Sulfasalazine

"目录号: HY-14655

NF-κBAutophagy-

Sulfasalazine是治疗类风湿关节炎和溃疡性结肠炎的药物。

NF-κBAutophagy

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生物活性

Description

Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis.

In Vitro

Treatment of SW620 colon cells with sulfasalazine inhibits TNFα-, LPS-, or phorbol ester-induced NFκB activation. NFκB–dependent transcription is inhibited by sulfasalazine at micro- to millimolar concentrations. TNFα-induced nuclear translocation of NFκB is prevented by sulfasalazine through inhibition of IκBα degradation[1]. Pre‐incubation with 5 mM of sulfasalazine alone significantly increases basal mRNA expression of all pro‐inflammatory cytokines with levels of IL‐6 mRNA increased by 80‐fold compared with vehicle control[2]. Once digested, sulfasalazine is cleaved into sulfapyridine and 5-aminosalicylic acid by colonic bacteria, and the latter, too, is reported to suppress NF-kappaB activity[3].

In Vivo

At low doses (0.25 mM), SAS is able to suppress glioma growth by over 60% compared to untreated controls[3].

Clinical Trial

NCT00637780

Pfizer

Arthritis, Juvenile Rheumatoid

June 2010

Phase 4

NCT01577966

University of Alabama at Birmingham

Brain Tumor

January 2012

NCT01312129

The Mind Research Network

Alcohol Dependence

March 2010

NCT00554203

Boston University

Coronary Artery Disease

July 2003

NCT01198145

Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)

Diarrhea-Gastrointestinal Complications-Unspecified Adult Solid Tumor, Protocol Specific

April 2011

Phase 3

NCT01659242

Singapore General Hospital

Rheumatoid Arthritis

July 2012

Phase 4

NCT01667029

Massachusetts General Hospital

Painful Neuropathy

May 2013

Phase 2

NCT00844142

Charite University, Berlin, Germany-Wyeth is now a wholly owned subsidiary of Pfizer

Moderate to Severe Active Axial Spondyloarthritis

November 2005

Phase 2

NCT03012763

University Medicine Greifswald

Pharmacokinetics-Magnetic Resonance Imaging-Administration, Oral

April 2016

Phase 1

NCT00579878

University of Nebraska

Rheumatoid Arthritis

December 1999

Phase 3

NCT02434861

Tesaro, Inc.

Chemotherapy-induced Nausea and Vomiting

May 2015

Phase 1

NCT02930343

Jawaharlal Institute of Postgraduate Medical Education & Research

Rheumatoid Arthritis

September 2016

Phase 4

NCT02456363

Chung Shan Medical University

Ankylosing Spondylitis

November 2009

Phase 2

NCT02638896

Zhixiang Huang-Health and Family Planning Commission of Guangdong

Ankylosing Spondylitis

January 2016

Phase 4

NCT00405275

VA Office of Research and Development-Canadian Institutes of Health Research (CIHR)-Rheumatoid Arthritis Investigational Network (RAIN)-National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)

Rheumatoid Arthritis

July 2007

NCT02374021

Brigham and Women's Hospital-Columbia University

Arthritis, Rheumatoid

July 2016

Phase 4

NCT00422227

Wyeth is now a wholly owned subsidiary of Pfizer

Rheumatoid Arthritis

June 2007

Phase 4

NCT00259610

University of Alabama at Birmingham-Amgen-Barr Laboratories-Pfizer

Rheumatoid Arthritis

May 2004

Phase 4

NCT00889694

Sun Yat-sen University

Early Ankylosing Spondylitis

October 2008

Phase 2-Phase 3

NCT00521924

Merck Sharp & Dohme Corp.-AESCA Pharma GmbH

Rheumatoid Arthritis

June 2007

Phase 3

NCT01709578

Sanofi

Rheumatoid Arthritis

October 2012

Phase 3

NCT01941095

Hoffmann-La Roche

Rheumatoid Arthritis

November 2013

Phase 3

NCT01768572

Sanofi-Regeneron Pharmaceuticals

Rheumatoid Arthritis

March 2013

Phase 3

NCT02057250

Sanofi-Regeneron Pharmaceuticals

RA

March 2014

Phase 3

NCT02373202

Sanofi-Regeneron Pharmaceuticals

Rheumatoid Arthritis

February 2015

Phase 3

NCT02433184

University of Leeds

Rheumatoid Arthritis

July 2011

Phase 4

NCT01596777

University Medicine Greifswald

Intestinal Obstruction

January 2010

Phase 1

NCT01596764

University Medicine Greifswald

Intestinal Obstruction

May 2011

Phase 1

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References

[1].Wahl C, et al. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J Clin Invest. 1998 Mar 1;101(5):1163-74.

[2].Sykes L, et al. Sulfasalazine augments a pro-inflammatory response in interleukin-1β-stimulated amniocytes and myocytes. Immunology. 2015 Dec;146(4):630-44.

[3].Chung WJ, et al. Sulfasalazine inhibits the growth of primary brain tumors independent of nuclear factor-kappaB. J Neurochem. 2009 Jul;110(1):182-93.

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