Concentration-QT modelling of the novel DHFR inhibitor P218 in healthy male volunteers.

ABSTRACT:

Aims

Given the increasing emergence of drug resistance in Plasmodium, new antimalarials are urgently required. P218 is an aminopyridine that inhibits dihydrofolate reductase being developed as a malaria chemoprotective drug. Assessing the effect of new compounds on cardiac intervals is key during early drug development to determine their cardiac safety.

Methods

This double-blind, randomized, placebo-controlled, parallel group study evaluated the effect of P218 on electrocardiographic parameters following oral administration of seven single-ascending doses up to 1000 mg in 56 healthy volunteers. Participants were randomized to treatment or placebo at a 3:1 ratio. P218 was administered in the fasted state with standardized lunch served 4 hours after dosing. 12-lead ECGs were r

SUBMITTER: Taubel J 

PROVIDER: S-EPMC9292718 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature