Abstract: Thrombotic diseases are common in clinical practice, and thrombolytic agents play a key role in the treatment during the acute period. Thrombolytic agents have developed rapidly since the discovery of streptokinase in 1933. The efficacy and safety of thrombolysis have been improved significantly as the agents progressed from the early generation without fibrin specificity to the current generation of gene recombinant drugs. With continuous exploration in clinical practice, thrombolytic agents that are used widely in the treatment during the acute period of thrombotic diseases are the key to reduce disability and mortality. However, current existing thrombolytic agents still have disadvantages such as severe bleeding, limited recanalization, short half-life, immunogenicity, high price, and so on. It still needs to explore new breakthroughs in the future.