Drug intelligence / Profile preview

volasertib + decitabine

Development stage
Discontinued
Lead developer
Oncoheroes Biosciences
Modality
Small Molecules
Administration
Intravenous
01

Overview

rejuvenative: **Volasertib + decitabine** is an experimental combination therapy evaluated for the treatment of acute myeloid leukemia (AML) in older adults (≥65 years) ineligible for standard intensive chemotherapy. **Volasertib** is a selective, potent small molecule inhibitor of cell-cycle kinase **Polo-like kinase 1 (PLK1)**, leading to mitotic arrest and apoptosis in cancer cells. It also inhibits other related kinases (PLK2 and PLK3) and may inhibit bromodomain and extraterminal family protein BRD4 in vitro. **Decitabine** is a hypomethylating agent that inhibits **DNA (cytosine-5)-methyltransferase**, causing DNA hypomethylation, reactivation of silenced tumor suppressor genes, decreased neoplastic proliferation, and increased expression of tumor suppressors. The combination was tested in phase 1 and early phase 2 trials, showing acceptable safety, determination of maximum tolerated dose, and modest response rates, but studies were **terminated** before reaching advanced development.

02

Targets

DNMT3B (DNA (cytosine-5)-methyltransferase 3B)DNMT3A (DNA methyltransferase 3 alpha)PLK3PLK2 (Polo-like kinase 2)DNMT1 (DNA (cytosine-5)-methyltransferase 1)

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