Drug intelligence / Profile preview

5-azacytidine + trastuzumab

Development stage
Preclinical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

This is a combination therapy consisting of 5-azacytidine (also known as azacitidine), a hypomethylating agent and cytidine nucleoside analog, and trastuzumab, a humanized monoclonal antibody targeting the HER2/neu receptor. 5-azacytidine incorporates into DNA and RNA, inhibiting DNA methyltransferase activity, leading to hypomethylation of DNA and reactivation of silenced genes involved in tumor suppression. Trastuzumab binds to the extracellular domain of the HER2/neu receptor (receptor tyrosine-protein kinase erbB-2), inhibiting downstream signaling pathways that promote cell proliferation in HER2-overexpressing cancers. This combination is being explored for potential synergistic antitumor effects by combining epigenetic modulation with targeted immunotherapy.

Other names
5-azacytidine and trastuzumabazacitidine + trastuzumab
02

Targets

DNMT1 (DNA (cytosine-5)-methyltransferase 1)ERBB2 (Erb-b2 receptor tyrosine kinase 2)DNMT3B (DNA (cytosine-5)-methyltransferase 3B)

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