tinostamustine

Tinostamustine is a first-in-class, bifunctional small molecule drug that combines an alkylating agent (bendamustine) with a pan-histone deacetylase inhibitor (vorinostat) in a single fusion molecule. This dual mechanism enables tinostamustine to both alkylate and cross-link DNA, causing direct DNA damage, while simultaneously inhibiting histone deacetylases (HDACs), which leads to chromatin relaxation and increased accessibility of the DNA to the alkylating component. The HDAC inhibition also interferes with cancer cell repair mechanisms and promotes apoptosis. Tinostamustine is being developed primarily for hematological malignancies such as T-cell prolymphocytic leukemia (T-PLL), multiple myeloma, Hodgkin lymphoma, peripheral T-cell lymphoma, cutaneous T-cell lymphoma, as well as for solid tumors including glioblastoma multiforme and various advanced/metastatic cancers like soft tissue sarcoma, small cell lung cancer, triple-negative breast cancer, ovarian cancer, endometrial cancer. It has received orphan drug designation for T-cell prolymphocytic leukemia[1][4][5][6][7][8].

Other names

bendamustine-vorinostat fusion molecule