Drug intelligence / Profile preview

tazemetostat + prednisolone

Development stage
Unknown
Lead developer
Ipsen
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

A combination of tazemetostat, an oral selective inhibitor of the histone-lysine N-methyltransferase EZH2 (a component of Polycomb Repressive Complex 2), and prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activity. Tazemetostat is mainly indicated for epithelioid sarcoma, follicular lymphoma, and other B-cell lymphomas, while prednisolone is a standard corticosteroid used in hematologic malignancies and other indications. The combination has been studied in relapsed/refractory diffuse large B-cell lymphoma (DLBCL) in phase 2 settings to determine efficacy and safety. Mechanistically, tazemetostat blocks aberrant histone methylation and may reverse dedifferentiation of cancer cells, while prednisolone exerts antiproliferative and lympholytic effects via glucocorticoid receptor modulation[2][3][4][5].

Other names
tazemetostat and prednisolone
02

Targets

EZH2 (Histone-lysine N-methyltransferase EZH2)GR (Glucocorticoid receptor)EZH1

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