Drug intelligence / Profile preview

LoDAC + azacitidine + MEC

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

LoDAC + azacitidine + MEC is an experimental combination regimen for the treatment of acute myeloid leukemia (AML). The regimen integrates three components: - **LoDAC (Low-dose cytarabine)**: a cytotoxic antimetabolite (pyrimidine analog) that inhibits DNA synthesis by incorporation into DNA and inhibition of DNA polymerase. - **Azacitidine**: a hypomethylating agent that incorporates into DNA and RNA, inhibiting DNA methyltransferase, leading to hypomethylation of DNA and reactivation of silenced tumor suppressor genes. It also has direct cytotoxic effects on abnormal hematopoietic cells in the bone marrow. - **MEC (mitoxantrone, etoposide, cytarabine)**: a chemotherapy regimen where mitoxantrone is a topoisomerase II inhibitor, etoposide is a topoisomerase II inhibitor causing DNA strand breaks, and cytarabine is as above. This combination leverages multiple mechanisms to exert antileukemic effects, including inhibition of DNA methylation, direct DNA damage, and interference with DNA replication and repair. It is investigated mainly in the context of relapsed or refractory AML, aiming to overcome resistance to single agents and improve remission rates.

02

Targets

TOP2A (DNA topoisomerase II)DNMT (DNA methyltransferase)DNA

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