Drug intelligence / Profile preview

tazemetostat + HMPL-689

Development stage
Unknown
Lead developer
HUTCHMED
Modality
Small Molecules
Administration
Oral
01

Overview

**Tazemetostat + HMPL-689** is an investigational combination therapy used for the treatment of relapsed or refractory lymphoma, including aggressive non-Hodgkin lymphoma and B-cell lymphoma subtypes[1][3][7]. Tazemetostat is a selective small molecule inhibitor of the enhancer-of-zeste-homolog-2 (EZH2), an epigenetic regulator implicated in cancer cell proliferation[7]. HMPL-689, also known as amdizalisib, is a potent and highly selective small molecule inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), a kinase involved in B-cell receptor signaling and the survival of malignant lymphocytes[2][4][7]. Preclinical data demonstrated synergistic anti-tumor effects for the combination, while early clinical results show promising efficacy and a manageable safety profile in lymphoma patients[7].

Other names
ezh2 inhibitor + PI3Kδ inhibitortazemetostat plus amdizalisib
02

Targets

PIK3CD (Phosphatidylinositol 3-kinase delta)EZH2 (Histone-lysine N-methyltransferase EZH2)

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