Solid tumours remain one of the biggest burdens of disease in the developed world, and at present, surgery remains the gold standard for treating patients with resectable disease. There is mounting evidence that changes in the extracellular matrix are critical in promoting the growth and metastatic dissemination of solid tumours. Particular focus has been on the role of targetable enzymes such as the lysyl oxidase family, which can post-translationally modify the tumour matrix. Lysyl Oxidase-like 2 (LOXL2) is known to be important in normal tissue development and homeostasis, as well as the onset and progression of solid tumours. Here we tested the anti-tumour properties of two generations of novel small molecule LOXL2 inhibitor in the MDA-MB-231 human model of breast cancer (1). We confirmed a functional role for LOXL2 activity in the progression of primary breast cancer. Inhibition of LOXL2 activity inhibited the growth of primary tumours and reduced primary tumour angiogenesis. Dual inhibition of LOXL2 and LOX showed a greater effect and also led to a lower overall metastatic burden in the lung and liver. Our data provides the first evidence to support a role for LOXL2 specific small molecule inhibitors as a potential therapy in breast cancer.