Drug intelligence / Profile preview

bruceantin

Development stage
Preclinical
Lead developer
National Cancer Institute
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Bruceantin is a natural product classified as a secotriterpenoid quassinoid, originally isolated from the plant Brucea antidysenterica. It acts primarily as an antineoplastic agent by inhibiting the peptidyl transferase elongation reaction during protein synthesis, leading to decreased protein and DNA synthesis. Bruceantin also exhibits antibiotic, antiamoebic, and antimalarial activities. Mechanistically, it downregulates c-MYC expression and induces apoptosis via caspase activation and mitochondrial pathways in cancer cells. Although phase I/II clinical trials were conducted for metastatic breast cancer and malignant melanoma without observed tumor regression (leading to termination of development for these indications), more recent preclinical studies have shown activity against leukemia, lymphoma, myeloma cell lines, and xenograft models[1][2][5][6].

Other names
bruceantin
02

Targets

PTC (50S ribosomal peptidyl transferase center)

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