What is the mechanism of action of gemcitabine?
What is the mechanism of action of gemcitabine?
The most important mechanism of action of gemcitabine is inhibition of DNA synthesis (Huang et al., 1991). When dFdCTP is incorporated into DNA, a single deoxynucleotide is incorporated afterwards, preventing chain elongation (Gandhi et al., 1996).
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 cancer does gemcitabine treat?
Gemcitabine, a pyrimidine nucleoside antimetabolite, is one of the most promising new cytotoxic agents. The drug has shown activity in a variety of solid tumors, and has been approved for the treatment of non-small cell lung cancer, pancreatic, bladder, and breast cancer.
Does gemcitabine cause hair loss?
v Hair loss is typically minimal with gemcitabine, but some patients do experience more hair loss than others. Hair growth should return upon completion of treatment. v Nausea and vomiting are not unusual but are less common today than in the past because of much improved anti-nausea medications.
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?
Structure for Gemcitabine hydrochloride (DBSALT000092)
| Property | Value | Source |
|---|---|---|
| Water Solubility | 0.824 mg/mL | ALOGPS |
| logP | 0.28 | ALOGPS |
| logP | -0.49 | ChemAxon |
| logS | -2.5 | ALOGPS |
When does gemcitabine side effects start?
The following side effects are common (occurring in more than 30%) for patients taking Gemcitabine: Flu-like symptoms(muscle pain, fever, headache, chills, fatigue) Fever (within 6-12 hours of first dose)
Can gemcitabine cause high blood pressure?
Posterior Reversible Encephalopathy Syndrome (PRES): PRES is a rare, reversible neurological disorder that can occur with the use of gemcitabine. Symptoms of PRES include seizure, high blood pressure, headache, confusion, fatigue, confusion, any changes in your vision, or difficulty walking or thinking.
