9-nitrocamptothecin liposomes

9-Nitrocamptothecin liposomes (9NC-LP) is a liposomal encapsulation of 9-nitrocamptothecin (also known as rubitecan), a semi-synthetic derivative of the cytotoxic alkaloid camptothecin. As a potent topoisomerase I inhibitor, 9-nitrocamptothecin stabilizes the "cleavable complex" formed between DNA and the topoisomerase I enzyme, preventing the re-ligation of single-strand DNA breaks and ultimately causing double-strand breaks during DNA replication, which triggers apoptosis. The liposomal formulation was developed to address the significant challenges associated with the parent compound, including its poor aqueous solubility and the rapid hydrolysis of its active lactone ring into an inactive carboxylate form at physiological pH. By protecting the lactone ring and altering the pharmacokinetic profile, the liposomal delivery system aims to enhance the drug's stability, prolong its circulation time, and improve its accumulation in tumor tissues. It has been investigated in various clinical and preclinical settings, particularly for hepatocellular carcinoma and lung cancer (often via aerosolized delivery).

Brand names

Inhaled OrathecinRubitecan (inhaled)

Other names

Liposomal 9-nitrocamptothecinLiposomal9-nitrocamptothecinLiposomal-9-nitrocamptothecinLiposomal rubitecan9-nitro-20(S)-camptothecin liposomes