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Medically reviewed by Last updated on Jun 11, 2020.


(strep toe ZOE sin)

Index Terms

  • Streptozotocin

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Zanosar: 1 g (1 ea)

Brand Names: U.S.

  • Zanosar

Pharmacologic Category

  • Antineoplastic Agent, Alkylating Agent
  • Antineoplastic Agent, Alkylating Agent (Nitrosourea)


Streptozocin inhibits DNA synthesis by alkylation and cross-linking the strands of DNA, and by possible protein modification; cell cycle nonspecific


Concentrates in liver, kidney, and pancreatic beta cells


Rapid; primarily hepatic


Urine (primarily; as parent drug and metabolites)

Onset of Action

1,500 mg/m2 once weekly: Onset of response: 17 days; median time to maximum response: 35 days

Half-Life Elimination

<1 hour (Perry 2012)

Use: Labeled Indications

Pancreatic neuroendocrine tumors: Treatment of metastatic islet cell carcinoma of the pancreas (symptomatic or progressive disease)

Off Label Uses

Adrenocortical carcinoma, metastatic

Data from a randomized, controlled, open-label, parallel-group study supports the use of streptozocin in the treatment of metastatic adrenocortical carcinoma. In this phase III study comparing mitotane in combination with etoposide, doxorubicin, and cisplatin (EDP regimen), to streptozocin in combination with mitotane, the response rate and progression free survival were significantly better with the EDP arm, although there was no difference in overall survival between the groups [Fassnacht 2012]. Data from a phase II study evaluating streptozocin (in combination with mitotane) also supports the use of streptozocin in the treatment of metastatic adrenal carcinoma; either complete or partial response occurred in 36.4% of patients resulting in a 2 year survival of 70% and a 5 year survival rate of 32.5% [Khan 2000].

Gastrointestinal neuroendocrine tumors

Data from a phase II/III randomized study supports the use of streptozocin (in combination with fluorouracil) in the treatment of gastrointestinal neuroendocrine (carcinoid) tumors [Sun 2005 [LOE B]]. Additionally, a small number of patients with gastrointestinal neuroendocrine tumors (GiNETs) were included in a study evaluating response to streptozocin (in combination with fluorouracil, leucovorin, and cisplatin) in patients with neuroendocrine tumors (including pancreatic and GI tumors); while patients with pancreatic neuroendocrine tumors had a higher response rate, patients with GiNETs also demonstrated objective responses and stable disease [Turner 2010 [LOE C]].


There are no contraindications listed within the manufacturer's labeling.

Dosing: Adult

Note: Streptozocin is associated with a high emetic potential; antiemetics are recommended to prevent nausea and vomiting (Hesketh 2017; Roila 2016).

Adrenocortical carcinoma, metastatic (off-label use): IV: 1,000 mg once daily for 5 days (cycle 1) followed by 2,000 mg on day 1 (subsequent cycles) every 3 weeks until disease progression or unacceptable toxicity (in combination with mitotane) (Fassnacht 2012; Khan 2000).

Gastrointestinal neuroendocrine tumors (off-label use): IV: 500 mg/m2 on days 1 to 5 every 10 weeks (in combination with fluorouracil) until disease progression or unacceptable toxicity (Sun 2005) or 1,000 mg/m2 once every 3 weeks for 3 cycles, if no progression may continue for up to a total of 6 cycles in the absence of unacceptable toxicity (in combination with leucovorin, fluorouracil and cisplatin) (Turner 2010).

Pancreatic neuroendocrine tumors (metastatic): IV:

Daily schedule: 500 mg/m2 once daily for 5 consecutive days every 6 weeks (in combination with either doxorubicin or fluorouracil) until disease progression or unacceptable toxicity (Moertel 1992)

Weekly schedule: 1,000 mg/m2 once weekly; if therapeutic response not achieved after 2 weeks, may escalate dose to a maximum of 1,500 mg/m2 weekly

Alternate schedules (off-label dosing): 1,000 mg/m2 once every 3 weeks for up to 6 cycles (in combination with leucovorin, fluorouracil and cisplatin) (Turner 2010) or 400 mg/m2 days 1 to 5 every 4 weeks (in combination with fluorouracil and doxorubicin) until disease progression or unacceptable toxicity (Kouvaraki 2004) or 500 mg/m2 on days 1 to 5 every 5 or 6 weeks (in combination with fluorouracil) for up to 1 year if best response is stable disease (Dilz 2015)

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing. Select dose cautiously, beginning at the lower end of dosing range.

Dosing: Adjustment for Toxicity

Bone marrow suppression: May require dosage reduction or discontinuation.

Dosing: Obesity

ASCO Guidelines for appropriate chemotherapy dosing in obese adults with cancer: Utilize patient’s actual body weight (full weight) for calculation of body surface area- or weight-based dosing, particularly when the intent of therapy is curative; manage regimen-related toxicities in the same manner as for nonobese patients; if a dose reduction is utilized due to toxicity, consider resumption of full weight-based dosing with subsequent cycles, especially if cause of toxicity (eg, hepatic or renal impairment) is resolved (Griggs 2012).


Reconstitute powder with 9.5 mL D5W or NS to a concentration of 100 mg/mL. May further dilute for infusion in D5W or NS.


IV: Streptozocin is associated with a high emetic potential; antiemetics are recommended to prevent nausea and vomiting (Dupuis 2011; Hesketh 2017; Roila 2016).

Administer as either a rapid IV injection or as short or prolonged infusion.

Irritant with vesicant-like properties; ensure proper needle or catheter placement prior to and during infusion; avoid extravasation.

Extravasation management: If extravasation occurs, stop infusion immediately and disconnect (leave cannula/needle in place); gently aspirate extravasated solution (do NOT flush the line); remove needle/cannula; elevate extremity.


Store intact vials at 2°C to 8°C (36°F to 46°F). Protect from light. The manufacturer recommends use within 12 hours of reconstitution; vial does not contain a preservative.

Drug Interactions

5-Aminosalicylic Acid Derivatives: May enhance the myelosuppressive effect of Myelosuppressive Agents. Monitor therapy

BCG (Intravesical): Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. Monitor therapy

Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Avoid combination

CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. Monitor therapy

Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Consider therapy modification

Dipyrone: May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased Avoid combination

Lenograstim: Antineoplastic Agents may diminish the therapeutic effect of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Consider therapy modification

Lipegfilgrastim: Antineoplastic Agents may diminish the therapeutic effect of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Consider therapy modification

Palifermin: May enhance the adverse/toxic effect of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy. Consider therapy modification

Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not defined.

Endocrine & metabolic: Decreased glucose tolerance, glycosuria, hyperglycemia, hypoalbuminemia, hypoglycemia, hypophosphatemia, increased lactate dehydrogenase

Gastrointestinal: Diarrhea, nausea, vomiting

Genitourinary: Anuria, azotemia, nephrotoxicity, proteinuria

Hepatic: Increased serum transaminases

Local: Injection site reaction (includes burning sensation at injection site, erythema at injection site, inflammation at injection site, irritation at injection site, swelling at injection site, tenderness at injection site)

Renal: Increased blood urea nitrogen, increased serum creatinine, renal insufficiency, renal tubular acidosis

<1%, postmarketing, and/or case reports: Anemia, bone marrow depression (nadir: 2 to 3 weeks), confusion, depression, diabetes insipidus, hepatic insufficiency, lethargy, leukopenia, metastases, thrombocytopenia

ALERT: U.S. Boxed Warning

Experienced physician:

Streptozocin should be administered under the supervision of a physician experienced in the use of cancer chemotherapeutic agents. A patient need not be hospitalized but should have access to a facility with a laboratory and supportive resources sufficient to monitor drug tolerance and to protect and maintain a patient compromised by drug toxicity. The physician must judge the possible benefit to the patient against the known toxic effects of this drug in considering the advisability of therapy with streptozocin. The physician should be familiar with the following text before making a judgment and beginning treatment.

Drug toxicities:

Renal toxicity is dose-related and cumulative and may be severe or fatal. Other major toxicities are nausea and vomiting, which may be severe and at times treatment-limiting. In addition, liver dysfunction, diarrhea and hematological changes have been observed in some patients.

Secondary malignancy:

Streptozocin is mutagenic. When administered parenterally, it has been found to be tumorigenic or carcinogenic in some rodents.


Concerns related to adverse effects:

• Bone marrow suppression: [US Boxed Warning]: Hematologic toxicity has been observed. Mild bone marrow suppression (rare) may occur (usually mild anemia); monitor blood counts weekly. May require dosage reduction or discontinuation.

• CNS effects: May cause confusion, lethargy or depression; caution patients about performing tasks that require mental alertness (eg, operating machinery or driving).

• Extravasation/tissue irritation: Streptozocin is an irritant with vesicant-like properties. Avoid extravasation. Local tissue irritation or inflammation (burning, edema, erythema, tenderness) may occur, but usually resolves within a few days.

• Gastrointestinal events: [US Boxed Warning]: Diarrhea has been observed. May cause severe nausea and vomiting. Streptozocin is associated with a high emetic potential; antiemetics are recommended to prevent nausea and vomiting (Dupuis 2011; Hesketh 2017; Roila 2016).

• Glucose intolerance: Mild-to-moderate glucose intolerance may occur; generally is reversible. Insulin shock with hypoglycemia has been observed.

• Hepatotoxicity: [US Boxed Warning]: Liver dysfunction has been observed. Hepatotoxicity may be characterized by elevated transaminases and LDH, or by hypoalbuminemia; monitor liver function weekly. Hepatic dysfunction may require dosage reduction or discontinuation.

• Renal toxicity: [US Boxed Warning]: Renal toxicity is dose-related and cumulative; may be severe or fatal. Azotemia, anuria, hypophosphatemia, glycosuria and renal tubular acidosis have been reported. Adequate hydration may reduce the risk for nephrotoxicity. Monitor renal function (BUN, serum creatinine, and serial urinalysis) and electrolytes prior to, weekly during, and after each treatment course. Mild proteinuria is an early sign of renal toxicity; if proteinuria is detected with urinalysis, obtain 24-hour urine collection. Avoid use in combination with other nephrotoxic medications. Use with caution in patients with pre-existing renal disease.

• Secondary malignancy: [US Boxed Warning]: Streptozocin is mutagenic; parenteral use is tumorigenic and carcinogenic in animals.

Other warnings/precautions:

• Experienced physician: [US Boxed Warning]: Should be administered under the supervision of an experienced cancer chemotherapy physician. Administer in a facility with sufficient access to lab and supportive resources for monitoring toxicities.

Monitoring Parameters

Renal function tests, including BUN, serum creatinine, and serial urinalysis, and serum electrolytes (at baseline, weekly during, and for 4 weeks after treatment); 24-hour urine collection if proteinuria is detected on urinalysis; liver function tests (weekly), CBC with differential and platelets (weekly), blood glucose; monitor infusion site

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Patient Education

What is this drug used for?

• It is used to treat pancreatic cancer.

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Diarrhea

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Infection

• Bleeding like vomiting blood or vomit that looks like coffee grounds; coughing up blood; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any severe or persistent bleeding.

• Kidney problems like unable to pass urine, blood in the urine, change in amount of urine passed, or weight gain.

• Liver problems like dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin.

• Low blood sugar like dizziness, headache, fatigue, feeling weak, shaking, fast heartbeat, confusion, increased hunger, or sweating.

• Severe nausea

• Vomiting

• Depression

• Confusion

• Severe loss of strength and energy

• Severe injection site redness, pain, swelling, or irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

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