SHR2554 + fluconazole

**SHR2554 + fluconazole** is a combination of an oral enhancer of zeste homolog 2 (EZH2) inhibitor, SHR2554, and the antifungal agent fluconazole. SHR2554 is a highly selective, small molecule inhibitor targeting EZH2, an epigenetic regulator implicated in various hematologic and solid tumors. Its primary mechanism involves inhibiting wild-type and mutant EZH2, thereby reducing H3K27me3 levels, promoting G1 cell cycle arrest, and inducing apoptosis in cancer cells. Fluconazole is a moderate inhibitor of CYP3A4; when administered concurrently, it significantly increases the systemic exposure (Cmax and AUC) of SHR2554 due to inhibition of its metabolism via CYP3A4. This combination is being investigated primarily to understand drug-drug interactions and optimize dosing strategies for oncology patients who may require both drugs for fungal infection prophylaxis or treatment and cancer therapy[1].

Other names

SHR2554 + fluconazoleSHR2554 and fluconazoleSHR-2554 and fluconazoleSHR 2554 and fluconazole