Tranexamic acid is an amino acid that is considered an analog of lysine. It is widely used in medicine as a hemostatic agent (stops or prevents bleeding) that inhibits the activation of the active site of plasmin. Plasmin is a protein, an enzyme in the blood that breaks down many plasma proteins, including fibrin, exhibiting anticoagulant action.
Besides the anticoagulant effect, plasmin stimulates the growth of melanocytes, melanin-producing cells. In addition, it promotes the synthesis of arachidonic acid, a precursor of prostaglandins and leukotrienes, which stimulate melanin production. So, plasmin has a considerable dual effect on melanin production.
As a plasmin antagonist, Tranexamic acid lessens melanin production and fights against hyperpigmentation, dark spots, and other discolorations. It is a well-studied, safe, and effective ingredient for topical applications. Combined with other skin whitening agents, especially Tranexamic acid and Niacin (vitamin B3) derivatives Tranexamoyl- and Nicotinyl-peptides, it potentiates their effect and improves skin whitening effectivity of the entire formulation.