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Evaluation of the Potential Effect of Iptakalim Hydrochloride on the QT Interval in Single- and

Nan Bai1, Jin Wang1, Haoyue Che1

  • 1Chinese People's Liberation Army General Hospital, Medicine Clinical Research Center, Beijing, China.

Clinical Pharmacology in Drug Development
|April 15, 2021
PubMed

Insights

Iptakalim hydrochloride (ITKL) did not prolong the QT interval in healthy subjects. This study assessed cardiac repolarization effects of ITKL, a hypertension drug, finding no significant QTc interval changes at therapeutic doses.

Area of Science:

  • Pharmacology
  • Cardiology
  • Clinical Trials

Background:

  • Cardiotoxicity is a major reason for drug withdrawal.
  • QT interval prolongation is a key indicator of drug-induced cardiotoxicity.
  • Assessing cardiac repolarization risk is vital for new antihypertensive drugs like Iptakalim hydrochloride (ITKL).

Purpose of the Study:

  • To evaluate the effect of Iptakalim hydrochloride (ITKL) on the corrected QT (QTc) interval.
  • To investigate the correlation between ITKL plasma concentration and QTc interval changes.
  • To determine the cardiac safety profile of ITKL regarding repolarization in healthy subjects.

Main Methods:

  • A randomized, double-blind, placebo-controlled study.
  • Single and multiple oral doses of ITKL (5-20 mg) administered to 83 healthy subjects.
  • Electrocardiograms (ECGs) and blood samples collected to monitor QTc interval and ITKL levels.

Main Results:

  • No significant prolongation of the QTc interval was observed at any tested plasma level of ITKL.
  • The maximum observed ΔΔQTcF effect was below the exclusion threshold of 10 milliseconds.
  • Even at twice the therapeutic dose (20 mg), ITKL did not affect QTc interval.

Conclusions:

  • Iptakalim hydrochloride (ITKL) does not prolong the QT interval in healthy subjects within the therapeutic dose range.
  • ITKL demonstrates a favorable cardiac safety profile concerning repolarization.
  • Further clinical evaluation can proceed with confidence in ITKL's cardiac safety.

Keywords:
CmaxQT intervalexposure responseiptakalim

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