Drug intelligence / Profile preview

ellipticine

Development stage
Unknown
Modality
Small Molecules
01

Overview

Ellipticine is a naturally occurring indole alkaloid and organic heterotetracyclic compound with potent antineoplastic activity. It acts as a DNA intercalating agent and inhibitor of topoisomerase II, leading to DNA damage and cell cycle arrest. Ellipticine is considered a prodrug that requires metabolic activation by cytochrome P450 enzymes (notably CYP1A and CYP3A), which generate reactive metabolites that form covalent DNA adducts. This results in induction of apoptosis via p53-dependent pathways and mitochondrial apoptotic mechanisms. Ellipticine has shown significant cytotoxicity against various cancer types in vitro and in vivo but has not progressed to clinical approval due to toxicity concerns such as mutagenicity[2][4][7].

Other names
5,11-dimethyl-6H-pyrido[4,3-b]carbazoleelliptisineH-pyrido[4,3-b]carbazole
02

Targets

TOP2A (DNA topoisomerase II)TOP2B (DNA topoisomerase II beta)

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