正在研发的抗疟药物的现状。
Status of antimalarial drugs under development.
作者信息
Olliaro P L, Trigg P I
机构信息
Steering Committee on Drugs for Malaria, UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases, World Health Organization, Geneva, Switzerland.
出版信息
Bull World Health Organ. 1995;73(5):565-71.
Abstract
Despite the urgent need of a new antimalarial drugs, particularly those against multiresistant falciparum malaria, only a limited number of drugs are now at an advanced stage of preclinical or clinical development. They include artemisinin derivatives, pyronaridine and benflumetol (all originally developed in China), as well as new antifolate combinations, the hydroxynaphoquinone atovaquone which has a novel mode of action, and a new 8-aminoquinoline which appears more active and less toxic than primaquine. Some of these drugs may become available in the next few years. It is therefore essential to find mechanisms to ensure that they are made available at an affordable price to the populations that really need them.
摘要
尽管迫切需要新型抗疟药物，尤其是针对多重耐药恶性疟的药物，但目前处于临床前或临床开发后期阶段的药物数量有限。这些药物包括青蒿素衍生物、咯萘啶和本芴醇（均最初在中国研发），以及新型抗叶酸联合用药、具有全新作用模式的羟基萘醌阿托伐醌，还有一种新型8-氨基喹啉，其活性似乎比伯氨喹更高且毒性更低。其中一些药物可能会在未来几年上市。因此，必须找到相应机制，以确保真正有需求的人群能够以可承受的价格获取这些药物。
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本文引用的文献
1
Pyronaridine: A new antimalarial drug.咯萘啶：一种新型抗疟药物。
Parasitol Today. 1991 Nov;7(11):310-3. doi: 10.1016/0169-4758(91)90267-r.
2
Treatment of Plasmodium falciparum malaria with pyrimethamine-sulfadoxine: selective pressure for resistance is a function of long elimination half-life.用乙胺嘧啶-磺胺多辛治疗恶性疟原虫疟疾：耐药性的选择性压力是长消除半衰期的一个函数。
Trans R Soc Trop Med Hyg. 1993 Jan-Feb;87(1):75-8. doi: 10.1016/0035-9203(93)90431-o.
3
4
PS-15: a potent, orally active antimalarial from a new class of folic acid antagonists.PS - 15：一种新型叶酸拮抗剂类强效口服抗疟药。
Am J Trop Med Hyg. 1993 Jul;49(1):121-6. doi: 10.4269/ajtmh.1993.49.121.
5
The chemotherapy of rodent malaria. XLIX. The activities of some synthetic 1,2,4-trioxanes against chloroquine-sensitive and chloroquine-resistant parasites. Part 2: Structure-activity studies on cis-fused cyclopenteno-1,2,4-trioxanes (fenozans) against drug-sensitive and drug-resistant lines of Plasmodium berghei and P. yoelii ssp. NS in vivo.啮齿动物疟疾的化学疗法。XLIX. 某些合成1,2,4-三恶烷对氯喹敏感和氯喹耐药寄生虫的活性。第2部分：顺式稠合环戊烯并-1,2,4-三恶烷（非诺赞）对伯氏疟原虫和约氏疟原虫ssp. NS药物敏感和耐药品系的体内构效关系研究。
Ann Trop Med Parasitol. 1993 Feb;87(1):9-16. doi: 10.1080/00034983.1993.11812734.
6
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7
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Clin Pharm. 1993 Aug;12(8):563-70.
8
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9
Drug resistance and the P-glycoprotein homologues of Plasmodium falciparum.恶性疟原虫的耐药性与P-糖蛋白同源物
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