Drug intelligence / Profile preview

amsacrine + cytarabine + mitoxantrone

Development stage
Unknown
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Amsacrine + cytarabine + mitoxantrone is a combination chemotherapy regimen used primarily in the treatment of acute myeloid leukemia (AML), particularly for consolidation therapy or in relapsed/refractory cases. Each component has a distinct mechanism of action: - **Amsacrine** is an intercalating agent and topoisomerase II inhibitor, disrupting DNA replication and repair. - **Cytarabine** (also known as Ara-C) is an antimetabolite that inhibits DNA synthesis by acting as a cytosine analog. - **Mitoxantrone** is a synthetic anthracenedione that intercalates into DNA, inhibits topoisomerase II, and induces double-strand breaks, leading to apoptosis. It also has immunosuppressive properties. This multiagent regimen aims to maximize anti-leukemic efficacy by combining drugs with complementary mechanisms. However, studies have shown that while this combination can induce remission in AML patients, it does not significantly improve long-term survival compared to high-dose cytarabine alone and may increase toxicity risks such as gastrointestinal and hepatic side effects[1][2].

02

Targets

TOP2A (DNA topoisomerase II)DNA polymerase familyDNA

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