Use of c-met inhibitors to treat cancers harbouring met mutations

Abstract

This specification relates to c-Met receptor tyrosine kinase ("c-Met") inhibitors and their use in the treatment of cancers characterised by certain MET mutations (e.g. cancers comprising cells that express a MET protein having a MET V1092I, MET H1094L or MET L1195F mutation); the use of MET mutation status to select patients suitable for treatment with a c-Met inhibitor; and to methods of treating cancers comprising cells that are characterised by certain MET mutations with a c-Met inhibitor.

Description

technical field [0001] This specification relates to c-Met receptor tyrosine kinase ("c-Met") inhibitors and their usefulness in the treatment of cancers characterized by certain MET mutations (such as cancers comprising cells expressing MET proteins with MET V1092I, METH1094L or MET L1195F mutation). The specification further relates to the use of MET mutation status to select patients suitable for treatment with c-Met inhibitors, and to methods of treating cancers characterized by certain MET mutations with c-Met inhibitors. Background technique [0002] MET protein, also known as c-Met receptor tyrosine kinase, is a transmembrane receptor essential for embryonic development and wound healing. The MET receptor is normally activated by interaction with its specific ligand, hepatocyte growth factor (HGF), and is the only high affinity cell surface receptor for HGF (Bottaro et al., 1991). MET receptors are deregulated in many types of human malignancies including renal, liv...

AI Technical Summary

Problems solved by technology

The METL1195F mutation was previously reported in papillary RCC patients (Schmidt et al., Nature Genetics 1997, Albiges et al., CCR2014), but functional investigations have not been performed before

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