TEQ101 is a small-molecule methionine aminopeptidase 2 (MetAP2) inhibitor licensed from global pharmaceutical company Merck KGaA, Darmstadt, Germany, and represents a novel class of orally available and reversible MetAP2 inhibitors. In vitro and in vivo data have shown a dual anti-tumor effect of TEQ101, inhibiting both cancer cell proliferation and the generation of new blood vessels necessary for tumor growth.