Gemcitabine (Gemzar)

General information

Class/mechanism: Pyrimidine analog; metabolized within cells to the active nucleoside forms: diphosphate (dFdCDP) and triphosphate (dFdCTP). Gemcitabine diphosphate inhibits ribonucleotide reductase, which catalyzes reactions that produce deoxynucleoside triphosphates for DNA synthesis. This inhibition of deoxynucleoside triphosphates helps gemcitabine triphosphate to compete with deoxycytidine triphosphate (dCTP) to be incorporated into DNA. DNA synthesis is halted, since only one additional nucleotide can be added to a DNA strand after gemcitabine is incorporated.
Route: IV
Extravasation: irritant

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Anaplastic large cell lymphoma
• Bladder cancer
• Bone cancer
• Breast cancer
• Cervical cancer
• Diffuse large B-cell lymphoma
• Esophageal cancer
• Extranodal NK/T-cell lymphoma, nasal type
• Head and neck cancer
• Hepatobiliary cancer
• Hodgkin lymphoma
• Mesothelioma
• Non-small cell lung cancer
• Ovarian cancer
• Pancreatic cancer
• Peripheral T-cell lymphoma
• Primary mediastinal B-cell lymphoma
• Renal cancer
• Sarcoma
• Small cell lung cancer
• Testicular cancer
• Transformed lymphoma
• Unknown primary

Patient drug information

• Gemcitabine (Gemzar) patient drug information (Chemocare)
• Gemcitabine (Gemzar) patient drug information (UpToDate)

History of changes in FDA indication

• 5/15/1996: Initial FDA approval (original label not available on Drugs @ FDA)
• 8/25/1998: Earliest label information on Drugs @ FDA:

1. Indicated in combination with cisplatin for the first-line treatment of patients with inoperable, locally advanced (Stage IIIA or IIIB) or metastatic (Stage IV) non-small cell lung cancer.
2. Indicated as first-line treatment for patients with locally advanced (nonresectable Stage II or Stage III) or metastatic (Stage IV) adenocarcinoma of the pancreas. Gemzar is indicated for patients previously treated with 5-FU.

• 5/19/2004: New FDA indication 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.
• 3/19/2010: New FDA indication for Ovarian Cancer in combination with carboplatin.
• 5/7/2013: FDA indication revised: in combination with carboplatin, for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy.