REVIEW Rubitecan is a camptothecin analog. Like other camptothecins, its antitumor activity is mediated through its inhibition of DNA topoisomerase I. It exists in equilibrium as 9-nitro-camptothecin and 9-amino-camptothecin. Both structures contain a lactone ring required for optimal activity; the carboxylic acid open-ring forms are significantly less active or inactive. A more acidic environment favors the lactone ring structure, whereas neutral or basic conditions favor the conversion to the carboxylic acid.
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Phase II study of rubitecan, an oral camptothecin in patients with advanced colorectal cancer who have failed previous 5-fluorouracil based chemotherapy.Patel H, Stoller R, Auber M, Potter D, Cai C, Zamboni W, Kiefer G, Matin K, Schmotzer A, Ramanathan RK.Invest New Drugs. 2006 Jul;24(4):359-63.
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