罗米地辛 (Istodax)

概览

Romidepsin is a histone deacetylase (HDAC) inhibitor used to treat cutaneous T-cell lymphoma.

作用机制

Romidepsin is a prodrug, where it becomes active once taken up into the cell. The active metabolite has a free thiol group, which interacts with zinc ions in the active site of class 1 and 2 HDAC enzymes, resulting in inhibition of its enzymatic activity. Certain tumors have over expressed HDACs and downregulated/mutated histone acetyltransferases. This imbalance of HDAC relative to histone acetyltransferase can lead to a decrease in regulatory genes, ensuing tumorigenesis. Inhibition of HDAC may restore normal gene expression in cancer cells and result in cell cycle arrest and apoptosis.

适应症

用于在已接受至少1次既往全身治疗的患者中皮肤T-细胞淋巴瘤的治疗(CTCL)。

• Cutaneous T-Cell Lymphoma (CTCL)