Nucleoside Analogs an Essential Class of Medicines
Nucleoside analogs represent one of the most important classes of medicine for the treatment of patients with cancer, infectious and autoimmune diseases. There are 38 FDA approved nucleoside analogs covering more than 100 indications.
Nucleoside analogs are central to the treatment of many solid and hematological tumors and will remain so for the foreseeable future, however their utility is limited by their inability to generate anti-cancer metabolites and their off-target toxicity.
Nucleoside analogs have several shortcomings.
ProTides: A New Era in Medicine
Our proprietary ProTide technology was invented by our late Chief Scientific Officer, Professor Christopher McGuigan, who conceived of and filed the original composition of matter patents for our initial ProTides. The unique feature of his discovery was the specific combination of aryl, ester and amino acid motifs that protect the phosphorylated (pre-activated) nucleoside analogs and facilitate entry into cancer cells. This phosphoramidate chemistry approach is the key to the ProTide technology. Every ProTide is distinct, Professor McGuigan with his team synthesized and tested thousands of compounds to identify the optimal ProTide phosphoramidate for each nucleoside analog.
Professor McGuigan’s work helped lead to the development of several FDA-approved anti-viral ProTides, including Gilead’s sofosbuvir, or Sovaldi®, tenofovir alafenamide fumarate, or TAF, a ProTide transformation of tenofovir or Viread® and remdesivir or Veklury®. Notably, the Sovaldi and TAF franchises were two of the most successful drug launches in the history of medicine as measured by first twelve months revenue post-launch.
Harnessing the Power of Phosphoramidate Chemistry
We are utilizing our proprietary phosphoramidate technology to develop more effective and safer anti-cancer medicines. Our ProTides are designed to overcome the shortcomings of nucleoside analogs, to generate much higher concentrations of the active anti-cancer metabolites in cancer cells and avoid the off-target toxicity associated with nucleoside analogs.
Unlike nucleoside analogs, ProTides are not broken down by deaminase and dehydrogenase enzymes. This makes ProTides more stable and improves their pharmacokinetic profile while also reducing the generation of toxic by-products that result from the breakdown of nucleoside analogs. Each of our ProTides is a distinct anti-cancer agent, with a different parent nucleoside analog, a specific phosphoramidate motif, a differentiated mode of action, and different target indications.