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4SC Discovery to host Symposium 'Drug Discovery in the Age of Epigenetics' on 24 September 2012

Leading international scientists from industry and academia discuss novel strategies of epigenetic tumour therapy

(lifePR) (Planegg-Martinsried, ) 4SC AG (Frankfurt, Prime Standard: VSC), a discovery and development company of targeted small molecule drugs for autoimmune diseases and cancer, announced today that its fully-owned subsidiary 4SC Discovery GmbH, which specialises in the discovery and early-stage research of novel therapeutic compounds will host a conference on 'Drug Discovery in the Age of Epigenetics' on 24 September 2012.

On the 1-day symposium to be held in Martinsried near Munich, Germany, about 40 selected international scientists from academia and industry (participation on personal invitation only) will discuss questions of the effects of epigenetic modifications on cancer origination and proliferation, and, based on these findings, about novel strategies to effectively treat cancer.

Speakers include some of the leading experts in the field of epigenetic cancer research in Europe: Professor Nick La Thangue (University of Oxford), who will give the key note lecture about 'HDAC inhibitors and predictive biomarkers'; Professor Martin Göttlicher (Helmholtz Institute, Munich); and Professor Steven A. Johnsen from the University Medical Center Hamburg-Eppendorf. The programme will be completed by presentations of industry projects showing promising novel approaches in epigenetic drug discovery and development in oncology, including Dr Ismael Moarefi (Chief Scientific Officer of Crelux), Dr Daniel Vitt (Chief Scientific Officer of 4SC) and Dr Bernd Hentsch (Chief Development Officer of 4SC). The full agenda of the symposium can be viewed at

Epigenetic regulation in tumour cells is a topic which is currently intensively discussed amongst oncologists involved in drug discovery and clinical development, as it opens up unprecedented intervention possibilities for new therapeutic concepts. An altered epigenetic signature is a hallmark of cancer cells. This can be addressed by novel therapeutic substances which reprogram transcription events in aberrant (abnormal) cells. The subsequent alteration of signalling pathways by novel therapies can lead to sensitization to conventional therapeutics and/or to apoptosis (tumour cell death). Moreover, such compounds may allow the pinpoint targeting of cancer stem cells, another emerging topic in oncology. New biomarkers directly monitor the effectiveness of the therapeutic intervention. They may allow for a more reliable stratification of patients (personalised medicine) and a better prediction of the course of disease and the effectiveness of the therapy, as well as additional treatment options. This can provide new opportunities and challenges for the drug discovery and development process which have to be seized and met with a new attitude by the pharmaceutical industry.

Dr Stefan Strobl, Managing Director of 4SC Discovery GmbH, comments: 'We are delighted that we have been able to win such well renowned speakers for this year's symposium, giving us an ideal opportunity for fruitful discussions between academia and industry on the highest scientific level. The symposium will also give us a platform for presenting 4SC's own drug discovery and development activities in this highly innovative field of research, which is currently and in the future definitely one of the most promising in oncology.'

About 4SC's epigenetic research and development portfolio in oncology

4SC is focusing strongly on epigenetic drug research and development and has several epigenetic drug candidates both in clinical development and in early-stage research.

Resminostat (4SC-201), 4SC's lead oncology compound, is an oral pan-histone-deacetylase (HDAC) inhibitor with an innovative epigenetic mechanism of action that potentially enables the compound to be deployed as a novel, targeted tumour therapy for a broad spectrum of oncological indications, as a monotherapy and in particular in combination with other cancer drugs. HDAC inhibitors have been shown to modify the DNA structure of tumour cells to cause their differentiation and programmed cell death (apoptosis) and are therefore considered to offer a mechanism of action that has the particular potential to halt tumour progression and induce tumour regression. Additionally, resminostat is also assumed to induce what is known as tumour cell (re-)sensitisation to other anti-cancer compounds. This process can suppress or reverse certain tolerance and resistance mechanisms which tumour cells often develop against cancer drugs. Therefore, supplementary treatment with resminostat can be expected to restore or significantly improve the efficacy of a previously administered cancer therapy which was no longer effective. Resminostat is currently being investigated in a broad clinical Phase II programme in the three indications liver cancer (hepatocellular carcinoma, HCC), Hodgkin's Lymphoma (HL), and colorectal cancer (CRC).

4SC-202 is the 4SC's second epigenetic drug candidate in clinical development. 4SC-202 is an orally administered selective class I deacetylase (DAC) inhibitor with a unique combination of anti-cancer mode of actions, namely epigenetic regulation and targeting of stemness. Via epigenetic modifications, 4SC-202 particularly mediates modulation of the Wnt signaling pathway and thus provokes the inhibition of properties which are essential for cancer stem cells. Proliferation inhibition with subsequent induction of apoptosis in cancer cell lines is the consequence of a strong G2/M arrest. These properties translate into excellent effectiveness in in vivo cancer models. Currently, 4SC-202 is being investigated in a Phase I clinical study in patients with advanced haematological indications.

Moreover, in its research and drug discovery activities in the field of epigenetics, 4SC Discovery GmbH engages in the discovery of novel drug candidates for several epigenetic targets including peptidyl arginine deiminases (PADs), MSK (mitogen- and stress-activated protein kinase) and protein deacetylase (DAC).

About 4SC Discovery GmbH

4SC Discovery GmbH is a wholly-owned subsidiary of 4SC AG that offers technologies and tailored research services covering drug discovery and chemical optimisation through to a preclinical development candidate. The company focuses its services on offering customers in the pharmaceutical, biotech and chemical industries the cost and time-to-market benefits that result from a drug discovery and optimisation process based on a powerful, computer-aided, screening and discovery platform. In addition, 4SC Discovery also applies its comprehensive pharmacological expertise to investigating new compounds in the areas of cancer and autoimmune disease - a strategy also intended to further enhance the clinical development pipeline for the 4SC Group. 4SC Discovery aims to engage in partnerships with pharmaceutical and biotech companies to accelerate the development of its research programmes and further advance their commercialisation.

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The group managed by 4SC AG discovers and develops targeted small-molecule drugs for the treatment of diseases with a high unmet medical need in various autoimmune and cancer indications. These drugs are intended to provide patients with innovative treatment options that are more tolerable and efficacious than existing therapies, and provide a better quality of life. At the end of June 2012, 4SC Group had 90 employees. The company was founded in 1997. 4SC AG has been listed on the Prime Standard of the Frankfurt Stock Exchange since December 2005.