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  • Thorough QT/QTc Evaluation of the Cardiac Safety of Secnidazole at Therapeutic and Supratherapeutic Doses in Healthy Individuals.

Thorough QT/QTc Evaluation of the Cardiac Safety of Secnidazole at Therapeutic and Supratherapeutic Doses in Healthy Individuals.

Journal of clinical pharmacology (2017-10-03)
Borje Darpo, Hongqi Xue, Nikki Adetoro, Barbara G Matthews, Helen S Pentikis
ZUSAMMENFASSUNG

SYM-1219, a novel oral granule formulation of secnidazole, is under development as single-dose treatment for bacterial vaginosis. This 4-way, randomized, crossover study evaluated the effects of SYM-1219 on electrocardiographic (ECG) parameters in 52 healthy subjects. Subjects were administered single doses of SYM-1219, 2 g (proposed therapeutic dose), 6 g (supratherapeutic dose), placebo, and moxifloxacin (positive control). Serial digital 12-lead ECGs were recorded pre- and postdose; blood samples were taken to determine plasma secnidazole concentrations. A high-precision QT technique measured ECGs. The primary end point was change from baseline QTcF (∆QTcF); data were analyzed with the objective of excluding QT effects >10 milliseconds at postdosing time points and with exposure-response analysis. Safety and tolerability were assessed. Single doses of 2 g and 6 g SYM-1219 did not have a clinically relevant effect on the QTcF interval; an effect >10 milliseconds could be excluded at all postdosing time points. A shallow slope of the exposure-response relationship was seen (0.058 millisecond per μg/mL; 90%CI 0.042, 0.073); in this model, the effect on QTc can be predicted to be <10 milliseconds up to a secnidazole plasma concentration of ∼125 μg/mL, approximately 3.4-fold higher than anticipated peak therapeutic plasma levels. The moxifloxacin QT response demonstrated assay sensitivity. The most frequently reported treatment-emergent adverse events with SYM-1219 were headache, dizziness, and nausea. This thorough QT study demonstrated that SYM-1219 in doses and plasma concentrations up to 3-fold above therapeutically relevant levels does not have a clinically concerning effect on ECG parameters, including the QT interval.

MATERIALIEN
Produktnummer
Marke
Produktbeschreibung

Sigma-Aldrich
Secnidazole, ≥98% (HPLC)