Globally, the incidence of thromboembolic diseases has increased in recent years, accompanied by an increase in patient mortality. Currently, several targeting delivery strategies have been developed to treat thromboembolic diseases. In this review, we discuss the mechanisms of thrombolysis and current anticoagulant drugs, particularly those with targeting capability, highlighting advances in the accurate treatment of thrombolysis with fewer adverse effects. Such approaches include magnetic drug-loading systems combined with molecular imaging to recanalize blood vessels and systems based on chimeric Arg-Gly-Asp (RGD) sequences that can target platelet glycoprotein receptor. With such progress in targeted antithrombotic drugs, targeted thrombolysis treatment shows significant potential benefit for patients.