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抗疟铁喹啉:从实验室到临床。

The antimalarial ferroquine: from bench to clinic.

机构信息

Unité de Catalyse et Chimie du Solide, CNRS UMR 8181, Université Lille Nord de France.

出版信息

Parasite. 2011 Aug;18(3):207-14. doi: 10.1051/parasite/2011183207.

DOI:10.1051/parasite/2011183207
PMID:21894260
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3671469/
Abstract

Ferroquine (FQ, SSR97193) is currently the most advanced organo-metallic drug candidate and about to complete phase II clinical trials as a treatment for uncomplicated malaria. This ferrocene-containing compound is active against both chloroquine-susceptible and chloroquine-resistant Plasmodium falciparum and P. vivax strains and/or isolates. This article focuses on the discovery of FQ, its antimalarial activity, the hypothesis of its mode of action, the current absence of resistance in vitro and recent clinical trials.

摘要

铁喹(FQ,SSR97193)是目前最先进的有机金属药物候选物,即将完成 II 期临床试验,作为治疗无并发症疟疾的药物。这种含二茂铁的化合物对氯喹敏感和氯喹耐药的恶性疟原虫和间日疟原虫株和/或分离株均有活性。本文重点介绍了 FQ 的发现、抗疟活性、作用机制假说、目前体外无耐药性以及最近的临床试验。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9d5/3671469/1fb86e291e1a/parasite-18-207-fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9d5/3671469/3908d70deefa/parasite-18-207-fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9d5/3671469/1fb86e291e1a/parasite-18-207-fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9d5/3671469/3908d70deefa/parasite-18-207-fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f9d5/3671469/1fb86e291e1a/parasite-18-207-fig2.jpg

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ACS Chem Biol. 2011 Mar 18;6(3):275-87. doi: 10.1021/cb100322v. Epub 2011 Jan 7.
2
Organometallic complexes: new tools for chemotherapy.金属有机配合物:化疗的新工具。
Curr Med Chem. 2010;17(25):2729-45. doi: 10.2174/092986710791859306.
3
Plasmodium vivax susceptibility to ferroquine.恶性疟原虫对铁喹的敏感性。
疟疾治疗药物研发的最新进展、挑战与动态
EXCLI J. 2024 May 6;23:672-713. doi: 10.17179/excli2023-6856. eCollection 2024.
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Discovery of New Broad-Spectrum Anti-Infectives for Eukaryotic Pathogens Using Bioorganometallic Chemistry.利用生物有机金属化学发现针对真核病原体的新型广谱抗感染药物。
J Med Chem. 2023 Dec 14;66(23):15867-15882. doi: 10.1021/acs.jmedchem.3c01333. Epub 2023 Nov 27.
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Steroids Bearing Heteroatom as Potential Drugs for Medicine.含杂原子甾体作为潜在的医药用药物
Biomedicines. 2023 Oct 3;11(10):2698. doi: 10.3390/biomedicines11102698.
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Investigation of new ferrocenyl-artesunate derivatives as antiparasitics.新型二茂铁基青蒿琥酯衍生物作为抗寄生虫药物的研究。
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