Drug intelligence / Profile preview

Emetine

Development stage
Phase 3
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

Emetine is a natural alkaloid derived from the root of the ipecac plant (Uragoga ipecacuanha). It has historically been used as both an anti-protozoal agent and an emetic (to induce vomiting)[1][7]. Its primary clinical use was in the treatment of severe invasive amoebiasis, where it acts as a tissue amoebicide, concentrating mainly in the bowel wall and liver[3]. Emetine exerts its effects by binding to the 40S subunit of eukaryotic ribosomes, thereby inhibiting protein synthesis[7]. This mechanism underlies both its antiparasitic activity and its laboratory use as a protein synthesis inhibitor. Emetine also displays additional pharmacological actions including inhibition of HIF-1α expression, disruption of Wnt/β-catenin signaling pathways in cancer cells, induction of apoptosis in various tumor cell types[8], and suppression of proliferation in pulmonary arterial hypertension models via downregulation of RhoA/Rho-kinase signaling[5]. Overuse can lead to serious toxicities such as cardiomyopathy and myopathy[7].

Other names
emetineipecac alkaloidemetinummethylcephaeline
02

Targets

40S (Small ribosomal subunit protein uS10)

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