青蒿琥酯/盐酸甲氟喹(Artesunate/Mefloquine Hydrochloride) - 药物靶点：ATP2A1 x SERCA2_在研适应症：恶性疟，疟疾_专利_临床

概要

基本信息

药物类型

小分子化药

别名

AS/MQ、ASMQ、ASMQ FDC

+ [6]

靶点

ATP2A1 x SERCA2

作用方式

抑制剂

作用机制

ATP2A1抑制剂(肌浆网/内质网钙ATP酶-1抑制剂)、SERCA2抑制剂(肌浆网/内质网钙ATP酶-2抑制剂)

治疗领域

感染

在研适应症

恶性疟疟疾

非在研适应症-

原研机构

Fundação Oswaldo Cruz

在研机构

Fundação Oswaldo Cruz

非在研机构-

最高研发阶段批准上市

首次获批日期

巴西 (2008-01-01),

疟疾

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C17H17ClF6N2O

InChIKeyWESWYMRNZNDGBX-YLCXCWDSSA-N

CAS号51773-92-3

关联

22

项与青蒿琥酯/盐酸甲氟喹相关的临床试验

NCT03939104

/ Completed临床3期IIT

A Multi-centre Randomised Controlled Non-inferiority Trial to Compare the Efficacy, Safety and Tolerability of Triple Artemisinin-based Combination Therapies Versus First-line ACTs + Placebo for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Asia

A partially blinded randomised controlled non-inferiority trial comparing the efficacy, tolerability and safety of Triple ACTs artemether-lumefantrine + amodiaquine (AL+AQ) and artesunate- mefloquine+piperaquine (AS-MQ+PPQ) with the ACTs artemether-lumefantrine + placebo (AL+PBO) and artesunate- mefloquine + placebo (AS-MQ+PBO) (with single-low dose primaquine in some sites) for the treatment of uncomplicated Plasmodium falciparum malaria to assess and compare their efficacy, safety, tolerability.

开始日期2021-06-30

申办/合作机构

University of Oxford

NCT03923725

/ Recruiting临床3期IIT

A Multi-centre Randomised Controlled Non-inferiority Trial to Compare the Efficacy, Safety and Tolerability of Triple Artemisinin-based Combination Therapies Versus First-line ACTs + Placebo for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Africa

A partially blinded randomised controlled non-inferiority trial comparing the efficacy, tolerability and safety of Triple ACTs artemether-lumefantrine+amodiaquine (AL+AQ) and artesunate-mefloquine+piperaquine (ASMQ+PPQ) and the ACTs artemether-lumefantrine+placebo (AL+PBO), artesunate-mefloquine+placebo (ASMQ+PBO) (with single-low dose primaquine in some sites) for the treatment of uncomplicated Plasmodium falciparum malaria to assess and compare their efficacy, safety, tolerability.

开始日期2020-09-01

申办/合作机构

University of Oxford

ACTRN12622000638730

/ Suspended临床2/3期IIT

Clinical and parasitological efficacy of artesunate-amodiaquine over 28 days in the treatment of uncomplicated falciparum malaria in Cambodia

开始日期2020-06-01

申办/合作机构

National Center for Parasitology, Entomology and Malaria Control

100 项与青蒿琥酯/盐酸甲氟喹相关的临床结果

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100 项与青蒿琥酯/盐酸甲氟喹相关的转化医学

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100 项与青蒿琥酯/盐酸甲氟喹相关的专利（医药）

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246

项与青蒿琥酯/盐酸甲氟喹相关的文献（医药）

2024-02-01·Transactions of the Royal Society of Tropical Medicine and Hygiene

Artesunate-mefloquine therapy for uncomplicated Plasmodium falciparum malaria: an updated systematic review and meta-analysis of efficacy and safety

Review

作者: Peixoto, Henry Maia ; Pereira, Ana Carolina Esteves da Silva ; de Freitas, Beatriz Sales ; Fernandes, Gabriel Haiek

AbstractTo provide a continuous update on the safety and efficacy of artesunate-mefloquine (ASMQ) compared with other artemisinin combination therapy (ACT) schemes used in the treatment of uncomplicated malaria caused by Plasmodium falciparum, this study updated and expanded the results of the systematic literature review published in 2016. Only randomised controlled clinical trials published from 1 January 2001 to 12 June 2023 from five databases were included in this study. The results related to efficacy, expressed through RR, were summarized in meta-analyses, performed according to the compared ACTs and with the intention-to-treat and per-protocol analyses. The results related to safety were synthesized in a descriptive manner. Thirty-two studies were included, of which 24 had been analysed in the 2016 review and eight new ones were added. Although the methodological quality of most studies was considered moderate, the body of evidence gathered indicates that ASMQ continues to be safe and effective for the treatment of uncomplicated infections caused by P. falciparum compared with other ACTs. However, the inclusion of two new studies, which identified failure rates exceeding 10%, suggests a possible reduction in the efficacy of ASMQ in the analysed locations. The incidence of serious adverse effects, such as seizure, encephalopathy and cardiac arrhythmia, was infrequent in both the ASMQ group and the comparison groups. After including new evidence, ASMQ is still recommended as a first-line treatment of uncomplicated malaria caused by P. falciparum, although local aspects need to be considered.

2024-01-01·Life Science Alliance

APR-246 increases tumor antigenicity independent of p53

Article

作者: Zappasodi, Roberta ; Merghoub, Taha ; Zhong, Hong ; Ouerfelli, Ouathek ; George, Mariam M ; Stockwell, Brent R ; Thach, Daniel ; Zamarin, Dmitriy ; Venkatesh, Divya ; Liu, Cailian ; Wolchok, Jedd D ; Budhu, Sadna ; Liu, Hengrui ; Yao, Zhong-Ke ; Campesato, Luis Felipe ; Michels, Judith

We previously reported that activation of p53 by APR-246 reprograms tumor-associated macrophages to overcome immune checkpoint blockade resistance. Here, we demonstrate that APR-246 and its active moiety, methylene quinuclidinone (MQ) can enhance the immunogenicity of tumor cells directly. MQ treatment of murine B16F10 melanoma cells promoted activation of melanoma-specific CD8+T cells and increased the efficacy of a tumor cell vaccine using MQ-treated cells even when the B16F10 cells lacked p53. We then designed a novel combination of APR-246 with the TLR-4 agonist, monophosphoryl lipid A, and a CD40 agonist to further enhance these immunogenic effects and demonstrated a significant antitumor response. We propose that the immunogenic effect of MQ can be linked to its thiol-reactive alkylating ability as we observed similar immunogenic effects with the broad-spectrum cysteine-reactive compound, iodoacetamide. Our results thus indicate that combination of APR-246 with immunomodulatory agents may elicit effective antitumor immune response irrespective of the tumor’s p53 mutation status.

2023-11-01·The Journal of Clinical Hypertension

Muscle quality is negatively related to hypertension prevalence in adults: Results from NHANES 2011–2014

Article

作者: Zhu, Caiyan ; Bai, Xiaopeng ; Zhao, Jia ; Shi, Shuai ; Wang, Yufeng

AbstractResistance training could counter hypertension and improve muscle quality (MQ), but current evidence about the correlation between MQ and hypertension is limited. The authors aimed to explore this correlation using the data of participants aged 20–59 from NHANES 2011–2014 via a cross‐sectional study. The MQ was quantified as handgrip strength (kg)/lean soft tissue mass (kg) of the dominant arm. Weighted multivariate logistic regression models were mainly utilized to investigate the MQ—hypertension association; linear trend tests and subgroup analysis were also conducted. Moreover, the authors employed weighted multivariate linear regression models to uncover the association between blood pressure (BP) and MQ. Four thousand four hundred and sixty‐nine individuals were enrolled, and 1167 were hypertensive. Hypertensive participants had a lower MQ than normotensive participants. In the totally adjusted model, each unit elevation in MQ was related to a 7% reduction in hypertension prevalence (p =.002). There was a decreasing trend in hypertension prevalence and in systolic BP as the MQ increased from the bottom to the top quartile across all three models (p for trend ≤.01), with a 28% difference (OR: 0.72, 95% CI: 0.54, 0.95) in hypertension prevalence and a 1.88 mm Hg (95% CI: −3.56, −0.20) difference in SBP between the top and bottom quartiles in the fully adjusted model. Subgroup analysis further confirmed the MQ—hypertension inverse association. In conclusions, the MQ was negatively associated with hypertension prevalence and systolic BP, which suggests the MQ may be a protective factor for hypertension and need to be improved.

100 项与青蒿琥酯/盐酸甲氟喹相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	P01B	-

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
恶性疟	巴西	-	2008-05-08
疟疾	巴西	Fundação Oswaldo Cruz	2008-01-01

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
恶性疟	药物发现	塞内加尔	-	-
恶性疟	药物发现	几内亚	-	-
恶性疟	药物发现	马拉维	-	-
恶性疟	药物发现	贝宁	-	-
恶性疟	药物发现	印尼	-	-
恶性疟	药物发现	菲律宾	-	-
恶性疟	药物发现	科特迪瓦	-	-
恶性疟	药物发现	巴布亚新几内亚独立国	-	-
恶性疟	药物发现	乍得共和国	-	-
恶性疟	药物发现	肯尼亚	-	-

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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


NCT01708876 (Pubmed \| Clin Infect Dis)	临床3期	间日疟原虫感染	103	Chloroquine	(膚願觸範糧醖壓鏇構築) = 衊壓壓網淵窪觸壓鹹夢憲夢醖糧簾製衊簾糧餘 (願觸繭窪築憲蓋鹽糧築, 46.8 ~ 75.6) 更多	-	2016-06-01
				Artesunate-mefloquine	夢範遞鹹鹹積廠衊膚鏇(糧壓蓋鏇顧鬱艱獵艱鏇) = 膚繭觸衊齋鹹繭願築繭遞憲齋繭遞遞鹽鹹鏇築 (願膚蓋淵餘簾餘鬱築網 ) 更多
NCT01708876 (ACT KNOW, Pubmed \| Lancet Infect Dis)	临床3期	诺氏疟原虫感染	252	Artesunate-mefloquine	鬱簾淵夢範網艱構餘鏇(鹽艱鏇簾願鑰醖鹹壓廠) = 顧鏇鬱廠窪齋醖願糧襯壓觸醖鑰淵憲鑰壓選襯 (選積壓願製鬱鏇窪膚膚 ) 更多	-	2016-02-01
				Chloroquine	鬱簾淵夢範網艱構餘鏇(鹽艱鏇簾願鑰醖鹹壓廠) = 簾艱襯齋繭鑰願網艱構壓觸醖鑰淵憲鑰壓選襯 (選積壓願製鬱鏇窪膚膚 ) 更多
NCT00373607 (Pubmed)	临床3期	恶性疟一线	522	mefloquine-artesunate	簾顧廠衊糧糧鑰醖簾夢(衊餘鬱構餘願選蓋憲積) = 齋餘網鹽願鑰膚鏇艱範鑰鹹顧願遞觸艱廠壓觸 (遞膚廠夢齋鏇選範壓網 ) 更多	-	2007-10-31
				dihydroartemisinin-piperaquine	簾顧廠衊糧糧鑰醖簾夢(衊餘鬱構餘願選蓋憲積) = 簾選醖襯壓遞夢憲廠鹽鑰鹹顧願遞觸艱廠壓觸 (遞膚廠夢齋鏇選範壓網 ) 更多