Stapled Peptides for Treatment of Cardiovascular Diseases and Inflammation


The invention is directed to small molecule mimetics of apolipoproteins that have an inter-helical hydrocarbon bond, which stabilizes helix formation.

Apolipoproteins facilitate the transport of lipids and cholesterol in the body. Mimetics of apolipoproteins have been used to treat cholesterol-related disorders. However, these mimetics are susceptible to degradation in biological fluids and as a result, their ability to bind cholesterol becomes diminished over time.

Scientists at NHLBI have devised methods to stabilize and improve the performance of apolipoprotein mimetic peptides, using a modified hydrocarbon chain (“stapled apolipoproteins”). These stapled apolipoproteins are superior to singular apolipoproteins in that they are more resistant to enzymatic degradation and efflux a greater amount of cellular cholesterol.

Stapled apolipoproteins can be used in the treatment of cardiovascular diseases, particularly for treatment of atherosclerosis.

Potential Commercial Applications: Competitive Advantages:
  • Treatment of inflammation and cardiovascular diseases, including hyperlipidemia, atherosclerosis, restenosis, and acute coronary syndrome.
  • Inclusion in oral, intravenous or transdermal peptide formulations.
 
  • Stapled apolipoproteins are more resistant to proteolysis and display enhanced bioavailability.
  • Stapled apolipoproteins are amenable to oral delivery and have increased permeability to the blood brain barrier.


Development Stage:
  • Pre-clinical
  • In vitro data available
  • In vivo data available (animal)


Inventors:

Alan Remaley (CC)  ➽ more inventions...

Marcelo Amar (NHLBI)  ➽ more inventions...

Imoh Ikpot (NHLBI)  ➽ more inventions...

Denis Sviridov (NHLBI)  ➽ more inventions...

David Osei-Hwedieh (NHLBI)  ➽ more inventions...


Intellectual Property:
US Application No. 61/480,986
PCT Application No. PCT/ US12/35870
US Application No. 14/114,386

Publications:
Osei-Hwedieh DO, et al. PMID 21172387

Collaboration Opportunity:

The NHLBI Lipoprotein Metabolism Section is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize Hydrocarbon-stapled Apolipoprotein Peptide Mimetics for the Treatment of Cardiovascular Diseases and Inflammation. For collaboration opportunities, please contact Denise Crooks, Ph.D. at crooksd@nhlbi.nih.gov.


Licensing Contact:
Michael Shmilovich, J.D.
Email: shmilovm@mail.nih.gov
Phone: 301-435-5019

OTT Reference No: E-126-2011-0
Updated: May 7, 2013