Drug intelligence / Profile preview

liposomal 9-nitrocamptothecin

Development stage
Unknown
Lead developer
Baylor College of Medicine
Modality
Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous, Inhalation, Aerosolized
01

Overview

**Liposomal 9-nitrocamptothecin** is a novel formulation of the topoisomerase I inhibitor **9-nitrocamptothecin**, encapsulated in liposomes to improve its stability, solubility, and therapeutic index[1][4][6][8]. This formulation allows for sustained release, reduced systemic toxicity, and targeted delivery, especially via aerosol or intravenous administration. Its mechanism is the **inhibition of DNA topoisomerase I**, causing DNA damage, cell cycle arrest, and apoptosis, particularly in rapidly dividing tumor cells. Liposomal delivery preserves the active lactone form of 9-nitrocamptothecin, further enhancing efficacy and reducing side effects compared to the unformulated drug[8]. Developed and studied as a treatment for various cancers, including hepatocellular carcinoma, pulmonary metastases, lung cancer, endometrial cancer, and others, liposomal 9-nitrocamptothecin has demonstrated improved antitumor effects and tolerability compared to oral or conventional preparations[1][2][4][6][7].

Brand names
Inhaled OrathecinRubitecan (inhaled)
Other names
liposomal 9-nitrocamptothecinliposomal9-nitrocamptothecinliposomal-9-nitrocamptothecinliposomal 9-nitro-20(S)-camptothecinaerosolized liposomal 9-nitro-20(S)-camptothecin
02

Targets

TOP1 (DNA Topoisomerase I)

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