terbogrel

Terbogrel is a small molecule, dual-acting thromboxane pathway modulator developed by Boehringer Ingelheim for the treatment of primary pulmonary hypertension (PPH). It functions as both an inhibitor of thromboxane-A synthase (TBXAS1) and an antagonist of the thromboxane A2 receptor (TBXA2R). By targeting both the production and the receptor-mediated effects of thromboxane A2, terbogrel was intended to reduce pulmonary vasoconstriction and platelet aggregation. Furthermore, the inhibition of thromboxane synthase was hypothesized to shunt prostaglandin endoperoxide intermediates toward the production of prostacyclin (PGI2), a potent vasodilator. Clinical development reached Phase 2, but the program was discontinued due to a high incidence of leg pain (cramps) in treated patients. This adverse event was significant enough to confound the primary efficacy endpoint, which was the change in six-minute walk distance.

Brand names

terbogrel

Other names

Terbogrel