SHR2554 + itraconazole

SHR2554 + itraconazole is a combination of two drugs: - **SHR2554** is an oral, small-molecule inhibitor that selectively targets enhancer of zeste homolog 2 (EZH2), a histone methyltransferase implicated in the development and progression of various lymphoid malignancies. By inhibiting EZH2, SHR2554 disrupts the methylation of histone H3 at lysine 27 (H3K27me3), leading to cell cycle arrest and apoptosis in cancer cells. It has shown promising antitumor activity in relapsed or refractory lymphomas and is under clinical investigation for several hematologic cancers[1][2][3][5]. - **Itraconazole** is an oral triazole antifungal agent that inhibits fungal ergosterol synthesis by blocking the enzyme 14α-demethylase. It is widely used to treat systemic and superficial fungal infections but has also been explored as an anticancer agent due to its ability to inhibit pathways such as Hedgehog signaling[6][8][10]. The combination "SHR2554 + itraconazole" specifically refers to co-administration for pharmacokinetic studies because itraconazole acts as a strong CYP3A4 inhibitor. Since SHR2554’s metabolism depends on CYP3A4, co-administration with itraconazole significantly increases plasma concentrations of SHR2554 by reducing its metabolic clearance[3]. This combination does not represent a marketed fixed-dose product but rather a regimen used in drug-drug interaction studies.