Assessing QTc Effects of Vericiguat Using Two Different Concentration-QTc Modeling Approaches

Clin Pharmacokinet. 2023 Nov;62(11):1639-1648. doi: 10.1007/s40262-023-01282-y. Epub 2023 Sep 6.

Abstract

Background and objectives: Vericiguat is a soluble guanylate cyclase stimulator indicated to reduce the risk of cardiovascular death and hospitalization due to heart failure. A dedicated QTc study in patients with chronic coronary syndromes demonstrated no clinically relevant QTc effect of vericiguat for exposures across the therapeutic dose range (2.5-10 mg). Interval prolongation concentration-QTc (C-QTc) modeling was performed to complement the statistical evaluations of QTc in the dedicated QTc study.

Methods: Individual time-matched, baseline- and placebo-corrected Fridericia-corrected QT interval values (ΔΔQTcF) were derived. Two approaches for ΔΔQTcF calculation were investigated: (1) ΔΔQTcF correction with data from a single baseline (as in the primary statistical analysis); and (2) ΔΔQTcF correction with a modeled baseline (considering all available individual non-treatment baselines). The ΔΔQTcF values were related to observed vericiguat concentrations with linear mixed-effects modeling.

Results: For both modeling approaches, a positive relationship was found between ΔΔQTcF and vericiguat concentration; however, the slope for the single-baseline approach was not statistically significant, whereas the slope from the modeled-baseline approach was statistically significant. The upper bound of the two-sided 90% confidence interval for model-derived QTc was < 10 ms at the highest observed exposure (745 μg/L; investigated dose range 2.5-10 mg).

Conclusion: By applying a single-baseline approach and a modeled-baseline approach that integrated all available QTc data across doses to characterize the QTc prolongation potential, this study showed that vericiguat 2.5-10 mg is not associated with clinically relevant QTc effects, in line with the conclusion from the primary statistical analysis.

Clinical trials registration number: ClinicalTrials.gov NCT03504982.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cross-Over Studies
  • Double-Blind Method
  • Electrocardiography*
  • Heart
  • Heart Rate
  • Heterocyclic Compounds, 2-Ring*
  • Humans

Substances

  • vericiguat
  • Heterocyclic Compounds, 2-Ring

Associated data

  • ClinicalTrials.gov/NCT03504982