Dienstag, 20. März 2018

  • Pressemitteilung BoxID 145976

4SC Announces Treatment of First Patient in a Phase I Study of 4SC-205

Oral Eg5 kinesin spindle protein inhibitor to be evaluated in solid tumour and malignant lymphoma patients

anegg-Martinsried, Germany, (lifePR) - 4SC AG (Frankfurt, Prime Standard: VSC) a drug discovery and development company focused on autoimmune and cancer indications, today announced the first treatment in a Phase I study evaluating 4SC-205, an oral Eg5 kinesin spindle protein inhibitor, in patients with solid tumours or malignant lymphomas.

This firstinman Phase I, open label, dose escalation trial, the "AEGIS" study, in patients to investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of orally administered 4SC-205. Six dosage cohorts (3+3 design) will be enrolled and patients will be treated for two to three week treatment cycles with dosing on days one and eight of each cycle. After six weeks of treatment patients will undergo radiological disease assessments. Patients may remain on therapy beyond the initial two therapy cycles as long as they tolerate the treatment and do not demonstrate progressive disease. The study will be performed in two centres in Germany and is expected to report results in 2011.

4SC-205 is an oral inhibitor of the kinesin spindle protein Eg5 (also known as kinesin-5, KIF11), a motor protein that has been shown to be of crucial importance for proper cell division (mitosis) by mediating chromosome separation to the daughter cells. Inhibition of Eg5 leads to cell cycle arrest by interfering with microtubules, a component of the mitosis machinery, leading to apoptosis (programmed cell death). Other antimitotic agents which directly target microtubules, such as taxanes, are used extensively as chemotherapeutics, however, these also frequently lead to severe peripheral neurological sideeffects. In contrast, targeting Eg5 is expected to provide an improved safety profile since its expression has been described to be confined to actively dividing (proliferating) cells. Therefore, 4SC-205 has the potential to generate a therapeutic effect analogous to other antimitotic drugs yet avoiding peripheral nerve damage commonly seen after taxane chemotherapy.

In preclinical studies 4SC-205 displayed encouraging antitumour activity in several in vitro and in vivo models.

Dr Bernd Hentsch, Chief Development Officer of 4SC commented, "With the commencement of this trial, we have now extended our oncology pipeline to include a third compound. This antimitotic agent, based on earlier preclinical results, could be positioned in a variety of cancer indications. Over the last twelve months 4SC has now established a strong, clinical stage oncology franchise investigating multiple, innovative approaches for the treatment of both solid and haematological cancers."

More information about this trial can be found on www.clinicaltrials.gov.

About 4SC-205

4SC-205 is a small molecule inhibitor of the human kinesin spindle protein Eg5 which is of crucial importance for proper cell division (mitosis). Eg5 interacts with microtubules, a component of the cellular mitosis machinery, and mediates the segregation of the two spindle poles resulting in the correct distribution of the chromosomes to the daughter cells. Inhibition of Eg5 leads to cell cycle arrest in mitosis und subsequent programmed cell death (apoptosis). Mitosis is the fundamental process leading to cell division and tissue proliferation. The mitotic spindle apparatus has been for decades a primary target for the development of antimitotic agents such as the taxanes and vinca alkaloids which are broadly used in cancer therapies as single chemotherapeutic agents or in combination. In preclinical tests 4SC-205 has proven to be a particularly effective inhibitor of tumour cell proliferation of various cancer origins, both in vitro and in vivo.

About 4SC

4SC AG (ISIN DE0005753818) is a drug discovery and development company focused on autoimmune and cancer indications. Vidofludimus (4SC-101), a small molecule, is currently in a Phase IIb study in rheumatoid arthritis and a Phase IIa exploratory study in inflammatory bowel disease. The company's lead oncology compound, resminostat (4SC-201), a pan histone deacetylase (HDAC) inhibitor, is in Phase II trials in hepatocellular carcinoma and Hodgkin's lymphoma. Two further oncology compounds, 4SC-203 and 4SC-205 are in Phase I studies. 4SC develops drug candidates until proofofconcept in order to generate value creating partnerships with the pharmaceutical industry in return for advance and milestone payments as well as royalties.

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 forwardlooking 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 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.

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