ARRY-382

ARRY-382 is a potent, highly selective, orally available small molecule inhibitor of the colony-stimulating factor 1 receptor (CSF1R; also known as cFMS), a receptor tyrosine kinase. By binding to and inhibiting CSF1R, ARRY-382 blocks colony-stimulating factor 1 (CSF1)-mediated signaling. This inhibition disrupts the function and proliferation of tumor-associated macrophages (TAMs) in the tumor microenvironment, potentially reducing immune suppression and inhibiting tumor cell proliferation in cancers that overexpress CSF1R. The drug has been investigated primarily for use in advanced solid tumors, including pancreatic ductal adenocarcinoma, PD-(L)1 inhibitor-refractory tumors, and platinum-resistant ovarian cancer—often in combination with pembrolizumab. Clinical trials have shown that while the combination was generally well tolerated, clinical benefit was limited[2][4][5][8].