KDU691 is an antimalarial compound.
1 It inhibits recombinant
P. vivax phosphatidylinositol 4-kinase (PI4K) with an IC
50 value of 1.5 nM. KDU691 is selective for
P. vivax PI4K over recombinant human PI4KβIII and PI3Kα, -β, -γ, and -δ (IC
50s = 7.9, 8.8, 2.4, 8, and 3.4 μM, respectively), as well as VPS34 (IC
50 = >9.7 μM) and 36 additional kinases in a panel of lipid and protein kinases (IC
50s = >10 μM). It is active against
P. falciparum and
P. yoelii schizonts (IC
50s = 0.06 and 0.04 μM, respectively), as well as
P. cynomolgi schizonts and hypnozoites (IC
50s = 0.11 and 0.2 μM, respectively).
2 KDU691 completely prevents, but does not eradicate established,
P. cynomolgi infection in rhesus monkeys when administered at a dose of 20 mg/kg.
3