复方磷酸萘酚喹(Artemisinin/Naphthoquine phosphate) - 在研适应症：恶性疟_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Compound Naphthoquine Phosphate、青蒿素/磷酸萘酚喹、Arco

靶点-

作用机制-

治疗领域

感染

在研适应症

恶性疟

非在研适应症-

原研机构

昆药集团股份有限公司

在研机构

昆药集团股份有限公司

非在研机构-

最高研发阶段批准上市

首次获批日期

中国 (2005-01-26),

恶性疟

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C24H34ClN3O9P2

InChIKeyQTYPWHKJEDCDNH-UHFFFAOYSA-N

CAS号173531-58-3

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关联

3

项与复方磷酸萘酚喹相关的临床试验

PACTR201710002665193 / SuspendedN/AIIT

Comparison Of The Efficacy Bioavailability, Safety Profile And Toxicity Of Artemisinin-Naphtoquinine-Primaquine (ArteGo) And Artemether ¿Lumefantrine In treatment of uncomplicated malaria in Lagos, Nigeria

开始日期2017-11-06

申办/合作机构-

NCT01930331 / Completed临床4期IIT

Safety, Tolerability, Pharmacokinetics and Efficacy, Phase Iv, Open Label Study of Fixed Arco® and Eurartesim® Therapies in Adults and Children With Uncomplicated P. Falciparum Malaria in Tanzania

Phase IV, single center, 2 arms randomized controlled, open label study. Study will be conducted over a period of 42 days to determine the safety, tolerability, pharmacokinetics and efficacy of ARCO.

开始日期2014-01-07

申办/合作机构

Ifakara Health Institute

ACTRN12610000913077 / Completed临床3期IIT

Efficacy of artesunate-pyronaridine and artemisinin-naphthoquine combination therapies compared with standard artemether-lumefantrine in children from Papua New Guinea with uncomplicated malaria who are monitored for recurrent malaria over 42 days post-treatment

开始日期2012-04-02

申办/合作机构

The University of Western Australia

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100 项与复方磷酸萘酚喹相关的临床结果

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100 项与复方磷酸萘酚喹相关的转化医学

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100 项与复方磷酸萘酚喹相关的专利（医药）

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27

项与复方磷酸萘酚喹相关的文献（医药）

2022-12-01·Parasites & Vectors2区 · 医学

Inhibitory effect of naphthoquine phosphate on Babesia gibsoni in vitro and Babesia rodhaini in vivo

2区 · 医学

ArticleOA

作者: Iguchi, Aiko ; Ji, Shengwei ; Galon, Eloiza May ; Zafar, Iqra ; Liu, Mingming ; Hasegawa, Yae ; Tuvshintulga, Bumduuren ; Li, Jixu ; Rizk, Mohamed Abdo ; Yokoyama, Naoaki ; Xuan, Xuenan

AbstractBackgroundDrug resistance and toxic side effects are major challenges in the treatment of babesiosis. As such, new drugs are needed to combat the emergence of drug resistance in Babesia parasites and to develop alternative treatment strategies. A combination of naphthoquine (NQ) and artemisinin is an antimalarial therapy in pharmaceutical markets. The present study repurposed NQ as a drug for the treatment of babesiosis by evaluating the anti-Babesia activity of naphthoquine phosphate (NQP) alone.MethodsAn in vitro growth inhibition assay of NQP was tested on Babesia gibsoni cultures using a SYBR Green I-based fluorescence assay. In addition, the in vivo growth inhibitory effect of NQP was evaluated using BALB/c mice infected with Babesia rodhaini. The parasitemia level and hematocrit values were monitored to determine the therapeutic efficacy of NQP and the clinical improvements in NQP-treated mice.ResultsThe half maximal inhibitory concentration of NQP against B. gibsoni in vitro was 3.3 ± 0.5 μM. Oral administration of NQP for 5 consecutive days at a dose of 40 mg/kg of body weight resulted in significant inhibition of B. rodhaini growth in mice as compared with that of the control group. All NQP-treated mice survived, whereas the mice in the control group died between days 6 and 9 post-infection.ConclusionThis is the first study to evaluate the anti-Babesia activity of NQP in vitro and in vivo. Our findings suggest that NQP is a promising drug for treating Babesia infections, and drug repurposing may provide new treatment strategies for babesiosis.Graphical Abstract

2019-08-01·Talanta

A novel and sensitive fluorescent assay for artemisinin with graphene quantum dots based on inner filter effect

Article

作者: Zhao, Xian-En ; Wang, Xiao ; Zhu, Shuyun ; Sun, Jing ; Yan, Xiaolu

The authors describe a novel method for the determination of artemisinin (ART) by using graphene quantum dots (GQDs) as the fluorescent probes. This method is based on the fact that ART can react with p-aminophenylboronic acid (p-ABA) to produce p-aminophenol (p-AP). While in the presence of tyrosinase (TYR), p-AP can be oxidized into 4-amino-1,2-benzoquinone, which effectively quenched the fluorescence of GQDs due to the inner filter effect (IFE). By making use of these reactions, a novel and sensitive fluorescent assay for ART has been developed. The calibration curve for the determination of ART is linear in the range of 0.1-5 μM and 5-55 μM with the detection limit of 33 nM, which is more sensitive than most of other methods. Some common coexisting substances including Ca²⁺, Na⁺, Mg²⁺, K⁺, PO₄^3-, starch, lactose, dextrin, and magnesium stearat have negligible effects on the fluorescence intensity of GQDs-TYR-p-ABA system. Finally, the sensing system was successfully applied to the detection of the compound naphthoquine phosphate tablet samples with satisfactory recoveries. This IFE-based GQDs fluorescence sensing strategy is facile and sensitive for the determination of ART because neither the surface modification nor the linking between the receptor and the fluorophore is required.

2019-07-01·Journal of Helminthology

Efficacy of artemisinin–naphthoquine phosphate against Schistosoma haematobium adult flukes: dose–effect relationship and tegumental alterations

Article

作者: Taman, A ; El Bardicy, S ; Ayoub, M ; El-Beshbishi, S N ; Tadros, M

AbstractSchistosoma haematobium and Schistosoma mansoni infections have broadly overlapping geographical distributions. Praziquantel is the only treatment for human schistosomiasis, so drug tolerance and/or resistance are major concerns. Artemisinin–naphthoquine phosphate (CO-ArNp), an artemisinin-based combination therapy endorsed by the World Health Organization as a gold standard therapy for malaria, has also been identified as a promising treatment for S. mansoni. In this in vitro study, we tested the effect of 1–40 μg/ml CO-ArNp on S. haematobium worms, and inspected tegumental changes by using scanning electron microscopy (SEM), aiming to determine if this combination therapy has a broad-spectrum antischistosomal activity. Incubation of S. haematobium adults with 20 or 30 μg/ml CO-ArNp caused 100% mortality of worms within 72 or 48 h, respectively. SEM examination showed extensive tegumental alterations such as oedema, constriction, shortening and loss of spines, fissuring, sloughing and perforation, resulting in exposure of the underlying basal lamina, mainly in treated male schistosomes. Besides the well-established potent efficacy, bioavailability, tolerability and safety of the antimalarial artemisinin–naphthoquine phosphate combined therapy, these results may also suggest its possible utilization as a new broad-spectrum antischistosomal agent.

100 项与复方磷酸萘酚喹相关的药物交易

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