作者: Isa E.L.M. Kuppens , Jos H. Beijnen , Jan H.M. Schellens
关键词: Exatecan 、 Topotecan 、 Apical membrane 、 Irinotecan 、 Medicine 、 Lurtotecan 、 Pharmacology 、 Internal medicine 、 Rubitecan 、 Oncology 、 Cancer 、 Oral administration
摘要: This article reviews the current status of topoisomerase I (top I) inhibitors in treatment gastrointestinal (GI) malignancies. We focus on oral drug administration, mode administration that is generally preferred by patients with cancer. However, great majority studies have been performed intravenous (I.V.) administration. The most extensively investigated GI malignancy phase I/II colorectal cancer (CRC), for which I.V. irinotecan currently approved United States and Europe. discuss activity efficacy as a single agent CRC combination regimens. Also, results obtained monotherapy other malignancies such esophageal, gastric, pancreatic are discussed. Few its clinical has not yet fully determined. Several top discussed, including topotecan, 9-aminocamptothecin, rubitecan, exatecan, lurtotecan. None these agents, given orally or intravenously, shown similar to irinotecan. several agents show promising malignancies, eg, rubitecan exatecan A complicating factor often encountered low variable bioavailability. can partly be explained high affinity efflux pumps BCRP (ABCG2) P-glycoprotein, highly expressed epithelial apical membrane tract. novel approach improve bioavailability temporary blockade transporter described.