Tafenoquine is an investigational 8-aminoquinoline
derivative with activity against the P.
CYP450 phenotyping and accurate mass identification of metabolites of the 8-aminoquinoline
, anti-malarial drug primaquine.
The endoperoxide OZ439, currently in Phase II clinical trials, and a new 8-aminoquinoline
, NPC-1161B, also demonstrated transmission-blocking potential.
A new 8-aminoquinoline
tafenoquine is on clinical trial as a potential replacement for primaquine to treat Plasmodium vivax malaria (Shanks 2001) and holds promise as a prophylactic against Plasmodium falciparum (Shanks 2001).
Tefenoquine, which is an 8-aminoquinoline
, has activity against blood-stage and liver-stage malaria parasite.
These include an 8-aminoquinoline
derivative under pre-clinical evaluation for the treatment of malaria, leishmania and pneumocystis pneumonia.
Primaquine, an 8-aminoquinoline was covalently coupled onto oxidized gum arabic via imine bond and simultaneously fabricated into microspheres of less than 2 [micro]m in size by heat denaturation in a reverse emulsion of 1:1 light paraffin oil and toluene stabilized by sorbitan sesquioleate as the surfactant.
Key words: gum arabic, polysaccharide, periodate oxidation, microspheres, drug delivery, primaquine, 8-aminoquinoline, sustained release, controlled release, polymer-drug conjugate.
Primaquine, an 8-aminoquinoline and some of its derivatives are potent drugs in the treatment of malaria as well as other parasitic diseases such as Leishmaniasis (1-8).
Mass administration of an antimalarial drug combining 4-aminoquinoline and 8-aminoquinoline
Structural features of Plasmodium cytochrome b that may underlie susceptibility to 8-aminoquinolines