Conopeptide Based Therapeutics for Acute Myocardial Infarction and Reperfusion Injury
Conopeptides are a highly specialized group of peptides produced by venomous conus sea snails. This class of naturally derived compounds is an extraordinarily large and diverse pharmacopoeia of bioactive molecules with potent and subtype selective activity against many molecular targets of interest in pharmaceutical drug development.
Conus sea snails use a complex venom "cocktail" composed of between 50 and 200 distinct and unique peptides to hunt prey such as fish, worms, and other snails. This complex mixture of conopeptides targets a variety of ion channels and receptors across many species (including human) with unprecedented potency and selectivity, resulting in very rapid and potent action. In general, conopeptides are water soluble, extremely stable, simple to manufacture and possess a low molecular weight.
The first conopeptide based drug, Elan´s PrialtTM (or Ziconotide), was approved by the FDA in December 2004. It was approved for the treatment of severe chronic pain and demonstrates the potency lying in this class of natural compounds. In a longlasting cooperation between Cognetix Inc., the University of Utah and the Max Planck Institute for Experimental Medicine three conopeptides (PVIIA or CGX-1051, RIIIK, and Conkunitzin) have been investigated regarding their therapeutic use in the field of myocardial ischemia, reperfusion injury, and organ protection.
PVIIA, the most advanced peptide, dramatically reduced infarct size in three animal models of acute myocardial ischemia/reperfusion. It has been shown to significantly reduce infarction when given after the onset of ischemia and prior to reperfusion in rabbits, rats and dogs in vivo. Importantly, no adverse hemodynamic effects (heart rate and blood pressure) have been observed at any dose tested. Preliminary safety data have been generated in mice showing no adverse effects up to 20mg/kg PVIIA.
In the U.S., approximately 500,000 patients present at hospitals each year with AMI (Acute Myocardial Infarction). While in-hospital mortality is low, a large number of the surviving patients suffer from intractable heart failure due to the extent of damage induced by ischemia/reperfusion.
Based on the data described above, we believe that PVIIA is a very promising compound for use as an adjunct to either a thrombolytic agent or mechanical reperfusion in patients presenting with acute myocardial infarction. The other peptides RIIIK and Conkunitzin have been studied intensively in vitro but have not been analyzed in animal models yet. They both display also a high selectivity and potency against their target molecules and are considered as excellent backup compounds for PVIIA.
We are looking for a cooperation or licensing partner who is interested in these peptides and is able to develop these exciting novel compounds into marketable assets.
Composition of matter and use patents have been filed for all three conopeptides mentioned above.
About Max-Planck-Innovation GmbH
Max Planck Innovation advises and supports scientists of the Max Planck Society in evaluating inventions and filing patent applications. They market patents and technologies to industry and coach founders of new companies based on research results from Max Planck Institutes. Every year, they evaluate about 130 inventions, of which 80 to 100 lead to the filing of a patent. In the last five years alone, they advised 28 spin-offs, closed more than 450 license deals and generated proceeds of more than EUR100m for inventors, institutes and the Max Planck Society. As a result, Max Planck Innovation is among the world's most successful technology transfer organizations. Max Planck Innovation was founded in 1970 as Garching Instrumente GmbH and operated under the name of Garching Innovation from 1993 to 2006.