FOG-001

Our unique Helicon™ technology is designed to interrupt the Wnt/β-catenin pathway in a way that others have thus far been unable to do, resulting in a drug that is uniquely suited to address one of the fundamental drivers of colorectal cancer and other tumor types.

The investigational therapy FOG-001 is a first-in-class competitive inhibitor — and the only direct inhibitor — of β-catenin interactions with the T-cell factor (TCF) family of transcription factors. By directly targeting the β-catenin:TCF protein-protein interaction, the most downstream node in the Wnt pathway, FOG-001 is intended to block the Wnt signaling pathway irrespective of the particular mutations driving disease (including APC and β-catenin).

We believe that a true functional inhibitor of the β-catenin:TCF interaction, which have been identified as an obligate pair driving tumors, may lead to significant efficacy for patients with Wnt/β-catenin-driven tumors, and that FOG-001 holds potential as both a monotherapy and in combinations.

FOG-001 combines key features that distinguish it from previously reported Wnt/β-catenin pathway modulators: FOG-001 acts inside the cell where it binds directly to the key oncogenic driver β-catenin; and FOG-001 blocks the Wnt pathway at the most downstream node, disrupting the interaction between β-catenin and the transcription factor TCF, thereby abrogating the signal transmission by which Wnt pathway mutations are believed to drive oncogenesis.

FOG-001 is currently being evaluated in a first-in-human Phase 1/2 clinical trial in patients with locally advanced or metastatic solid tumors.