The original S42909 compound has been submitted to numerous preclinical evaluations to assess safety. No safety alerts have been identified using a standard battery of tests including receptor binding, CNS, cardiovascular and reparatory function. Furthermore, there were no target organs for toxicity identified in repeated dose toxicity studies up to 26 weeks PO in rats and up to 39 weeks in dogs. S42909 demonstrated no mutagenic potential with/without metabolic activation in vitro and no clastogenic effect in vivo. No embryotoxicity nor teratogenicity were identified as well.

Seven (7) Phase I clinical studies have been completed using several formulations of S42909 during the first stage of clinical development. Up to 259 healthy male volunteers received S42909 in the above trials and overall, no safety concerns arose from the phase I clinical trials and no potential or identified risks have been detected for S42909 during this phase of development.

In order to assess the therapeutic effectiveness of S42909 in treating venous leg ulcers (VLU), a Phase IIa (POC) was conducted. In this trial, the primary objective was to look at the overall dose-response relationship with S42909 on improving healing of VLU, on top of standard of care (compression and local wound care) after 4 weeks of treatment.

Future Development Opportunities

Development of several analogs of S42909. These analogs would be subject to a plethora of preclinical evaluations with the objective to improve the inherent properties of the molecule with regards to solubility and bioavailability. In parallel, these new chemical entities will be used in different formulations in a concerted effort to improve the therapeutic effectiveness of these compound in treating venous leg ulcers.

Based on in vitro and in vivo models on wound healing and ischemia/reperfusion, S42909 is expected to improve ulcer healing through its main effect on microcirculation. Consequently, S42909 can be looked at improving diabetic foot ulcers, mixed venous/arterial disease, as well as pressure ulcers (bed sores).