New Approach to Enhance the Performance of Oral Camptothecins. SP1060C-O – a NewHighly Active Block Copolymer-Topotecan Composition with Selective and SustainedAbsorption of the Drug Lactone Form

摘要

SP1010C-O is an oral formulation oftopotecan that has increased bioavailabilityof the active lactone drug form. SP1060C-Ohas been shown to be considerably moreactive than the parent marketed drugadministered by either intravenousinjection, or orally. Relatively to otherknown formulations of camptothecins,SP1060C-O provides the highest lactoneto-carboxilate ratio in plasma and tumordrug accumulation, which results insignificantly higher anticancer activity andwell tolerable toxicity as demonstrated inseveral relevant animal models.