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Valemetostat

Generic Name
Valemetostat
Drug Type
Small Molecule
Chemical Formula
C26H34ClN3O4
CAS Number
1809336-39-7
Unique Ingredient Identifier
60RD0234VE

FDA Approves Daiichi Sankyo's Dato-DXd for Breast Cancer, Expanding Treatment Options

The FDA has granted approval for Daiichi Sankyo's Dato-DXd for breast cancer treatment, marking the drug's first US approval and second global authorization. This unexpected early approval strengthens the company's market position, with additional potential in non-small-cell lung cancer (NSCLC) treatment on the horizon.

EZH2 Inhibitors Enhance Lymphoma Immunotherapy in Preclinical Models

• EZH2 inhibitors, like tazemetostat and valemetostat, enhance T-cell-based immunotherapies against B-cell non-Hodgkin lymphomas in preclinical models. • Combining EZH2 inhibitors with CAR-T cell therapy led to 100% survival in treated mice, compared to 11 days with CAR-T therapy alone. • EZH2 inhibitors improve immunotherapy by increasing lymphoma cell visibility to T cells and reducing immunosuppressive regulatory T cells. • Clinical trials (NCT05934838 and NCT05994235) are underway to evaluate EZH2 inhibitors with immunotherapies in B-cell lymphomas.

Valemetostat Shows Promise in Relapsed/Refractory Peripheral T-Cell Lymphoma

• A Phase II trial of valemetostat demonstrated a 44% objective response rate in patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). • The median duration of response to valemetostat was 11.9 months, with a median progression-free survival of 5.5 months in PTCL patients. • Valemetostat showed a manageable safety profile, with the most common grade 3 or 4 adverse events being thrombocytopenia, anemia, and neutropenia. • The study suggests valemetostat, a dual EZH1 and EZH2 inhibitor, could be a valuable treatment option for relapsed or refractory PTCL.
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