Government-Owned Inventions; Availability for Licensing
The inventions listed below are owned by an agency of the U.S. Government and are available for licensing to achieve expeditious commercialization of results of federally-funded...
The inventions listed below are owned by an agency of the U.S. Government and are available for licensing to achieve expeditious commercialization of results of federally-funded research for the benefit of the public health.
FOR FURTHER INFORMATION CONTACT:
Licensing information may be obtained by communicating with Vidita Choudhry, Ph.D., National Heart, Lung, and Blood, Office of Technology Transfer and Development, 31 Center Drive Room 4A25, MSC2479, Bethesda, MD 20892-2479; telephone: 301-594-4095; email:
vidita.choudhry@nih.gov. A signed Confidential Disclosure Agreement may be required to receive any unpublished information.
SUPPLEMENTARY INFORMATION:
Technology description follows.
Novel Spironolactone Analogues as Anti-Inflammatory Therapeutics
Available for licensing and commercial development are patent rights covering a new class of spironolactone anti-inflammatory drugs, pharmaceutical compositions thereof, and their uses in treating inflammation. These new compounds present treatment options for treating a broad range of chronic inflammatory conditions such as atherosclerosis, autoimmune diseases, and chronic inflammatory lung disease.
Inflammation contributes to many forms of acute and chronic diseases such as cardiovascular disease and chronic respiratory disease, which result in a substantial percent of mortality worldwide. There is still need for clinically approved therapeutic strategies that effectively reduce pathologic inflammation. One promising candidate is Spironolactone (SPL), a mineralocorticoid receptor antagonist that was originally utilized by NIH investigators against pulmonary arterial hypertension. It has become recently elucidated that SPL suppresses inflammation by promoting proteasomal degradation of xeroderma pigmentosum type B (XPB), an integral subunit of the transcription factor TFIIH that activates inflammatory genes. Researchers at the National Heart, Lung, and Blood Institute (NHLBI) have developed twenty-nine (29) different SPL-based analogues, all of which demonstrate an effective potency at safe dosage levels, making them advantageous compared to known SPLs. Several lead compounds demonstrate potent, dose-dependent XPB degradation and inhibition of key inflammatory signaling pathways, including AP-1 and NF-kB, at concentrations significantly lower than those required for SPL. These analogs may be useful for treating multiple inflammatory disease and related conditions without deleterious side effects.
Potential Commercial Applications:
A class of novel anti-inflammatory drugs (long-term immunosuppressants) for the treatment for a wide variety of inflammatory disorders, such as (but not limited to):
Pulmonary arterial hypertension
Atherosclerosis
Lupus erythematosus
Rheumatoid arthritis
Chronic obstructive pulmonary disease (COPD)
Asthma
Development Stage:
Early Stage
In vitro data available
Inventors:
Jason Elinoff (NHLBI), Li-Yuan Chen (NHLBI), Rolf Swenson (NHLBI), and Venkatareddy Sabbasani (NHLBI).
Intellectual Property:
NIH Reference No. E-029-2026-0-US-01; U.S. Provisional Patent Application 64/044,506 filed April 20, 2026.
35 U.S.C. 209
37 CFR part 404