Gemcitabine Hydrochloride

What it is and how it works

Mechanism of Action Gemcitabine kills cells undergoing DNA synthesis and blocks the progression of cells through the G1/S-phase boundary. Gemcitabine is metabolized by nucleoside kinases to diphosphate (dFdCDP) and triphosphate (dFdCTP) nucleosides. Gemcitabine diphosphate inhibits ribonucleotide reductase, an enzyme responsible for catalyzing the reactions that generate deoxynucleoside triphosphates for DNA synthesis, resulting in reductions in deoxynucleotide concentrations, including dCTP. Gemcitabine triphosphate competes with dCTP for incorporation into DNA.

Indications

Gemcitabine for injection is a nucleoside metabolic inhibitor indicated: in combination with carboplatin, for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy. in combination with paclitaxel, for first-line treatment of metastatic breast cancer after failure of prior anthracycline-containing adjuvant chemotherapy, unless anthracyclines were clinically contraindicated. in combination with cisplatin, for the treatment of non-small cell lung cancer. as a single agent for the treatment of pancreatic cancer. Ovarian Cancer Gemcitabine for injection in combination with carboplatin is indicated for the treatment of patients with advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy. Breast Cancer Gemcitabine for injection in combination with paclitaxel is indicated for the first-line treatment of patients with metastatic breast cancer after failure of prior anthracycline-containing adjuvant chemotherapy, unless anthracyclines were clinically contraindicated.

Dosage and administration (summary)

Gemcitabine for injection is for intravenous use only. Ovarian Cancer: 1000 mg/m 2 over 30 minutes on Days 1 and 8 of each 21-day cycle. Breast Cancer: 1250 mg/m 2 over 30 minutes on Days 1 and 8 of each 21-day cycle. Non-Small Cell Lung Cancer: 1000 mg/m 2 over 30 minutes on Days 1, 8, and 15 of each 28-day cycle or 1250 mg/m 2 over 30 minutes on Days 1 and 8 of each 21-day cycle. Pancreatic Cancer: 1000 mg/m 2 over 30 minutes once weekly for the first 7 weeks, then one week rest, then once weekly for 3 weeks of each 28-day cycle.

Contraindications

Gemcitabine for injection is contraindicated in patients with a known hypersensitivity to gemcitabine. Reactions include anaphylaxis . Patients with a known hypersensitivity to gemcitabine.

Warnings and precautions

Schedule-Dependent Toxicity: Increased toxicity with infusion time greater than 60 minutes or dosing more frequently than once weekly. Myelosuppression: Monitor for myelosuppression prior to each cycle and reduce or withhold dose for severe myelosuppression. ( 5.2 , 5.8 ) Severe Cutaneous Adverse Reactions (SCARs): Permanently discontinue gemcitabine injection if SCARs occur. Pulmonary Toxicity and Respiratory Failure: Discontinue gemcitabine for injection for unexplained dyspnea or other evidence of severe pulmonary toxicity.

Pregnancy

Pregnancy Risk Summary Based on animal data and its mechanism of action, gemcitabine for injection can cause fetal harm when administered to a pregnant woman . There are no available data on the use of gemcitabine for injection in pregnant women.

Storage and supply

Gemcitabine for Injection, USP is a white to off-white lyophilized powder available in sterile single-dose vials individually packaged in a carton containing: NDC Gemcitabine for Injection, USP Package Factor 16714- 909 -01 200 mg white to off-white, lyophilized powder 1 vial per carton in a 10-mL size sterile single-dose vial 16714- 930 -01 1 g wh…

Source: Gemcitabine Hydrochloride (Gemcitabine) — US FDA prescribing information, 2025-02-03, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.