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HIV Protease Inhibitors, Ritonavir and Saquinavir are Potent Inhibitors of Calcium Activated Neutral Peptidases, Calpains

Posted Jun 09 2010 5:00pm

Description of Invention:
This invention discloses a novel use for compounds that are inhibitors of the HIV Protease: specifically, the invention shows that HIV protease inhibitors are also potent inhibitors of Calcium Activated Neutral Proteases (Calpain). Activation of calpain plays a central role in tissue destructive processes following tissue trauma caused by, for example, stroke, heart attack, brain trauma, and spinal cord injury. Thus specific inhibition of calpain is an important therapeutic target in these disease processes. The estimated total market for these classes of therapeutic agents is on the order $500 million to 1 billion annually. The inventor has specifically demonstrated that in vitro the HIV protease inhibitors ritonavir and saquinavir are also potent inhibitors of calpain. This technology has a variety of practical applications: 1) Existing HIV proteases may be used as calpain inhibitors; 2) Existing HIV protease inhibitors which are FDA approved drugs will require less studies to develop as therapeutics; 3) HIV proteases inhibitors are small molecules with oral availability; 4) Other lead compounds developed as HIV protease inhibitors, but not commercialized, may be reevaluated as calpain inhibitors; 5) HIV protease inhibitors used as calpain inhibitors will not require chronic administration; and 6) calpain inhibitors may address therapeutic areas where there are not current effective therapies.

Paolo B Depetrillo (NIAAA)
Wenshuai Wan (NIAAA)

Patent Status:
HHS, Reference No. E-041-2000/0
US, , Patent No. 6,448,245, Issued 19 Sep 2002
HHS, Reference No. E-041-2000/0

Internal Medicine
Internal Medicine - Therapeutics
Central Nervous System
Central Nervous System - Therapeutics
In-vitro Data

For Additional Information Please Contact:
Fatima Sayyid MHPM
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325 Room 21,
Rockville, MD 20852
United States
Phone: 301-435-4521
Fax: 301-402-0220

Ref No: 1219

Updated: 06/2010

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