About: Gemcitabine Hydrochloride Emulsion     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Gemcitabine Hydrochloride Emulsion
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
  • Nucleic Acid, Nucleoside, or Nucleotide
Preferred_Name
  • Gemcitabine Hydrochloride Emulsion
PDQ_Open_Trial_Search_ID
  • 747250
PDQ_Closed_Trial_Search_ID
  • 747250
FULL_SYN
  • Gemcitabine Hydrochloride EmulsionPTNCI
  • D07001-F4CNNCI
DEFINITION
  • 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.NCI
code
  • C105613
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