Gemcitabine Hydrochloride Emulsion
An orally available nanoparticle-based formulation containing the hydrochloride salt form of gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue, with antineoplastic activity. The formulation consists of an oil-in-water emulsion in which gemicitabine is solubilized in the excipient matrix containing a mixture of oil and (co)surfactants. Upon oral administration, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA, resulting in premature termination of DNA replication and the induction of apoptosis. Further, dFdCDP inhibits ribonucleotide reductase and reduces the deoxynucleotide pool available for DNA synthesis. Compared to gemcitabine alone, the emulsion allows for increased oral bioavailability and decreases its susceptibility to deamination and deactivation by cytidine deaminase. [ ]
Term info
Gemcitabine Hydrochloride Emulsion
- D07001-F4
- Gemcitabine Hydrochloride Emulsion
NCIT_C128784, NCIT_C157711, NCIT_C157712
CL446450
747250
747250
Gemcitabine Hydrochloride Emulsion
Pharmacologic Substance, Nucleic Acid, Nucleoside, or Nucleotide
C105613
Term relations
- Ribonucleotide Reductase Inhibitor
- Pyrimidine Antagonist
- Chemical_Or_Drug_Has_Physiologic_Effect some DNA Synthesis Inhibition
- Chemical_Or_Drug_Has_Mechanism_Of_Action some Enzyme Inhibition
- Chemical_Or_Drug_Has_Physiologic_Effect some Positive Regulation of Apoptosis
- Chemical_Or_Drug_Affects_Gene_Product some Ribonucleotide Reductase
- Chemical_Or_Drug_Has_Physiologic_Effect some Nucleotide Biosynthesis Process