YAP-TEAD inhibitors represent a promising therapeutic strategy to address unmet medical needs.
Our primary oncology program aims to disrupt the interaction between YAP and TEAD, which is an interaction that occurs along the Hippo signalling pathway and plays a key role in the oncogenic process.
In preclinical studies, we observed that our compounds prevented the formation of the YAP/TEAD transcriptional complex, reduced the expression of YAP/TEAD target genes and displayed anti-proliferative effects in cancer cell lines controlled by the Hippo signalling pathway.
Further, in xenograft models, we observed that our compounds inhibited gene expression and cell proliferation in cell lines sensitive to YAP, and were associated with tumour regression, both as a monotherapy and in combination with approved cancer therapies.
We are in the process of selecting an oncology drug development candidate for our Hippo program, with which we anticipate entering pre-clinical development in 2019.