How is gemcitabine metabolized?

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.

What is survival rate of patients getting gemcitabine?

Background: Adjuvant chemotherapy following curative resection is the standard treatment for pancreatic adenocarcinoma (PC). Randomized clinical trials using gemcitabine have shown a median overall survival (mOS) of 2 years and a 5-year survival rate of 15-20%.

Does gemcitabine make you tired?

Feeling sleepy. Constipation, diarrhea, throwing up, and upset stomach are common with this drug. If these happen, talk with your doctor about ways to lower these side effects. Call your doctor right away if any of these effects bother you, do not go away, or get very bad.

How effective is gemcitabine for pancreatic cancer?

Since 1997, gemcitabine therapy has been the standard first-line treatment for patients with unresectable locally advanced or metastatic pancreatic cancer. Among patients with metastatic disease, the 5-year survival rate is only 2%,1 and 1-year survival rates of 17 to 23% have been reported with gemcitabine.

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.

Is gemcitabine soluble in water?

Solubility: Soluble in water; slightly soluble in methanol; almost insoluble in 100% ethanol or polar organic solvents.

What are the side effects of gemcitabine?

Side Effects

  • Black, tarry stools.
  • bloating or swelling of the face, arms, hands, lower legs, or feet.
  • blood in the urine or stools.
  • chest pain.
  • cloudy urine.
  • coughing up blood.
  • difficult or labored breathing.
  • difficulty in moving.

How strong is Gemzar?

Dosage for Gemzar The recommended dose of Gemzar is 1000 mg/m2 as an intravenous infusion over 30 minutes on Days 1 and 8 of each 21-day cycle, in combination with carboplatin AUC 4 intravenously after Gemzar administration on Day 1 of each 21-day cycle.

Does gemcitabine cause weight gain?

Some patients may develop fluid retention, which can cause swelling in the feet and/or ankles or face or gain weight. Fluid can also build up in the lungs and cause you to feel short of breath. Notify your healthcare team if you have any swelling, unexpected weight gain, or shortness of breath.

Does gemcitabine weaken the immune system?

We conclude that gemcitabine therapy (1) is not immunosuppressive and (2) may enhance responses to specific vaccines or immunotherapy administered to activate or support immune responses directed toward driving effector immunity to cancer cells.

Can gemcitabine cure cancer?

Gemcitabine injection is also used to treat pancreas cancer that has advanced or spread to the other parts of the body in patients who have been previously treated with fluorouracil. Gemcitabine interferes with the growth of cancer cells, which are eventually destroyed.

How long does a person with pancreatic cancer have to live?

Potentially Curable If Caught Very Early For patients who are diagnosed before the tumor grows much or spreads, the average pancreatic cancer survival time is 3 to 3.5 years.

How is gemcitabine metabolized in the body?

Gemcitabine undergoes intracellular metabolism, via nucleoside kinases, to produce two active metabolites (gemcitabine diphosphate and gemcitabine triphosphate) and also undergoes deamination to an active uracil metabolite.

What are the research topics in gemcitabine?

Dive into the research topics of ‘Gemcitabine: Metabolism, mechanisms of action, and self-potentiation’. Together they form a unique fingerprint. Plunkett, W., Huang, P., Xu, Y. Z., Heinemann, V., Grunewald, R., & Gandhi, V. (1995).

What is the active metabolite of gemcitabine (dFdCTP)?

Gemcitabine is 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.

What is gemcitabine for pancreatic cancer?

Electronic address: [email protected]. Gemcitabine is the first-line treatment for pancreatic adenocarcinoma, but is increasingly used to treat breast, bladder, and non-small cell lung cancers. Despite such broad use, intrinsic and acquired chemoresistance is common.