A highly-promising family of antiviral and anticancer molecules

Introduction

The prodrug concept dictates that a pharmacological substance is administrated under an inactive form made up of two main components: the drug itself and a vector able to deliver the drug to the target cell. Once in the cell, the chemical bond between the vector and the drug is cleaved via in vivo metabolisation, thus releasing the active drug towards the target. This principle enhances the selectivity of the drug and reduces its toxicity towards non-target cells.

Novel Synthesis Pathway

Researchers at the Molecular Pharmacochemistry Department (Université Joseph Fourier, Grenoble-1) have recently developed a synthesis pathway giving access to a novel class of antiviral or antitumoral thionucleoside prodrugs. In the cell, these compounds compete with the natural primary substrate of DNA and RNA synthesis, therefore inhibiting cell proliferation. Such a mechanism can therefore potentially lead to many promising anti-viral and anti cancer applications. To date, this novel family has been successfully tested on HIV infected human cells and tumoral cell lines.

Features

Benefits

With many anti-cancer and HIV treatments becoming less and less effective as a result of drug resistance, this technology demonstrates considerable potential as a means of creating novel antiviral or anticancer drugs.

Key laboratory results (novel molecules originating from this process):

High efficacy demonstrated on

- HIV infected human cells, with EC₅₀ averaging 5-10 µM

- human cancer cells, with CC₅₀ averaging 10-20 µM

Intellectual Property

The synthesis pathway, associated molecules and their use in pharmaceutical preparations for the treatment of viral infections and cancers are covered by a European patent application # PCT/FR2007/001784.

Technology Status

Floralis is currently looking for partners to further develop this promising technology which demonstrates significant potential in the development of antiviral and anticancer molecules.

Contacts

Mathieu TILQUIN
(Technology Transfer)
+33(0)4 76 00 78 41
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