Article
Effects of drug efflux proteins and topoisomerase I mutations on the camptothecin analogue gimatecan.
Investigational new drugs - 1 Jun 2008
Gounder Murugesan K, Nazar Ahamed S, Saleem Ahamed, Pungaliya Pooja, Kulkarni Diptee, Versace Richard, Rubin Eric H
Abstract excerpt
Clinically relevant resistance to the currently approved camptothecins, irinotecan and topotecan, is poorly understood but may involve increased expression of ATP-dependent drug transporters such as ABCG2 (breast cancer resistant protein, BCRP). Gimatecan (ST1481) is a lipophilic 7-substituted camptothecin derivative that exhibits potent anti-tumor activity in a variety of preclinical cancer models and is under...
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