The invention relates to inhibitors of the urokinase type plasminogen activator receptor (uPAR). The generated inhibitors are bivalent uPAR ligands containing the receptor binding domains of the extracellular protease urokinase type plasminogen activator (uPA) and of the extracellular matrix protein vitronectin (VN) in different configurations linked by a scaffold. The present invention also refers to the above molecules for use as a medicament in particular for treatment of cancer and for diagnostic purposes.