Definition

An orally available inhibitor of methionine aminopeptidase II type (MetAP2) with potential antiangiogenic and antineoplastic activities. Upon administration, APL-1202 binds to and reversibly inhibits MetAP2, thereby preventing MetAP2-mediated signal transduction pathways. This may suppress endothelial cell growth and inhibit tumor angiogenesis, resulting in tumor cell death. MetAP2, a member of the dimetallohydrolase family, is upregulated in certain tumor cell types and plays a key role in angiogenesis, proliferation and survival.