Gemcitabine Hydrochloride for Injection
Function and Efficacy
This product is a cell cycle specific antimetabolite drug, which mainly acts on tumor cells in the DNA synthesis phase, that is, S phase cells. Under certain conditions, it can prevent the progression from G1 phase to S phase. It has obvious cytotoxic activity against various cultured human and mouse tumors. Its anticancer activity is related to the drug resistance mode. For example, daily administration will lead to animal death, while the anticancer activity is very small. When the drug is given once every 3 to 4 days, it has good anticancer activity against various tumors in mice at non-lethal doses. Gemcitabine is a prodrug and is a good substrate for deoxythymidine kinase phosphorylation in cells. It is converted into the following metabolites under the action of enzymes: gemcitabine monophosphate (dFdCMP), gemcitabine diphosphate (dFdCDP) and gemcitabine triphosphate (dFdCTP), of which dFdCDP and dFdCTP are active products. dFdCDP inhibits ribonucleotide reductase and reduces the amount of deoxynucleotides (especially dCTP) required for repair of DNA synthesis. Low levels of dCTP transfer normal negative feedback inhibition of deoxyside kinase, resulting in more accumulation of dFdCTP. At the same time, dFdCDP inhibits the deamination of dFdCMP by deoxycytidine aminoaminase induced by dCT, and dFdCTP directly inhibits deoxycytidine deamination, thereby converting more dFdCMP into active metabolites dFdCDP, dFd-CTP, and dFdCTP competes with dCTP to enter the DNA chain, insert into the site of deoxycytidine in the DNA chain, and allow guanosine to pair with it. The gemcitabine molecule is shielded by this guanosine to prevent it from being removed and repaired by ribonuclease exonuclease, and then DNA chain synthesis stops, leading to DNA breakage and cell death.
Ingredients
2-Deoxy-2,2-difluorodeoxycytidine hydrochloride
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Gemcitabine hydrochlorideIngredients |
Cell cycle specific antimetabolites mainly act on tumor cells in the DNA synthesis phase (S phase) and can prevent the progression from G1 phase to S phase. It is converted into active metabolites dFdCDP and dFdCTP by enzymes in cells. The former inhibits ribonucleotide reductase and reduces the production of deoxynucleotides; the latter competitively binds with dCTP to enter the DNA chain, causing DNA synthesis to stop and induce cell death. It has obvious cytotoxic activity against a variety of human and mouse tumors, and the anticancer effect is related to the method of administration. More |
122111-03-9 | 61 |
Indication
Non-small cell lung cancer, pancreatic cancer, bladder cancer, breast cancer and other solid tumors.
Usage and Dosage
The recommended dose of gemcitabine for adults is 1000 mg/m2 intravenous infusion for 30 minutes once a week for three consecutive weeks, followed by a one-week break, and repeated every four weeks. The dose is reduced accordingly based on the patient's toxicity. Elderly patients: Elderly patients over 65 years old can also tolerate it well. Although age has an effect on the clearance and half-life of gemcitabine, there is no evidence that elderly patients need to adjust the dose.
Adverse Reactions
1. Blood system: bone marrow suppression, anemia, leukopenia and thrombocytopenia may occur. 2. Gastrointestinal tract: about 2/3 of patients have abnormal liver transaminase, mostly mild, non-progressive damage; about 1/3 of patients have nausea and vomiting reactions, and 20% of patients need drug treatment. 3. Kidney: about 1/2 of patients have mild proteinuria and hematuria, and some cases have unexplained renal failure. 4. Allergies: about 25% of patients have skin rashes, 10% of patients have itching, and less than 1% of patients may have bronchospasm. 5. Others: about 20% of patients have flu-like symptoms; the incidence of edema/peripheral edema is about 30%; the incidences of hair loss, lethargy, diarrhea, oral toxicity and constipation are 13%, 10%, 8%, 7% and 6% respectively.
Precautions
Patients who are allergic to this drug are contraindicated
Storage
Store at room temperature (15°C to 30°C)
Packaging Specification
0.2g (calculated as gemcitabine)
Manufacturer
Lianyungang JARI Pharmaceutical Co., Ltd.
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Founded in:
2004-07-20 -
Address:
No. 18 Zhenhua Road, Lianyungang City -
Tax NO.:
913207007635748894 -
Registered Funds:
100 million yuan -
Email: