Development episode of tranexamic acid - hemostasis, whitening, and the future

Tranexamic acid is now widely recognized as an extremely versatile drug that is used not only as a hemostatic agent, but also for melasma, skin whitening, and inflammation suppression. Its development has been passed down as an episode of particularly great medical significance and social impact among Japanese pharmaceutical research in the 1960s.

This drug was developed by a doctor and researcher who belonged to the Department of Biochemistry at Okayama University School of Medicine at the time.Dr. Shosuke Okamotoand his wifeDr. Utako OkamotoIt is. In Japan, this is attracting attention as a rare example of a husband and wife developing a drug together.

Origin: Searching for the “key” to stop the bleeding

In the late 1950s, as Japan gradually moved from post-war turmoil to a period of high economic growth, the development of medical care became an urgent need. In particular, there was an urgent need in the medical field to establish a treatment method for massive bleeding during childbirth and surgical operations. Dr. Shosuke Okamoto focused on the mechanism of bleeding and hypothesized that ``the reason why bleeding does not stop within the body is due to excessive fibrinolysis (dissolution of fibrin).''

There is an enzyme called ``plasmin'' in the blood that has the function of dissolving blood clots. However, if this action becomes excessive, bleeding may become unstoppable. This is called "hyperfibrinolysis." Dr. Okamoto thought that by suppressing the action of plasmin, it might be possible to achieve a hemostatic effect.

Improvement from epsilon-aminocaproic acid

This idea itself was advanced at the time, and there was already a drug called ε-aminocaproic acid (EACA) that had a similar effect. However, EACA had problems with side effects and sustainability of effects. As the Okamotos continued their research aimed at creating a safer and more effective antifibrinolytic drug, they made structural improvements to EACA.tranexamic acidsuccessfully synthesized.

Tranexamic acid competitively inhibits the lysine-binding site of plasmin by binding strongly to it. As a result, excessive decomposition of the thrombus is suppressed and a hemostatic effect is exerted. This was an innovative approach to bleeding disorders.

Dramatic effects in obstetrics and gynecology

Tranexamic acid's effectiveness was first demonstrated in the field of obstetrics and gynecology. It is indicated for abnormal bleeding caused by postpartum bleeding, menorrhagia, uterine fibroids, etc., and has shown a clearly higher hemostatic effect compared to conventional treatments. In particular, in many cases, hysterectomies could be avoided, and the drug was highly praised as a ``therapeutic drug that is gentle on women's bodies.''

It has also come to be used to prevent bleeding after surgery, otorhinolaryngology, and dental surgery, and even as an adjunct therapy for hemophilia patients, and its range of indications has expanded dramatically.

“Discovery” as a whitening agent

The potential of tranexamic acid has expanded even further. From the late 1980s to the 1990s, a series of clinical reports showed that oral administration of tranexamic acid was effective in treating melasma and age spots. This is because tranexamic acid prevents pigmentation by suppressing the action of plasminogen activator, which promotes melanin production.

Based on these findings, tranexamic acid has attracted attention not only for medical use but also in the cosmetics and whitening supplement industries. Currently, in addition to oral medicines prescribed by doctors, it is also applied to OTC medicines and cosmetics.

Expansion to the world and now

Tranexamic acid has since been approved around the world, and has received high praise internationally as a ``life-saving drug'' as a hemostatic agent, used to treat massive bleeding caused by trauma, and even on the battlefield and in emergency rescue settings. In particular, its inclusion on the ``list of essential medicines'' by the World Health Organization (WHO) demonstrated its usefulness and reliability to the world.

In conclusion

Tranexamic acid is an extremely unique drug in that a single molecule has multiple effects such as ``hemostasis'', ``inhibition of inflammation'', and ``whitening''. Behind its development were the Okamotos' persistent research and the pure desire of medical professionals to ``create a drug that can save someone's life.''

This drug, which continues to be active at the forefront of medical care more than 60 years later, is the pride of Japanese pharmaceutical research and holds many possibilities for the future.