The biased signalling profile of dual FPR1 / FPR2 agonist, favouring ERK1/2-Akt cell survival signalling, away from pro-inflammatory/ cell death mechanisms (e.g. Ca2+ mobilization), provides novel triple shield therapy against MI
- Reperfusion Injury following Myocardial Infarction 30m patients; market size US$7.8bn in 2015 globally
- Compound annual growth rate of cardiovascular diseases in China is 21.6%; costing US$6.8bn by 2022
Key players include Eustralis Pharmaceuticals Ltd., NeuroVive Pharmaceutical AB, Nyken BV, Stealth Peptides, Inc., Scynexis, Inc., and Vasade Biosciences, Inc
- Coronary heart disease (CHD), most commonly characterised by myocardial infarction (MI), is the number one cause of death in advanced economies.
- Reperfusion therapies, including surgical and drug therapy, promptly restore blood flow to blood-deprived heart tissue and limit infarct size. However, the return of blood flow can result in additional cardiac damage and complications; this is referred to as reperfusion injury
- Reperfusion injury accounts for up to 50% of the final size of a myocardial infarct and is caused by localised inflammation of the heart tissue
- The incidence of one-year mortality and HF post MI is high and represents a significant burden
- There is need for novel cardioprotective therapies targeting myocardial reperfusion injury to reduce MI size, preserve heart function and prevent the onset of heart failure
- Patent granted in 2016 for “a method of treatment and compounds for use therein”.
- Identified small-molecule drug candidate which acts as a biased, dual FPR1 / FPR2 agonist and provides cardioprotection in well-characterised animal models of ischemia-reperfusion injury
- Currently no agent has been clinically approved for treatment of reperfusion injury
- Small molecule dual FPR1 / FPR2 agonist compound 17b provides novel “triple shield” therapy: limiting cardiac inflammation; preserving cardiomyocyte viability; preserving contractile function
- Superior cardioprotection over other conventional FPR agonists
- Dual FPR1 / FPR2 agonists represent and innovative pharmacotherapy, offering multiple advantages to existing therapies post MI (none of which exploit ligand selectivity)
- Compound 17b has been proven to provide cardioprotection in well-characterised animal models of ischemia-reperfusion injury
- Compound 17b, is a dual FPR1 / FPR2 agonist which provides novel “triple shield” therapy against MI:
- Limiting cardiac inflammation
- Preserving cardiomyocyte viability
- Preserving contractile function
- Superior cardioprotection over other conventional FPR agonists lacking selectivity
- Broad US and EU Patent granted in 2015 for “a method of treatment and compounds for use therein”.
|Protects against Cardiac Injury||Protects against Necrosis|
|Protects against Cardiac Remodelling||Reduces Inflammation|