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GSK2256098 is a tablet that blocks an enzyme called FAK, which meningiomas missing the NF2 gene rely on. In the Alliance A071401 trial it slowed progression in recurrent NF2-mutant meningiomas, one of the first positive results for a targeted drug in this tumour.
GSK2256098 is a small-molecule inhibitor of focal adhesion kinase developed by GSK. Loss of NF2 (merlin), the commonest driver in meningioma, makes cells dependent on FAK signalling for growth on and adhesion to their matrix, which preclinical work showed could be exploited.
In Alliance A071401, a genomically guided phase 2 trial that assigns progressive meningiomas to drugs by mutation, the FAK-inhibitor arm for NF2-mutant tumours met its progression-free survival endpoint: six-month progression-free survival was 83 percent for grade 1 and 33 percent for grade 2 to 3 tumours, with good tolerability (Journal of Clinical Oncology, 2023). The meningioma page names it as the first mutation-matched treatment to show activity in the disease.
An ATP-competitive inhibitor of focal adhesion kinase; meningiomas that have lost the NF2 tumour suppressor merlin depend on FAK signalling, so blocking it is a synthetic-lethal approach to NF2-mutant tumours. Connects to FAK (PTK2).
1.GSK2256098 slips into a pocket on FAK (PTK2).
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
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