Drug intelligence / Profile preview

SHR2554 + rifampin

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

SHR2554 + rifampin is a combination of two drugs. SHR2554 is an oral, small-molecule inhibitor of enhancer of zeste homolog 2 (EZH2), a histone-lysine methyltransferase involved in epigenetic regulation and oncogenesis. It selectively inhibits both wild-type and mutant EZH2 enzymes, leading to reduced H3K27Me3 levels in lymphoma cells, cell cycle arrest at G1 phase, induction of apoptosis, and inhibition of tumor growth[1][3][5]. Rifampin is a well-known antibiotic that acts as a potent inducer of cytochrome P450 enzymes (notably CYP3A4) and is commonly used to study drug-drug interactions due to its strong effect on hepatic metabolism. The combination may be studied primarily for pharmacokinetic interaction purposes because co-administration with CYP3A4 modulators like rifampin can significantly alter the exposure and efficacy profile of SHR2554[3]. There are no indications that this combination itself has been developed or approved as a therapeutic regimen; rather, it serves as an investigational pairing for understanding metabolic interactions.

02

Targets

RNAP (Bacterial dna-dependent RNA polymerase)EZH2 (Histone-lysine N-methyltransferase EZH2)

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