tazemetostat + acalabrutinib

Tazemetostat + acalabrutinib is an experimental combination therapy consisting of two small molecule drugs: **tazemetostat**, a potent, orally available inhibitor of the enhancer of zeste homolog 2 (EZH2), and **acalabrutinib**, a highly selective second-generation Bruton tyrosine kinase (BTK) inhibitor. Tazemetostat inhibits methylation activity of EZH2, a histone methyltransferase important for B-cell maturation and proliferation; acalabrutinib irreversibly inhibits BTK, blocking B-cell receptor signaling required for malignant B-cell survival and proliferation. Both drugs are investigated individually and in combination for B-cell malignancies, particularly mantle cell lymphoma (MCL) and follicular lymphoma, including populations with acquired resistance to BTK inhibitors.