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Information about Streptozocin

Streptozocin is a unique antineoplastic agent used to treat metastatic pancreatic islet cell carcinoma. 


Liver safety of Streptozocin

Streptozocin has been associated with a high rate of serum enzyme elevation during therapy and to rare instances of severe, clinically apparent acute liver injury.

Mechanism of action of Streptozocin

Streptozocin (strep" toe zoe' sin), which was formerly known as streptotozocin, is an antineoplastic antibiotic isolated initially from Streptomyces achromogenes.  Structurally, streptozocin is a methylnitrosourea attached to a single molecule of glucosamine and acts as an alkylating agent causing DNA damage and interfering with synthesis.  Streptozocin has high affinity for the cell surface glucose transporter GLUT 2 which is highly expressed on beta cells of the islets of Langerhans.  As a consequence, streptozocin has differential toxicity to beta cells.  In animal models, streptozocin caused loss of pancreatic islet cells, resulting in a decrease in serum insulin and diabetes.  Used initially as a means of creating an animal model of type 1 diabetes, streptozocin was later used clinically to treat insulin-secreting islet cell tumors.  It was tried, but had little effect in other malignancies.  Streptozocin was approved for use in the chemotherapy of metastatic pancreatic islet cell carcinoma in the United States in 1982 and is still used, but largely in combination with other chemotherapeutic agents such as doxorubicin and fluorouracil.  In addition, it has been used off label to treat other neuroendocrine neoplasms. 

FDA approval information for Streptozocin

Streptozocin is available as a powder for reconstitution in 1 gram vials under the brand name Zanosar.  The typical dose is 500 mg/m2 daily for 5 days every 6 weeks or as 1 gram once weekly intravenously until a remission is achieved or significant toxicity intervenes. 

Side effects of Streptozocin

  • Common side effects of streptozocin therapy are nausea, vomiting, diarrhea, abdominal discomfort and local infusion site reactions. 
  • These immediate reactions can be followed by renal dysfunction (proteinuria, proximal tubular injury, phosphaturia, acute renal failure), bone marrow suppression (anemia, neutropenia) and hepatotoxicity.

  Alphabetic list of antineoplastic agents - 0-9 - A1 - A2 - A3 - A4 - A5 -A6 - B - C - D - E - F - G - H - I - JK - L - M - NO - PQ - R - S - T - UVW - XYZ

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