4SC Announces First-in-Man Phase I Results for 4SC-203
News Jan 09, 2011
4SC AG, a drug discovery and development company, has announced successful completion of its First-in- Man Phase I study in healthy volunteers with the multi-target kinase inhibitor 4SC-203.
In this randomized, double-blind, placebo-controlled, Phase I dose escalation study the safety, tolerability, and pharmacokinetics of 4SC-203 was assessed in 60 healthy, male volunteers aged 20 to 46 years. Cohorts of eight subjects each, randomized in a 6:2 ratio (active:placebo), received ascending single intravenous doses of the compound.
The dose range comprised 0.041 to 2.5 mg/kg, which corresponds to a total dose of 2.5 to 150 mg for an individual of 60 kg body weight.
4SC-203 proved to be safe and was well tolerated by all subjects. Only 33% of volunteers experienced adverse events, which were all graded of mild intensity with the exception of three events which were moderate. No dose-dependent increase in the number of Treatment-Emergent Adverse Events and no Serious Adverse Event were observed.
No changes in physical and laboratory parameters were recorded and no target organ toxicity occurred. Pharmacokinetics of 4SC-203 in the investigated concentration range of the applied doses displayed the expected dose-dependent increase, providing an excellent basis for the further clinical development of 4SC-203.
4SC-203 is an intravenously administered, small molecule, multi-target kinase inhibitor. In vitro and in vivo studies have shown a strong selectivity profile against FLT3 and FLT3 mutants. In addition, selectivity was shown against VEGF receptors, which are required for angiogenesis, the formation of new blood vessels necessary for the progression of solid tumours.
The compound is being assessed in further preclinical testing in order to establish its potential in various indications, including the treatment of solid tumours. This compound was discovered in collaboration with ProQinase GmbH, Freiburg, Germany.