A Multi-part, Multi-center PLATform Study to Assess the Efficacy, Safety, Tolerability and Pharmacokinetics of Anti-malarial Agents Administered as Monotherapy and/or Combination Therapy IN Patients With Uncomplicated Plasmodium Falciparum Malaria

Platform study to evaluate the efficacy and safety of anti-malarial agents in patients with uncomplicated Plasmodium falciparum malaria

开始日期2024-01-23

申办/合作机构

Novartis Pharmaceuticals Corp.

CTRI/2022/03/041310

/ Recruiting临床2期

An adaptive, randomized, active-controlled, open-label, sequentialcohort, multicenter study to evaluate the efficacy, safety,tolerability, and pharmacokinetics of intravenous cipargamin(KAE609) in adult and pediatric participants with severePlasmodium falciparum malaria (KARISMA – KAE609’s Role inSevere Malaria) - NA

开始日期2022-04-01

申办/合作机构

Novartis Healthcare Pvt Ltd.

NCT04675931

/ Completed临床2期

An Adaptive, Randomized, Active-controlled, Open-label, Sequential Cohort, Multicenter Study to Evaluate the Efficacy, Safety, Tolerability and Pharmacokinetics of Intravenous Cipargamin (KAE609) in Adult and Pediatric Participants With Severe Plasmodium Falciparum Malaria (KARISMA - KAE609's Role In Severe Malaria)

The purpose of this study is to identify the safe and effective dose of intravenous cipargamin in participants with moderately severe and severe malaria.
The study also intends to evaluate clinical treatment success using a novel clinical endpoint for drug development in severe malaria.
Severe malaria is a medical emergency and is affecting primarily young children in Africa. Injectable artesunate is the standard of care for the treatment of severe malaria and is highly efficacious. However, the spread of artemisinin-resistance in Plasmodium falciparum in Asian countries poses a threat for future treatment of patients with this life-threatening disease. To mitigate this risk, there is a need of another drug in malaria endemic countries. Cipargamin treatment results in rapid clearance of parasites including artemisinin resistant parasites.

开始日期2022-03-07

申办/合作机构

Novartis Pharmaceuticals Corp.

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100 项与 Cipargamin 相关的临床结果

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100 项与 Cipargamin 相关的转化医学

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100 项与 Cipargamin 相关的专利（医药）

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项与 Cipargamin 相关的文献（医药）

2025-09-08·ACS Infectious Diseases

Identification of α-Azacyclic Acetamide-Based Inhibitors of P. falciparum Na⁺ Pump (PfATP4) with Fast-Killing Asexual Blood-Stage Antimalarial Activity by Phenotypic Screening.

Article

作者: Phillips, Margaret A ; Posner, Bruce A ; Casas, Arturo ; Lee, Seungheon ; Kumar, Ashwani ; Striepen, Josefine ; Ready, Joseph M ; Deni, Ioanna ; Imlay, Leah S ; Charman, Susan A ; Thathy, Vandana ; Fairhurst, Kate J ; Lawong, Aloysus K ; Laleu, Benoît ; Niederstrasser, Hanspeter ; Lehane, Adele M ; Fidock, David A ; Xing, Chao

Malaria treatments are compromised by drug resistance, creating an urgent need to discover new drugs. We used a phenotypic high-throughput screening (HTS) platform to identify new antimalarials, uncovering three related pyrrole-, indole-, and indoline-based series with a shared α-azacyclic acetamide core. These compounds showed fast-killing activity on asexual blood-stage Plasmodium falciparum parasites, were not cytotoxic, and disrupted parasite intracellular pH and Na⁺ regulation similarly to cipargamin (KAE609), a clinically advanced inhibitor of the P. falciparum Na⁺ pump (PfATP4). PfATP4 is localized to the parasite plasma membrane and is essential for maintaining a low cytosolic Na⁺ concentration. Resistance selections on P. falciparum parasites with two α-azacyclic acetamide analogs identified mutations in PfATP4, and cross-resistance was observed across the α-azacyclic acetamides and KAE609, confirming PfATP4 as the target. PfATP4 is a well-established antimalarial target, and identification of additional PfATP4 inhibitors provides alternative avenues to disrupt its function.

2025-06-01·CLINICAL MICROBIOLOGY AND INFECTION

The non-artemisinin antimalarial drugs under development: a review

Review

作者: Mombo-Ngoma, Ghyslain ; Zoleko Manego, Rella ; Duparc, Stephan ; Ramharter, Michael ; Kremsner, Peter Gottfried ; Okwu, Dearie Glory

BACKGROUND:

In 2022, malaria caused approximately 249 million cases and 608,000 deaths, primarily in Africa. Current treatments target asexual blood-stage parasites, gametocytes, and liver hypnozoites. Standard guidelines recommend a 3-day course of artemisinin-based combination therapies as a first-line treatment of uncomplicated malaria and parenteral artesunate for severe malaria. However, the emergence of partial resistance to artemisinin derivatives threatens the treatment efficacy, highlighting the urgent need for novel antimalarial drugs.

OBJECTIVES:

This review summarizes recent progress in the clinical development of antimalarials particularly non-artemisinin compounds under target product profile-1.

SOURCES:

Data were gathered from Medicines for Malaria Venture (MMV)'s portfolio and clinical trial databases between 2020 and 2024.

CONTENT:

Sixteen clinical trials were reviewed, including safety and efficacy studies involving healthy volunteers, experimentally infected volunteers, asymptomatic Plasmodium falciparum carriers and malaria patients. Six trials evaluated the safety and tolerability of MMV533, ZY19489, INE963, GSK701/MMV367 and intravenous KAE609 in healthy volunteers. Efficacy trials involving experimentally infected volunteers assessed ZY19489 and GSK701/MMV367, whereas studies on asymptomatic carriers tested ZY19489/ferroquine and cabamiquine/pyronaridine. Trials on malaria patients investigated combinations of ganaplacide/lumefantrine-SDF, cabamiquine/pyronaridine, both oral and intravenous cipargamin and INE963.

IMPLICATIONS:

Although attrition remains a possibility, several promising candidate drugs with novel modes of action are advancing through clinical development. Many are expected to become available for treating uncomplicated and severe malaria within the next decade. These new antimalarials could significantly enhance malaria treatment, reduce resistance, and support global health efforts towards malaria control, elimination and, potentially, eradication.

2025-04-24·JOURNAL OF MEDICINAL CHEMISTRY

Optimization and Characterization of N-Acetamide Indoles as Antimalarials That Target PfATP4

Article

作者: MacRaild, Christopher A. ; Jarman, Kate E. ; Ashton, Trent D. ; Jagoe, Hannah ; Lehane, Adele M. ; Sutherland, Colin J. ; Creek, Darren J. ; Awalt, Jon Kyle ; Famodimu, Mufuliat T. ; Lee, Serena ; Chowdury, Mrittika ; Brand, Stephen ; Stewart, Lindsay ; Calic, Petar P. S. ; Kristan, Mojca ; Gancheva, Maria R. ; Sleebs, Brad E. ; Coyle, Rachael ; Mansouri, Mahta ; Ooi, Zi Kang ; Cowman, Alan F. ; Delves, Michael J. ; Zhang, Xinxin ; Penington, Jocelyn S. ; Mao, Emma Y. ; Vasanthan, Santhya ; Fidock, David A. ; Sheth, Tanaya ; Loi, Katie ; Baum, Jake ; Yeo, Tomas ; Zhou, Qingmiao ; Dans, Madeline G. ; Giannangelo, Carlo ; Churchyard, Alisje ; Baud, Delphine ; Jackson, Paul F. ; Wilson, Danny W. ; de Koning-Ward, Tania F. ; Qiu, Deyun ; Lee, Marcus C. S.

To discover new antimalarials, a screen of the Janssen Jumpstarter library against Plasmodium falciparum uncovered the N-acetamide indole hit class. The structure-activity relationship of this chemotype was defined and culminated in the optimized frontrunner analog WJM664, which exhibited potent asexual stage activity and high metabolic stability. Resistant selection and whole-genome sequencing revealed mutations in PfATP4, which was validated as the target by showing that analogs exhibited reduced potency against parasites with resistance-conferring mutations in PfATP4, a metabolomic signature similar to that of the PfATP4 inhibitor KAE609, and inhibition of Na⁺-dependent ATPase activity consistent with on-target inhibition of PfATP4. WJM664 inhibited gamete development and blocked parasite transmission to mosquitoes but exhibited low efficacy in aPlasmodium berghei mouse model, which was attributed to ATP4 species differentiation and its moderate systemic exposure. Optimization of these attributes is required for N-acetamide indoles to be pursued for development as a curative and transmission-blocking therapy.

项与 Cipargamin 相关的新闻（医药）

2025-04-09

·CPHI制药在线

合成生物学在医药领域的研究现状与进展

关注并星标CPHI制药在线合成生物学作为一门融合生物学、基因组学、工程学和信息学的学科，正在引领着“第三次生物科学变革”。合成生物学在医药领域的应用主要体现在以下两个方面：手性医药化学品的绿色制造、植物天然产物的微生物重组合成。其通过定向设计和理性改造生物体，为解决全球气候变暖、实现碳中和目标以及推动医药、能源、材料等行业的产业升级提供了新的途径。接下来，我们将深入探讨合成生物学在医药领域的应用进展，重点关注手性医药化学品的绿色制造和植物天然产物的生物制造。一、手性医药化学品的绿色制造：生物催化技术的崛起手性医药化学品是医药化学品的重要组成部分，在许多药物分子中扮演着关键角色。然而，传统的化学合成方法存在底物合成困难、催化剂昂贵且易中毒失活、产品ee值低等问题，难以满足日益增长的医药需求。此外，传统的化学合成方法存在底物合成困难、催化剂昂贵且易中毒失活。生物催化技术为手性医药化学品的绿色制造提供了新的解决方案。利用微生物或酶作为催化剂，生物催化技术具有条件温和、环境友好、高效、高选择性的特点，可以有效地解决传统化学合成方法的弊端。1.1生物催化中常用的酶氧化还原酶：如羰基还原酶、亚胺还原酶、烯还原酶等，可以催化氧化还原反应，在手性胺类、手性醇类和手性氨基酸的合成中发挥重要作用。转移酶：如转氨酶，可以催化氨基基团的转移，在手性胺类化合物的合成中具有重要作用。裂解酶：如腈水解酶、卤醇脱卤酶等，可以催化底物的裂解反应，在手性醇类和手性氨基酸的合成中发挥重要作用。1.2生物催化在手性医药化学品合成中的应用实例西他列汀中间体：利用羰基还原酶和转氨酶的串联反应，可以实现西他列汀中间体的高效合成，转化率超过95%，ee值超过99.5%。抗疟药cipargamin的中间体：利用转氨酶催化反应，可以实现抗疟药cipargamin 的中间体的高效合成，合成规模达到50 g，收率84.5%。普瑞巴林：利用羰基还原酶催化反应，可以实现普瑞巴林的高效合成，ee值达到99.8%。二、植物天然产物的微生物重组合成：突破资源限制传统的植物提取方式存在资源限制、提取过程繁琐、收率低等问题。植物天然产物是药物及其先导化合物的重要来源，在近40年获批上市的药物中，天然产物及其衍生物约占25%。然而，传统的植物提取方式存在资源限制、提取过程繁琐、收率低等问题，难以满足社会发展的需求。合成生物学技术为植物天然产物的生产提供了新的途径。通过将药用植物基因组装、编辑到微生物细胞中，可以构建微生物细胞工厂，实现植物天然产物的微生物重组合成。这种方法可以突破植物资源限制，具有环境友好、生产速度快、易于大规模生产等多种优势。2.1 微生物重组合成植物天然产物的实例黄花素：通过将黄花蒿中的关键基因导入酵母细胞，可以实现黄花素前体青蒿酸的高效合成，产量达到45 g/L。人参皂苷：通过将人参中的关键基因导入酵母细胞，可以实现人参皂苷Rh2和人参皂苷CK的高效合成，产量分别达到2.25 g/L和5 g/L。β-胡萝卜素：通过将类胡萝卜素合成途径的关键基因导入解脂耶氏酵母细胞，可以实现β-胡萝卜素的高效合成，产量达到39.5 g/L。白藜芦醇：通过将白藜芦醇合成途径的关键基因导入解脂耶氏酵母细胞，可以实现白藜芦醇的高效合成，产量达到22.5 g/L。2.2 微生物重组合成植物天然产物的优势突破资源限制：不受植物生长周期、生长环境和地理分布的限制，可以大规模生产植物天然产物。环境友好：不需要使用化学试剂和溶剂，减少了对环境的污染。生产速度快：微生物发酵速度快，可以缩短生产周期。易于大规模生产：可以采用发酵罐进行大规模生产，满足市场需求。三、合成生物学引领医药产业变革合成生物学技术正在快速发展，并在医药领域展现出巨大的应用潜力。我国“十四五”规划和2035年远景目标纲要中已明确将合成生物学列为科技前沿领域之一。3.1 合成生物学在医药领域的应用前景开发新的药物：通过合成生物学技术，可以构建微生物细胞工厂，生产具有生物活性的天然产物及其衍生物，为开发新的药物提供先导化合物。降低药物生产成本：合成生物学技术可以实现植物天然产物的微生物重组合成，突破植物资源限制，降低药物生产成本。提高药物生产效率：合成生物学技术可以构建高效的微生物细胞工厂，提高药物生产效率，满足日益增长的医药需求。开发个性化药物：合成生物学技术可以构建个性化的微生物细胞工厂，生产针对特定疾病的药物，实现个性化医疗。3.2 合成生物学在医药领域的挑战技术瓶颈：合成生物学技术尚处于发展阶段，仍存在一些技术瓶颈，如基因编辑技术、细胞工厂构建技术等。安全性问题：合成生物学技术构建的微生物细胞工厂可能存在安全风险，需要进行严格的安全性评估。伦理问题：合成生物学技术涉及对生物体的改造，需要考虑伦理问题。总结总的来说，合成生物学技术为植物天然产物的生产提供了新的途径，突破了传统植物提取方式的限制，展现出巨大的应用潜力。通过构建高效的微生物细胞工厂，可实现植物天然产物的绿色、高效、规模化生产，满足日益增长的医药需求。然而，微生物重组合成植物天然产物技术仍处于发展阶段，面临着诸多挑战。未来，需开发更先进的基因编辑技术、细胞工厂构建技术和产物提取纯化方法，以推动这项技术的成熟和产业化应用。参考资料：[1] 尹梦琦,赵建志.基于合成生物学技术改造酵母高效合成萜类化合物[J].齐鲁工业大学学报,2025,39(1):36-46.[2] 洪明明,唐林林,宋杰.基于环状单链DNA的医学合成生物学[J/OL].生命科学,1-21.[3] 朱华伟,李寅.合成生物制造2025[J].生物工程学报,2025,41(1):1-78.作者简介：雅韵，从事药物治疗机制、药物临床试验与药物研发等。END2025金笔奖征文活动开启，来投稿吧！领取CPHI & PMEC China 2025展会门票智药研习社课程预告来源：CPHI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com▼更多制药资讯，请关注CPHI制药在线▼点击阅读原文，进入智药研习社~

临床研究

2024-11-29

·CPHI制药在线

抗疟疾药物研发进展

关注并星标CPHI制药在线在全球健康的版图中，疟疾一直是一块难以攻克的“顽疾”。据世界卫生组织（WHO）统计，2021年全球约有2.47亿疟疾病例，61.9万人因此失去生命，其中95%的病例和96%的死亡发生在撒哈拉以南非洲地区。疟疾不仅严重威胁人类健康，还对经济发展造成巨大阻碍，每年导致该地区约120亿美元的经济损失。今天，就让我们深入了解疟疾的现状、抗疟药物的研发进展，以及未来面临的挑战与希望。 1、现有抗疟疗法及耐药困境（1）常用药物与疗法当前，治疗非重症恶性疟原虫疟疾，主要依靠以青蒿素为基础的联合疗法（ACTs）。其中，蒿甲醚 - 苯芴醇（artemether lumefantrine，AL）在非洲市场占据了75%的份额，青蒿琥酯 - 阿莫地喹（artesunate amodiaquine）则作为二线选择，拥有24%的市场占有率。这些药物在一定程度上有效控制了疟疾的发展，但它们也面临着日益严峻的耐药问题。除了ACTs，还有双氢青蒿素 - 哌喹（dihydroartemisinin piperaquine，DHA - PPQ）、阿托伐醌 - 氯胍（atovaquone proguanil，Malarone）等药物组合，但使用相对较少。对于重症疟疾，静脉注射青蒿琥酯（artesunate）是首选治疗方法，金鸡纳霜（quinine）也可作为替代选择。而针对间日疟原虫疟疾的根治，氯喹（Chloroquine）与伯氨喹（primaquine）或他非诺喹（tafenoquine）的联合使用是常见方案；孕期间歇性预防治疗则采用磺胺多辛 - 乙胺嘧啶（sulfadoxine-pyrimethamine，SP）；在非洲的季节性疟疾高发地区，对于6个月至5岁（部分国家至10岁）的儿童，每月使用SP和阿莫地喹进行季节性疟疾化学预防（SMC）（图1）。（2）药物耐药性问题疟原虫耐药问题由来已久，20世纪初有对奎宁耐药的报告，50年代起氯喹和SP耐药性在疟疾流行区扩散，致死亡人数上升。21世纪ACTs虽为一线疗法，但耐药问题仍存。东南亚大部分地区DHA - PPQ因耐药失效，非洲大陆AL虽仍有效，但卢旺达已现青蒿素部分耐药，乌干达恶性疟原虫临床分离株对咯萘啶（pyronaridine）和DHA敏感性降低，这些耐药现象严重威胁全球疟疾防控成效。图1.在疟原虫生命周期下的疟疾治疗来源：出自参考文献【1】 2、抗疟药物研发进展（1）传统与现代的研发策略在抗疟药物研发的漫长历程中，传统策略主要包括从天然产物中分离和修饰活性成分，以及筛选化合物库、设计已知靶点抑制剂等。然而，这种基于天然产物的研发方式面临着诸多挑战，如供应不稳定、成分多变、生物测定引导分馏后复杂混合物相关的实际挑战。此外，对现有天然产物进行改进以克服耐药性的难度较大，这使得研发人员不得不寻求新的方法。随着科学技术的发展，现代抗疟药物研发主要采用表型筛选和基于靶点和虚拟药效团的方法。表型筛选：通过对全细胞寄生虫培养进行大规模化学库筛选，可发现具有新颖作用模式的化合物，许多在研药物由此发现，但靶点未知会给后续优化带来困难。基于靶点和虚拟药效团方法：基于靶点的方法可开发新的生化测定，合理设计化合物，但可能成本高且存在耐药风险；虚拟筛选虽初期成本低，但需大量后续工作确认化合物与靶点的结合及对寄生虫的功能抑制，目前尚未产生具有强细胞活性的新化合物。（2）新靶点及治疗药物为了开发更有效的抗疟药物，科学家们已经发现了一些具有潜力的靶点，如细胞色素B（CytB）、二氢蝶酸合成酶（DHPS）、二氢叶酸还原酶 - 胸苷酸合成酶（DHFR - TS）和血红素等，这些都是已有的临床验证靶点（图2）。此外，还有一些较新的靶点，如ATP酶4（ATP4）、延伸因子2（eEF2）、脯氨酰tRNA合成酶（PRS）和磷脂酰肌醇4 - 激酶（PI4K）等。图2.具有临床验证的抗疟靶点来源：出自参考文献【1】在抗疟药物的研发进程中，众多药物处于不同的研究阶段（图3），给我们带来了新的希望。患者探索阶段： ZY - 19489是一种快速杀伤无性血液阶段寄生虫且耐药倾向低的化合物，在志愿者感染研究中，其安全性、药代动力学和抗疟活性表现优异，支持其进一步开发。 ferroquine是一种含二茂铁基环的4 - 氨基喹啉类药物，具有快速杀伤和长半衰期的特点，与ZY - 19489组合使用，有望实现儿童疟疾的单剂量治疗，为应对ACTs耐药性提供了潜在解决方案。 cabamiquine对寄生虫无性肝、血和性阶段均有活性，但其耐药性发展较快，因此与咯萘啶联用，以增强疗效并延缓耐药性的产生。 ganaplacide对无性肝、血和性阶段的恶性疟原虫均有强效作用，与优化配方的苯芴醇联用，在临床研究中取得了积极结果，有望成为自2000年以来首个非ACT治疗药物。 cipargamin可使寄生虫僵化并快速清除，对传播阻断也有效，但由于存在耐药风险，目前正在探索注射用新配方，以确保其长期有效性。临床I期阶段： atoguanil是阿托伐醌 - 氯胍的新配方，旨在提高药物的疗效和安全性。 MMV688533是通过基于同源性的筛选策略发现的TCP - 1候选药物，其作用机制虽尚未完全明确，但耐药风险低，在实验室条件下难以产生耐药性，目前正在进行临床I期研究。 INE963是诺华发现的快速杀伤化合物，对无性血液阶段寄生虫具有高效作用，且耐药倾向低，近期已进入临床I期试验，后续还将在治疗组合的II期试验中进行评估。临床前阶段：共有11种候选小分子和1种抗体正在深入研究。其中， MMV183是一种抑制AcAS的抗代谢物，具有显著的传播阻断和无性血液阶段活性； GSK701是酰基辅酶A合成酶ACS10和ACS11的新型抑制剂，具有TCP - 1活性特征； WM382和BRD5018分别是 plasmepsins IX和X以及FRS的抑制剂，具有多阶段活性，对寄生虫的多个生命周期阶段均有作用； SC83288是一种新型注射候选药物，用于治疗重症疟疾，但其作用机制尚不清楚； GSK484和IWY357是通过表型筛选发现的快速杀伤化合物，具有低耐药倾向，虽然其结构和作用机制尚未公布，但在抗疟药物研发中具有潜在价值； MMV371是阿托伐醌前药，ELQ - 331是ELQ - 300的口服前药，两者均通过抑制寄生虫CytB发挥作用； S011 - 1793是下一代4 - 氨基喹啉，能够克服氯喹和PPQ耐药性； MMV1793609是PfATP4抑制剂，具有低剂量高效的特点，是2022年发现的备选药物。图3.抗疟药物研发进展和研发管线来源：出自参考文献【1】 3、抗疟之路的未来挑战与展望疟疾防控工作面临着诸多复杂的挑战，疟原虫耐药机制研究复杂，实验室研究多基于单基因变化，但实际临床分离株往往涉及多个突变，且寄生虫遗传背景对耐药性产生的影响机制尚不明确，不同地区疟原虫的遗传差异也导致耐药性表现和传播方式各异。此外，药物递送与药代动力学也存在难题，例如长效注射剂面临疗效持续时间、体积和安全性等挑战，不同人群对药物代谢和反应的差异也增加了研发复杂性...... 尽管挑战重重，但过去15年在疟疾防控方面取得了一定成果，新靶点不断被发现，候选药物进入研发管线，新治疗方法如首个疟疾疫苗获批问世。这些成绩的取得离不开全球各方的紧密合作，未来仍需进一步加强合作，整合资源、加大研发投入、鼓励创新，通过共享数据、技术和经验来加速抗疟药物研发进程，实现疟疾的有效控制和消除。疟疾防控是全球性持久战，每一次突破都使我们向战胜疟疾的目标更近一步，我们应共同关注和支持抗疟工作，期待人类能早日摆脱疟疾威胁。参考文献 [1]Siqueira-Neto, Jair L et al. “Antimalarial drug discovery: progress and approaches.” Nature reviews. Drug discovery vol. 22,10 (2023): 807-826. doi:10.1038/s41573-023-00772-9 [2]Carter, Richard, and Kamini N Mendis. “Evolutionary and historical aspects of the burden of malaria.” Clinical microbiology reviews vol. 15,4 (2002): 564-94. doi:10.1128/CMR.15.4.564-594.2002 [3]Rasmussen, Charlotte et al. “Current and emerging strategies to combat antimalarial resistance.” Expert review of anti-infective therapy vol. 20,3 (2022): 353-372. doi:10.1080/14787210.2021.1962291 END 【智药研习社近期直播预告】来源：CPHI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com ▼更多制药资讯，请关注CPHI制药在线▼ 点击阅读原文，进入智药研习社~

临床研究孤儿药

2018-04-17

·BioSpace

Novartis to Spend $100M on Malaria Initiative

Mosquito-borne illnesses are a major concern in many parts of the world. One of the nastier viruses carried by mosquitoes, malaria, was responsible for the deaths of more than 445,000 people in 2016. One biotech is aiming to make a difference. Mosquito-borne illnesses are a major concern in many parts of the world. One of the nastier viruses carried by mosquitoes, malaria, was responsible for the deaths of more than 445,000 people in 2016. One biotech is aiming to make a difference. This morning Novartis announced a five-year commitment in the fight against malaria . Swiss-based Novartis said it will invest more than $100 million to advance research and the development of “next-generation treatments” to combat emerging resistance to artemisinin and other currently used antimalarials. With an increased focus on malaria treatments, Novartis is contributing to the World Health Organization’s target of reducing malaria-related child mortality by at least 90 percent by 2030. Novartis will further help expand access to pediatric antimalarials and implement healthcare system strengthening programs in four sub-Saharan countries, including Nigeria and the Democratic Republic of the Congo, the company announced. While the company is investing large sums of money into new developments, Novartis said it will keep in mind the end costs for users, many of whom are in impoverished areas. The company said it will implement an equitable pricing strategy to “maximize patient access in malaria-endemic countries when these new treatments become available.” “Resistance to treatment presents the biggest threat to the incredible progress that has been made in the fight against malaria in the past 20 years. We cannot afford to wait; this is why we are committing to advance the research and development of next-generation treatments,” Novartis Chief Executive Officer Vas Narasimhan said in a statement. “At the same time, we need to work to ensure that our innovation reaches those most in need, even those in the most remote locations.” Novartis said it will work with stakeholders to support the retail end of things. With the $100 million investment, Novartis said it will advance the company’s malaria pipeline through 2023. The aim is to complete clinical trials for two malaria candidates, KAF156 and KAE609 (currently in Phase IIb and Phase IIa respectively. Both drug candidates are part of a new class of medicines designed for their ability to treat malaria in different ways from current therapies, Novartis said. Novartis, which launched the first fixed-dose artemisinin-based compounds treatment for malaria in 1999, said some experts are concerned that malaria parasites could become resistant to ACTs in the next two decades. Between 2000 and 2015 deaths from malaria have dropped by more than 60 percent, Novartis said.

临床2期

100 项与 Cipargamin 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Cipargamin	-	DB12306

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
急性疟疾	临床2期	泰国	Novartis Pharmaceuticals Corp.	2013-07-01
急性疟疾	临床2期	越南	Novartis Pharmaceuticals Corp.	2013-07-01
恶性疟	临床2期	泰国	Novartis Pharmaceuticals Corp.	2013-07-01
恶性疟	临床2期	越南	Novartis Pharmaceuticals Corp.	2013-07-01
间日疟原虫感染	临床2期	泰国	Novartis Pharmaceuticals Canada, Inc.	2012-01-01
疟疾	临床1期	比利时	Novartis Pharmaceuticals Corp.	2020-07-22

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临床结果

适应症

分期

评价

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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


NCT04321252 (Pubmed \| Antimicrob Agents Chemother) 人工标引	临床1期	-	17	Cipargamin 10.5 mg	淵廠構衊廠齋鏇齋鏇窪(憲遞繭鹹簾製鏇鬱襯遞) = Cipargamin was well tolerated with commonly reported mild gastrointestinal, neurological, and genitourinary events. 夢膚淵鏇壓網襯艱鏇鑰 (鬱窪艱醖鏇範鑰觸鏇積 ) 更多	积极	2024-07-26
NCT03334747 (Pubmed) 人工标引	临床2期	恶性疟	-	KAE609	鏇鏇製簾淵網製網鹽衊(獵襯蓋廠鑰窪齋願醖齋) = 夢壓窪遞襯淵廠夢遞觸醖餘鏇選襯遞獵夢繭觸 (觸顧鑰壓衊襯膚壓糧遞 ) 更多	积极	2021-08-19
NCT03334747 (Pubmed) 人工标引	临床2期	恶性疟	-	rtemether-lumefantrine	壓醖選憲蓋窪鏇鹽選壓(糧夢範廠獵網鏇艱繭窪) = 淵艱簾鹽構餘夢襯遞鑰餘衊壓網夢製觸願鹹淵 (窪獵淵築積簾淵製遞鏇 )	积极	2021-08-19
NCT02543086 (Pubmed \| Antimicrob Agents Chemother)	临床1期	-	8	Cipargamin 10mg	築遞齋築選醖範簾鏇艱(觸製壓窪鬱築範鑰鬱製) = Serious adverse liver function changes were observed in three subjects, which led to premature study termination 壓夢構憲齋夢鑰獵膚糧 (鏇餘簾膚鬱齋獵窪顧淵 )	-	2021-01-20
NCT01836458 (Pubmed \| Antimicrob Agents Chemother)	临床2期	恶性疟	25	cipargamin 30 mg	範顧願鏇繭製衊齋憲夢(艱範蓋鏇製鏇淵壓襯繭) = 簾衊築築窪製衊齋窪夢鹽製遞膚膚選壓獵醖製 (餘鏇鏇網顧餘積餘壓遞 )	-	2017-02-01
NCT01836458 (CTgov)	临床2期	-	25	KAE609 (Dose 1: 30 mg)	鬱網餘獵獵鹽願選艱構(淵鬱鏇鹹繭齋鑰廠築鬱) = 蓋遞艱繭網鹽願餘鹽遞選鹹鏇廠選膚醖醖鹽艱 (網憲淵網範餘壓積築糧, 顧顧遞糧積壓鹹選壓選 ~ 淵獵糧繭鏇網鬱壓廠鑰) 更多	-	2016-10-31
NCT01836458 (CTgov)	临床2期	-	25	KAE609 (Dose 2: 20 mg)	鬱網餘獵獵鹽願選艱構(淵鬱鏇鹹繭齋鑰廠築鬱) = 膚鹹製窪鬱鹽範餘遞壓選鹹鏇廠選膚醖醖鹽艱 (網憲淵網範餘壓積築糧, 蓋遞窪壓壓壓築鏇壓繭 ~ 獵糧艱衊網鹽鹹獵襯憲) 更多	-	2016-10-31
NCT01860989 (CTgov)	临床2期	急性疟疾 \| 恶性疟	11	KAE609	膚鹽鑰築窪遞餘積淵醖 = 淵衊憲淵壓齋淵壓範構襯夢淵鏇糧齋衊醖蓋範 (艱壓鹹窪鬱願範選願鹹, 齋網網簾壓簾願觸淵窪 ~ 夢顧鬱網鑰蓋憲糧構憲) 更多	-	2015-09-03
NCT01524341 (Pubmed \| N Engl J Med)	临床2期	恶性疟 \| 间日疟原虫感染	-	KAE609 30 mg	遞鹽艱繭鏇窪鹽齋簾衊(鑰糧構憲構淵鹹網淵餘) = 膚築獵艱觸艱蓋淵鏇餘觸選構築糧範遞窪繭齋 (艱壓選鏇網繭觸鹹顧築 ) 更多	-	2014-07-31