Drug intelligence / Profile preview

azacitidine + trametinib + venetoclax

Development stage
Unknown
Lead developer
University of Texas MD Anderson Cancer Center
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

azacitidine + trametinib + venetoclax is a combination therapy regimen being investigated at the University of Texas M.D. Anderson Cancer Center. It consists of the oral MEK inhibitor trametinib, the hypomethylating agent azacitidine, and the BCL-2 inhibitor venetoclax. This triplet regimen is specifically designed to treat patients with myeloid malignancies, including acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), and chronic myelomonocytic leukemia (CMML), who harbor RAS pathway-activating mutations. By simultaneously inhibiting the MAPK/ERK signaling pathway (via trametinib), blocking the anti-apoptotic protein BCL-2 (via venetoclax), and inducing DNA hypomethylation (via azacitidine), the therapy aims to overcome resistance mechanisms commonly seen in RAS-mutated myeloid cancers.

Other names
Trametinib with Azacitidine and VenetoclaxAzacitidine, Venetoclax and Trametinib
02

Targets

MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)DNMT1 (DNA (cytosine-5)-methyltransferase 1)MCL1 (Myeloid cell leukemia sequence 1)

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