Drug intelligence / Profile preview

azacitidine + cytarabine + erlotinib + filgrastim + homoharringtonine

Development stage
Unknown
Lead developer
Xinqiao Hospital
Modality
Recombinant Proteins and Enzymes, Small Molecules
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 familyCSF3R (Granulocyte colony-stimulating factor receptor)DNMT1 (DNA (cytosine-5)-methyltransferase 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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