Clinical stage biopharmaceutical company Congenia has started healthy volunteer enrolment in Phase I trial of GNX-5086, a potent small molecule inhibitor of a novel target involved in modulating stress induced cell death mPTP.
Designed to assess the safety and tolerability and pharmacokinetics of single ascending doses of GNX-5086, the randomised, double-blind, placebo-controlled study is expected to enrol 33 healthy volunteers.
The company is developing GNX-5086 against cardiac reperfusion injury (RI) that contributes significantly to the morbidity and mortality subsequent tomyocardial infarction (MI), which has no existing therapies.
Being developed for intravenous administration to infarcted patients just prior to percutaneous coronary intervention (PCI), GNX-5086 has the capability to increase the capacity of isolated mitochondria to retain calcium and consequently protect the mitochondria from calcium overload in stress situations.
Through a longstanding preclinical collaboration with the Drug Discovery Program of the European Institute of Oncology (DDP-IEO), GNX-5086 was selected as lead compound.
The effectiveness of GNX-5086 in attenuating RI and reducing infarct size was demonstrated in in-vivo studies using a rabbit model of acute myocardial infarction when administered just prior to heart reperfusion.
The company filed a clinical trial application (CTA) to begin the Phase I study of GNX-5086 on 4 July in the Netherlands and won approval by the local regulatory authorities on 24th of the same month.