A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the antimalarial agents KAE609 and piperaquine (PPQ)

Background KAF156 is a novel imidazolopiperazine anti-malarial with activity against pre-erythrocytic liver stages, asexual and sexual blood stages. Based on in vitro data, a two-way pharmacokinetic interaction was hypothesized for KAF156 use in combination with piperaquine (PPQ) as both drugs are CYP3A4 substrates and inhibitors. Potential combination effects on the QT interval were also assessed.