Pressemitteilung BoxID: 134829 (4SC AG)
  • 4SC AG
  • Fraunhoferstr. 22
  • 82152 Planegg-Martinsried
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  • Yvonne Alexander
  • +49 (89) 700763-66

European Patent Granted for the Small-Molecule 4SC-101

A DHODH and Interleukin-17 Inhibitor in Rheumatoid Arthritis and Inflammatory Bowel Disease

(lifePR) (Planegg-Martinsried, Germany, ) 4SC AG (Frankfurt, Prime Standard: VSC), a drug discovery and development company, today announced that the European Patent Office has granted patent EP1392642, which covers its lead auto-immune compound 4SC-101. This small molecule is a DHODH and IL-17 inhibitor which is currently in Phase II trials in rheumatoid arthritis and inflammatory bowel disease.

The patent, entitled "novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents" protects the manufacturing, composition of matter and use in diseases of a novel group of compounds which inhibit DHODH, including 4SC-101. 4SC has already obtained a patent for 4SC-101 from the United States Patent and Trademark office, which was issued in 2006. In addition, patents have been granted in Canada, Russia, New Zealand, South Africa and Mexico.

Ulrich Dauer, CEO of 4SC, commented: "We are pleased to have now received a European patent to cover the composition of matter of our lead auto-immune compound 4SC-101, in addition to the already granted US patent, securing us complete protection of exclusivity and freedom to operate. We look forward to an exciting year in 2010, as we are expecting clinical results for this small-molecule in an exploratory Phase IIa study in inflammatory bowel disease, as well as in a Phase IIb study in rheumatoid arthritis, firmly positioning us in the small-molecule space within these growing indications."

About 4SC-101

4SC-101 is a novel, orally administered small molecule that is classified as a synthetic DMARD as it aims to slow the disease progression of rheumatoid arthritis. The compound also has broad therapeutic potential in other autoimmune diseases such as inflammatory bowel disease, multiple sclerosis and psoriasis. 4SC-101 inhibits dihydroorotate dehydrogenase (DHODH), which acts as a highly selective inhibitor of the biosynthesis of pyrimidines, thereby halting the proliferation of rapidly multiplying cells, in particular of lymphocytes which are involved in the pathology of autoimmune disorders. 4SC also recently demonstrated in pre-clinical tests that 4SC-101 inhibits the expression of IL-17, a pro-inflammatory cytokine that has a pathogenic role in autoimmune disorders.

About Rheumatoid Arthritis

Rheumatoid Arthritis is a chronic inflammatory joint disease that afflicts 0.5 - 1% of the population; women are three times more likely to get arthritis than men. In the late stage of the disease, irreversible damage to joint cartilage and bones occurs. Causes of this disease are genetic as well as autoimmune factors. Besides pain-relieving medicines, so-called disease-modifying medicines (DMARDs = disease modifying anti-rheumatic drugs) can be used in treatment. They differ from other groups of drugs used in the treatment of rheumatoid diseases, since only they are able to stop or reduce damage caused from chronic inflammation to the joint cartilage or bone. In the most favourable cases, some DMARDs can also induce repair of damage to joints and provide support for the repair of changes that have already occurred. DMARDS can be synthetic small molecules or antibodies.

About Inflammatory Bowel Disease

Inflammatory bowel disease (IBD) is a group of inflammatory conditions of the gastrointestinal tract. The main forms of IBD are Crohn's disease and ulcerative colitis, chronic diseases which are constituted by acute-disease flare ups and symptom-free phases. IBD patients suffer from abdominal pain, rectal bleeding, diarrhea, weight loss, fatigue and other extra-intestinal symptoms. Although the causes of IBD are not completely understood, it is assumed that a disregulated immune response results in inflammatory mediators, such as IL-17, that attack the patient's intestinal mucosa and trigger the symptoms. Crohn's disease is characterised by an inflammatory affliction of part of or the whole digestive tract, while ulcerative colitis is a disease of the colon and the rectum only. IBD leads to a considerable reduction in quality of life, but may also involve severe complications requiring immediate surgery. Current therapeutic options for patients are largely limited to the use of anti-inflammatory steroids applied either systemically or locally for the treatment of the symptoms, as well as biological (anti-TNF-alpha) agents.

Legal Note

This document may contain projections or estimates relating to plans and objectives relating to our future operations, products, or services; future financial results; or assumptions underlying or relating to any such statements; each of which constitutes a forward-looking statement subject to risks and uncertainties, many of which are beyond our control. Actual results could differ materially, depending on a number of factors.


4SC AG (ISIN DE0005753818) is a drug discovery and development company focused on autoimmune and cancer indications. The company currently has three clinical programs, with three further clinical trials planned to commence in 2009. 4SC-101, a small molecule, is in a Phase IIb study in rheumatoid arthritis as well as in a Phase IIa exploratory study in inflammatory bowel disease. The company's lead oncology compound, 4SC-201, a histone deacetylase (HDAC) inhibitor, is in a Phase II trial in hepatocellular carcinoma and is due to commence a further Phase II trial in Hodgkin's lymphoma in 2009. Drug candidates are developed until proof-of-concept in order to generate value creating partnerships with the pharmaceutical industry in return for advance and milestone payments as well as royalties.

4SC was founded in 1997, has 93 employees, and is listed on the Prime Standard of the Frankfurt Stock Exchange since December 2005.

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