Clinical pharmacology of oral gemcitabine in patients with advanced solid tumors

摘要

Gemcitabine (dFdC) is an anticancer agent used i.v. in the treatment of a number of solid tumor types including pancreatic and non-small cell lung (NSCL) cancer. dFdC is metabolised to dFdU by cytidine deaminase particularly in the liver and as a prodrug it has to be intracellularly phosphorylated by deoxycytidine kinase to its main active triphosphate metabolite (dFdCTP) (Heinemann et al., 1992). Preclinical models reveal high activity of continuous exposure compared with intermittent exposure. In patients the most optimal therapy to achieve continuous exposure is by applying oral dosing.