Definition

An extended-release (ER) formulation of APL-1501, an orally available inhibitor of methionine aminopeptidase II type (MetAP2), with potential antiangiogenic and antineoplastic activities. Upon administration, ER MetAP2 inhibitor APL-1501 is released from the formulation over an extended period of time and targets, 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. Compared to APL-1202, APL-1501 has improved pharmacokinetic (PK) characteristics. The ER formulation allows for controlled drug release, enhanced drug plasma exposure time and reduced medication intake frequency.