Camptothecin lurtotecan

First generation of topi inhibitors were developed as drugs from camptothecins, a family of compounds derived from wood and bark of the Chinese tree Camptotheca acuminata) [9, 10], Many of these are already in clinical use or clinical trials, including irinotecan, topotecan, exatecan, rubitecan, and lurtotecan. Irinotecan (CPT-11) is bioactivated in liver by carboxylesterase to the active metabolite SN-38, 1000-fold more active [11]. Irinotecan received in 1998 FDA approval for treatment of metastatic colorectal cancer after failure of treatment with 5FU [12],... 

Current clinical investigations with topoisomerase I inhibitors include the feasibihty of oral administration of topotecan and irinotecan, the use of a liposomal lurtotecan formulation (NX211), and the use of a pegylated derivative of the naturally occurring camptothecin, which is soluble in aqueous solutions even at low pH values (3,10). 

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