Inhibition of tankyrase may expand the capability of Immune checkpoint inhibitors, like the PD-1 receptor, in numerous of tumors including melanoma, non-small cell lung carcinoma, kidney carcinoma and as recent evidence suggests a range of further solid tumors.
We are seeking partners for co-development and licensing of the technology.
The scientists have developed a class of novel WNT inhibitor compounds exhibiting high specificity for tankyrase and demonstrated proof of concept in mouse models for cancer by effectively reducing catenin levels in selected cancer cells by targeting the pathway gate keeper tankyrase . A successful animal POC model shows a statistically relevant additive or synergistic effect of tankyrase inhibition on PD-1/PDL1 immune checkpoint inhibitors in a melanoma model as measured by tumor size.
The lead compound has been extensively characterized by PK/ADME, and for 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.
To further advance the chemotype of the proprietary tankyrase inhibitor to optimized lead/preclinical lead stage, and to show its efficacy in combination with anti PD-1 immune modulators in isogenic, immune-competent mouse melanoma models and a human melanoma cell line panel.
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).
A provisional patent application covering the new leading compounds was filed in December 2016.