Medicinal molecules targeting the fibrinolytic system have been successfully used in clinical treatments or have been subjected to clinical trials, including the uPA inhibitor Upamostat for cancer treatment, r-tPA for acute thrombotic diseases, the radioactive uPAR-binding peptide for PET cancer diagnosis, and the plasmin inhibitor aprotinin for postsurgical hemostasis. The gene discussed is PLAU; the disease is cancer.