|
– A Small Molecule Inhibitor of DHODH and of Interleukin-17 (IL-17) Signalling
Planegg-Martinsried, GERMANY | November 9, 2009 | 4SC AG (Frankfurt, Prime Standard: VSC), a drug discovery and development company, today announced the dosing of the first patient in its Phase IIb trial evaluating the combination of 4SC’s oral, synthetic, disease-modifying anti-rheumatic drug (DMARD) 4SC-101 (formerly SC12267) and methotrexate (MTX) in mild to moderate rheumatoid arthritis (RA) patients.
4SC-101 will be investigated in RA patients in the “COMPONENT” study entitled “A Randomized, Double Blind, Placebo-Controlled, Phase II Study to Evaluate Efficacy, Safety, and Pharmacokinetics of SC12267 (35 mg) in Combination with Methotrexate compared to Methotrexate Alone in Patients with Rheumatoid Arthritis”. This study will primarily evaluate the efficacy of the combination of 4SC-101 and MTX in RA patients, compared to methotrexate alone. The trial will comprise 244 patients in two study arms of 122 patients each. The first arm will receive 4SC-101 (35 mg) plus MTX, while the other group will receive placebo plus MTX. 4SC 101 and MTX will be administered orally for a total study duration of 13 weeks per patient. Patients eligible for the study must have active RA and have received weekly doses of MTX (10 25 mg/week) for a minimum of 3 months prior to Day 1 dosing and have received a stable MTX dose of 10–25 mg/week for at least 6 weeks prior to Day 1 dosing.
The primary endpoint of the study is ACR20, a 20% reduction in the number of swollen and tender joints, and a reduction of 20% in three of the following five parameters: physician’s global assessment of disease, patient’s global assessment of disease, patient’s assessment of pain, C reactive protein or erythrocyte sedimentation rate, and degree of physical disability in Health Assessment Questionnaire (HAQ) score. ACR50, ACR70, DAS28, safety parameters and pharmacokinetics will also be evaluated as secondary endpoints. The study will be performed at 15 rheumatology-experienced trial centres in Poland, Romania, Bulgaria and the Czech Republic. 4SC expects completion of enrolment towards the end of 2010.
Dr Ulrich Dauer, Chief Executive Officer of 4SC commented: “We strongly believe that 4SC-101 has the potential to become the second-line, synthetic DMARD of choice for RA patients responding insufficiently to MTX therapy alone, whilst offering a favourable safety and tolerability profile. Our expectation is based upon promising data generated in a pre-clinical RA model using the combination of 4SC-101 and MTX, and on results obtained in an earlier Phase IIa study using 4SC-101 as mono-therapy treatment in RA patients. I am delighted that 4SC continues to achieve corporate milestones in a timely manner to advance important therapies for patients in need of new treatment options.”
More information about both trials can be found on www.clinicaltrials.gov.
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 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 inflammatory skin conditions. 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 4SC
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 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.
About 4SC
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 IIa exploratory study in inflammatory bowel diseases and is due to commence a Phase IIb study in rheumatoid arthritis. 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. For further information please visit www.4sc.com.
SOURCE: 4SC AG |
