We show that Enz transcriptionally inhibits u-PAR gene expression, downregulates the tumour progression-related molecules HIF1α and VEGFC, and also upregulates the tumour-suppressor genes VHL, RASSF1, and FHIT. Furthermore, our findings suggest that an si-u-PAR/sh-u-PAR knockdown sensitises resistant NSCLC cells to Enz and induces apoptosis. This evidence concerns the gene HIF1A and neoplasm.