Drug intelligence / Profile preview

9-hydroxycamptothecin

Development stage
Preclinical
Lead developer
CHRISTUS Stehlin Foundation for Cancer Research
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

9-Hydroxycamptothecin is a natural cytotoxic alkaloid and a derivative of camptothecin, primarily found in the *Camptotheca acuminata* tree. It functions as a DNA topoisomerase I inhibitor, stabilizing the covalent complex between the enzyme and DNA, which prevents DNA religation and leads to lethal double-strand breaks during the S-phase of the cell cycle. While it is a structural isomer of the more extensively studied 10-hydroxycamptothecin, 9-hydroxycamptothecin has demonstrated potent antineoplastic activity in various preclinical cancer models. Beyond its established role in oncology, recent structure-affinity driven repurposing studies have identified the compound as a potential therapeutic candidate for immune-mediated chronic inflammatory diseases, specifically ulcerative colitis and psoriasis.

Other names
9-Hydroxycamptothecine9-OH-CPT
02

Targets

TOP1 (DNA Topoisomerase I)

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