What is the structure of gemcitabine?

What is the structure of gemcitabine?

C9H11F2N3O4
Gemcitabine/Formula

Is gemcitabine soluble in water?

Structure for Gemcitabine hydrochloride (DBSALT000092)

What class of drug is gemcitabine?

Gemcitabine is in a class of medications called antimetabolites. It works by slowing or stopping the growth of cancer cells in your body.

How is gemcitabine metabolized?

Gemcitabine is metabolized intracellularly by nucleoside kinases to the active diphosphate (dFdCDP) and triphosphate (dFdCTP) nucleosides. The cytotoxic effect of gemcitabine is attributed to a combination of two actions of the diphosphate and the triphosphate nucleosides, which leads to inhibition of DNA synthesis.

How does gemcitabine inhibit DNA synthesis?

Gemcitabine inhibits DNA synthesis by intracellular conversion by deoxycytidine kinase to the active diphosphate (dFdCDP) and triphosphate (dFdCTP) nucleosides that lead to competitive inhibition of DNA polymerase.

How do you dissolve gemcitabine?

Gemcitabine (100mg) should be dissolved in 5ml of Saline, freeze aliquots and store at -20. Dose at 100 ul i.p./20 g mouse once a week.

What is the pH of gemcitabine?

The recommended dose for gemcitabine is 1000 mg/m2, given by 30-minute infusion. The dose should be given on Days 1, 8 and 15 of each 28-day cycle in combination with cisplatin….Hide table of contents.

What is the purpose of gemcitabine?

Gemcitabine is used to treat certain types of cancer (including breast, lung, ovarian, pancreatic). It is a chemotherapy drug that works by slowing or stopping the growth of cancer cells.

How is gemcitabine excreted?

More than 75 % of gemcitabine is metabolised to dFdU and excreted in the urine in the first 24 h [19]. This clearance is independent of dose over the linear range (i.e., up to 3650 mg/m2), but proportional to creatinine clearance.

Does gemcitabine induce apoptosis?

Gemcitabine can induce apoptosis in cancer cells through GSK-3β and PAP inhibition, and TP53INP1 and GSK-3βser9 activation.

What is the mechanism of action of gemcitabine dFdCDP?

Gemcitabine is in the nucleoside analog family of medication. It works by blocking the creation of new DNA, which results in cell death. The form of gemcitabine with two phosphates attached (dFdCDP) also has activity; it inhibits the enzyme ribonucleotide reductase (RNR), which is needed to create new nucleotides.

What is the pharmacokinetics of gemcitabine?

Gemcitabine pharmacokinetics are linear and are described by a 2-compartment model. Population pharmacokinetic analyses of combined single and multiple dose studies showed that the volume of distribution of gemcitabine was significantly influenced by duration of infusion and gender.

Does gemcitabine inhibit thymidylate synthetase?

Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occurs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate by deoxycitidine kinase.

How do you get gemcitabine into the cell membrane?

Gemcitabine is hydrophilic and must be transported into cells via molecular transporters for nucleosides (the most common transporters for gemcitabine are SLC29A1 SLC28A1, and SLC28A3). After entering the cell, gemcitabine is first modified by attaching a phosphate to it, and so it becomes gemcitabine monophosphate (dFdCMP).