Streptozocin
Streptozotocin (2-Deoxy-2-(3-methyl-3-nitrosoureido)-D-glucopyranose)
Also known as: Zanosar · NSC-85998 · streptozotocin · U-9889
Reviewed by the VetSheet Veterinary TeamUpdated Apr 5, 2026Evidence-based veterinary reference
This is a rate-based continuous infusion (CRI) dose. Calculate the infusion rate; do not use simple weight scaling.
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Dosing by species
🌎 NA — North America🌍 EU — Europe
Dogs
| Indication | Dose | Route | Frequency | Duration | Region |
|---|---|---|---|---|---|
| Recurrent insulinoma after surgery (investigational) | Begin saline diuresis: Give normal saline at 18-20 mL/kg/hour for 7-8 hours. Over the 4th-5th hour, give streptozocin in the saline solution at a dose of 500 mg/m 2 IV. Give an antiemetic (e.g., butorphanol) at the end of the 7-hour period. | IV | Once | 7-8 hours total | 🌎 NA |
| Pancreatic islet cell tumors | Normal saline is given IV at 18.3 mL/kg/hr for 3 hours, then streptozocin is administered at 500 mg/m 2 over two hours with the saline diuresis continuing. After streptozocin infusion completed, continue saline diuresis for another 2 hours. Butorphanol is administered as an antiemetic immediately after streptozocin. | IV | May repeat at 3 week intervals | Until evidence of tumor progression, recurrence of hypoglycemia, or drug toxicity | 🌎 NA |
- Recurrent insulinoma after surgery (investigational): Requires aggressive fluid therapy.
- Pancreatic islet cell tumors: Monitor for myelosuppression and nephrotoxicity.
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Streptozocin is an antineoplastic antibiotic originally derived from Streptomyces achromogenes, though commercial products are prepared synthetically. In veterinary medicine, it is primarily utilized for its targeted toxicity to pancreatic beta cells, making it a key treatment for recurrent, inoperable, or metastatic insulinomas in dogs.
- Clinical Pearl: Insulinomas are functional tumors of the pancreas that secrete excess insulin, leading to life-threatening hypoglycemia. Streptozocin selectively destroys these neoplastic cells, helping to control hypoglycemia and slow tumor progression.
- Due to its severe toxicity profile, its use is generally reserved for refractory cases where surgical resection is incomplete or impossible.
Mechanism of action
Streptozocin acts primarily as an alkylating agent.
- DNA Damage: It cross-links DNA strands → inhibits DNA synthesis and prevents precursor incorporation into DNA.
- Beta-Cell Toxicity: The drug enters cells via the GLUT2 transporter, which is highly expressed on pancreatic beta cells. Once inside, it causes a species-specific diabetogenic effect in dogs by reducing nicotinamide adenine dinucleotide (NAD) and ATP concentrations → irreversible beta cell necrosis.
- While it possesses antibacterial activity against gram-positive and gram-negative bacteria, its severe cytotoxicity precludes its use as an antibiotic.
Safety & warnings
Contraindications
- Patients without a confirmed histologic diagnosis of insulinoma
- Patients with completely resectable tumors
- Pregnancy (unless benefits outweigh risks; FDA Category C)
Adverse effects
- Serious, permanent renal toxicity
- Severe and protracted vomiting and nausea
- Mild myelosuppression
- Elevated liver enzymes
- Severe tissue necrosis if extravasated (vesicant)
Precautions
CRITICAL WARNING: Streptozocin is highly nephrotoxic. Aggressive IV saline diuresis is absolutely mandatory before, during, and after administration to prevent permanent renal failure.
- Must be used with extreme caution in patients with decreased renal, bone marrow, or hepatic function.
- Vesicant: Severe tissue necrosis will occur if the drug extravasates outside the vein. Ensure a perfectly placed, patent IV catheter.
- Nursing Safety: It is unknown if it is excreted in milk. Consider using milk replacer due to the potential for serious adverse reactions in nursing offspring.
Drug interactions
Streptozocin may prolong the half-life of doxorubicin; dosage adjustment may be required.
Additive or synergistic myelosuppression may occur.
May cause additive nephrotoxicity when used concurrently.
Can block the diabetogenic effects of streptozocin without altering its antineoplastic activity; this may be beneficial or detrimental depending on the clinical goal.
Monitoring
- Blood glucose (to assess efficacy)
- Baseline and post-treatment renal function tests (including urinalysis)
- CBC (for myelosuppression)
- Baseline and pre-retreatment liver function tests
- Hydration status (especially for the first few days after treatment or if vomiting is a problem)
Pharmacokinetics
Absorption
Must be administered IV. Cytotoxic nature precludes other routes.
Distribution
Distributes to most tissues; concentrations in the pancreas are higher than those found in plasma.
Metabolism
Metabolized, probably in the liver.
Elimination
Both unchanged and metabolized drug are excreted in the urine.
Overdose
Severe toxicity may result if acutely overdosed, primarily manifesting as acute renal failure, severe gastrointestinal distress, and myelosuppression. Dosages must be calculated carefully based on body surface area (m^2). Treatment is supportive, focusing on aggressive fluid diuresis and management of uremia and cytopenias.
Available products
Formulations
- Powder for injection
Human-labeled
- Streptozocin Powder for Injection: 1 gram (100 mg/mL) in vials; Zanosar® (Genesia Sicor); (Rx)
Regulatory status
No regulatory data for: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Storage & stability
Store lyophilized powder in the refrigerator and protect from light. Stable for at least 3 years after manufacture (1 year if stored at room temperature). Reconstitute with Dextrose 5% or 0.9% sodium chloride. The reconstituted solution is stable for 48 hours at room temperature and 96 hours if refrigerated, but as no preservative is added, the manufacturer recommends using the drug within 12 hours of mixing.
Client information
- Purpose: Your dog has been prescribed streptozocin to treat an insulinoma (a tumor of the pancreas that causes dangerously low blood sugar).
- Hospitalization Required: Because this drug can be very hard on the kidneys, your dog will need to stay in the hospital to receive continuous IV fluids before, during, and after the treatment to flush the kidneys and protect them from damage.
- Side Effects: Nausea and vomiting are very common. Your veterinarian will administer strong anti-nausea medications to keep your dog as comfortable as possible.
- Experimental Nature: This is considered an 'investigational' or off-label treatment in veterinary medicine. Strict follow-up monitoring of blood sugar, kidney values, and blood counts is absolutely essential.
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.