Dafra Pharma and CCR-KEMRI have initiated the first in man clinical Phase 1 study
using single oral doses of 50 mg, 100 mg and 150 mg of oleylphosphocholine in healthy
adult males (protocol DRD140-L2.2012, SSC #2512). The study made use of a capsule
formulation of oleylphophocholine containing 50 mg of active ingredient. The subjects of
the first three cohorts were receiving one, two or three of those capsules as a single dose.
Based on the positive results obtained so far, two additional cohorts of 10 volunteers are
now planned to be dosed with single dose of 200 mg and 250 mg, upon approval by
KEMRI IRB. The capsule formulation of oleylphosphocholine was of limited shelf life and was only
meant to be used for early clinical studies. Since the initiation of the Phase 1 trial, the
pharmaceutical research around the formulation of oleylphosphocholine has progressed
and the final formulation of the active ingredient intended to be marketed has become
available. This formulation is in the form of 50 mg oral solid tablets. Our intention is to
continue the Phase 1 protocol DRD140-L2.2012, SSC #2512 with this new formulation,
but before, we wish to confirm that both the capsule and tablet formulations of the active
ingredient are comparable in terms of safety/tolerance, and pharmacokinetics.The primary objective is to evaluate safety and tolerability of single dose 100 mg
oleylphosphocholine oral solid tablets in healthy male volunteers.The secondary objective is to obtain data on pharmacokinetics following oral
administration of single dose 100 mg tablets oleylphosphocholine in human, and to
calculate bioequivalence with the capsule formulation