Ligand id: 9108

Name: ARRY-382

No information available.
Summary of Clinical Use
A dose escalating clinical trial in patients with selected advanced or metastatic cancers (NCT01316822) has been completed. The record relating to this trial on the website was last updated/verified in 2012. More recently Phase 1/2 trial NCT02880371 has begun, to evaluate ARRY-382 in combination with anti-PD-1 checkpoint inhibitor pembrolizumab in adult patients with selected advanced solid tumours.
Mechanism Of Action and Pharmacodynamic Effects
Colony stimulating factor (CSF) 1 drives macrophage-mediated immune suppression in the tumour microenvironment. CSF1R inhibitors, such as ARRY-382 bind to and inhibit the activity of CSF1R. This compound is therefore predicted to inhibit tumour cell proliferation in CSF1R-overexpressing tumours, by inhibiting activity of tumour-associated macrophages (TAMs). CSF-1 plays an essential role in macrophage differentiation and proliferation.