Arterolane maleate(Arterolane maleate)

概要

基本信息

药物类型

小分子化药

别名

Arterolane、Synperoxolane、Trioxolane 7

+ [4]

靶点-

作用机制-

治疗领域

感染

在研适应症-

非在研适应症

恶性疟

原研机构

Sun Pharmaceutical Industries Ltd.

在研机构-

非在研机构

MMV Medicines for Malaria Venture

Ranbaxy Laboratories Ltd.

最高研发阶段无进展临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C26H40N2O8

InChIKeySVDSPJJUJMMDFX-FCOKHIGASA-N

CAS号959520-73-1

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关联

3

项与 Arterolane maleate 相关的临床试验

CTRI/2011/11/002129 / Completed临床3期

A phase III, open label, randomized, parallel group, multicentric trial comparing the safety and efficacy of fixed dose combination tablets of arterolane maleate and piperaquine phosphate (PQP) with chloroquine tablets in patients with acute uncomplicated Plasmodium vivax malaria

开始日期2011-10-17

申办/合作机构

Ranbaxy Laboratories Ltd.

CTRI/2009/091/000101 / Completed临床3期

A Phase III, double-blind, randomised, multicenter trial comparing the safety and efficacy of fixed dose combination tablets of arterolane maleate and piperaquine phosphate (PQP) with CoartemÂ® (artemether-lumefantrine tablets) in patients with acute uncomplicated Plasmodium falciparum malaria

开始日期2009-11-20

申办/合作机构

Ranbaxy Laboratories Ltd.

NCT00362050 / Completed临床2期IIT

A Phase II, Double-Blind, Parallel-Group, Randomized, Dose-Ranging Study Assessing the Antimalarial Activity and Safety of RBx 11160 Administered for 7 Days in Patients With Acute Uncomplicated Plasmodium Falciparum Malaria

The trial will identify the best dose of the synthetic peroxide RBx11160 to treat uncomplicated malaria. Patients will be treated over 7 days with daily doses of 50, 100 or 200 mg RBx11160.
The study is designed to assess the antimalarial activity and safety of 3 dose levels of RBx 11160 administered once daily for 7 consecutive days. The primary endpoint will be the time to 90% parasite clearance. In future regulatory studies, RBx 11160 is likely to be administered in combination with another antimalarial agent since the development plan follows the current recommendation of WHO for the treatment of uncomplicated malaria. However, it is critical to gather data on RBx 11160 when used as monotherapy in adult patients suffering from acute uncomplicated P. falciparum malaria. In malaria-endemic regions, an adult population is defined on the basis of immune status rather than the legal age of consent. Thus, patients as young as 13 years of age can be enrolled provided consent has been obtained from a legal guardian in accordance with local practices and regulations. This study will be conducted in compliance with International Conference on Harmonization (ICH) Good Clinical Practice (GCP).

开始日期2006-06-01

申办/合作机构

MMV Medicines for Malaria Venture

[+2]

100 项与 Arterolane maleate 相关的临床结果

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100 项与 Arterolane maleate 相关的转化医学

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100 项与 Arterolane maleate 相关的专利（医药）

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67

项与 Arterolane maleate 相关的文献（医药）

2022-08-30·Rapid Communications in Mass Spectrometry

Comprehensive metabolite identification study of arterolane using hydrophilic interaction liquid chromatography with quadrupole‐time‐of‐flight mass spectrometry

Article

作者: Niguram, Prakash ; Kate, Abhijeet S.

RationaleIn 2012, arterolane (ART) in combination with piperaquine received approval in India for the treatment of plasmodium‐induced malaria; however, to date, a detailed metabolite identification study of ART has not been reported. Being polar in nature, ART shows early elution on reversed‐phase columns which might be the rate‐limiting factor of its systematic analytical studies. We have utilized hydrophilic interaction liquid chromatography (HILIC) to separate in vitro and in vivo metabolites of ART.MethodsThe possible sites of metabolism were predicted by XenoSite software to obtain an initial assessment. In vitro studies were conducted by incubating the drug with liver microsomes such as human, rat and human S9 fractions. Later, in vivo studies were performed to check the metabolites in urine, faeces and plasma. The samples were pooled and subjected to the protein precipitation method before analysis by liquid chromatography/quadrupole‐time‐of‐flight mass spectrometry (LC/QTOFMS).ResultsWe have observed 15 metabolites in this study which were phase I metabolites formed due to hydroxylation, dihydroxylation, peroxide bond scission and oxidation. Here, we report 11 metabolites of ART for the first time. The metabolic pathways and plausible structures were proposed according to accurate mass measurements and its MS/MS data.ConclusionsThe present study comprehensively reports the in vitro and in vivo metabolism of ART mentioning 11 novel metabolites. Here, extensive use of HILIC has helped to efficiently separate various metabolites. These findings would help prospects of ART disposition and its congeners.

2022-02-23·Science Translational Medicine1区 · 医学

Therapeutic efficacy of antimalarial drugs targeting DosRS signaling in Mycobacterium abscessus

1区 · 医学

Article

作者: Belardinelli, Juan Manuel ; Charman, Susan A. ; Pearce, Camron ; Podell, Brendan K. ; Dartois, Véronique ; Avanzi, Charlotte ; de Moura, Vinicius C. N. ; Li, Wei ; Gonzalez-Juarrero, Mercedes ; Wiersma, Crystal J. ; Nick, Jerry A. ; Whittel, Nicholas ; Vennerstrom, Jonathan L. ; Wells, Timothy N. C. ; Wang, Han ; Angala, Bhanupriya ; Williams, John T. ; Jones, Victoria ; Schenkel, Alan R. ; Jackson, Mary ; Verma, Deepshikha ; Zimmerman, Matthew ; Abramovitch, Robert B. ; Ordway, Diane J. ; Malcolm, Kenneth C. ; Johnson, Benjamin K.

A search for alternative Mycobacterium abscessus treatments led to our interest in the two-component regulator DosRS, which, in Mycobacterium tuberculosis , is required for the bacterium to establish a state of nonreplicating, drug-tolerant persistence in response to a variety of host stresses. We show here that the genetic disruption of dosRS impairs the adaptation of M. abscessus to hypoxia, resulting in decreased bacterial survival after oxygen depletion, reduced tolerance to a number of antibiotics in vitro and in vivo, and the inhibition of biofilm formation. We determined that three antimalarial drugs or drug candidates, artemisinin, OZ277, and OZ439, can target DosS-mediated hypoxic signaling in M. abscessus and recapitulate the phenotypic effects of genetically disrupting dosS . OZ439 displayed bactericidal activity comparable to standard-of-care antibiotics in chronically infected mice, in addition to potentiating the activity of antibiotics used in combination. The identification of antimalarial drugs as potent inhibitors and adjunct inhibitors of M. abscessus in vivo offers repurposing opportunities that could have an immediate impact in the clinic.

2021-12-01·BMC Chemistry3区 · 化学

Quantitative analysis of doxorubicin hydrochloride and arterolane maleate by mid IR spectroscopy using transmission and reflectance modes

3区 · 化学

ArticleOA

作者: Kaur, Khushpal ; Singh, Ranjit ; Bansal, Ranju

AbstractBackgroundEnvironment-friendly fast and accurate mid-infrared spectroscopic methods have been developed for the quantitative analysis of doxorubicin hydrochloride (DOX) and arterolane maleate (ALM) in bulk and marketed formulations. Both transmittance and reflectance modes have been used for the analysis and a comparison has been drawn for better accuracy. The analytical methods were validated in accordance with International Council for Harmonisation (ICH) guidelinesResultsThe proposed methods have been successfully developed and validated for the quantification of doxorubicin and arterolane maleate in solid bulk and dosage form. High recovery values in both the modes, while analysing DOX and ALM, indicated good accuracy of the methods. The methods showed excellent repeatability and intermediate precision [% RSD (Relative Standard Deviation < 2.0%]. The assay values of the drugs in solid dosage forms were also found close to the labelled claim.ConclusionThe proposed Fourier transform infrared (FT-IR) spectroscopic methods were found to be specific, reproducible, valid and could be used as general methods for the quantification of most of the solid drug preparations such as tablets, capsules and powders.

100 项与 Arterolane maleate 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Arterolane maleate	P01BX02	-

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
恶性疟	临床2期	印度	MMV Medicines for Malaria Venture	2006-06-01
恶性疟	临床2期	泰国	Ranbaxy Laboratories Ltd.	2006-06-01
恶性疟	临床2期	泰国	MMV Medicines for Malaria Venture	2006-06-01
恶性疟	临床2期	坦桑尼亚	MMV Medicines for Malaria Venture	2006-06-01
恶性疟	临床2期	印度	Ranbaxy Laboratories Ltd.	2006-06-01
恶性疟	临床2期	坦桑尼亚	Ranbaxy Laboratories Ltd.	2006-06-01

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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


CTRI/2011/11/002129 (Pubmed \| Malar J)	临床3期	间日疟原虫感染	317	Fixed-dose combination of arterolane maleate and piperaquine phosphate	(廠廠顧衊夢簾選憲淵鏇) = 1.3 vs 3.2% 鹹鏇艱範襯鹹顧齋夢獵 (範網廠壓鏇蓋夢淵夢壓 ) 更多	-	2016-01-27
				Chloroquine
NCT00362050 (RBx/MMV05-06, Pubmed \| Clin Infect Dis)	临床2期	恶性疟	230	Arterolane 50 mg	鏇鑰選襯選觸範選壓鏇(夢選構衊衊網積蓋餘餘) = 選衊網獵齋淵壓淵膚廠積鹹積鏇夢蓋餘窪鹹襯 (襯鏇繭鬱積壓壓選窪淵 ) 更多	-	2010-09-15
				Arterolane 100 mg	鏇鑰選襯選觸範選壓鏇(夢選構衊衊網積蓋餘餘) = 鏇遞製繭夢願鹽範構蓋積鹹積鏇夢蓋餘窪鹹襯 (襯鏇繭鬱積壓壓選窪淵 ) 更多