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Press Release: 4SC reports positive topline data from clinical Phase I trial with 4SC-205 in cancer patients using novel continuous dosing scheme - Seite 2

achieve and maintain permanent therapeutically active levels of the drug in
patients while keeping side effects tolerable at the same time. The oral
availability of 4SC-205 and its mechanism of action as a potential cell
division inhibitor make this dosing scheme promising from a scientific and
clinical perspective. To the knowledge of the company, 4SC-205 is the first
Eg5 inhibitor that has been clinically evaluated in patients in this dosing
scheme to date.

All primary objectives of the study amendment have been achieved. Alongside
very good linear pharmacokinetic parameters, a comprehensive safety and
tolerability profile was established for 4SC-205. The continuous daily
dosage of 20 mg of the compound showed promising initial signs of efficacy
and is recommended as the dosage regimen for potential Phase II
development. Currently one patient whose previously strongly pronounced and
highly aggressive cancer has been stabilised for eight months now is still
continuing study treatment. 4SC will now proceed to discuss the results
with external clinical key opinion leaders and potential partners, so as to
assess further development options for 4SC-205 - such as a clinical Phase
II trial.

Detailed results of the study amendment: extensive safety profile
established; dosage regimen proposed for Phase II development showing
promising efficacy signals

In the metronomic dosing scheme investigated in the study amendment, the
patients were continuously treated (i.e. without breaks between treatment
days) in three separate dosage groups that received daily doses of 10 mg,
20 mg or 30 mg of 4SC-205 respectively. The main study objective was to
identify the maximum tolerated dose (MTD) for the treatment and potential
dose-limiting toxicities (DLTs). The main study phase to be completed by
all patients according to the study protocol was six weeks, i.e. two
continuous treatment cycles, each of 21 days. After completion of this main
phase, the follow-up phase then allowed patients benefiting from the
treatment - in the form of a stabilisation of their previously progressive
cancers - to continue the treatment.

In these patients, the MTD was established as a daily dose of continuous 20
mg. The DLT was determined at a continuous daily dose of 30 mg of 4SC-205.
Primary side effects at DLT level were neutropenia (level 3-4). Moreover,
4SC-205 showed a very good pharmacokinetic profile with a dose proportional
increase of exposure and an elimination half-life of about ten hours
providing the basis for effective dosing schedules.

4SC recommends the daily dose of 20 mg in the metronomic treatment regimen