Dihydropyrimidine dehydrogenase inhibitory fluoropyrimidines : A novel class of oral antineoplastic agents

摘要: Protracted intravenous regimens of 5-fluorouracil (5-FU) produce fewer toxic effects and greater response rates than do bolus infusion regimens. An effective oral regimen would allow a protracted course 5-FU without the need for central venous lines associated increase in complications, such as thrombosis, infection, line slippage. Dihydropyrimidine dehydrogenase (DPD) is primary catabolic enzyme 5-FU. The varying levels DPD located gastrointestinal tract make absorption resultant plasma erratic. use pro-drugs and/or inhibitors can overcome this problem dosing fluoropyrimidines. In Japan, fluoropyrimidines have been used decades gained widespread acceptance treatment cancer. More recently, encouraging clinical results led to development new generation fluoropyrimidines, commonly referred inhibitory that specifically target DPD. Several are advanced stages United States. As studies shown so far, fluoropyrimidine prolong exposure 5-FU, while causing effects, may therapeutic advantage over