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drug-monograph
streptozocin
Other Names
Zanosar®
Appearance
Clear, pale yellow solution mixed into larger bags of fluids
B - Mechanism of Action and Pharmacokinetics
Streptozocin is a synthetic antineoplastic agent, consisting of a nitrosourea moiety interposed between a methyl group and a glucosamine. Although its mechanism of action is not completely clear, streptozocin is known to inhibit DNA synthesis. Streptozocin is cell cycle phase-nonspecific and non-cross-resistant with other nitrosoureas.
Absorption
| Bioavailability | Not active orally, poorly absorbed (17-25%) |
Distribution
Liver, kidney, intestine and pancreas
| Cross blood brain barrier? | Parent drug: No; Metabolites: Yes |
| Volume of distribution | 43.8 L |
| PPB | No information found |
Metabolism
Liver and kidneys; spontaneously degrades to methylcarbonium ion
| Active metabolites | Methylcarbonium ion, nitrosourea metabolite |
| Inactive metabolites | yes |
Elimination
| Urine | 60 – 70% in 24 hours (10% unchanged drug) |
| Feces | < 1 % |
| Half-life | 35 - 40 minutes |
C - Indications and Status
Health Canada Approvals:
Other Uses:
- Symptomatic/progressive metastatic pancreatic (islet cell) cancer
Other Uses:
- Neuroendocrine tumours (metastatic carcinoid)
D - Adverse Effects
Emetogenic Potential:
High
Extravasation Potential: Vesicant
| ORGAN SITE | SIDE EFFECT* (%) | ONSET** | |||
|---|---|---|---|---|---|
| Dermatological | Nail disorder | I E | |||
| Gastrointestinal | Anorexia | E | |||
| Diarrhea | E | ||||
| Nausea (common) | I | ||||
| Vomiting (common) | I | ||||
| General | Fatigue | E | |||
| Hematological | Eosinophilia | E | |||
| Myelosuppression (10-20%; mild to moderate; may be severe; nadir 1-2 weeks) | E | ||||
| Hepatobiliary | Hepatic failure (rare) | E | |||
| ↑ LFTs (25%) | E | ||||
| Hypersensitivity | Hypersensitivity (fever, chills) | I | |||
| Infection | Sepsis | E | |||
| Injection site | Injection site reaction (burning, pain) | I | |||
| Metabolic / Endocrine | Glucose intolerance | E | |||
| Neoplastic | Leukemia (secondary) | L | |||
| Nervous System | Confusion | E | |||
| Depression | E | ||||
| Renal | Nephrogenic diabetes insipidus | ||||
| Nephrotoxicity (up to 75%; anuria, glycosuria, proteinuria, renal tubular acidosis) | E D | ||||
* "Incidence" may refer to an absolute value or the higher value from a reported range.
"Rare" may refer to events with < 1% incidence, reported in post-marketing, phase 1 studies,
isolated data or anecdotal reports.
Dose-limiting side effects are underlined.
** I = immediate (onset in hours to days) E = early (days to weeks)
D = delayed (weeks to months) L = late (months to years)
Nephrotoxicity is the dose-limiting toxicity and occurs in up to 75% of patients. Renal toxicity is dose-related, cumulative and may be fatal. Transient, reversible proteinuria occurs and is often the first sign of nephrotoxicity. Dose reduction or discontinuation is suggested if significant renal toxicity occurs. Hypokalemia, proximal renal tubular acidosis and Fanconi syndrome have been documented in 15-25% of patients. Monitor for the development of proteinuria, hypophosphatemia or a decline in 24-hour creatinine clearance that may precede any elevation of serum creatinine or BUN. The role of hydration in decreasing streptozocin-induced nephrotoxicity has not been clearly defined.
Severe nausea and vomiting beginning 1-4 hours following administration occur in most patients and may persist for more than 24 hours; some patients may require discontinuation of the drug. In up to 20% of patients, there may be a sudden release of insulin, with insulin shock (hypoglycemia) occurring within 24 hours of treatment. Mild to moderate, reversible abnormalities of glucose tolerance have been reported. Glycosuria has been observed and may result from the drug's effect on the proximal renal tubule.
The tissue necrosis that occurs with extravasation may happen days to weeks after the treatment. Patients must be observed for delayed reactions and prior injection sites carefully inspected.
E - Dosing
Refer to protocol by which patient is being treated. A repeat course should only be administered if the patient’s renal, hematologic and hepatic functions are within acceptable limits.
Adults:
Intravenous:
q1w: 1 g/m2 weekly for 2 weeks, then increase according to patient response;
maximum single dose: 1.5 g/m2
q6w: 500 mg/m2/day x 5 days (dose escalation on this schedule not recommended)
Dosage in combination:
- Reduced dose may be required
Dosage with Toxicity:
Dosage with myelosuppression:
Modify according to protocol by which patient is being treated; if no guidelines available, refer to Appendix 6 "Dosage Modification for Hematologic and Non-Hematologic Toxicities".
Dosage with toxicity: Reduce dose if nephrotoxicity occurs. (Refer to "Dosage with Renal Impairment" section)
Dosage with Hepatic Impairment:
Consider dose reduction or discontinuation if significant hepatic toxicity occurs.
Dosage with Renal Impairment:
Contraindicated with pre-existing renal impairment.
Creatinine clearance (mL/min) |
% usual dose |
10-50 |
75% |
<10 |
Avoid or treat with caution at prescriber discretion at reduced dose |
Children:
The safety and effectiveness of streptozocin in pediatric patients have not been established.
F - Administration Guidelines
- Mix in 50-250 mL bag (NS (preferred) or D5W); Infuse over 30 to 60 minutes.
- Incompatible with allopurinol, aztreonam or piperacillin/tazobactam
G - Special Precautions
Other:
Streptozocin is contraindicated in patients with known hypersensitivity to the drug, or pre-existing renal disease.
This drug should not be used in combination with or concomitantly with other potential nephrotoxins.
Streptozocin is mutagenic, teratogenic, carcinogenic and is an abortifacient. Acute leukemia, renal neoplasms and atypia of various cells have been reported. Streptozocin crosses the placenta and should not be used in pregnancy. Animal studies suggest fertility impairment with streptozocin. Breast feeding is not recommended due to the potential secretion into breast milk.
H - Interactions
| AGENT | EFFECT | MECHANISM | MANAGEMENT |
|---|---|---|---|
| Nephrotoxic drugs (i.e. aminoglycosides, amphotericin B, methotrexate) | ↑ nephrotoxicity | Additive toxicity | Caution, avoid concomitant use |
| Carmustine, or other drugs with similar cytotoxic effects | ↑ myelosuppression | Additive toxicity | Caution |
| Doxorubicin | ↑ toxicity of doxorubicin | Increased half-life of doxorubicin | Caution, consider reduced dose of doxorubicin |
| phenytoin | ↓ cytotoxic effect of streptozocin on beta cells of the pancreas | Uncertain | Avoid concomitant use |
| Corticosteroids | Risk of severe hyperglycemia | Uncertain | Caution; monitor |
I - Recommended Clinical Monitoring
Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.
Recommended Clinical Monitoring
| Monitor Type | Monitor Frequency |
|---|---|
| Liver function tests | Baseline and regular |
| CBC | Baseline and regular |
| Urinalysis (for proteinuria) | Regular |
| Renal function tests | Baseline and weekly, until 4 weeks after drug administration |
Clinical assessment for local toxicity |
At each visit |
Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version
Suggested Clinical Monitoring
| Monitor Type | Monitor Frequency |
|---|---|
| Serum glucose levels | Baseline and regular |
K - References
Cancer Drug Manual (the Manual), 1994, British Columbia Cancer Agency (BCCA).
Product Monograph: Zanosar® (streptozocin). Pfizer Canada, Inc., March 30, 2009.
Streptozocin: AHFS Drug Information. American Society of Health-System Pharmacists, 2009.
October 2017 edited other indication
L - Disclaimer
Refer to the New Drug Funding Program or Ontario Public Drug Programs websites for the most up-to-date public funding information.
The information set out in the drug monographs, regimen monographs, appendices and symptom management information (for health professionals) contained in the Drug Formulary (the "Formulary") is intended for healthcare providers and is to be used for informational purposes only. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects of a particular drug, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for a given condition. The information in the Formulary is not intended to constitute or be a substitute for medical advice and should not be relied upon in any such regard. All uses of the Formulary are subject to clinical judgment and actual prescribing patterns may not follow the information provided in the Formulary.
The format and content of the drug monographs, regimen monographs, appendices and symptom management information contained in the Formulary will change as they are reviewed and revised on a periodic basis. The date of last revision will be visible on each page of the monograph and regimen. Since standards of usage are constantly evolving, it is advised that the Formulary not be used as the sole source of information. It is strongly recommended that original references or product monograph be consulted prior to using a chemotherapy regimen for the first time.
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Last Updated: July 21, 2026
