CONCO

Work Package Leader: George MILJANICH (Toxinomics Foundation)

Participants: Atheris Laboratories, Toxinomics Foundation, CEA, CNRS, University of Geneva

Pre-Clinical and Drug Development

Pre-clinical studies will be conducted on at least one extremely promising lead compound (XEP-018, patent pending) already identified by two partners of this Consortium. During the first year a scale-up process will be developed to synthesise this lead compound in large amounts and submit it to in-depth repeated bioassay screenings and lead optimisation.

In parallel, various cone snail venoms will be screened for structurally related analogues that will be characterised, synthesised and tested comparatively. Once the best compound is selected, it will be evaluated for intellectual property rights and if the project is economically viable it will be further developed under the guidance of experts present on the board of the Toxinomics Foundation. This will include in vitro, ex vivo and in vivo validation on relevant models with efficacy, potency, stability and early toxicity in animal models.

The next steps will ideally be conducted under GLP standards using adequately formulated GMP production batches if the budget allows so. Pre-clinical animal studies with metabolism, genetic toxicity, monitoring, acute and repeated toxicity will be conducted by the Foundation, while analytical PK-ADME studies (pharmacokinetics, absorption, distribution, metabolism and excretion) will be taken in charge by Atheris. This should result in the filing of an Investigational New Drug (IND) in view to phase-I clinical trials. Should the first lead compound not lead to satisfactory results, it is expected to select another lead compound from the discovery programme of the project.

Prof André Ménez, a world leader in the field of bioactive substances originating from animal venoms, will coordinate this workpackage with the help of renowned legal, ethical, regulatory, marketing, pharmaceutical and clinical experts.

- Picture by T. Parel -