Drug intelligence / Profile preview

harringtonine

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

Harringtonine is a natural alkaloid isolated from plants of the genus Cephalotaxus, particularly Cephalotaxus harringtonia. It acts as a protein synthesis inhibitor by blocking the initiation of polypeptide synthesis in eukaryotic cells. Specifically, it immobilizes ribosomes after translation initiation by inhibiting peptide bond formation and aminoacyl-tRNA binding at the ribosomal A site[1][3][4]. This mechanism leads to potent antitumor activity and apoptosis induction in rapidly dividing cells. Harringtonine has demonstrated antiviral properties against several viruses including influenza and chikungunya virus[1]. It has been investigated for use in hematological malignancies such as acute myeloid leukemia, myelodysplastic syndromes, Philadelphia chromosome positive chronic myelogenous leukemia, and polycythemia vera[5]. Common side effects include gastrointestinal symptoms such as nausea, vomiting, diarrhea, and fatigue[2].

Other names
HarringtoninCephalotaxine, 4-methyl (2R)-2-hydroxy-2-(3-hydroxy-3-methylbutyl)butanedioate (ester)Cephalotaxine, 4-methyl-, 2-hydroxy-2-(3-hydroxy-3-methylbutyl)butanedioate (ester), (3(R))-Alkaloid C from cephalotaxus
02

Targets

60S (Eukaryotic 60S ribosomal subunit)

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