tirazamine

Tirazamine is a hypoxia-activated prodrug (HAP) developed by Hangzhou Ruizhen Pharmaceutical for the treatment of intermediate-stage hepatocellular carcinoma (HCC). The drug is specifically designed for administration via transarterial injection followed by hepatic artery embolization, a procedure termed TATE (Transarterial Tirazamine Injection followed by Embolization). In the hypoxic environment induced by the embolization of the tumor's blood supply, tirazamine is enzymatically reduced by intracellular reductases to form a highly reactive benzotriazinyl radical. This radical induces lethal DNA double-strand breaks, selectively targeting tumor cells within the hypoxic core of the lesion while sparing well-oxygenated healthy tissues. Tirazamine is currently being evaluated in a randomized Phase II/III clinical trial in China (CTR20243479) comparing TATE with tirazamine to conventional transarterial chemoembolization (TACE) using epirubicin.

Other names

提拉扎明