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Antifibrotic effects of oxetanyl sulfoxides

詳細技術說明

Technology: Currently, there are only two approved therapies for Idiopathic Pulmonary Fibrosis (IPF), pirfenidone and nintedanib, which are minimally effective at slowing the disease. These treatments are not effective at all in halting or reversing the progression of IPF. Therefore, there remains a great need for more effective therapies. Researchers at MUSC and Pitt have found that a novel compound, MMS-350, can significantly reduce pro-fibrotic factors and ECM proteins both in vitro and in vivo. Figure 1 demonstrates that in bleomycin treated mice oral doses of MMS-350 ameliorates fibrosis histologically (A), quantitatively reduces collagen α2I within 5 days of treatment (3B),  results in a large reduction of hydroxyproline levels (3C), reduces weight loss and increases survival (87.5% vs 62.5%). MMS-350 is also useful in preventing, mitigating and/or treating injury caused by radiation exposure.Overview: The pulmonary fibrosis market in the US and EU is projected to be worth more than $1.1B in 2017. A successful pulmonary fibrosis treatment could likely be applied to additional fibrosis diseases, including kidney and liver due to similar disease mechanisms. The hallmark of pulmonary fibrosis is thickening and scarring of the tissue caused by increased deposition of extracellular matrix (ECM) proteins such as collagen and fibronectin. Fibrosis is the final stage of many diseases such as IPF, liver cirrhosis, and certain autoimmune disorders.  Scarring causes irreversible damage that usually leads to low quality of life, transplantation or death.   Applications: Treatment of idiopathic pulmonary fibrosis, treatment of fibroproliferative disorders and systemic sclerosis, treatment or prophylactic for radiation induced damageAdvantages:  Low toxicity, oral bioavailability, high solubility, treat and decrease fibrosis, radioprotector, radiomitigatorKey Words: Fibrosis, scleroderma, IPF, MMS-350, bis-oxetanyl sulfoxide, bleomycin, autoimmune Inventors: Carol Feghali-Bostwick and Peter Wipf       Patent Status: US Patent US 9,676,738 and Divisional US 15/499,535MUSC-FRD Technology ID: P1641

*Abstract

None

*Principal Investigation

Name: Carol Feghali-bostwick, Professor

Department: Rheumatology

Name: Peter Wipf, Distinguished Professor

Department: Chemistry

國家/地區

美國