XXXX kinase inhibitors: New class of antimalarials on the horizon?

@entity2857 @entity3964 @entity506 @entity311 @entity4149 @entity2213
Development of the antimalarial drug resistant strains has currently become a major public health challenge. There is an urgent need to develop new antimalarial drugs. @entity4149 kinase inhibitors (TKIs) are receiving increasing attention as anticancer therapy. It has revolutionarised the management of CML to say the least. TKIs are also increasingly being implicated in complicated but vital life cycle of @entity311 parasite. Hence we tested two commonly used but different classes of TKIs ( @entity2213 and @entity2857 ) in-vitro for their antimalarial activity and possible synergistic activity with existing antimalarial drug. Antimalarial activity was tested with the help of modified WHO microtest technique in-vitro for five different @entity3964 laboratory strains (3D7, Dd2, 7G8, MRC2, PKL9). @entity2213 and @entity2857 showed a promising antimalarial activity with all the strains. These compounds caused dose dependent inhibition of parasite maturation. The isobologram analysis of the interactions of these TKIs with standard antimalarial drug, @entity506 revealed distinct patterns of synergism, additivity and antagonism at different ratios. @entity2213 showed worthwhile synergism with @entity506 indicating @entity2213 and other @entity4149 kinase inhibitors may have significant antimalarial activity and can be used in combination therapy.
