Drug intelligence / Profile preview

afeletecan

Development stage: Phase 2
Lead developer: Bayer
Modality: Small Molecules
Administration: Intravenous, Parenteral, Subcutaneous, Intraperitoneal, Inhalation

Overview

Afeletecan is a water-soluble camptothecin derivative conjugated to a carbohydrate moiety exhibiting antineoplastic activity. It functions by stabilizing the topoisomerase I-DNA covalent complex, which inhibits both the initial cleavage reaction and religation steps. This leads to the inhibition of DNA replication, double-strand DNA breakage, and ultimately triggers apoptosis. The carbohydrate moiety is designed to stabilize the lactone form of camptothecin in the blood. It is classified as a small molecule drug.

Other names: afeletecan [INN]AFELETECAN [WHO-DD]afeletecanumAfeletecan free baseCamptothecin, ester with N-((p-((3-O-methyl-beta-L-fucopyranosyl)oxy)phenyl)thiocarbamoyl)-L-histidyl-L-valine

Targets

TOP1 (DNA Topoisomerase I)

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