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dexamethasone + idarubicin + cytarabine + methotrexate

Development stage
Preclinical
Lead developer
Merck
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intrathecal, Intravenous, Oral
01

Overview

This is a combination chemotherapy regimen consisting of four drugs—dexamethasone, idarubicin, cytarabine, and methotrexate. Each component has a distinct mechanism of action: - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties. - **Idarubicin** is an anthracycline antibiotic that intercalates DNA and inhibits topoisomerase II, leading to DNA damage and apoptosis in rapidly dividing cells. - **Cytarabine (Ara-C)** is an antimetabolite that inhibits DNA synthesis by acting as a cytosine nucleoside analog. - **Methotrexate** is an antimetabolite and antifolate agent that inhibits dihydrofolate reductase, blocking the synthesis of tetrahydrofolate required for purine and thymidylate synthesis. This combination has been used primarily in the treatment of hematologic malignancies such as primary central nervous system lymphoma (PCNSL) and acute myeloid leukemia (AML). The regimen may be referred to as part of protocols like IDARAM or similar multi-agent regimens when combined with other agents such as rituximab[2][4][7]. The goal of combining these agents is to exploit their synergistic effects on malignant cells while targeting different pathways involved in cell proliferation.

02

Targets

GR (Glucocorticoid receptor)TOP2A (DNA topoisomerase II)DHFR (Dihydrofolate reductase)DNA polymerase family

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