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Drug intelligence / Profile preview
zandelisib + tazemetostat
- Development stage
- Discontinued
- Lead developer
- MEI Pharma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
zandelisib + tazemetostat is an investigational combination therapy being evaluated for the treatment of relapsed or refractory follicular lymphoma. Zandelisib (formerly ME-401) is an oral, highly selective small molecule inhibitor of the delta isoform of phosphatidylinositol 3-kinase (PI3Kδ), which plays a critical role in the proliferation and survival of B-cell malignancies. Tazemetostat is a first-in-class oral small molecule inhibitor of the histone methyltransferase EZH2 (Enhancer of Zeste Homolog 2), an epigenetic regulator that is frequently mutated or overexpressed in follicular lymphoma. By simultaneously inhibiting the PI3K signaling pathway and modulating epigenetic gene expression, this combination therapy aims to overcome resistance mechanisms and provide synergistic anti-tumor activity. The regimen is currently being studied in a Phase 1/2 clinical trial (NCT05604417) led by Dr. Jacob Soumerai at the Dana-Farber Cancer Institute, with support from MEI Pharma.
- Other names
- zandelisibtazemetostat
02
Targets
EZH2 (Histone-lysine N-methyltransferase EZH2)PIK3CD (Phosphatidylinositol 3-kinase delta)
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