Technology Bundle ID

Stapled Peptides for Treatment of Cardiovascular Diseases and Inflammation

Linked ID
Lead Inventors
Alan Remaley (CC)
David Osei-Hwedieh (NHLBI)
Denis Sviridov (NHLBI)
Imoh Ikpot (NHLBI)
Marcelo Amar (NHLBI)
Development Status
  • Pre-clinical
  • In vitro data available
  • In vivo data available (animal)
Disease Areas
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.
Commercial Applications
  • Treatment of inflammation and cardiovascular diseases, including hyperlipidemia, atherosclerosis, restenosis, and acute coronary syndrome.
  • Inclusion in oral, intravenous or transdermal peptide formulations.
Competitive Advantages
  • 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.