Urokinase-type　plasminogen　activator　receptor　(uPAR)　mediates　a　multitude　of　biological　activities,　has　key　roles　in　several　clinical　indications,　including　malignancies　and　inflammation,　and,　thus,　has　attracted　intensive　research　over　the　past　few　decades.　The　pleiotropic　functions　of　uPAR　can　be　attributed　to　its　interaction　with　an　array　of　partners.　Many　inhibitors　have　been　developed　to　intervene　with　the　interaction　of　uPAR　with　these　partners.　Here,　we　review　the　development　of　these　classes　of　uPAR　inhibitor　and　their　inhibitory　mechanisms　to　promote　the　translation　of　these　inhibitors　to　clinical　applications.