Ferroquine(Ferroquine) - 药物靶点：Hemozoin_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Hemozoin

作用机制

疟色素抑制剂

治疗领域

感染

在研适应症-

非在研适应症

恶性疟

原研机构

Sanofi

在研机构-

非在研机构

Sanofi

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C23H24ClFeN3

InChIKeyDDENDDKMBDTHAX-UHFFFAOYSA-N

CAS号185055-67-8

关联

4

项与 Ferroquine 相关的临床试验

NCT05911828 / Not yet recruiting临床1期

Phase Ib, Single-center, Randomized, Study to Determine Safety, Tolerability, and Pharmacokinetics of Different Orally Administered Regimens of the Combination ZY19489-Ferroquine in Adult Asymptomatic Plasmodium Falciparum Carriers

Malaria is caused by protozoan parasites of the genus Plasmodium and it is the most important parasitic disease in terms of mortality and morbidity. Estimates of 247 million malaria cases and 619.000 deaths worldwide were reported by WHO for the year 2021 (1). Plasmodium falciparum can lead to severe malaria and accounts for 90% of malaria deaths that mainly occur in children below the age of 5 years in Sub-Saharan Africa.
A simplified treatment regimen, ideally a single-day cure (or at most 2-day dosing regimen), of uncomplicated malaria due to P. falciparum would be the magic in the antimalarial armamentarium. Improving treatment adherence is one of the key factors in reducing mortality and morbidity and also the transmission of malaria, and such a regimen would substantially increase adherence. To find a new non-artemisinin combination therapy with a shorter regimen, ideally, a single-dose cure, with low resistance potential would be the aim. The two compounds tested here are ZY19489, a triaminopyrimidine, and ferroquine (FQ), a next-generation 4-aminoquinoline. Both compounds show unique features in terms of long half-life, and activity against current drug-resistant strains.
Therefore, the main goal of this clinical trial is to assess the safety of the ZY19489-FQ combination given as a 1- or 2-day dose regimen.

开始日期2024-08-01

申办/合作机构

Zydus Lifesciences Ltd.

NCT02497612 / Terminated临床2期

A Randomized, Double-blind, Phase IIb Study to Investigate the Efficacy, Safety, Tolerability and Pharmacokinetics of a Single Dose Regimen of Ferroquine (FQ) With Artefenomel (OZ439) in Adults and Children With Uncomplicated Plasmodium Falciparum Malaria

Primary Objective:
To determine whether a single dose combination of OZ439 (Artefenomel)/FQ (Ferroquine) was an efficacious treatment for uncomplicated Plasmodium falciparum malaria in adults and children.
Secondary Objectives:
To evaluate the efficacy of OZ439/FQ:
To determine the incidence of recrudescence and re-infection.
To determine the time to relief of fever and parasite clearance.
To evaluate the safety and tolerability of OZ439/FQ in adults and children.
To characterize the pharmacokinetics of OZ439 in plasma, FQ and its active metabolite SSR97213 in blood.
To determine the blood/plasma ratio for FQ and SSR97213 in some participants at limited time points in selected sites.

开始日期2015-07-25

申办/合作机构

Sanofi

[+1]

ACTRN12613001040752 / Completed临床2期IIT

An experimental study to characterize the effectiveness of ferroquine against early Plasmodium falciparum blood stage infection in healthy volunteers

开始日期2013-10-17

申办/合作机构

QIMR Berghofer Medical Research Institute

100 项与 Ferroquine 相关的临床结果

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100 项与 Ferroquine 相关的转化医学

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100 项与 Ferroquine 相关的专利（医药）

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85

项与 Ferroquine 相关的文献（医药）

2024-08-01·Bioorganic Chemistry

Exploring antimalarial potential: Conjugating organometallic moieties with organic fragments for enhanced efficacy

Review

作者: Hafizah Mukhtar, Nur ; Suhaily Saaidin, Aimi ; Huda Abd Karim, Nurul ; Ismail, Norzila ; Yee Ling, Lau ; Ebihara, Masahiro ; Aqilah Zahirah Norazmi, Nur ; Ravindar, Lekkala ; Kartini Agustar, Hani ; Hamizah Ali, Amatul ; Izzaty Hassan, Nurul

In the search for novel ligands with efficacy against various diseases, particularly parasitic diseases, molecular hybridization of organometallic units into biologically active scaffolds has been hailed as an appealing strategy in medicinal chemistry. The conjugation to organometallic fragments can be achieved by an appropriate linker or by directly coordinating the existing drugs to a metal. The success of Ferroquine (FQ, SR97193), an effective chloroquine-ferrocene conjugate currently undergoing the patient-exploratory phase as a combination therapy with the novel triaminopyrimidine ZY-19489 for malaria, has sparked intense interest in organometallic compound drug discovery. We present the evolution of organometallic antimalarial agents over the last decade, focusing on the parent moiety's class and the type of organometallics involved. Four main organometallic antimalarial compounds have been chosen based on conjugated organic moieties: existing antimalarial drugs, other clinical drugs, hybrid drugs, and promising scaffolds of thiosemicarbazones, benzimidazoles, and chalcones, in particular. The presented insights contribute to the ongoing discourse on organometallic compound drug development for malaria diseases.

2024-07-01·The Chemical Record

Ferrocenyl Azoles: Versatile N‐Containing Heterocycles and their Anticancer Activities

Review

作者: Sadanala, Bhavya Deepthi ; Trivedi, Rajiv

AbstractThe medicinal chemistry of ferrocene has gained its momentum after the discovery of biological activities of ferrocifen and ferroquine. These ferrocenyl drugs have been designed by replacing the aromatic moiety of the organic drugs, tamoxifen and chloroquine respectively, with a ferrocenyl unit. The promising biological activities of these ferrocenyl drugs have paved a path to explore the medicinal applications of several ferrocenyl conjugates. In these conjugates, the ferrocenyl moiety has played a vital role in enhancing or imparting the anticancer activity to the molecule. The ferrocenyl conjugates induce the cytotoxicity by generating reactive oxygen species and thereby damaging the DNA. In medicinal chemistry, the five membered nitrogen heterocycles (azoles) play a significant role due to their rigid ring structure and hydrogen bonding ability with the biomolecules. Several potent drug candidates with azole groups have been in use as chemotherapeutics. Considering the importance of ferrocenyl moiety and azole groups, several ferrocenyl azole conjugates have been synthesized and screened for their biological activities. Hence, in the view of a wide scope in the development of potent drugs based on ferrocenyl azole conjugates, herein we present the details of synthesis and the anticancer activities of ferrocenyl compounds bearing azole groups such as imidazole, triazoles, thiazole and isoxazoles.

2024-03-08·ACS Infectious Diseases

Antifungal and Antiparasitic Activities of Metallocene-Containing Fluconazole Derivatives

Article

作者: Mitreva, Makedonka ; Gambino, Dinorah ; Ballesteros-Casallas, Andres ; Salinas, Gustavo ; Weil, Tobias ; Vinck, Robin ; Gasser, Gilles ; Cariou, Kevin ; Blacque, Olivier ; Scalese, Gonzalo ; Pérez Díaz, Leticia ; Sakanari, Judy A ; Bulman, Christina A ; Lin, Yan ; Paulino, Margot

The search for new anti-infectives based on metal complexes is gaining momentum. Among the different options taken by researchers, the one involving the use of organometallic complexes is probably the most successful one with a compound, namely, ferroquine, already in clinical trials against malaria. In this study, we describe the preparation and in-depth characterization of 10 new (organometallic) derivatives of the approved antifungal drug fluconazole. Our rationale is that the sterol 14α-demethylase is an enzyme part of the ergosterol biosynthesis route in Trypanosoma and is similar to the one in pathogenic fungi. To demonstrate our postulate, docking experiments to assess the binding of our compounds with the enzyme were also performed. Our compounds were then tested on a range of fungal strains and parasitic organisms, including the protozoan parasite Trypanosoma cruzi (T. cruzi) responsible for Chagas disease, an endemic disease in Latin America that ranks among some of the most prevalent parasitic diseases worldwide. Of high interest, the two most potent compounds of the study on T. cruzi that contain a ferrocene or cobaltocenium were found to be harmless for an invertebrate animal model, namely, Caenorhabditis elegans (C. elegans), without affecting motility, viability, or development.

100 项与 Ferroquine 相关的药物交易

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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	加蓬	Sanofi	2009-10-01
恶性疟	临床2期	坦桑尼亚	Sanofi	2009-10-01
恶性疟	临床2期	贝宁	Sanofi	2009-10-01
恶性疟	临床2期	喀麦隆	Sanofi	2009-10-01
恶性疟	临床前	肯尼亚	Sanofi	2009-10-01
恶性疟	临床前	布基纳法索	Sanofi	2009-10-01

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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


NCT02497612 (Pubmed \| Malar J) 人工标引	临床2期	恶性疟	373	artefenomel+ferroquine	(構築顧繭壓膚遞鹹鬱網) = 78.4% [64.7; 88.7%] to 91.7% [81.6; 97.2%] for the 400 mg to 1200 mg 醖窪衊鬱製淵網選壓觸 (遞願網憲積範構範淵夢 ) 更多	不佳	2021-05-19
NCT02497612 (FALCI, CTgov)	临床2期	恶性疟	377	Placebo+Artefenomel+Ferroquine SSR97193 (Ferroquine (up to 400 mg) + Artefenomel (up to 800 mg))	積壓顧選廠糧積齋簾齋(構蓋醖鹽淵餘繭艱積積) = 鑰觸憲鬱構選鑰積鹹廠鏇獵壓醖膚範襯衊鹽夢 (鑰壓餘願願醖鹹衊蓋鏇, 簾選衊鹽衊鏇選艱壓範 ~ 廠構鹽鬱夢壓鏇壓膚獵) 更多	-	2020-10-19
				Placebo+Artefenomel+Ferroquine SSR97193 (Ferroquine (up to 600 mg) + Artefenomel (up to 800 mg))	積壓顧選廠糧積齋簾齋(構蓋醖鹽淵餘繭艱積積) = 窪廠築鏇築鬱網願憲憲鏇獵壓醖膚範襯衊鹽夢 (鑰壓餘願願醖鹹衊蓋鏇, 願選艱廠鹹顧網艱壓艱 ~ 願選鹹廠顧積遞衊顧齋) 更多
NCT00988507 (Pubmed \| Lancet Infect Dis)	临床2期	恶性疟	326	Artesunate 4 mg/kg + Ferroquine 2 mg/kg	鬱齋積遞構糧顧餘廠選(構衊壓淵壓蓋鹹艱鏇顧) = 糧築範齋鏇夢蓋願蓋衊艱襯醖醖鑰製淵網積鑰 (艱壓鏇憲醖鏇網鏇鬱衊, 90 ~ 100)	积极	2015-12-01
				Artesunate 4 mg/kg + Ferroquine 4 mg/kg	鬱齋積遞構糧顧餘廠選(構衊壓淵壓蓋鹹艱鏇顧) = 選糧鹹選蓋餘構遞憲遞艱襯醖醖鑰製淵網積鑰 (艱壓鏇憲醖鏇網鏇鬱衊, 93 ~ 100)