Ligand id: 9841

Name: merestinib

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 7
Topological polar surface area 106.31
Molecular weight 552.17
XLogP 6.5
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Merestinib (LY2801653) has reached Phase 2 clinical development as a potential therapeutuc to treat various solid tumours. It is being evaluated as a single agent in Phase 2 clinical trial NCT02920996 (for NSCLC with MET transformation or other advanced solid tumours with NTRK1, 2, or 3 rearrangements), and in combination with other oncotherapeutics in separate trials.
Mechanism Of Action and Pharmacodynamic Effects
The proto-oncogene c-Met is overexpressed or mutated in many tumours where its dysregulated signalling plays key roles in cellular proliferation, survival, invasion, metastasis, and angiogenesis of the developing tumour. Merestinib binds to c-Met and inhibits its signalling capacity.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02920996 Merestinib In Non-Small Cell Lung Cancer And Solid Tumors Phase 2 Interventional Dana-Farber Cancer Institute