II. Indications

  1. FDA Approved
    1. Pancreatic Adenocarcinoma
    2. Non-Small Cell Lung Cancer
    3. Metastatic Breast Cancer
    4. Advanced Ovarian Cancer
  2. Off-Label Use: Advanced Cancers, Recurrent, Metastatic or Persistent
    1. Bladder Cancer
    2. Cervical Cancer
    3. Ewing Sarcoma
    4. Hepatobiliary Cancer
    5. Lymphoma (Hodgkin Lymphoma, Non-Hodgkin Lymphoma)
    6. Nasopharyngeal Cancer
    7. Osteosarcoma
    8. Renal Cell Carcinoma
    9. Small Cell Lung Cancer
    10. Soft Tissue Sarcoma
    11. Testicular Cancer (germ cell tumors)
    12. Thymic Cancer
    13. Uterine Sarcoma

III. Mechanism

  1. See Antimetabolite Chemotherapy
  2. Broad Spectrum, antineoplastic antimetabolite
    1. PyrimidineNucleoside analog of deoxycytidine
  3. Gemcitabine is a prodrug, metabolized to active metabolites by deoxycytidine kinase on infusion
    1. dFdCDP (difluorodeoxycytidine diphosphate)
      1. Inhibits ribonucleotide reductase
      2. Decreases the Nucleotide source for DNA synthesis, and potentiates dFdCTP uptake by DNA
    2. dFdCTP (difluorodeoxycytidine triphosphate)
      1. Competes with dCTP (deoxycytidine triphosphate)
      2. Incorporated into DNA, blocking DNA Polymerase and DNA Replication

IV. Medications

  1. Gemcitabine IV Solution in 200, 1000 and 2000 mg vials

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Pharmacokinetics

  1. Hepatic and peripheral blood deamination to inactive metabolite (difluorouridine)

VII. Adverse Effects

  1. Alopecia
  2. Fever
  3. Hematuria or Proteinuria
  4. Hepatotoxicity
  5. Myelosuppression
  6. Rash
  7. Other uncommon, but serious adverse effects
    1. Pulmonary Eosinophilia
    2. Thrombotic Thrombocytopenic Purpura
    3. Hemolytic-Uremic Syndrome
    4. Thrombotic Microangiopathy

VIII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception
    2. Men should also not father children while taking Decitabine, and for 2 months after
  3. Monitoring
    1. Complete Blood Count with Platelets
    2. Liver Function Test
    3. Renal Function test

X. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Ontology: gemcitabine (C0045093)

Definition (NCI) A broad-spectrum antimetabolite and deoxycytidine analogue with antineoplastic activity. Upon 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. This locks DNA polymerase thereby resulting in "masked termination" during DNA replication. On the other hand, dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis. The reduction in the intracellular concentration of dCTP potentiates the incorporation of dFdCTP into DNA.
Definition (NCI_NCI-GLOSS) The active ingredient in a drug that is used to treat pancreatic cancer that is advanced or has spread. It is also used with other drugs to treat breast cancer that has spread, advanced ovarian cancer, and non-small cell lung cancer that is advanced or has spread. It is also being studied in the treatment of other types of cancer. Gemcitabine blocks the cell from making DNA and may kill cancer cells. It is a type of antimetabolite.
Definition (CSP) antimetabolite used in the treatment of pancreatic, lung, and other cancers.
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH C056507
SnomedCT 108811008, 386920008
English 2',2'-DFDC, 2',2'-difluoro-2'-deoxycytidine, 2',2'-difluorodeoxycytidine, dFdCyd, 2'-deoxy-2'-difluorocytidine, 2'-Deoxy-2',2'-difluorocytidine, Difluorodeoxycytidine, dFdC, 2'Deoxy-2',2'-Difluorocytidine, 1-(2-Oxo-4-amino-1,2-dihydropyrimidin-1-yl)-2-deoxy-2,2-difluororibose, gemcitabine [Chemical/Ingredient], 2,2 difluorodexoycytidine, gemcitabine, GEMCITABINE, Gemcitabine, Gemcitabine (product), Gemcitabine (substance), difluorodeoxycytidine
Spanish gemcitabina (producto), gemcitabina (sustancia), gemcitabina

Ontology: Gemcitabine hydrochloride (C0771488)

Definition (NCI_NCI-GLOSS) A drug used to treat pancreatic cancer that is advanced or has spread. It is also used with other drugs to treat breast cancer that has spread, advanced ovarian cancer, and non-small cell lung cancer that is advanced or has spread. It is also being studied in the treatment of other types of cancer. Gemcitabine hydrochloride blocks the cell from making DNA and may kill cancer cells.
Definition (NCI) The hydrochloride salt of an analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.
Definition (PDQ) The hydrochloride salt of an analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41213&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41213&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C961" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH C056507
SnomedCT 412187004
English Gemcitabine Hydrochloride, 2'Deoxy-2',2'-Difluorocytidine, Hydrochloride, Difluorodeoxycytidine Hydrochloride, 1-(2-Oxo-4-amino-1,2-dihydropyrimidin-1-yl)-2-deoxy-2,2-difluororibose, hydrochloride, Gemcitabine hydrochloride, gemcitabine hydrochloride (medication), GEMCITABINE HYDROCHLORIDE, gemcitabine HCl, gemcitabine hydrochloride, Gemcitabine hydrochloride (substance)
Spanish clorhidrato de gemcitabina (sustancia), clorhidrato de gemcitabina