt antipsychotic doses and consider patients' sex in treatment decisions. The protocol was registered in the International Prospective Register of Systematic Reviews (PROSPERO); registration no. CRD42020181467.

项与伊潘立酮相关的新闻（医药）

2026-03-31

·乐研品牌

2026年一季度FDA新药审批亮相：6款小分子及多肽创新药破局肿瘤、罕见病等六大领域

2026 年第一季度，FDA 共批准 6 款小分子及多肽类新药。这些药物凭借全球首创、靶点稀缺、满足临床刚需三大核心优势，在肿瘤、罕见病、免疫性皮肤病等领域实现重要突破。多款产品精准直击临床未满足需求，对应市场规模从数亿至数百亿美元不等；加之全球同靶点药物布局差异明显，部分赛道已形成独家垄断格局。核心亮点、市场需求与全球同靶点布局企业总览 1.Relacorilant：全球首款获批的口服型、选择性糖皮质激素受体拮抗剂（SGRA），可有效破解肿瘤化疗耐药难题。在全球超百亿美元规模的卵巢癌靶向治疗市场中，铂类耐药卵巢癌领域仍存在显著临床未满足需求。目前，全球范围内 SGRA 靶点仅有本品获批，Corcept Therapeutics 为该靶点独家布局企业，其适应症正逐步拓展至子宫内膜癌、胰腺癌等多个癌种。 2.Icotrokinra：全球首款靶向 IL-23 受体的口服多肽药物，有效解决了传统生物制剂需注射给药的不便问题。全球银屑病药物市场规模已超 200 亿美元，但针对中重度斑块状银屑病及难治部位病变，患者仍缺乏便捷的治疗方案。IL-23 通路虽已有乌司奴单抗、古塞奇尤单抗等多款注射型生物药获批，但目前该通路口服制剂仅有强生一款实现上市。 3.Linerixibat：美国首款获批用于原发性胆汁性胆管炎（PBC）胆汁淤积性瘙痒的治疗药物，通过肠道局部发挥作用大幅降低了系统性副作用。随着全球 PBC 患病人数持续增加，胆汁淤积性瘙痒已成为患者最主要的临床痛苦来源，且此前长期缺乏针对性治疗药物。Linerixibat 作为首个获批该适应症的 IBAT 抑制剂，成功填补了这一临床空白，目前同类在研药物数量有限。 4.Milsaperidone：多巴胺D2/5-HT2双受体拮抗的新型抗精神病药，可同时覆盖精神分裂症与双相I型障碍躁狂发作。全球抗精神分裂药物市场2024年已接近200亿美元，现有药物存在副作用大、患者依从性低的问题。D2/5-HT2双靶点玩家以奥氮平、利培酮等二代药物为主，Milsaperidone为该靶点新型迭代产品，差异化优势显著。 5.Difamilast：非类固醇类PDE4抑制剂，为2岁及以上特应性皮炎患者提供了安全有效的激素替代治疗方案。目前全球特应性皮炎药物市场规模已超150亿美元，其中儿童及轻中度患者对无激素外用药物的需求尤为迫切。在PDE4抑制剂靶点领域，虽已有克立硼罗等药物获批，但大冢制药凭借儿童适应症的独家获批，实现了该赛道的差异化布局，凸显独特竞争优势。 6.Copper histidinate：Menkes病自1962年发现以来首款获批药物，填补罕见病治疗百年空白。Menkes病为罕见X连锁隐性遗传病，全球发病率约1/10万，此前暂无任何获批治疗药物，Sentynl Therapeutics为该疾病及对应铜离子补充靶点全球独家布局企业。 Section.01 — Leyan.com — （CAS号：1496510-51-0；商品名：Lifyorli） Relacorilant 药物背景由 Corcept Therapeutics 开发，于 2026 年 03 月 25 日获得 FDA 批准与白蛋白结合型紫杉醇联用，用于治疗既往接受过1～3种系统治疗(须含贝伐单抗)、对铂类化疗药耐药的卵巢上皮癌、输卵管癌或原发性腹膜癌患者。Relacorilant是首个获得FDA批准的选择性糖皮质激素受体拮抗剂（SGRA）。目前Corcept Therapeutics正在推进该药物在卵巢癌及多种其他严重疾病中的开发（NCT06906341，NCT07259317），包括内源性高皮质醇症以及子宫内膜癌、宫颈癌、胰腺癌和前列腺癌。作用机制皮质醇在肿瘤发生发展中起到多方面作用：它可以通过抑制细胞凋亡，使肿瘤对化疗产生抵抗，从而降低治疗效果；在某些癌症中，还可能通过激活致癌基因促进肿瘤生长。此外，皮质醇会抑制人体免疫系统，使机体对疾病的抵抗能力下降。Relacorilant是一种口服选择性糖皮质激素受体拮抗剂，可通过与糖皮质激素受体结合而不与机体其他激素受体结合，从而调节皮质醇活性。相关专利 WO2022140600 A1，WO2022134033 A1，WO2013177559 A2 相关文献 J. Med. Chem.2017, 60, 3405-3421. 乐研可提供Relacorilant的关键分子砌块 1028398 1023825 1044280 1122434 Section.02 — Leyan.com — （CAS号：2763602-16-8；商品名：Icotyde） Icotrokinra 药物背景由强生公司（Janssen）开发，于 2026 年 03 月 17 日获得 FDA 批准，用于治疗12岁及以上、体重至少 40 公斤且适合系统治疗或光疗的青少年及成人中重度斑块状银屑病患者。Icotrokinra是全球首款且是唯一一款靶向 IL-23 受体的口服类多肽药物，它解决了传统生物制剂注射不便的痛点，尤其为头皮、生殖器等难治部位病变提供了强效、便捷的解决方案。目前该药物正在推进银屑病关节炎（NCT06878404，NCT06807424）、溃疡性结肠炎（NCT07196748）、克罗恩病（NCT07196722）等适应症的开发。作用机制 IL-23是介导银屑病的核心通路，可促进Th17细胞增殖，进而促进一系列炎症因子的分泌。Icotrokinra能够与IL-23受体高亲和力结合，强效抑制IL-23及其下游信号转导。其独特的环肽结构设计使之具备良好的胃肠道稳定性和渗透性，从而可有效提升口服吸收和生物利用度。相关专利 WO2022140600 A1，WO2022134033 A1，WO2013177559 A2 乐研可提供Icotrokinra的关键分子砌块 1023843 1017257 1025142 1022781 1441230 1171765 Section.03 — Leyan.com — （CAS号：1345982-69-5；商品名：Lynavoy） Linerixibat 药物背景由葛兰素史克公司（GlaxoSmithKline）开发，于 2026 年 03 月 17 日获得 FDA 批准，用于治疗原发性胆汁性胆管炎（PBC）成人患者的胆汁淤积性瘙痒。Linerixibat是首个在美国获批治疗该适应症的药物，代表着 PBC 瘙痒治疗领域的一个重要里程碑。作用机制 Linerixibat作为一种高选择性、强效且肠道限制性的回肠胆汁酸转运蛋白（IBAT）抑制剂，通过特异性阻断回肠末端对胆汁酸的主动重吸收，打断肠肝循环并促进胆汁酸随粪便排泄，显著降低血清胆汁酸水平及其下游瘙痒介质（如溶血磷脂酸LPA和自分泌运动因子ATX）的循环积累，进而减少这些物质对皮肤感觉神经纤维上TGR5、MRGPRX4及TRPA1/TRPV1等受体的刺激以缓解胆汁淤积性瘙痒。该药物主要在肠道局部发挥作用，可有效避免对肝脏FXR信号通路和全身脂质代谢的干扰，降低了系统性不良反应的风险。相关专利 WO2022136335 A1，WO2016020785 A1，WO2011137135 A1 相关文献 J. Med. Chem.2013, 56, 5094-5114. 乐研可提供Linerixibat的关键分子砌块 1069404 1611759 1139016 1948603 Section.04 — Leyan.com — （CAS号：501373-88-2；商品名：Bysanti） Milsaperidone 药物背景由Vanda Pharmaceuticals 开发，于 2026 年 02 月 20 日获得 FDA 批准，用于治疗成人精神分裂症以及成人双相 I 型障碍相关躁狂发作或混合发作的急性期治疗。目前Vanda Pharmaceuticals正在推进该药物作为难治性重度抑郁障碍的辅助治疗的III期临床研究（NCT06830044）。作用机制：Milsaperidone治疗上述适应症的机制尚不明确，可能是通过多巴胺 D2 受体拮抗与5-羟色胺 2（5-HT₂）受体拮抗的协同作用介导。Milsaperidone和iloperidone（一种已上市抗精神病药物）在体内可迅速相互转化，其体外受体结合特性与iloperidone相似。相关专利 WO2022140600 A1，WO2022134033 A1，WO2013177559 A2 乐研可提供Milsaperidone的关键分子砌块 1601111 1069245 1054380 1225758 Section.05 — Leyan.com — （CAS号：937782-05-3；商品名：Adquey） Difamilast 药物背景由大冢制药（Otsuka）开发，于 2026 年 02 月 12 日获得 FDA 批准，用于2岁及以上成人和儿童轻中度特应性皮炎（AD）的局部治疗。该批准为美国数百万AD患者提供了另一种选择，为可能导致长期副作用的类固醇药物提供了更安全的替代方案。该药物软膏曾于2021年9月在日本获批用于2岁及以上儿童和成人轻中度AD的局部治疗。作用机制特应性皮炎是一种慢性炎症性皮肤病，以剧烈瘙痒和反复发作的皮损为特征，传统外用糖皮质激素虽有效，但长期使用可能带来皮肤萎缩、色素改变等副作用。Difamilast是一种新型非类固醇类磷酸二酯酶4（PDE4）抑制剂，该酶在皮肤炎症和瘙痒中起着重要作用。通过阻断PDE4，它可以改变细胞信号传导并降低皮肤中的某些炎症信号，为糖皮质激素类药物提供了更安全的替代方案。其缓解湿疹的确切机制尚不完全清楚。相关专利 JP2021059538 A，WO2019194211 A1，WO2017115780 A1，US9181205 B2，WO2014034958 A1，JP2008308496 A，WO2007058338 A2 乐研可提供Difamilast的关键分子砌块 1020165 1020963 1022175 Section.06 — Leyan.com — （CAS号：13870-80-9；商品名：Zycubo） Copper histidinate 药物背景由Sentynl Therapeutics公司开发，于 2026 年 01 月 12 日获得 FDA 批准，是一种通过皮下注射给药的铜-组氨酸复合物，用于治疗儿童Menkes病。Copper histidinate是该疾病自1962年首次被描述以来的首个且是唯一一个获得FDA批准的药物。这一突破性进展不仅代表了罕见病药物研发的重大胜利，更凝聚了几代医学研究者六十余年的不懈探索。作用机制 Menkes 病是一种由 ATP7A 基因突变所致的 X 连锁隐性遗传病。ATP7A 蛋白功能缺陷会导致肠道铜吸收障碍，铜离子在肠道上皮细胞内滞留而无法进入血液循环，同时难以跨越血脑屏障进入中枢神经系统，最终造成全身多组织铜缺乏及铜依赖酶功能障碍。Copper histidinate 作为铜替代治疗药物，可通过皮下注射将铜以组氨酸螯合形式直接递送入血，绕过 ATP7A 介导的肠道吸收与血脑屏障转运缺陷。该复合物可借助氨基酸转运体进入全身细胞及脑组织，在胞内释放具有生物活性的铜离子，恢复细胞色素 C 氧化酶、赖氨酰氧化酶、超氧化物歧化酶等关键铜依赖酶的功能，进而改善神经元能量代谢、结缔组织交联与机体抗氧化防御能力。总结整体而言，本季度获批的小分子新药首创性与精准化兼备：肿瘤和免疫靶点持续突破，罕见病小分子填补空白，口服多肽优势凸显，彰显了小分子新药的研发活力。关于乐研乐研品牌隶属于上海皓鸿生物医药科技有限公司，是上市企业皓元医药（股票代码：688131）子公司。专注服务于医药研发领域，经过多年快速发展，已成为集研发、定制合成和销售于一体的高端试剂品牌。乐研拥有享誉业内的自主研发技术能力，秉承“研发实力打造高品质”的理念进行产品的开发，始终致力于为国内外化学和医药研发领域用户提供最优质的产品和最专业的服务，乐研开发和打造的产品系列主要包括： 90000+ 分子砌块、合成试剂、医药中间体和相关的仪器耗材。能满足用户从mg级到kg级、从标准化到定制化的实验室综合需求。乐研的所有产品仅用作科学研究，我们不为任何个人用途提供产品和服务。

2026-03-18

·医药观澜

数十款新药迈入临床开发！精神分裂症患者正在迎来治疗新希望

编者按：精神分裂症是一种严重的慢性精神疾病，影响全球上千万人。近年来，随着科学家对疾病遗传学和神经生物学机制认识的不断深入，该领域迎来了新一轮新药研发热潮。比如，当前全球范围内有数十款针对精神分裂症的新药管线处于积极的临床研发阶段，多靶点、多机制的药物研发正在不断拓展患者的潜在治疗选择。为助力全球合作伙伴开发创新精神疾病疗法，药明康德作为全球医药创新的赋能者，已构建完善的中枢神经系统（CNS）药物研发能力体系，覆盖从早期筛选到IND申报的完整流程。凭借深厚的技术积累与丰富经验，药明康德正加速推动全球合作伙伴的CNS药物研发进程，携手为患者带来改变生命的创新疗法。精神分裂症是一种慢性且常导致残疾的精神疾病，会影响患者的思考、感受和行为方式。精神分裂症的核心症状包括阳性症状（如幻觉和妄想）、阴性症状（如动机和愉悦感缺失以及社交退缩）和认知症状（如记忆、注意力和决策方面的缺陷）。根据世界卫生组织统计，全球约2400万人受到其影响。尽管已有创新疗法问世，但依然难以满足临床需求，许多患者仍面临症状改善不足及难以耐受的副作用等问题。近年来，随着科学家对疾病遗传学和神经生物学机制认识的不断深入，精神分裂症领域迎来了新一轮新药研发热潮。根据《自然》子刊Nature Reviews Drug Discovery近日发表的综述介绍，过去以多巴胺D2受体为核心的治疗模式，正逐步被更加多元的神经递质与神经网络调节策略所补充。从谷氨酸系统、胆碱能系统，到神经可塑性、炎症与代谢调节，多靶点、多机制的药物研发正在不断拓展精神分裂症的治疗选择。公开资料显示，除了已经获批上市的药物，全球范围内有数十款针对精神分裂症的管线处于积极的临床研发阶段。这些新药以小分子药物为主，靶点涉及5-HT7、CHRM4、CHRM1、GlyT1、HTR2C、TAAR1、KAT2、PDE4等等。图片来源：123RF 精神分裂症新药研发迎新进展近一年以来，精神分裂症领域的新药研发取得诸多新进展，包括多款在研新药取得新的监管、临床进展，还有一些深耕该领域的新锐公司获得新一轮融资，等等。比如，今年2月，Vanda Pharmaceuticals宣布，美国FDA已批准Bysanti（milsaperidone）片剂上市，用于急性治疗I型双相情感障碍（BP-I）相关的躁狂发作或混合发作，以及用于治疗成人精神分裂症。Milsaperidone是一种新化学实体，为iloperidone（一种已上市抗精神病药物）的前药，经口服给药后可迅速转化为iloperidone。Milsaperidone属于非典型抗精神病药物类别，同时作用于某些5-羟色胺和多巴胺受体，这些受体被认为与其治疗效应密切相关。再如，2025年12月，再鼎医药宣布呫诺美林曲司氯铵胶囊（xanomeline和trospium chloride，即KarXT）在中国获批治疗成人精神分裂症。不同于传统靶向多巴胺的抗精神病药物的机制，呫诺美林曲司氯铵胶囊通过选择性作用于大脑中的毒蕈碱型乙酰胆碱能M1和M4受体影响核心疾病通路。该产品此前于2024年获美国FDA批准，被认为代表了该领域数十年来新机制的精神分裂症药物。 2025年3月，Otsuka Pharmaceutical和灵北（Lundbeck）宣布，欧盟委员会（EC）已批准Rxulti（brexpiprazole）用于治疗13岁及以上青少年的精神分裂症。Rxulti是一种非典型口服抗精神病药，每日服用一次。它通过对血清素及多巴胺系统活性的调节产生作用。在2018年，Rxulti在欧盟获批用于治疗成人精神分裂症。还有一些新药获批进入临床研究阶段：比如，2025年11月，绿叶制药宣布其新一代5-羟色胺2A型受体（5-HT2AR）反向激动剂和5-羟色胺2C型受体（5-HT2CR）拮抗剂LY03017已获得FDA许可开展临床试验。LY03017拟用于治疗精神分裂症阴性症状等疾病，其通过5-HT2AR受体反向激动作用及5-HT2C受体拮抗作用，抑制腹侧纹状体多巴胺释放，促进前额叶皮层多巴胺释放，有潜力改善精神分裂症阴性症状。再如，2025年3月，恩华药业1类新药NH140068片获批临床，拟开发治疗精神分裂症。这是一款适于口服的多种神经递质受体激动剂。临床前试验结果表明，它可以激动多巴胺、5-羟色胺和痕量胺的相关受体，具有改善精神分裂症阳性和阴性症状且副作用小的潜力。除了上述新药，还有多款精神分裂症新药已经进入3期临床开发阶段，有望在不久的将来惠及患者。比如，《自然》子刊Nature Reviews Drug Discovery近日发表的综述介绍了几款处于3期临床阶段的新兴机制精神分裂症疗法，包括勃林格殷格翰（Boehringer Ingelheim）开发的iclepertin，其通过抑制甘氨酸转运体1（GlyT1）以提高突触间隙中甘氨酸浓度，从而增强NMDAR信号；再如大冢制药（Otsuka）开发的TAAR1激动剂ulotaront，TAAR1能够调节多巴胺和5-羟色胺神经传递，并通过与多巴胺系统的相互作用产生抗精神病效应，而无需直接阻断D2受体。新锐融资方面也迎来新进展。比如，2026年1月，纽欧申医药宣布正式完成数千万美元的A+轮融资，融资资金用于推进公司多条中枢神经系统（CNS）创新药物管线的研发，包括拟开发治疗精神分裂症的NS-136。NS-136为新型选择性M4毒蕈碱型乙酰胆碱受体正向变构调节剂，靶向M4受体的正向变构调节是一种新作用机制，不仅能有效治疗精神分裂症的阳性症状，且避免了传统抗精神病药物可能引发的运动障碍等副作用，还显示出改善阴性症状和认知功能障碍的潜力。2025年11月，NS-136完成2期临床试验的首例患者给药，针对精神分裂症。 2025年12月，Syremis Therapeutics宣布正式成立，并完成1.65亿美元融资。该公司聚焦精神健康领域的重大未满足需求，其中主打项目ST-905是一款高效的M1/M4毒蕈碱受体激动剂，现处于1期临床开发阶段，拟用于治疗精神分裂症。 2025年9月，LB Pharmaceuticals宣布其在美国首次公开募股（IPO）中成功筹集2.85亿美元，用于推动其核心产品LB-102的临床开发，包括支持该药开展针对精神分裂症的3期临床试验。LB-102是一种每日一次的口服小分子疗法，为一种苯甲酰胺类抗精神病药物。在2期临床研究中，与安慰剂相比，所有剂量的LB-102可显著改善急性精神分裂症成年患者的精神分裂症阳性和阴性症状量表（PANSS）总分。 2025年8月，Leal Therapeutics宣布完成3000万美元A轮融资，以推进用于治疗神经退行性和神经精神疾病的神经代谢疗法。Leal公司的管线机制基于一个核心原则，即纠正大脑中的代谢失衡。该公司的主要项目LTX-001是一种口服脑渗透小分子，通过抑制线粒体酶谷氨酰胺酶来靶向过量的谷氨酸，用于治疗精神分裂症等CNS领域疾病。除了上述进展，全球范围内还有多款精神分裂症创新疗法处于积极的临床开发阶段，并取得新进展。限于篇幅，此处不再一一介绍。很高兴看到这些创新疗法取得积极进展，为患者带来新的治疗希望。一体化CRDMO平台赋能CNS疗法创新总体而言，精神分裂症被认为是一种具有高度生物学异质性的复杂疾病，其症状涉及多条神经环路和分子通路。随着遗传学和神经生物学研究的持续深入，未来精神分裂症治疗有望逐步迈向个体化治疗时代，为患者带来更加有效且安全的治疗方案。在这一持续发展的领域中，药明康德正成为全球创新者推进精神分裂症等CNS疾病药物研发的重要合作伙伴。公司已建立多项CNS专属的药物代谢与药代动力学（DMPK）研究能力。例如，其独特的“漏斗（Funnel）”体外检测模型具有较高预测准确性，能够有效区分可穿透血脑屏障的化合物与因被动扩散能力不足或受外排转运蛋白影响而难以进入中枢的化合物，从而帮助合作伙伴更快速地识别潜力候选分子，加速研发进程。在早期筛选之外，药明康德还为合作伙伴提供多样化的定制化研究策略，包括脑室内或鞘内给药研究、微透析技术、在啮齿类及大型动物模型中进行脑脊液连续采样、精确解剖并分离近20种不同脑区组织，以及利用全身自显影（QWBA）系统展示药物在脑内的分布情况。这些能力不仅适用于小分子药物，也广泛支持蛋白质、寡核苷酸等大分子疗法的开发，从早期筛选一直延伸至IND申报阶段。通过提供先进而可靠的CNS研发平台，药明康德持续赋能全球合作伙伴，加速创新疗法的开发与转化，持续造福全球患者。参考资料： [1]WHO官网. From https://www.who.int/news-room/fact-sheets/detail/schizophrenia [2]同行致远 | 不再只盯多巴胺：精神分裂症新药研发正在打开多条新通路.From https://mp.weixin.qq.com/s?__biz=MzAwMDA5NTIxNQ==&mid=2650124031&idx=1&sn=5b2cfea9b24a957804f649da69104ae4&chksm=83ecff6a3585ae1cb2967b0c5d0cb7a164cefff23ec0fcb92ce22b617fd10542b06f6c95aacc#rd 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「医药观澜」微信公众号回复“转载”，获取转载须知。

2026-03-08

·EINPresswire

Alternative to Meds Center Highlights Long-Term Fanapt Risks and Individualized Antipsychotic Tapering Support

Sedona inpatient program educates on iloperidone side effects, anticholinergic burden, and holistic alternatives for schizophrenia and bipolar symptoms Long-term exposure may affect multiple body systems, especially in vulnerable individuals. ” — Alternative to Meds Center SEDONA, AZ, UNITED STATES, March 8, 2026 / EINPresswire.com / -- Alternative to Meds Center (ATMC) is bringing attention to the potential long-term effects of Fanapt (generic name: iloperidone), an atypical antipsychotic prescribed for schizophrenia and bipolar-related conditions. Although the medication has been available for approximately 15 years, ATMC notes that long-term outcome data remains comparatively limited, and many individuals are not fully informed about potential risks associated with extended use. Fanapt is commonly prescribed as a maintenance medication, often intended for long-duration treatment. While it is designed to influence dopamine and serotonin signaling in the brain, the precise mechanisms and long-term neurological implications are still not fully understood. “For individuals who have been on antipsychotic medications for years, questions about long-term safety are valid and deserve careful evaluation,” said a representative of Alternative to Meds Center. “We believe patients should have access to complete information and individualized options—including supervised tapering where appropriate.” Reported Concerns with Long-Term Fanapt Use Published literature, FDA labeling, and clinical reporting have identified several potential risks associated with long-term use of iloperidone and other antipsychotics. These may include: • Elevated blood sugar and weight gain • Changes in heart rhythm, including potentially serious cardiac effects • Abnormal involuntary movements that may become persistent • Liver injury • Lowered white blood cell count • Increased prolactin levels, potentially affecting reproductive and bone health • Cognitive dulling, impaired judgment, or motor slowing • Swallowing difficulties (dysphagia), increasing risk of choking or pneumonia • Dopamine supersensitivity-related symptoms • Increased overall mortality risk in certain populations ATMC emphasizes that individuals experiencing new or worsening symptoms should consult their prescribing physician promptly. Patients may also report adverse reactions through the FDA’s MedWatch reporting system. Anticholinergic Burden and Nervous System Impact Fanapt has been identified as having anticholinergic effects, meaning it can suppress acetylcholine activity—a neurotransmitter essential for memory, muscle movement, digestion, heart function, and glandular secretion. Prolonged suppression of acetylcholine may contribute to cognitive impairment, urinary retention, digestive complications, and vision changes. In some cases, excessive anticholinergic burden can lead to toxicity requiring medical attention. Symptoms may include confusion, flushed skin, fever, urinary retention, blurred vision, agitation, or delirium. “The cumulative impact of anticholinergic load is often overlooked,” the ATMC representative added. “Long-term exposure may affect multiple body systems, especially in vulnerable individuals.” Comparing Fanapt to Other Antipsychotics Comparative reviews of antipsychotic medications suggest that Fanapt performs similarly to many other drugs in its class when it comes to symptom reduction. While it may present fewer instances of certain side effects such as akathisia or sedation compared to some alternatives, it carries its own distinct risk profile—including prolactin elevation and cardiovascular concerns. ATMC encourages individuals to recognize that medications within the same class can differ significantly in side effect patterns, withdrawal challenges, and long-term health implications. Dose Reduction and Individualized Tapering Emerging research suggests that some individuals experience improvement in emotional blunting, over-sedation, and cognitive clouding after carefully supervised dose reductions of antipsychotic medications. However, tapering must be personalized and medically managed to reduce destabilization risks. Alternative to Meds Center specializes in medically supervised tapering within a structured inpatient setting. The program integrates lab testing, nutritional stabilization, metabolic support, and holistic therapies designed to strengthen the body while medication adjustments are made. “For nearly two decades, we have worked with clients seeking alternatives to lifetime medication use,” the ATMC representative said. “Our focus is always on safety, personalization, and long-term stability.” Exploring Alternatives Beyond Long-Term Medication ATMC’s treatment model emphasizes identifying and addressing root contributors to psychiatric symptoms—including nutritional imbalances, toxin exposure, stress burden, sleep disruption, and metabolic factors—rather than relying solely on long-term pharmacological suppression. The center provides education on antipsychotic withdrawal strategies and alternative mental health approaches, encouraging individuals to consult experienced professionals before making medication changes. Individuals seeking more information about long-term Fanapt risks, antipsychotic withdrawal, or holistic mental health programs are encouraged to contact Alternative to Meds Center directly. Alternative to Meds Center Alternative to Meds Center +1 877-503-0770 email us here Visit us on social media: LinkedIn Instagram Facebook YouTube TikTok X Other Legal Disclaimer: EIN Presswire provides this news content "as is" without warranty of any kind. We do not accept any responsibility or liability for the accuracy, content, images, videos, licenses, completeness, legality, or reliability of the information contained in this article. If you have any complaints or copyright issues related to this article, kindly contact the author above.

上市批准

100 项与伊潘立酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02666	伊潘立酮	N05AX14	DB04946

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
躁郁症1型	美国	Vanda Pharmaceuticals, Inc.	2024-04-02
躁狂	美国	Vanda Pharmaceuticals, Inc.	2024-04-02
精神分裂症	美国	Vanda Pharmaceuticals, Inc.	2009-05-06

未上市

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
急性精神分裂症	临床3期	美国	Vanda Pharmaceuticals, Inc.	2005-11-18
急性精神分裂症	临床3期	印度	Vanda Pharmaceuticals, Inc.	2005-11-18
原发性肥大性骨关节病	临床2期	美国	Vanda Pharmaceuticals, Inc.	2022-06-01
帕金森病	临床2期	美国	Vanda Pharmaceuticals, Inc.	2022-06-01
情绪易怒	临床2期	美国	Novartis Pharmaceuticals Corp.	2013-07-01
入睡和睡眠障碍	临床2期	美国	Novartis Pharmaceuticals Corp.	2013-07-01
创伤后应激障碍	临床2期	美国	Novartis Pharmaceuticals Corp.	2013-07-01

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临床结果

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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


NCT01291511 (FDA_CDER) 人工标引	临床3期	精神分裂症	303	Iloperidone	艱獵夢獵壓齋鹽網膚艱(鬱遞壓構選廠艱壓選選) = patients treated with iloperidone experienced a statistically significant longer than patients who received placebo 夢鹽願夢獵窪繭鬱繭壓 (淵鑰壓鑰醖範壓夢醖齋 )	积极	2026-02-20
FDA_CDER 人工标引	临床3期	精神分裂症	706	Risperidone	遞餘夢繭願齋鬱願夢齋(遞艱壓製獵壓製繭鬱鏇) = treatment groups were superior to the placebo group 簾壓餘顧繭選繭鹽積淵 (簾觸遞夢淵願蓋膚糧糧 ) 更多	积极	2026-02-20
NCT04819776 (FDA_CDER) 人工标引	临床3期	躁郁症1型	392	Placebo	願積顧構積觸簾淵網製(選壓壓壓遞廠襯蓋簾鹽) = 糧壓觸廠窪鏇膚蓋獵淵獵夢衊選夢獵艱願廠獵 (醖襯糧淵醖鹽願壓觸獵, 4.64)	积极	2026-02-20
NCT00254202 (FDA_CDER) 人工标引	临床3期	精神分裂症	604	Iloperidone	獵網襯夢襯繭窪範窪憲(憲齋鹹構齋襯淵構獵鏇) = The 24 mg/day iloperidone treatment group was superior to the placebo treatment group 構衊顧衊蓋築繭廠淵襯 (構顧齋願獵鏇選構艱範 ) 更多	积极	2026-02-20
				Ziprasidone
NCT00254202 (CTgov)	临床3期	急性精神分裂症	593	Iloperidone (Iloperidone)	簾鑰築衊艱襯繭鏇遞獵(齋鹽膚構築選壓獵襯窪) = 選夢鬱築築衊積廠窪製鹽鑰窪願繭觸蓋鹹構願 (鏇衊構壓壓構網鹹鑰鏇, 1.03) 更多	-	2024-12-13
				Ziprasidone (Ziprasidone)	簾鑰築衊艱襯繭鏇遞獵(齋鹽膚構築選壓獵襯窪) = 廠範齋醖淵願憲鹹憲築鹽鑰窪願繭觸蓋鹹構願 (鏇衊構壓壓構網鹹鑰鏇, 1.44) 更多
NCT04819776 (CTgov)	临床3期	躁狂 \| 躁郁症1型	417	Iloperidone (Iloperidone)	製顧製憲憲範顧蓋餘憲(襯壓憲膚鑰醖齋築鑰顧) = 艱簾蓋選鹹壓網獵餘鑰鹹築淵淵鬱範齋夢觸鬱 (築糧範鹽觸網簾夢製窪, 0.64) 更多	-	2024-04-16
				Iloperidone Placebo (Placebo)	製顧製憲憲範顧蓋餘憲(襯壓憲膚鑰醖齋築鑰顧) = 簾衊鹹獵鏇醖糧蓋廠醖鹹築淵淵鬱範齋夢觸鬱 (築糧範鹽觸網簾夢製窪, 0.63) 更多
NCT01291511 (REPRIEVE, CTgov)	临床3期	精神分裂症	635	Iloperidone (Iloperidone)	衊鬱觸構鏇膚憲製獵觸(壓網衊製繭憲糧衊遞範) = 願壓鑰艱製窪糧憲構獵齋鏇膚夢簾構網糧膚鹽 (餘餘製積觸淵蓋壓繭膚, 觸顧鹹築淵鏇襯製選構 ~ 廠選網膚夢範膚醖鏇淵) 更多	-	2023-07-17
				Placebo (Placebo)	衊鬱觸構鏇膚憲製獵觸(壓網衊製繭憲糧衊遞範) = 壓鏇願獵夢憲鑰鏇憲鏇齋鏇膚夢簾構網糧膚鹽 (餘餘製積觸淵蓋壓繭膚, 繭衊鹽顧積醖襯網鑰積 ~ 獵齋鑰窪獵壓鹽齋齋範) 更多
NCT01917318 (CTgov)	临床2期	入睡和睡眠障碍 \| 创伤后应激障碍 \| 情绪易怒	1	Placebo+Iloperidone (Iloperidone / Placebo)	簾鬱選窪鏇鬱醖築範顧(顧餘製顧獵窪積夢積糧) = 鬱鑰糧衊顧願鑰遞餘膚顧鬱遞願積醖顧鹽遞壓 (築構顧夢築憲鹹鹽築衊, 夢醖積築製網餘鏇廠鹽 ~ 構製餘網鹹壓壓膚鏇憲) 更多	-	2020-01-31
				Placebo+Iloperidone (Placebo / Iloperidone)	簾糧壓淵選範鏇餘鏇夢 = 廠繭淵鹹構繭鹽觸願憲築膚顧遞選鏇衊選築顧 (餘鑰遞膚網築鬱廠壓積, 淵願獵襯鬱壓夢築餘餘 ~ 範壓蓋鹹醖衊觸積壓範) 更多
NCT01920802 (CTgov)	临床4期	-	31	olanzapine (Olanzapine)	鑰繭鬱鹹鹽選鹹獵醖淵(顧鏇壓艱鏇構鬱網範積) = 製積夢顧衊鹹網鹽製願糧鏇網窪遞糧繭餘鬱蓋 (鬱鑰壓顧製選鹹選淵壓, 1.0) 更多	-	2017-03-20
				iloperidone (Iloperidone)	鑰繭鬱鹹鹽選鹹獵醖淵(顧鏇壓艱鏇構鬱網範積) = 積繭壓艱襯獵夢窪鑰觸糧鏇網窪遞糧繭餘鬱蓋 (鬱鑰壓顧製選鹹選淵壓, 0.7) 更多
NCT01291511 (REPRIEVE, Pubmed \| CNS Drugs) 人工标引	临床3期	精神分裂症	303	Iloperidone	構繭膚網網積觸選獵繭(憲糧廠構廠顧願鬱襯繭) = 選鏇艱齋獵鹹網範鑰鹽壓簾顧簾鏇壓築窪糧醖 (壓顧膚範製壓壓夢築遞 ) 更多	积极	2016-08-01
				Placebo	構繭膚網網積觸選獵繭(憲糧廠構廠顧願鬱襯繭) = 觸願憲餘願鏇衊餘糧襯壓簾顧簾鏇壓築窪糧醖 (壓顧膚範製壓壓夢築遞 ) 更多