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Drug intelligence / Profile preview
azacitidine + cytarabine + erlotinib + filgrastim + homoharringtonine
- Development stage
- Unknown
- Lead developer
- Xinqiao Hospital
- Modality
- Small Molecules, Recombinant Proteins and Enzymes
- Administration
- Oral, Subcutaneous, Intravenous
01
Overview
azacitidine + cytarabine + erlotinib + filgrastim + homoharringtonine is an experimental combination chemotherapy regimen being investigated for the treatment of relapsed or refractory acute myeloid leukemia (AML). Developed by the Second Affiliated Hospital of the Army Medical University (Xinqiao Hospital), this regimen builds upon the established HAG protocol (homoharringtonine, cytarabine, and filgrastim) by adding the hypomethylating agent azacitidine and the EGFR inhibitor erlotinib. The mechanism of action is multi-faceted: azacitidine induces DNA demethylation to restore tumor suppressor gene expression; erlotinib inhibits EGFR signaling, which may be aberrantly active or contribute to resistance in AML; homoharringtonine inhibits protein synthesis; cytarabine acts as an antimetabolite interfering with DNA synthesis; and filgrastim (G-CSF) is used to mobilize leukemic blasts into the S-phase of the cell cycle, increasing their sensitivity to the cytotoxic agents.
- Other names
- Azacitidine-Erlotinib-HAG
02
Targets
60S (Eukaryotic 60S ribosomal subunit)DNA polymerase familyDNMT1 (DNA (cytosine-5)-methyltransferase 1)EGFR (Epidermal growth factor receptor)CSF3R (Granulocyte colony-stimulating factor receptor)
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