Tankyrase appears to be the central druggable biotarget in the Wnt/b-catenin signalling pathway, which is involved in a number of malignancies, including cancer. Targeting tankyrase represents a novel therapeutic strategy for cancer, which has attracted substantial industry interest. However, to date, no tankyrase-specific inhibitor has progressed to clinical trials.
We have developed a class of novel compounds exhibiting high specificity for tankyrase and demonstrated proof of concept in relevant animal models for cancer . The most advanced candidate is the industry standard for specific inhibition of tankyrase and is available as a research agent. The compound has been extensively characterized by PK/ADME, and exhibits properties highly suitable for formulation as a topical drug for skin cancers. Other lead compounds are being developed for systemic administration of other cancers and disorders.
The class of molecules is protected by an international patent application (WO 2012/076898A1) which has led to a granted patent in the US (9096587), and is pending in other jurisdictions.