GSK2254233A

GSK2254233A is a small molecule inhibitor of focal adhesion kinase (FAK), a non-receptor tyrosine kinase also known as protein tyrosine kinase 2 (PTK2). Developed by GSK, the compound was designed to target the ATP-binding site of FAK, thereby inhibiting its autophosphorylation and downstream signaling. FAK is a key mediator in the signaling pathways initiated by integrins and growth factor receptors, playing a vital role in regulating cell adhesion, migration, invasion, and survival—processes that are frequently dysregulated in malignant cells. GSK2254233A was evaluated in a Phase 1 clinical trial for patients with advanced solid tumors to assess its safety, pharmacokinetics, and pharmacodynamics. However, the clinical development of GSK2254233A was terminated by the sponsor in 2012 following a strategic review of their oncology pipeline, in favor of other candidates such as the sibling FAK inhibitor GSK2256098.