Development of the new antimalarial drug pyronaridine: a review.
This report outlines the structure scheme and development of a new antimalarial drug pyronaridine, which was synthesized from either 2-aminopyridine or pyridine. A series of in vivo and in vitro experimental studies and the assessment of toxicity revealed pyronaridine to be a promising agent against erythrocytic stage of malaria parasites. It exhibited low toxicity and had no cross-resistance to chloroquine. Clinical administration in malaria cases showed high efficacy and mild side-effects. In order to retard the development of resistance of Plasmodium falciparum to pyronaridine, a combination of pyronaridine/sulfadoxine/pyrimethamine was used in the treatment of chloroquine-resistant falciparum malaria in Hainan Province. Further in vivo test was carried out to monitor the sensitivity of P. falciparum to this combined formula for 5 years (1986-1990) in Diaoluo area where chloquine-resistant falciparum malaria was prevalent. Drug resistance was not demonstrated in this field study.
Chen
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Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, Shanghai.
Zheng
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D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry; D002319:Cardiovascular System / Q000187:drug effects; D002738:Chloroquine / Q000627:therapeutic use; D004285:Dogs; D004341:Drug Evaluation; D004353:Drug Evaluation, Preclinical; D004351:Drug Resistance; D004359:Drug Therapy, Combination; D000882:Haplorhini; D006801:Humans; D007273:Injections, Intramuscular; D007928:Lethal Dose 50; D016778:Malaria, Falciparum / Q000188:drug therapy*; D051379:Mice; D009287:Naphthyridines / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry; D011739:Pyrimethamine / Q000008:administration & dosage; D011817:Rabbits; D013413:Sulfadoxine / Q000008:administration & dosage
D000962:Antimalarials; D009287:Naphthyridines; D013413:Sulfadoxine; D002738:Chloroquine; C027871:pyronaridine; D011739:Pyrimethamine