Description

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

Market Size

  • 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

Investment Landscape

Key players include Eustralis Pharmaceuticals Ltd., NeuroVive Pharmaceutical AB, Nyken BV, Stealth Peptides, Inc., Scynexis, Inc., and Vasade Biosciences, Inc

Background

  • 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

Status

  • 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

Competitive Advantage

  • 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)

Lab Notes

  • 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:
    1. Limiting cardiac inflammation
    2. Preserving cardiomyocyte viability
    3. 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 

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