Single Centre Open-label, Non-randomised, 3-treatment, 2-period, Pharmacokinetic Drug Interaction Study of Single Oral Dose of Acoziborole With Sequential Co-administration of Midazolam and Dextromethorphan in Healthy Male Participants

To assess Drug drug interactions between Acoziborole and Dextromethorphan and Midazolam in healthy male volunteers.

开始日期2023-02-09

申办/合作机构

Drugs for Neglected Diseases initiative

NCT05433350

/ Completed临床2/3期IIT

Pharmacokinetic, Efficacy, Safety, and Tolerability Study of a Single Dose of Acoziborole Under Fasting Conditions in Paediatric Patients From 1 to 14 Years of Age and With g-HAT: a Multicentre, Open-label Study

Acoziborole has been studied in an open-label pivotal Phase II/III trial (DNDi-OXA-02-HAT) in the DRC and Guinea. As the numbers of reported cases diminish, resources for surveillance and specialised screening will also taper. This decrease, coupled with the loss of diagnostic skills and disease management expertise, will lead to a weak and less specialised HAT technical environment. The history of g-HAT has shown that outbreaks or re-emergence of the disease have already happened under different circumstances when surveillance was relaxed or simply because the populations at risk live in areas of political instability, limiting access to specialised care. Even with a steady decrease of reported incidence, no model can currently predict that HAT could not re-emerge.
Although g-HAT is predominantly a disease of adults, children are also affected at diverse rates depending on the geographical and behavioural characteristics in the different areas of disease transmission. Hence efforts are needed to develop a paediatric formulation from a new generation of oral HAT treatments.

开始日期2022-07-09

申办/合作机构

Drugs for Neglected Diseases initiative

NCT05256017

/ Completed临床2/3期IIT

Safety and Tolerability Study of Acoziborole in g-HAT Seropositive Non-parasitologically Confirmed Subjects: a Multicentre Randomised Double-blind Placebo-controlled Study

Human African trypanosomiasis (HAT) or sleeping sickness is a tropical disease which is endemic in sub-Saharan Africa. Most cases of HAT are due to the parasite Trypanosoma brucei gambiense (T.b. gambiense), which is transmitted by the bite of the tsetse fly. HAT can be fatal without diagnosis and treatment. Several treatment options are currently available to treat HAT caused by the T.b. gambiense parasite (g-HAT), but these treatments can be administered only after demonstrating via microscopy the presence of the parasite in a body fluid. However, there are factors such as low parasitaemia and the complexity and low sensitivity of parasitological methods that make such demonstration difficult. It has been demonstrated that a variable proportion (mainly depending on the prevalence) of such g-HAT "sero-suspects" are confirmed cases and, therefore, remain potential reservoirs of the parasite and a source of new infections hindering the efforts to eliminate the disease.
The drug acoziborole was evaluated in a study called "DNDi-OXA-02-HAT". During this study, patients with g-HAT from the DRC and Guinea took a single dose of acoziborole. This study showed that acoziborole has a high efficacy and is safe for treating patients with confirmed g-HAT .
The present study is called "DNDi-OXA-04-HAT". It included seropositive participants from the DRC and Guinea who did not have parasites detected via microscopy in a body fluid. Its objective was to collect data on the safety and tolerability of a single dose of acoziborole compared to a placebo (i.e. a dummy treatment). The results of this study would help decide if acoziborole can be used in the population of g-HAT seropositive individuals and help eliminate the HAT disease.

开始日期2021-12-30

申办/合作机构

Drugs for Neglected Diseases initiative

100 项与 Acoziborole 相关的临床结果

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100 项与 Acoziborole 相关的转化医学

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100 项与 Acoziborole 相关的专利（医药）

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项与 Acoziborole 相关的文献（医药）

2025-06-01·COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

To Explore Potential Inhibitors against Various Enzymatic Targets of Human African Trypanosomiasis

Review

作者: Bagchi, Soumya Ranjan ; Brahma, Sayandeep ; Samadder, Asmita ; Moitra, Susmita ; Nandi, Sisir

Synthetic drugs currently prescribed for the treatment of Human African Trypanosomiasis (HAT) are non-specific, toxic, demand extended therapeutic regimes and are of varying efficacy. Along with the challenging demographic and socio-economic hurdles, the everincreasing risk of drug resistance is another major problem to be addressed. Cysteine protease, Heat shock proteins (HSP-90), Trypanothione reductase (TR), Farnesyl diphosphate synthase, Glucose-6-phosphate dehydrogenase, UP-4-galactose epimerase, and Cytidine triphosphate synthetase are potential enzymatic targets for the development of novel inhibitors against HAT which are the main focus of this review. The potential enzymatic targets of Trypanosoma brucei, especially small molecules like cysteine proteases and heat shock proteins are identified as major candidates for the sustenance of the parasite, their proliferation, infection, and spread of the disease. The development of new compounds to combat the disease by thorough ligand modification has been explored in the current review. Extracting these compounds and studying their efficacy, toxicity, and target mechanism extensively, this review has proposed a list of different compounds, including some synthetic and natural compounds along with multi-target inhibitors such as acoziborole, fexinidazole, etc. Potential inhibitors against these enzymatic targets of the T. brucei are important candidates for designing novel therapeutics against HAT. Multi-target inhibitors have also been identified as crucial molecules because of their potential advantage against the development of drug resistance.

2025-03-13·CLINICAL MICROBIOLOGY REVIEWS

Transforming the chemotherapy of human African trypanosomiasis

Review

作者: Barrett, Michael P.

SUMMARY:

Prior to 2019, when the orally available drug fexinidazole began its clinical use, the treatment of human African trypanosomiasis (HAT) was complex and unsatisfactory for many reasons. Two sub-species of the Trypanosoma brucei parasite are responsible for HAT, namely the rhodesiense form found in East and Southern Africa and the gambiense form found in Central and West Africa. Diseases caused by both forms manifest in two stages: stage 1 before and stage 2 after central nervous system involvement. Prior to 2019, different drugs were required for each of the two parasite sub-species at each stage. Gambiense disease required pentamidine or nifurtimox-eflornithine combination therapy, while for rhodesiense disease, suramin or melarsoprol was given for stages 1 and 2, respectively. These drugs all suffered complications including protracted administration regimens involving multiple injections with drug-induced adverse effects common. Today, a single drug, fexinidazole, can be given orally in most cases for both diseases at either stage. Another compound, acoziborole, effective in both stages 1 and 2 gambiense disease with a single dosing is anticipated to become available within a few years. Moreover, the recent engagement of multilateral organizations in seeking other compounds that could be used in HAT therapy has also been successful, and a rich vein of new trypanocides has been discovered. Here, the clinical use, modes of action, and resistance risks for drugs used against HAT are discussed.

2024-12-01·Artificial intelligence in the life sciences

Pharmacological profiles of neglected tropical disease drugs

作者: Greco, Alessandro ; Gadiya, Yojana ; Karki, Reagon ; Zaliani, Andrea ; Gul, Sheraz ; Deecke, Clara

According to the World health Organization there are a group of 20 diverse infectious Neglected Tropical Disease (NTD) conditions that primarily affect populations in low-income and developing regions.Despite the limited attention and funding compared to other health concerns, significant efforts to develop drugs for treating and controlling NTDs have been made.However, there is room for developing NTD drugs with improved safety, efficacy and ecotoxicol. profiles.In order to facilitate this, we have adapted our existing validated data-driven workflows for understanding disease comorbidity to systematically evaluate the approved drugs that target the major World Health Organization defined NTDs.The foundation for this work comprised assembling the physicochem., biol. and clin. properties of each NTD drug and identifying patterns that reveal the underlying cause of their efficacy and side-effect profiles.Subsequently, computational methods were employed to identify analogs with potentially improved profiles and validated in a case study focusing on the teratogenic antileishmanial drug miltefosine.The wider impact of NTD drugs with regards to a One Health cross-disciplinary perspective at the human-animal-environment interface are also discussed.

项与 Acoziborole 相关的新闻（医药）

2026-04-12

·Pharm-Patent

Acoziborole研究进展（V1,2026.4.12更新）

1、研究机构：辉瑞制药、Anacor Pharmaceuticals、赛诺菲制药、Scynexis、Drugs for Neglected Diseases initiative、Advinus 2、剂型及给药途径：普通片剂; 口服给药；颗粒剂; 口服给药 3、别名：AN-5568、SCYX-7158、Acoziborole Winthrop、Oxaborole SCYX-7158 4、靶点：CPSF3 5、结构式 6、发表论文标题内容类型适应症企业技术平台来源发表日期 Clinical and veterinary trypanocidal benzoxaboroles target CPSF3 靶点/标志物验证非洲锥虫病 Anacor Pharmaceuticals University of Dundee Proc Natl Acad Sci U S A IF=9.1 2018-09-18 7、专利布局公开（公告）号专利主题发明名称申请日法律状态 US9440994B2 化合物含硼小分子抗原虫剂 2010-08-06 US8115026B2 化合物含硼小分子 2009-12-02 US10301329B2 化合物含硼小分子作为抗原生动物剂 2016-08-03 8、研究历程 2024年04月08日，由Drugs For Neglected Diseases Initiative开展临床三期试验，用于治疗非洲锥虫病。（NCT06356974） 2023年02月09日，由Drugs For Neglected Diseases Initiative在马来西亚开展临床一期试验，用于治疗非洲锥虫病。（NCT05947604） 2021年12月30日，由Drugs For Neglected Diseases Initiative在刚果民主共和国和几内亚开展临床三期试验，用于治疗非洲锥虫病和血管钙化。（NCT05256017; NCT05433350） 2021年04月27日，治疗非洲锥虫病的研究暂无进展。（NCT04270981） 2020年09月04日，由赛诺菲开展临床前研究试验。（https://dndi.org/press-releases/2020/innovative-single-dose-oral-sleeping-sickness-treatment-to-be-co-developed-by-sanofi-and-dndi/） 2020年02月05日，由Drugs For Neglected Diseases Initiative在英国开展临床一期试验，用于治疗非洲锥虫病。（NCT04270981） 2016年10月11日，由Drugs For Neglected Diseases Initiative在几内亚开展临床三期试验，用于治疗非洲锥虫病。（NCT05256017; NCT03087955; NCT05433350） 2015年06月24日，治疗寄生虫感染、原虫感染、锥虫病和非洲锥虫病的研究暂无进展。（NCT01533961） 2012年02月01日，由Drugs For Neglected Diseases Initiative在法国开展临床一期试验，用于治疗寄生虫感染、原虫感染、锥虫病和非洲锥虫病。（NCT01533961） 9、临床试验登记号试验标题试验药适应症原始适应症申办/合作机构试验状态试验分期开始日期完成日期国家/地区 NCT05947604 Single Centre Open-label, Non-randomised, 3-treatment, 2-period, Pharmacokinetic Drug Interaction Study of Single Oral Dose of Acoziborole With Sequential Co-administration of Midazolam and Dextromethorphan in Healthy Male Participants 盐酸咪达唑仑 (糖浆剂, 口服) | Acoziborole (片剂, 口服) | 氢溴酸右美沙芬 (糖浆剂, 口服) 非洲锥虫病 Trypanosomiasis, African Drugs for Neglected Diseases initiative Completed 临床1期 2023-02-09 2023-05-03 马来西亚 NCT05433350 Pharmacokinetic, Efficacy, Safety, and Tolerability Study of a Single Dose of Acoziborole Under Fasting Conditions in Paediatric Patients From 1 to 14 Years of Age and With g-HAT: a Multicentre, Open-label Study Acoziborole (片剂, 口服) 布氏锥虫感染 | 非洲锥虫病 | 肝素诱导血小板减少 Trypanosomiasis, African | Trypanosoma Brucei Gambiense; Infection | Sleeping Sickness Drugs for Neglected Diseases initiative Completed 临床2/3期 2022-07-09 2026-03-31 几内亚 | 刚果（金） NCT05256017 Safety and Tolerability Study of Acoziborole in g-HAT Seropositive Non-parasitologically Confirmed Subjects: a Multicentre Randomised Double-blind Placebo-controlled Study Acoziborole 布氏锥虫感染 | 非洲锥虫病 | 肝素诱导血小板减少 Trypanosomiasis, African | Trypanosoma Brucei Gambiense; Infection | Sleeping Sickness Drugs for Neglected Diseases initiative Completed 临床2/3期 2021-12-30 2023-08-03 几内亚 | 刚果（布） NCT03087955 Efficacy and Safety Study of Acoziborole (SCYX-7158) in Patients With Human African Trypanosomiasis (HAT) Due to Trypanosoma Brucei Gambiense: a Multicentre, Open-label, Prospective Study Acoziborole 非洲锥虫病 Trypanosomiasis, African | Gambiense Trypanosomiasis | Sleeping Sickness Drugs for Neglected Diseases initiative | Gates Foundation (United States) Completed 临床2/3期 2016-10-11 2020-09-08 几内亚 | 刚果（金） NCT01533961 Randomized, Double-blind, Placebo-controlled Sequential Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of SCYX-7158 After Single Oral Ascending Doses in Healthy Male Volunteers Acoziborole 非洲锥虫病 Trypanosomiasis | Trypanosomiasis, African | Protozoan Infections | Parasitic Diseases Drugs for Neglected Diseases initiative Completed 临床1期 2012-02-01 2015-03-01 法国 10、临床结果标题登记号来源分期适应症评价人数用药方案结果评价发布日期申办/合作机构主要研究药物来源链接 Synapse链接 Efficacy and Safety Study of Acoziborole (SCYX-7158) in Patients With Human African Trypanosomiasis (HAT) Due to Trypanosoma Brucei Gambiense: a Multicentre, Open-label, Prospective Study NCT03087955 CTgov 临床2/3期非洲锥虫病 208 Acoziborole(Late-stage HAT) Percentage of Participants With Late-stage HAT Whose Treatment Outcome Was a Success at Month 18 According to Adapted World Health Organization (WHO) Criteria = 95.2 % (95%CI, 91.2 ~ 97.7) - 2025-09-17 Drugs for Neglected Diseases initiative | Gates Foundation (United States) Acoziborole https://clinicaltrials.gov/ct2/show/results/NCT03087955 https://synapse.zhihuiya.com/clinical-result-detail/a42200482e4d8e8a3e5509aa0802a2a5 Efficacy and Safety Study of Acoziborole (SCYX-7158) in Patients With Human African Trypanosomiasis (HAT) Due to Trypanosoma Brucei Gambiense: a Multicentre, Open-label, Prospective Study NCT03087955 CTgov 临床2/3期非洲锥虫病 208 Acoziborole(Early- and Intermediate-stage HAT) Percentage of Participants With Early- and Intermediate-stage HAT Whose Treatment Outcome Was a Success at Month 18 According to Adapted WHO Criteria = 100.0 % (95%CI, 94.1 ~ 100.0) - 2025-09-17 Drugs for Neglected Diseases initiative | Gates Foundation (United States) Acoziborole https://clinicaltrials.gov/ct2/show/results/NCT03087955 https://synapse.zhihuiya.com/clinical-result-detail/a42200482e4d8e8a3e5509aa0802a2a5 Safety and Tolerability Study of Acoziborole in g-HAT Seropositive Non-parasitologically Confirmed Subjects: a Multicentre Randomised Double-blind Placebo-controlled Study NCT05256017 CTgov 临床2/3期布氏锥虫感染 | 非洲锥虫病 | 肝素诱导血小板减少 1208 Acoziborole(Acoziborole) Occurrence of Any TEAEs = 195 Pts - 2025-03-20 Drugs for Neglected Diseases initiative Acoziborole https://clinicaltrials.gov/ct2/show/results/NCT05256017 https://synapse.zhihuiya.com/clinical-result-detail/95d4e525d2892e4d2950528d20429ea0 Safety and Tolerability Study of Acoziborole in g-HAT Seropositive Non-parasitologically Confirmed Subjects: a Multicentre Randomised Double-blind Placebo-controlled Study NCT05256017 CTgov 临床2/3期布氏锥虫感染 | 非洲锥虫病 | 肝素诱导血小板减少 1208 Placebo(Placebo) Occurrence of Any TEAEs = 69 Pts - 2025-03-20 Drugs for Neglected Diseases initiative Acoziborole https://clinicaltrials.gov/ct2/show/results/NCT05256017 https://synapse.zhihuiya.com/clinical-result-detail/95d4e525d2892e4d2950528d20429ea0 Determination of the Optimal Single Dose Treatment for Acoziborole, a Novel Drug for the Treatment of Human African Trypanosomiasis: First-in-Human Study NCT01533961 Pubmed 临床1期非洲锥虫病 128 Acoziborole 960mg Plasma concentration = appeared rapidly in plasma (at 1 h), reached tmax between 24 and 72 h, and remained stable for up to 96 h, after which a slow decrease was quantifiable until 14 weeks after dosing 积极 2023-03-01 Drugs for Neglected Diseases initiative Acoziborole https://pubmed.ncbi.nlm.nih.gov/36763327/ | https://doi.org/10.1007/s40262-023-01216-8 https://synapse.zhihuiya.com/clinical-result-detail/25829a05e84332d58e8234e252d3aa2d Efficacy and safety of acoziborole in patients with human African trypanosomiasis caused by Trypanosoma brucei gambiense: a multicentre, open-label, single-arm, phase 2/3 trial NCT03087955 Pubmed 临床2/3期非洲锥虫病 208 Acoziborole Treatment success rate(18-month) = 95.2 % (95%CI, 91.2 ~ 97.7) 积极 2022-11-29 Drugs for Neglected Diseases initiative | Gates Foundation (United States) Acoziborole https://pubmed.ncbi.nlm.nih.gov/36460027/ https://synapse.zhihuiya.com/clinical-result-detail/202202805a52ad4ea89ed8e25532e2a9 11、转化医学研究亮点主题期刊/会议出版日期药物适应症机构 Mass balance, pharmacokinetics, metabolism, and excretion of radiolabeled acoziborole, a potential novel treatment for human African trypanosomiasis, following single microtracer oral dose to humans - 1期临床研究 Antimicrob Agents Chemother 2025-11-05 Acoziborole 非洲锥虫病 Nederlandse Organisatie voor Toegepast-Natuurwetenschappelijk | Drugs for Neglected Diseases initiative | PhinC Development | Quotient Sciences Ltd. | Sanofi R&D, Pharmacokinetics, Dynamics and Metabolism Towards elimination: Challenges in community participation to a gHAT ‘screen and treat’ strategy using the new oral drug acoziborole in the Democratic Republic of the Congo - 3期临床研究 PLoS Negl Trop Dis 2025-06-20 Acoziborole 非洲锥虫病 Institute of Tropical Medicine Efficacy and safety of acoziborole in patients with human African trypanosomiasis caused by Trypanosoma brucei gambiense: a multicentre, open-label, single-arm, phase 2/3 trial 该研究评估了acoziborole对非洲锥虫病（由布鲁氏锥虫引起）患者的安全性和有效性。研究结果显示，acoziborole对晚期非洲锥虫病患者的治疗成功率为95.2％，对所有患者的治疗成功率为98.1％。研究还发现，acoziborole的不良事件较少且轻度或中度，且无死亡与药物治疗相关。因此，acoziborole在阻断非洲锥虫病传播方面具有很高的潜力，有助于实现世界卫生组织2030年的目标。 2/3期临床研究 Pubmed 2023-04-01 Acoziborole 非洲锥虫病 Swiss Tropical & Public Health Institute | Ministry of Health, Republic of Liberia | University of Basel SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis SCYX-7158是一种口服活性苯硼酸酯，用于治疗第2期非洲人锥虫病。非洲人锥虫病在撒哈拉以南的非洲是一个重要的公共卫生问题，影响数十万人。现有的治疗方法存在安全性差、治疗方案复杂、疗效有限和成本高等问题。我们发现并优化了一类新型小分子硼含化合物苯硼酸酯，最终确定SCYX-7158作为非洲人锥虫病的有效、安全和口服治疗药物。SCYX-7158对Trypanosoma brucei具有活性，包括T. b. rhodesiense和T. b. gambiense，对小鼠非洲人锥虫病模型也具有疗效，并且具有口服、代谢稳定和中枢神经系统渗透性等生物药代动力学特性。SCYX-7158已被选定进入临床前研究，并有望在2011年进入I期临床试验。药物发现/临床前 PLoS Negl Trop Dis 2011-06-28 Acoziborole 非洲锥虫病 SCYNEXIS, Inc.

临床3期临床2期临床1期

2026-03-26

·搜狐新闻

突破性进展：含硼药物Acoziborole有望根除昏睡病，单剂量疗法获欧盟积极评估

2月，欧洲药品管理局（European Medicines Agency, EMA）对Acoziborole给出了积极的科学意见，这是一种针对早期和晚期昏睡病的单剂量疗法，为在受该疾病影响的撒哈拉以南非洲国家注册和分发铺平了道路。这种苯并恶唑硼化合物将成为仅有的第六种含有硼的许可药物，硼的化学性质对该药物的疗效至关重要。被忽视疾病药物研发倡议组织（Drugs for Neglected Diseases initiative, DNDi）的研发主管Charles Mowbray表示，这并非该类别中唯一的活性分子。“我们非常兴奋，苯并恶唑硼类化合物可能在治疗寄生虫疾病方面有其他用途。” Acoziborole的硼原子提供了关键的灵活性，使其能够到达大脑和身体其他部位的寄生虫感染处，而苯并恶唑硼环结构减缓了新陈代谢并延长了其半衰期。（背景延伸：药物的半衰期是指药物在生物体内浓度下降一半所需的时间，半衰期越长，药物在体内的作用时间越长。） DNDi是一家合作药物研究和开发非营利组织，总部位于瑞士日内瓦。在盖茨基金会的资助下，它汇集了公共和私人合作伙伴，历时二十多年开发了该药物。赛诺菲（Sanofi）现在将生产Acoziborole，该药物将通过世界卫生组织（World Health Organization, WHO）免费分发。他们的目标是到2030年消除这种疾病。“我们希望今年晚些时候首先在刚果民主共和国获得上市批准，并希望其他国家也能紧随其后，”Mowbray说。 EMA的决定是其“欧盟全民用药计划”（EU-Medicines for all programme）的一部分，该计划促成了WHO对该药物的资格预审，并使相关国家能够更快地注册。该倡议成立于2004年，旨在基于与欧洲使用的药物相同的严格标准，促进低收入和中等收入国家的患者获得安全、有效和高质量的药物。（背景延伸：“欧盟全民用药计划”旨在确保发展中国家能够以可负担的价格获得基本药物，从而改善全球健康状况。）昏睡病，又称非洲人类锥虫病（Human African trypanosomiasis, HAT），由布氏锥虫（Trypanosoma brucei）寄生虫引起，并通过受感染的采采蝇传播。如果不加以治疗，寄生虫会进入大脑，最终导致死亡。根据DNDi的数据，1998年报告了40,000例病例，另有300,000例疑似未确诊病例。当时，唯一的晚期治疗方法是一种痛苦且有毒的注射用砷衍生物。但DNDi和其他机构开发了几项改进措施，包括在2018年推出了首个口服10天疗程的药物fexinidazole，这是一种硝基咪唑类抗菌剂，使病例减少到每年600例。共同发明人Robert Jacobs表示，现在Acoziborole为根除疾病提供了真正的希望。Jacobs现已退休，曾是硼药物专家Anacor Pharmaceuticals的化学主管，该公司创建了最初的苯并恶唑硼化合物库，并发现了针对该寄生虫的首个活性。“这是一种单剂量疗法，三片药，并且鉴于今天观察到的安全性，可以广泛使用。我认为这才是真正令人兴奋的地方，”他说。Anacor于2016年被辉瑞（Pfizer）收购。弗吉尼亚理工大学（Virginia Tech）的有机硼化合物专家Webster Santos表示，硼化合物一直被认为是有毒的，但“这是一种误解”。他说，这来自非常古老的数据。尽管他说硼的亲电特性确实使其容易产生脱靶效应，这使得硼药物的开发“比标准的的小分子药物更长更困难”。 “这是一种单剂量疗法，三片药。我认为这才是真正令人兴奋的地方。” 但这些亲电特性也是其独特的超能力。Santos解释说：“[它]与路易斯碱（Lewis bases），如氧和氮结合”，这使其能够靶向蛋白质内的特定氨基酸序列并阻断正常功能。“通常，硼喜欢结合1,2-二醇，因此这种螯合使其对靶向非常有吸引力，”Santos补充道。到目前为止，只有少数几种含有硼的许可药物，包括Anacor的苯并恶唑硼化合物库中的其他两种。 Acoziborole通过抑制一种名为CPSF3（切割和多腺苷酸化特异性因子3）的mRNA加工酶来杀死锥虫，这种酶对寄生虫的基因表达至关重要。“硼绝对是该化合物效用的关键，”Jacobs说。该药物可以形成四面体硼酸酯，与酶内的两个锌原子位点结合，并模拟RNA中的磷酸盐，从而阻断通常被加工的RNA分子占据的空间。相同位置的碳原子无法做到这一点。 Jacobs说，硼的构型转换能力对于Acoziborole的成功及其进入受感染患者大脑并杀死寄生虫的能力也“绝对至关重要”。中性分子可以通过血脑屏障，但随后可以转化为活性带负电的硼酸酯。“人们可以通过选择分子其余部分的取代基来轻松调整每种物质的含量，”他说。现在的希望是，可以开发出更多基于硼的化合物来治疗寄生虫疾病。Santos说，Anacor的化合物库包含其他靶点的命中，还有几种化合物正在临床试验中。苯并恶唑硼类化合物似乎特别有效，因为环状支架增加了药物在体内的半衰期。总的来说，Jacobs说硼化合物具有很大的潜力，“剩下的只是药物化学领域的创造力和探索的决心。”（背景延伸：苯并恶唑硼类化合物的环状结构能够提高药物的代谢稳定性，从而延长其在体内的作用时间，这对于提高药物疗效和减少给药频率具有重要意义。）返回搜狐，查看更多

2026-03-23

·清华全球发展与健康传播中心

健康与发展前沿第122期 | 儿童死亡率下降趋缓，多数死亡本可避免（2026年3月第4期）

本期目录一、重点事件 ●儿童死亡率下降趋缓，多数死亡本可避免 Child Mortality Progress Slows Despite Preventable Deaths ●英国在大幅预算削减背景下调整援助战略 UK Shifts Aid Strategy Amid Deep Budget Cuts ●美国麻疹病例激增，麻疹消除状态受威胁 US Measles Cases Surge, Threatening Elimination Status ●亚洲开发银行超额完成粮食安全目标并启动扩展战略 Asian Development Bank Surpasses Food Security Target, Launches Expanded Strategy ●阿根廷完成退出世界卫生组织程序 Argentina Completes Withdrawal from WHO ● 非洲诊所卫生条件不足加剧孕产妇败血症风险 Poor Sanitation in Clinics Drives Maternal Sepsis Risk in Africa 二、重点领域环境/气候 ●气温上升或抑制体育活动，并增加健康负担 Rising Heat May Reduce Physical Activity and Increase Health Burden 粮食/农村发展/贫困 ●世界粮食计划署警告：中东冲突或将致饥饿人口创历史新高 WFP Warns Middle East Conflict Could Push Hunger to Record Levels 传染病观察 ●欧洲批准单剂治疗昏睡病新药 Single-Dose Sleeping Sickness Treatment Approved in Europe ●斯威士兰推出长效艾滋病预防药物来那卡帕韦（Lenacapavir） Eswatini Rolls Out Long-Acting HIV Prevention Drug Lenacapavir ●非洲领导人在非盟峰会上警告疟疾资金危机 African Leaders Warn of Malaria Funding Crisis at AU Summit 非传染性疾病 ●英国研究人员探索智能凝胶技术用于精准药物递送 UK Researchers Explore Smart Gel Technology for Precision Drug Delivery 疫苗开发和交付 ●研究证实新型脑膜炎疫苗在非洲大规模接种中的安全性 Study Confirms Safety of New Meningitis Vaccine at Scale in Africa ●SK生物科学获新资金推进RSV抗体候选产品研发 SK Bioscience Advances RSV Antibody Candidate with New Funding 三、活动预告 ●3月24日：世界防治结核病日 March 24: World TB Day 2026 ●3月26日：应对抗疟药耐药性挑战 March 26: Staying Ahead of Antimalarial Drug Resistance ●4月5-7日：同一健康峰会 April 5–7: One Health Summit ●4月13-18日：世界银行春季会议(美国华盛顿特区) April 13-18: World Bank Group/IMF Annual Spring Meeting 一、重点事件 ●儿童死亡率下降趋缓，多数死亡本可避免 3月18日，联合国发布最新估计显示，2024年全球共有490万名儿童在五岁前死亡，其中包括230万名新生儿，大多数死亡本可通过低成本干预措施和获得优质医疗服务避免。尽管自2000年以来五岁以下儿童死亡率已下降超过一半，但自2015年以来降幅明显放缓（超过60%），对实现2030年终止可预防儿童死亡的目标构成威胁。撒哈拉以南非洲和南亚仍是负担最重地区，新生儿死亡占总数近一半；主要死因包括早产、肺炎、分娩并发症、疟疾及其他传染病。严重急性营养不良直接导致约10万人死亡，主要集中在巴基斯坦、索马里和苏丹，并间接造成更多死亡。报告警告称，尽管大量证据表明，持续投资于疫苗、营养以及专业助产服务，能够带来显著的健康和经济回报，但全球资金转移和援助削减正使孕产妇和儿童健康项目面临压力。[1] ●英国在大幅预算削减背景下调整援助战略 3月20日，英国在削减援助预算的背景下公布新的发展优先事项，官员称此举标志着从“捐助方”向“投资方”的“根本性”转变。根据这一为期三年的计划，到2029年，70%的区域性援助将重新配置到脆弱和受冲突影响国家。与此同时，将大幅削减双边援助，尤其是在非洲地区，相关资金预计将大幅下降。这一调整属于超过60亿英镑整体削减的一部分，与国防支出增加相关。英国同时重申将继续支持全球疫苗免疫联盟（Gavi）和抗击艾滋病、结核病和疟疾全球基金（Global Fund），但将终止对全球根除脊髓灰质炎行动倡议和“大流行基金”的资助。官员表示，这些调整体现出向世界银行和非洲开发银行等多边渠道倾斜的战略方向，多家援助机构则警告，此类削减可能带来显著的全球性影响。[2] ●美国麻疹病例激增，麻疹消除状态受威胁 3月20日，美国疾病控制与预防中心（CDC）报告称，美国麻疹病例已升至1,487例，新增确诊病例125例，预计在夏季前将超过去年全年水平。2025年报告病例数达2,285例，为1991年以来最高记录。官员警告称，在今年晚些时候的正式评估中，美国可能失去其自2000年实现的麻疹消除状态。[3] ●亚洲开发银行超额完成粮食安全承诺并启动扩展战略 3月17日，亚洲开发银行宣布，已超额完成其在2022—2025年间为提升亚洲及太平洋地区粮食安全所作的140亿美元承诺，并正推进一项到2030年总规模达400亿美元的新议程。该战略标志着由以农业为主的支持模式，向更加综合的粮食体系路径转型。亚洲开发银行同时公布多项新的合作安排，包括计划在2026年亚洲及太平洋粮食系统论坛上与“AIM for Scale”倡议达成合作，并与盖茨基金会及阿联酋携手，扩大面向农民和牧民的气象咨询服务及数字化工具应用。[4] ●阿根廷完成退出世界卫生组织程序 3月17日，阿根廷外交部长表示，阿根廷已正式完成退出世界卫生组织（WHO）的相关程序，此举紧随美国此前的类似决定。阿根廷政府早在一年前即宣布有意退出这一联合国卫生机构，理由是对其在新冠疫情应对中的表现存在关切。根据相关国际协议，阿根廷已在规定期限内完成全部退出流程。[5] ●非洲诊所卫生条件不足加剧孕产妇败血症风险 3月18日，水援助组织（WaterAid）发布报告指出，在撒哈拉以南非洲，约每九名分娩女性中就有一人罹患危及生命的孕产妇败血症，主要与产科医疗机构供水与卫生条件不足有关。该评估覆盖10个国家的医疗机构，结果显示，65%的机构缺乏基本清洁设施，66%无法提供洗手所需的清洁用水或肥皂，近80%的机构缺乏可正常使用的厕所。赞比亚情况最为严重，98.8%的诊所缺乏基本卫生设施，其次为加纳和马拉维，凸显孕产妇健康基础设施仍存在显著短板。[6] 二、重点领域环境/气候 ●气温上升或抑制体育活动，并增加健康负担 3月17日，《柳叶刀·全球健康》发表的一项研究指出，随着全球气温持续升高，户外体育活动将变得更加困难和危险，至2050年每年可能因此导致超过50万人死亡。目前，全球约三分之一的成年人未达到世界卫生组织推荐的每周运动量，由此增加2型糖尿病、心血管疾病及部分癌症的风险，约占全球成年死亡的5%。研究进一步发现，当月平均气温超过27.8℃时，每增加一个这样的月份，全球身体活动不足比例可能上升约1.5个百分点，在低收入和中等收入国家可达1.85个百分点。[7] 粮食/农村发展/贫困 ● 世界粮食计划署警告：中东冲突或致饥饿人口创历史新高 3月17日，世界粮食计划署（WFP）警告称，如果中东冲突持续加剧并扰乱全球经济，2026年全球饥饿人口可能达到历史新高。最新分析显示，如果冲突持续且油价维持在每桶100美元以上，可能新增4500万人陷入严重粮食不安全状况，使该群体总规模在现有3.18亿人的基础上进一步扩大——这一数字在过去五年中已增长约三倍。自2月底以来，航运通道受阻已导致粮食援助交付延误。报告指出，撒哈拉以南非洲和亚洲由于对粮食和燃料进口依赖度较高，面临的风险尤为突出。[8] 传染病观察 ● 欧洲批准单剂治疗昏睡病新药 3月16日，美国国家公共广播电台（NPR）报道，欧洲药品管理局已批准新药阿科齐硼罗（acoziborole），用于治疗昏睡病（又称非洲人类锥虫病）。这是首个单剂疗法，预计最早将于2027年投入使用。该药物由被忽视疾病药物研发倡议组织（DNDi）与赛诺菲合作开发，并获得包括盖茨基金会在内的多方资助支持。与现有治疗相比，acoziborole可避免部分严重副作用，有望提高患者的治疗可及性和依从性。目前，刚果民主共和国卫生部门和世界卫生组织正对该药进行评估，以决定是否纳入相关治疗指南，但资金不足仍可能制约其在高负担地区的推广应用。[9] ● 斯威士兰推出长效艾滋病预防药物来那帕韦（Lenacapavir） 3月17日，斯威士兰宣布开始推广长效艾滋病预防药物来那帕韦（Lenacapavir），自去年12月以来，已有约2000人接受该注射。由此，斯威士兰成为继美国及其他七个非洲高负担国家之后，引入该药物的国家之一。该国国家艾滋病防治项目官员表示，初期需求强劲，首批供应几乎已用尽。尽管取得显著进展，自2010年以来新增艾滋病毒感染已大幅下降，但患病率仍然较高，在15至49岁人群中，约每四人中就有一人感染艾滋病毒。[10] ●非洲领导人在非盟峰会上警告疟疾资金危机 3月18日，在埃塞俄比亚首都亚的斯亚贝巴举行的第39届非洲联盟（AU）峰会上，随着《2025年非洲联盟疟疾进展报告》的发布，非洲多国领导人就疟疾防控面临的日益严重的资金短缺表达紧急关切。该报告显示，非洲大陆疟疾防控进展停滞，国际资助下降，相关威胁加剧，而全球97%的疟疾死亡发生在非洲。在“非盟催化框架”下，旨在到2030年终结艾滋病、结核病并消除疟疾，目前仅有5个国家达到阶段性目标。与会领导人警告，若资金再减少30%，可能新增约1.46亿例疟疾病例，并导致近40万人死亡，其中绝大多数为5岁以下儿童。[11] 非传染性疾病 ●英国研究人员探索智能凝胶技术用于精准药物递送 3月19日，《经济时报》报道，谢菲尔德大学启动了一项为期三年、经费达100万英镑的研究项目，旨在利用创新的智能凝胶技术改进脑癌及皮肤疾病的药物递送方式。该研究将冷大气等离子体（Cold Atmospheric Plasma，CAP）与分子印迹技术相结合，探索针对胶质母细胞瘤、自身免疫性疾病及侵袭性真菌感染的靶向治疗方案。研究的关键在于构建能够协同整合CAP与药物递送系统的平台，从而在病灶部位实现可控、精准的局部给药。这一技术路径有望在提高疗效的同时减少全身性副作用，但其跨学科集成难度仍构成主要技术瓶颈。[12] 疫苗开发和交付 ●研究证实新型脑膜炎疫苗在非洲大规模接种中的安全性 3月18日，全球疫苗免疫联盟（Gavi）发布报告称，新型五价脑膜炎球菌疫苗Men5CV在大规模接种中显示出良好的安全性。该结论来自其推广过程中开展的首个真实世界安全性研究。研究基于2024年在尼日利亚和尼日尔实施的疫情应对接种行动，覆盖超过480万人，结果与既往临床试验一致。相关发现为各国扩大该疫苗的应用提供了有力支持。脑膜炎是一种进展迅速的细菌感染，可在数小时内导致严重残疾甚至死亡。[13] ●SK生物科学获新资金推进RSV抗体候选产品研发 3月18日，SK生物科学宣布获得全球健康技术研究投资基金会（Research Investment for Global Health Technology Foundation）资助，用于推进RSM01的临床开发，RSM01是一种用于预防呼吸道合胞病毒（RSV）感染的单克隆抗体候选产品。此前，该项目已获得盖茨医学研究所（由盖茨基金会支持的非营利机构）的授权。RSM01最初由Adimab与盖茨医学研究所联合开发，后者还完成了该产品的早期研究和Ⅰa期临床试验。[14] 三、活动预告 ➢ 3月24日：世界防治结核病日 2026年世界防治结核病日以“是的！我们能够终结结核病！”为主题，强调通过强有力的国家领导、增加国内和国际投资、加快采纳世界卫生组织的建议与创新措施、并通过有效的多部门协作，来扭转结核病流行趋势。[15] ➢ 3月26日：应对抗疟药耐药性挑战本次由国际适宜卫生科技组织（PATH）主办的线上论坛，邀请来自世界抗疟药耐药性网络（WWARN）、疟疾药物研发伙伴关系（MMV）以及 Jhpiego 的专家，共同探讨在耐药性不断加剧的背景下，如何维持以青蒿素为基础的联合疗法（ACTs）的疗效这一紧迫挑战。会议将评估当前耐药趋势，并重点探讨 STOP-AMDR 项目如何通过推动协同策略、优化诊断工具和支持政策制定，巩固数十年来在疟疾防控领域取得的成果。注册链接见此。[16] ➢ 4月5-7日：同一健康峰会值世界卫生日之际，法国将在里昂举办“同一健康峰会”（One Health Summit），召集各国元首、政策制定者、科学家以及民间社会代表，共同推动在人类健康、动物健康和生态系统健康之间的协同行动。会议讨论将聚焦疾病的主要驱动因素，包括人畜共患病威胁、抗微生物耐药性、可持续粮食体系以及环境污染问题，并为法国2026年担任七国集团（G7）主席国积聚势头。[17] ➢ 4月13-18日：世界银行春季会议（美国华盛顿特区）世界银行集团与国际货币基金组织（IMF）春季会议将在华盛顿特区举行。将召开发展委员会和国际货币与金融委员会会议，审议两大机构的工作进展。届时各国政府官员、机构负责人及政策制定者将与会，重点讨论新的气候融资目标、债务问题以及其他全球关键议题。[18] Sources： [1]https://www.theguardian.com/global-development/2026/mar/18/millions-children-worldwide-dying-preventable-causes-under-five-report;https://www.who.int/news/item/18-03-2026-progress-in-reducing-child-deaths-slows-as-4.9-million-children-die-before-age-five [2]https://www.theguardian.com/global-development/2026/mar/19/poorest-countries-lose-uk-aid-56-per-cent-budget-cut; https://www.devex.com/news/uk-lays-out-the-development-priorities-of-a-shrinking-aid-budget-112118 [3]https://www.cidrap.umn.edu/measles/us-measles-outbreak-approaches-1500-cases [4]https://www.devdiscourse.com/article/business/3841006-adb-surpasses-14-billion-food-security-commitment-to-transform-asias-food-systems [5]https://www.rfi.fr/en/international-news/20260317-argentina-withdraws-from-world-health-organization [6]https://www.telegraph.co.uk/global-health/women-and-girls/one-in-nine-african-mothers-will-face-life-threatening-seps/ [7]https://www.telegraph.co.uk/global-health/climate-and-people/rising-global-temperatures-eroding-ability-to-exercise/ [8]https://www.wfp.org/news/wfp-projects-food-insecurity-could-reach-record-levels-result-middle-east-escalation;https://www.nytimes.com/2026/03/17/world/middleeast/iran-strikes-hunger-record-levels.html [9]https://www.npr.org/2026/03/16/g-s1-113246/sleeping-sickness-drug-treatment-tsetse-fly [10] https://www.reuters.com/business/healthcare-pharmaceuticals/eswatini-starts-administering-lenacapavir-curb-spread-hiv-2026-03-17/ [11] https://healthwise.punchng.com/malaria-resurgence-feared-as-africa-faces-funding-decline/ [12] https://health.economictimes.indiatimes.com/news/industry/brain-tumours-take-control-of-sugar-metabolism-to-grow-study-suggests/129653787 [13] https://www.gavi.org/vaccineswork/new-vaccine-stop-deadly-meningitis-epidemics-confirmed-be-safe [14] https://www.koreaherald.com/article/10697174[15]https://www.who.int/campaigns/world-tb-day/2026 [16]https://path.zoom.us/webinar/register/WN_Ne8FoQvcTru4D5aEt2OLJw#/registration [17]https://oneplanetsummit.fr/en/events-16/one-health-summit-305 [18]https://www.worldbank.org/en/meetings/splash/about *图片均来源于网络，如有侵权，请联系删除。

100 项与 Acoziborole 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Acoziborole	-	DB13086

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
布氏锥虫感染	申请上市	欧盟	Sanofi	2026-02-27
布氏锥虫感染	申请上市	欧盟	DNDi Japan	2026-02-27
肝素诱导血小板减少	临床3期	几内亚	Drugs for Neglected Diseases initiative	2021-12-30
肝素诱导血小板减少	临床3期	刚果共和国	Drugs for Neglected Diseases initiative	2021-12-30
非洲锥虫病	临床3期	刚果民主共和国	Drugs for Neglected Diseases initiative	2016-10-11
非洲锥虫病	临床3期	几内亚	Drugs for Neglected Diseases initiative	2016-10-11

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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


NCT03087955 (OXA002, CTgov)	临床2/3期	非洲锥虫病	208	Acoziborole (Late-stage HAT)	鑰襯憲廠膚獵顧醖簾遞 = 糧鑰網餘壓鑰鏇選顧構鏇壓網壓鹽獵簾選鑰選 (夢鑰積積選醖衊窪壓壓, 顧蓋襯積餘齋網鹽積鏇 ~ 廠製觸醖顧遞構範遞觸) 更多	-	2025-09-17
NCT03087955 (OXA002, CTgov)	临床2/3期	非洲锥虫病	208	Acoziborole (Early- and Intermediate-stage HAT)	餘壓醖夢構積鏇蓋糧夢 = 鹹築襯遞衊鹽憲夢齋糧顧願構遞鹹膚願簾壓鏇 (鹹構鑰淵艱繭鏇襯窪築, 壓餘繭遞選餘鹹築觸淵 ~ 鏇醖糧蓋範鹹醖鹹獵範) 更多	-	2025-09-17
NCT05256017 (OXA004, CTgov)	临床2/3期	布氏锥虫感染 \| 非洲锥虫病 \| 肝素诱导血小板减少	1,208	Acoziborole (Acoziborole)	廠衊衊繭膚鏇範顧願鬱 = 觸蓋鏇鑰遞製襯艱糧鏇淵鑰構壓艱繭憲廠繭繭 (衊壓鹹衊願構鹽範鏇糧, 壓鹹選構製獵蓋觸遞觸 ~ 網願襯鹽築觸壓壓鑰獵) 更多	-	2025-03-20
NCT05256017 (OXA004, CTgov)	临床2/3期	布氏锥虫感染 \| 非洲锥虫病 \| 肝素诱导血小板减少	1,208	Placebo (Placebo)	廠衊衊繭膚鏇範顧願鬱 = 製衊壓夢鑰衊觸艱願衊淵鑰構壓艱繭憲廠繭繭 (衊壓鹹衊願構鹽範鏇糧, 憲淵獵鹽網繭鑰製築膚 ~ 獵艱糧齋窪餘鬱鏇簾網) 更多	-	2025-03-20
NCT01533961 (Pubmed \| Clin Pharmacokinet)	临床1期	非洲锥虫病	128	Acoziborole 960mg	壓構網餘鹽糧遞艱積餘(淵襯簾齋憲艱願憲製壓) = appeared rapidly in plasma (at 1 h), reached tmax between 24 and 72 h, and remained stable for up to 96 h, after which a slow decrease was quantifiable until 14 weeks after dosing 膚鏇鏇鏇鏇鏇遞齋築顧 (鏇築遞夢鏇蓋窪憲壓積 ) 更多	积极	2023-03-01
NCT03087955 (Pubmed) 人工标引	临床2/3期	非洲锥虫病	208	Acoziborole	廠製遞膚糧餘願遞憲鏇(構鹽構繭網鑰構窪網夢) = 淵憲鬱襯築願構壓餘膚膚膚衊夢遞觸觸鏇糧膚 (壓獵網鹽糧憲築齋夢顧, 91.2 ~ 97.7) 更多	积极	2022-11-29