|Bioavailability||25–30% (rubitecan and 9-AC; in dogs)|
|Protein binding||97% (rubitecan), 65% (9-AC)|
|Biological half-life||15–18 hours (rubitecan), 18–22 hours (9-AC)|
|Excretion||Bile and feces (major proportion), urine (the minor one)|
|Chemical and physical data|
|Molar mass||393.349 g/mol|
|3D model (JSmol)|
|(what is this?)|
On January 2005, Supergen withdrew the NDA for rubitecan, based on feedback indicating that the current data package would not be sufficient to gain US approval, and on January 2006, the Marketing Authorization Application (MAA) filed with the European Medicines Agency (EMA) was also withdrawn.
Large scale production of Rubitecan has encountered problems. The direct nitration of camptothecin results in regioselectivity problems. One way that has been used to synthesize Rubitecan is to nitrate 10-hydroxycamptothecin than remove the hydroxyl functional group.
Use as Anti-Cancer Drug
Rubitecan is a compound used extensively in cancer research. Rubitecan is an effective drug against pancreatic cancer and other solid tumors. One major problem is the lack of oral bioavailability due to low permeability and poor water solubility. One study shows 9-NC-SD through Soluplus1-based solid dispersion system is a much more effective delivery method than free 9-NC.
- "Withdrawal Assessment Report for Orathecin (rubitecan). Applicant: EuroGen Pharmaceuticals, Ltd" (PDF). European Medicines Agency. 30 November 2007. pp. 4–8. Retrieved 15 July 2016.
- "Drugs.com, SuperGen completes submission of New Drug Application (NDA) for Orathecin as an oral treatment for pancreatic cancer". Retrieved 2008-03-25.
- "Drugs.com, SuperGen's New Drug Application for Orathecin (rubitecan) capsules accepted by FDA for filing". Retrieved 2008-03-25.
- "Drugs.com, SuperGen Announces Withdrawal of Orathecin NDA". Retrieved 2008-03-25.
- "Press release from the EMEA website regarding withdrawal of Orathecin MAA" (PDF). Retrieved 2008-03-25.
- "A Practical Regiospecific Synthesis of 9-Nitrocamptothecin" (PDF). Retrieved 2017-10-10.
- "Soluplus® based 9-nitrocamptothecin solid dispersion for peroral administration" (PDF). Retrieved 2017-10-10.
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