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-

权益机构-

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

23

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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77

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·Nature Medicine1区 · 医学

Antimalarial artesunate–mefloquine versus praziquantel in African children with schistosomiasis: an open-label, randomized controlled trial

1区 · 医学

Article

作者: Cissé, Badara ; Potters, Idzi ; Mbodj, Ousmane Thiam ; Mbow, Moustapha ; Paredis, Linda ; Smekens, Bart ; Faye, Babacar Thiendella ; Tsoumanis, Achilleas ; Van Herrewege, Yven ; Brosius, Isabel ; Rosanas-Urgell, Anna ; Bottieau, Emmanuel ; De Hondt, Annelies ; Mboup, Souleymane ; Burm, Christophe ; Gueye, Cheikh Tidiane ; Arango, Diana ; Polman, Katja ; Roucher, Clémentine ; Richter, Joachim

AbstractSchistosomiasis treatment entirely relies on a single drug, praziquantel, prompting research into alternative therapeutics. Here we evaluated the efficacy and safety of the antimalarial combination artesunate–mefloquine for the treatment of schistosomiasis in a proof-of-concept, pragmatic, open-label, randomized controlled trial in primary schools of six villages endemic for schistosomiasis in northern Senegal. Children (6–14 years) were eligible if Schistosoma eggs were detected by microscopy in urine and/or stool. In total, 726 children were randomized 1:1 to praziquantel (standard care: 40 mg kg−1 single dose; n = 364) or to artesunate–mefloquine (antimalarial dosage: artesunate 4 mg kg−1 and mefloquine 8 mg kg−1 daily for three consecutive days; n = 362). Eight children not meeting the inclusion criteria were excluded from efficacy analysis. Median age of the remaining 718 participants was 9 years; 399 (55.6%) were male, and 319 (44.4%) female; 99.3% were infected with Schistosoma haematobium and 15.2% with S. mansoni. Primary outcomes were cure rate, assessed by microscopy, and frequency of drug-related adverse effects of artesunate–mefloquine versus praziquantel at 4 weeks after treatment. Cure rate was 59.6% (208/349) in the artesunate–mefloquine arm versus 62.1% (211/340) in the praziquantel arm. The difference of −2.5% (95% confidence interval (CI) −9.8 to 4.8) met the predefined criteria of noninferiority (margin set at 10%). All drug-related adverse events were mild or moderate, and reported in 28/361 children receiving artesunate–mefloquine (7.8%; 95% CI 5.4 to 11.0) versus 8/363 (2.2%; 95% CI 1.1 to 4.3) receiving praziquantel (P < 0.001). Artesunate–mefloquine at antimalarial dosage was moderately safe and noninferior to standard-care praziquantel for the treatment of schistosomiasis, predominantly due to S. haematobium. Multicentric trials in different populations and epidemiological settings are needed to confirm these findings. ClinicalTrials.gov identifier: NCT03893097.

2022-12-22·Journal of Parasitology Research

Anemia, Thrombocytopenia, and Changes in Biochemical Parameters Occurring in Patients with Uncomplicated Plasmodium falciparum Malaria: Data Analysis from Antimalarial Efficacy-Randomized Trials in Dakar and Kaolack Regions, Senegal

Article

作者: NDiaye, Jean Louis ; Gaye, Oumar ; NDiaye, Magatte ; Faye, Babacar ; Sylla, Khadime ; Lelo, Souleye ; Tine, Roger ; Abiola, Annie ; Sow, Doudou ; Folly, Kuaku ; NDiaye, Léon Amath

Background. Artemisinin-based Combination Therapies (ACTs) are widely used in the treatment of uncomplicated malaria. Plasmodium falciparum infection is often accompanied by disturbances of hematological and biochemical parameters. The objective of this study was to evaluate the changes in biochemical and hematological parameters during uncomplicated malaria in patients treated with ACTs. Methods. Data from patient with uncomplicated Plasmodium falciparum malaria were pooled from different open-randomized trial evaluating the efficacy of Artesunate-Mefloquine (ASMQ), Artesunate-Amodiaquine (ASAQ), Artemether-Lumefantrine (AL), and Dihydro-artemisinin-Piperaquine (DHAPQ) combinations. Biochemical (transaminases, creatinine, and bilirubin) and hematological (hemoglobin and platelet levels) parameters were performed at baseline (D0) and at day 7 after treatment (D7). Data were analyzed as both continuous and categorical variables with 95% confidence interval. Risks and trends were calculated using multivariate logistic random effect models. Results. A total of 720 patients with completed biological data were included in the analysis (320 in the AL arm, 160 in the ASMQ arm, 120 in the DHAPQ arm, and 88 in the ASAQ arm). The mean age of the patients was

9.43 \pm 9.1

years. Male subjects represented 58.47% (sex ratio was 1.4 for males). The mean hemoglobin level at inclusion (D0) was 9.79 g/dl and anemia (

Hb < 11 g / dl

) was 71.43% (

aOR = 1.16 [0.68 - 1.98]

p = 0.57

). At D7, hemoglobin level was 9.63 g/dl and anemia was significantly more frequent (78.29% [

p = 0.002

]). The mean platelet count at day 0 was 154075.5 platelets/mm3 of blood and 339328.7 platelets/mm3 at day 7. Thrombocytopenia was about 53.61% and was associated with malaria (

aOR = 3.4 [2.18 - 5.3]

p < 10^{- 3}

). 19.58% of patients had abnormal ALT and 40.28% had abnormal AST at D0. 27.22% of patients had normal bilirubin at D0. Renal function was normal in all patients in the study. Normalization of transaminases was noted between D0 and D7. The percentage of subjects with normal bilirubin increased between D0 and D7. Renal function did not vary significantly between D0 and D7. Conclusion. Results from this analysis showed that subjects with high parasitaemia had a greater risk of anemia and thrombocytopenia. Artemisinin combinations were well-tolerated as no major biological disturbances were noted. The effects of ACTs on hematologic and biochemical parameters were not different.

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	菲律宾	-	-
恶性疟	药物发现	科特迪瓦	-	-
恶性疟	药物发现	老挝	-	-
恶性疟	药物发现	乍得共和国	-	-
恶性疟	药物发现	多哥	-	-
恶性疟	药物发现	肯尼亚	-	-
恶性疟	药物发现	几内亚	-	-
恶性疟	药物发现	印尼	-	-
恶性疟	药物发现	马里	-	-
恶性疟	药物发现	马拉维	-	-

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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


NCT03893097 (SchistoSAM, Pubmed \| Nat Med) 人工标引	临床3期	血吸虫病	718	Praziquantel	餘顧築遞蓋齋鏇簾糧襯(蓋獵網構鏇鏇範顧顧蓋) = 廠襯艱遞遞願鹹襯鑰糧窪積網簾淵餘鏇願鏇鹹 (觸觸憲顧顧網窪鑰觸壓 ) 更多	非劣	2024-01-01
				Artesunate-mefloquine	餘顧築遞蓋齋鏇簾糧襯(蓋獵網構鏇鏇範顧顧蓋) = 鹽選餘鏇憲鹽構夢鹹鑰窪積網簾淵餘鏇願鏇鹹 (觸觸憲顧顧網窪鑰觸壓 ) 更多
NCT01708876 (Pubmed \| Clin Infect Dis)	临床3期	间日疟原虫感染	103	Chloroquine	(鹽夢願網齋觸遞鑰製觸) = 遞選獵顧襯範蓋淵廠觸獵網鏇鏇糧願糧衊襯夢 (壓憲鏇壓夢糧襯鑰鬱襯, 46.8 ~ 75.6) 更多	-	2016-06-01
				Artesunate-mefloquine	蓋網窪夢觸鑰積鹽醖築(鹹蓋選衊廠獵衊廠鹽衊) = 餘遞廠廠積廠築醖蓋選簾鏇構築遞鑰鹽獵願餘 (壓蓋積網網鬱艱鑰製窪 ) 更多
NCT01708876 (ACT KNOW, Pubmed \| Lancet Infect Dis)	临床3期	诺氏疟原虫感染	252	Artesunate-mefloquine	積醖糧餘顧蓋壓築鏇衊(選觸醖繭繭鑰蓋製選鹽) = 鹹鏇襯餘構衊構襯鬱簾繭蓋簾壓顧壓鹹獵壓鏇 (襯繭獵遞願鑰築製簾鏇 ) 更多	-	2016-02-01
				Chloroquine	積醖糧餘顧蓋壓築鏇衊(選觸醖繭繭鑰蓋製選鹽) = 鹹獵構觸壓鹽窪壓繭獵繭蓋簾壓顧壓鹹獵壓鏇 (襯繭獵遞願鑰築製簾鏇 ) 更多
NCT00373607 (Pubmed)	临床3期	恶性疟一线	522	mefloquine-artesunate	構積淵襯顧顧淵遞顧淵(製獵築淵鏇鹹網艱淵鹹) = 顧構膚選衊鬱艱鏇範網壓窪齋積鹽遞願鏇遞選 (齋蓋廠壓獵鏇製糧艱繭 ) 更多	-	2007-10-31
				dihydroartemisinin-piperaquine	構積淵襯顧顧淵遞顧淵(製獵築淵鏇鹹網艱淵鹹) = 膚糧積遞遞壓積範顧築壓窪齋積鹽遞願鏇遞選 (齋蓋廠壓獵鏇製糧艱繭 ) 更多