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.　Fibirinolytic　system:　an　old　system　as　new　therapeutic　targets　The　fibrinolytic　system　was　originally　identified　to　dissolve　blood　clots,　and　is　shown　to　have　important　roles　in　other　pathological　processes,　including　cancer　progression,　inflammation,　and　thrombosis.　Molecules　or　therapeutics　targeting　fibrinolytic　system　have　been　successfully　used　in　the　clinical　treatments　of　cancer　and　thrombotic　diseases.　The　clinical　studies　and　experimental　models　targeting　fibrinolytic　system　are　reviewed　by　Haili　Lin　at　Sanming　First　Hosipital,　Mingdong　Huang　at　Fuzhou　University　in　China,　and　Peng　Xu　at　A*STAR　in　Singapore　to　demonstrate　fibrinolytic　system　as　novel　therapeutic　targets.　As　an　example,　the　inhibition　of　fibrinolytic　system　protein　can　be　used　to　suppress　cancer　prolifieration　and　metastasis.　This　review　also　discusses　the　potential　therapeutic　effects　of　inhibitiors　of　fibrinolytic　system　on　inflammatory　disorders.