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Novartis has changed the rules of the game to a new generation of antimalarial drugs
2014-08-02
来源:转载自第三方
Nuo Hua (Novartis) published in July 31st, the anti malaria drug KAE609 (cipargamin) a proof of concept of positive data from the clinical trials, 21 patients infected with Plasmodium falciparum (P.falciparum) or (P.vivax) of Plasmodium vivax malaria patients without complications but participated in this study. The researchers found that, KAE609 is rapidly cleared (average 12 hours) in patients with uncomplicated malaria Plasmodium falciparum and Plasmodium vivax, including those resistant plasmodium. Relevant data have been published in the "new England Journal of medicine" (New England Journal of Medicine).
At present, Novartis has 2 in the research of anti malaria drug candidate, KAE609 and KAF156, 2 belong to a new class of anti malarial compounds, different mechanisms and the current therapy, is critical to prevent the emergence of drug resistance. In addition, Novartis has determined that PI4K is a new drug targets, is expected to be used in prevention and treatment of malaria, blocking.
Malaria is a life-threatening disease, mainly through the bite of infected mosquitoes, the parasite (Plasmodium falciparum and Plasmodium vivax) caused by the spread to humans. In the global scope, it kills over 600000 people a year, mostly Africa children.
In the prevention and treatment of malaria in battle, KAE609 is expected to be a game changing drug. KAE609 is the first screw indole ketone compounds, play the antimalarial activity through a novel mechanism of action, the mechanism of KAE609 action involves inhibition of a P cation transporter ATP enzyme 4 (PfATP4), the concentration of the enzymes of parasites, sodium ion. In view of the KAE609 also seems to gametocyte, so it may help prevent the spread of the disease. In vitro, for a variety of parasitic current drug resistance, KAE609 also exhibits strong antimalarial activity. At present, Novartis is planning a phase IIb clinical study.
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