BT-114143

BT-114143 is a novel, potent small-molecule plasminogen activation inhibitor developed to treat and prevent bleeding conditions caused by hyperfibrinolysis. It features a phosphoric acid functional group and was designed using structure-based drug design with nonclassical bioisosteres. BT-114143 demonstrates significantly higher affinity for human plasminogen than existing antifibrinolytics such as tranexamic acid (TXA) and epsilon-aminocaproic acid (EACA), showing approximately ten-fold greater antifibrinolytic potency compared to TXA in preclinical studies. The drug is being developed primarily for intravenous administration, with additional formulations under development for intramuscular injection to address emergency situations like postpartum hemorrhage, trauma, natural disasters, and battlefield injuries. Preclinical safety has been confirmed in GLP toxicology studies. As of 2025, BT-114143 is undergoing Phase I/Ib clinical trials in China for abnormal uterine bleeding and other hyperfibrinolysis-related bleedings[1][2][3][4][5].