Esophageal cancer chemotherapy drug gemcitabine experimental study

By | January 22, 2012

Gemcitabine deoxy nucleoside analogues Anhui cell slightly, and its chemical structure similar to cytarabine, as ribonucleotide reductase inhibitors.Experimental study of gemcitabine in cells through the cell slightly eyelashes deoxy nucleoside kinases, into bioactive nucleoside diphosphate (dFdCDP) and nucleoside triphosphate (dFdCTP), has anti-tumor effect.
dFdCDP inhibiting ribonucleotide reductase, resulting in DNA synthesis of cells produce the required reduction of dCTP, but also with the dCTP dFdCTP competitive binding DNA, thereby inhibiting DNA synthesis.
Experimental study of gemcitabine, a combination of the DNA chain elongation dFdCTP blocked, causing programmed cell death, called apoptosis. Pharmacokinetic study of gemcitabine in vivo plasma protein binding with very little, half-life of 32 – 94min, the volume of drug distribution and gender. The total clearance rate was 30 – 90L / (, by age and gender impact.
Experimental Study of Gemcitabine, drug metabolism in the body inactive dFdu (past two-fluorodeoxyglucose in urine), 99% of the urinary excretion of parent drug excretion was less than 10%. Gemcitabine is cell cycle specific agents, acting on S, can prevent the G1 to S phase of transformation.

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