The　function　of　the　fibrinolytic　system　was　first　identified　to　dissolve　fibrin　to　maintain　vascular　patency.　Connections　between　the　fibrinolytic　system　and　many　other　physiological　and　pathological　processes　have　been　well　established.　Dysregulation　of　the　fibrinolytic　system　is　closely　associated　with　multiple　pathological　conditions,　including　thrombosis,　inflammation,　cancer　progression,　and　neuropathies.　Thus,　molecules　in　the　fibrinolytic　system　are　potent　therapeutic　and　diagnostic　targets.　This　review　summarizes　the　currently　used　agents　targeting　this　system　and　the　development　of　novel　therapeutic　strategies　in　experimental　studies.　Future　directions　for　the　development　of　modulators　of　the　fibrinolytic　system　are　also　discussed.　©　2020,　The　Author(s).