Olanzapine

Roluperidone has been de-risked by consistent positive results in two prior pivotal trials and remains the only late-stage drug candidate for this high-need population Efficacy topline data expected 2H 2027 BURLINGTON, Mass., March 31, 2026 (GLOBE NEWSWIRE) -- Minerva Neurosciences, Inc. (Nasdaq: NERV), a clinical-stage biopharmaceutical company focused on the development of therapies to treat central nervous system disorders, today announced that the first patient has been screened in its global, confirmatory Phase 3 clinical trial evaluating roluperidone as monotherapy for the treatment of negative symptoms of schizophrenia. Negative symptoms, including avolition (severe lack of motivation), anhedonia (inability to experience pleasure) and social withdrawal can lead to profound personal and functional impairment and represent one of the greatest unmet needs in schizophrenia. There are currently no FDA-approved treatments with this indication. The Phase 3 trial will enroll approximately 380 patients across roughly 40 clinical sites worldwide, including the United States (US) and multiple European countries. This confirmatory Phase 3 trial follows productive discussions with the FDA on the overall design and efficacy assessments. It builds directly on Minerva’s clinical success in the prior pivotal Phase 2b and Phase 3 trials (C03 and C07), both of which demonstrated consistent improvements in negative symptoms with the 64 mg dose of roluperidone. “Initiation of this confirmatory Phase 3 trial is an important milestone for Minerva and for patients living with persistent and impairing negative symptoms of schizophrenia,” said Dr. Remy Luthringer, Executive Chairman and CEO of Minerva Neurosciences. “With no approved treatments for this indication in the US, roluperidone remains the only late-stage candidate in development for this population. The study builds directly on our prior experience showing consistent results across the two earlier trials and our execution strategy gives us confidence in our timelines.” “Patients with schizophrenia often live with persistent negative symptoms such as avolition and anhedonia - challenges that remain even when positive symptoms are controlled with current therapies,” said Dr. Elan Cohen, Principal Investigator at CenExel Marlton, New Jersey and Lead Coordinating Investigator for the trial. “By evaluating roluperidone in a population with stable positive symptoms, this trial isolates its potential to improve these core drivers of disability while laying the groundwork for a broader treatment strategy. Strengthening motivation, cognition, and functioning may ultimately support more comprehensive symptom control over time, and the consistency seen in prior studies makes this confirmatory Phase 3 trial especially compelling.” About the Phase 3 MIN-101C19 Trial The global Phase 3 MIN-101C19 trial will enroll approximately 380 adults aged 18–55 with moderate to severe negative symptoms of schizophrenia, confirmed by a Positive and Negative Syndrome Scale (PANSS) negative subscale score greater than 20 and stable positive symptoms for at least six months. The trial utilizes a two-part design. The overall objective of the study is to confirm the effect of roluperidone on primary negative symptoms at 12 weeks compared to placebo and to evaluate longer-term relapse of positive symptoms compared with commonly prescribed antipsychotic medications for an additional 40 weeks. The trial is designed to minimize variability and maximize sensitivity to treatment effect, including standardized assessments, and comprehensive caregiver engagement. Topline data from the 12-week Phase A portion (i.e., primary efficacy endpoint) of the trial are expected in the second half of 2027. The trial’s operational model includes intensive rater training, real-time monitoring of scoring data, and structured caregiver outreach to support safety tracking, functional assessments, and adherence. Phase A is a12-week, randomized, double-blind, placebo-controlled phase during which patients will receive 64 mg of roluperidone or placebo to evaluate the primary endpoint: change from baseline in the Marder Negative Symptoms Factor Score (NSFS), which is a factor-analytic composite created from selected PANSS items. The sole key secondary endpoint is the change from baseline in the Personal and Social Performance (PSP) total score. Other secondary endpoints include a broad set of additional clinical measures, including PANSS subscales, Clinical Global Impression – Severity (CGI-S), Clinical Global Impression – Improvement (CGI-I), the Calgary Depression Scale, avolition-specific analyses, and patient and caregiver treatment-satisfaction ratings. Phase B extends the trial for 40 weeks using a double-dummy, active-controlled, randomized design comparing continued roluperidone with three commonly prescribed antipsychotic medications (risperidone, aripiprazole, or olanzapine). This phase is designed to compare relapse rates between treatment groups. Relapses of positive symptoms will be evaluated using a rigorous, multi-component definition incorporating psychometric endpoints based on PANSS score worsening, and clinically meaningful events such as hospitalization or dangerous behavior. About Minerva Neurosciences Minerva Neurosciences, Inc. is a clinical-stage biopharmaceutical company focused on developing product candidates to treat CNS diseases. Minerva’s goal is to transform the lives of patients with improved therapeutic options, including roluperidone for negative symptoms of schizophrenia. For more information, please visit the Company’s website . Forward-Looking Safe Harbor Statement This press release contains forward-looking statements which are subject to the safe harbor provisions of the Private Securities Litigation Reform Act of 1995, as amended. Forward-looking statements are statements that are not historical facts, reflect management’s expectations as of the date of this press release, and involve certain risks and uncertainties. Forward-looking statements include, but are not limited to, statements herein with respect to implied or express statements regarding the anticipated clinical benefits and market opportunities associated with roluperidone, including its potential to address clinical and regulatory challenges; and the expected timeline, design, and conduct of Minerva’s Phase 3 trial of roluperidone. These forward-looking statements are based on our current expectations and may differ materially from actual results due to a variety of factors including, without limitation, trials and studies may be delayed and may not have satisfactory outcomes, and earlier trials and studies may not be predictive of later trials and studies; the design and rate of enrollment for clinical trials, including the current design of the confirmatory Phase 3 trial evaluating roluperidone may not enable successful completion of the trial(s); the commercial opportunity for roluperidone in negative symptoms of Schizophrenia may be smaller than anticipated; Minerva may be unable to obtain and maintain regulatory approvals; Minerva may experience uncertainties inherent in the initiation and completion of clinical trials and clinical development; Minerva’s future financial performance and position may not improve, resulting in difficulties in implementing Minerva’s business strategy, and plans and objectives for future operations; the expected sufficiency of Minerva’s existing cash resources and runway may not be accurate resulting in the need for additional financing sooner than anticipated or unexpected liquidity constraints; the internal and external costs required for Minerva’s ongoing and planned activities, and the resulting impact on expense and use of cash, may be higher than expected, which may cause the company to use cash more quickly than expected or to change or curtail some of Minerva’s plans or both; the need to align with collaborators or partners may hamper or delay development and regulatory efforts or increase costs; uncertainties of patent protection and litigation; general economic conditions; and other factors that are described under the caption “Risk Factors” in Minerva’s filings with the Securities and Exchange Commission, including its Annual Report on Form 10-K for the year ended December 31, 2025, filed with the Securities and Exchange Commission. Copies of reports filed with the SEC are posted on Minerva’s website at The forward-looking statements in this press release are based on information available to the Company as of the date hereof, and the Company disclaims any obligation to update any forward-looking statements, except as required by law. Contacts: Investor inquiries: Frederick Ahlholm Chief Financial Officer Minerva Neurosciences, Inc. info@minervaneurosciences.com Corey Davis, Ph.D. LifeSci Advisors, LLC 212-915-2577 cdavis@lifesciadvisors.com

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。