Drug intelligence / Profile preview

bortezomib + decitabine

Development stage
Unknown
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination therapy consisting of the proteasome inhibitor bortezomib and the hypomethylating agent decitabine. This regimen is being investigated for the treatment of acute myeloid leukemia (AML), including relapsed, refractory, or previously untreated cases. Bortezomib inhibits the 26S proteasome, leading to the disruption of protein homeostasis and induction of apoptosis in cancer cells. Decitabine is a cytidine antimetabolite that incorporates into DNA and inhibits DNA methyltransferase, resulting in DNA hypomethylation and the reactivation of tumor suppressor genes. The combination aims to enhance the antileukemic effect through synergistic mechanisms, where proteasome inhibition may sensitize cells to the epigenetic modifications induced by decitabine.

Other names
bortezomib and decitabinedecitabine and bortezomibVelcade and Dacogen
02

Targets

PSMB5 (Proteasome subunit beta Type-5)DNMT1 (DNA (cytosine-5)-methyltransferase 1)DNMT3A (DNA methyltransferase 3 alpha)DNMT3B (DNA (cytosine-5)-methyltransferase 3B)

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