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Brand Name :
Zanosar
(United States) [Available]Synonyms :
Streptozocin
Class :
Antineoplastic agents and Nitrosoureas
Brand Name :
Zanosar
(United States) [Available]Synonyms :
Streptozocin
Class :
Antineoplastic agents and Nitrosoureas
Dosage Forms & StrengthsÂ
powder for injectionÂ
1g/vialÂ
Metastatic Islet Cell Cancer Of Pancreas
Single-agent therapy:
1000
mg/m^2
Intravenous (IV)
1
week
,may increase to no more than 1500 mg per m²
Combination therapy: 500 mg per m² per day IV for five days for every 4-6Weeks
Dose Adjustments
Renal Impairment:
CrCl >50 mL/min: May administer full dose
CrCl: 10-50 mL/min: 75% of regular dose
CrCl: <10 mL/min: 50% of regular dose
may have an increased neutropenic effect when combined with deferiprone
may have an increased myelosuppressive effect when combined with ropeginterferon alfa-2b
may increase the Myelosuppressive effect of each other when combined
when both drugs are combined, there may be an increased risk or severity of adverse effects    
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of infection    
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of neutropenia    
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
myelosuppressive agents may diminish the therapeutic effect of BCG
may have an increased myelosuppressive effect when combined with fexinidazole
abiraterone acetate and niraparibÂ
may increase the neutropenic effect of myelosuppressive agents
dipyridamole: it may decrease the therapeutic effect of myelosuppressive agents
olopatadine: it may decrease the therapeutic effect of myelosuppressive agents
paraldehyde: it may decrease the therapeutic effect of myelosuppressive agents
when both drugs are combined, there may be an increased risk or severity of infection   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of infection   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
when both drugs are combined, there may be an increased risk or severity of adverse effects   
It may enhance the serum concentration when combined with alkalinizing agents
methoxypolyethylene glycol-epoetin betaÂ
combining streptozocin with methoxy polyethylene glycol-epoetin beta can raise the risk or severity of thrombosis
myelosuppressive Agents may enhance the adverse/toxic effect of clozapine
myelosuppressive Agents may enhance the myelosuppressive effect of Olaparib
myelosuppressive Agents may enhance the neutropenic effect of deferiprone
may enhance the effect of myelosuppressive agents
may enhance the effect of myelosuppressive agents
may have an increased myelosuppressive effect when combined with myelosuppressive agents
may have an increased myelosuppressive effect when combined with olaparib
may have an increased adverse effect when combined with clozapine
may have an increased adverse effect when comb
may decrease the therapeutic effect when combined with BCG vaccine
may have an increased myelosuppressive effect when combined with myelosuppressive agents
may increase the toxic effect of myelosuppressive agents
It may enhance the serum concentration when combined with alkalinizing agents
It may diminish the excretion when combined with alkalinizing agents
It may enhance the serum concentration when combined with alkalinizing agents
It may enhance the serum concentration when combined with alkalinizing agents
It may enhance the serum concentration when combined with alkalinizing agents
It may enhance the serum concentration when combined with alkalinizing agents
It may enhance the risk of adverse effects when combined with Hormone Antagonists
ozanimod: it may decrease the therapeutic effect of myelosuppressive agents
tofacitinib: it may decrease the therapeutic effect of myelosuppressive agents
when both drugs are combined, there may be an enhanced therapeutic efficacy and reduced toxicity of anticancer drugs by synergism 
The immunosuppressive effect of immunosuppressants (cytotoxic chemotherapy) may be increased by denosumab
Streptozocin is a nitrosourea chemotherapy agent that exerts its effect by alkylating DNA, leading to DNA strand crosslinking and interference with DNA replication and transcription. It also modifies proteins and may inhibit enzymes involved in DNA synthesis, contributing to its cytotoxic effects. The presence of a glucose moiety allows selective uptake by pancreatic islet cells, enhancing its targeting of certain tumors.Â
Streptozocin is primarily active against pancreatic islet cell tumors (neuroendocrine tumors) due to its selective affinity. It has also shown limited efficacy against other slow-growing endocrine and hormone-secreting tumors.Â
Adverse drug reactions:  Â
Frequency definedÂ
>10%  Â
Hypoglycemia  Â
Metabolic changes  Â
Myelosuppression   Â
Nephrotoxicity  Â
Vomiting  Â
Frequency Not Defined  Â
Chills  Â
Confusion Lethargy Depression  Â
Fever  Â
Decreased liver function  Â
Hematologic toxicity  Â
Injection site reactions  Â
Jaundice  Â
Nausea  Â
Nail changes  Â
Nephrogenic diabetes insipidus
Streptozocin should be given only by a qualified cancer specialist in a medical setting equipped to manage potential toxic effects. The drug poses a serious risk of kidney damage, which is dose-dependent and can be irreversible or fatal. It may also cause severe nausea and vomiting, sometimes limiting treatment. Other possible side effects include liver issues, diarrhea, and blood cell abnormalities. In laboratory studies, streptozocin has shown mutagenic and tumor-causing potential in rodents. Therefore, the decision to use this medication must involve a careful assessment of the potential benefits versus risks for each patient.Â
ContraindicationsÂ
Known hypersensitivityÂ
Severe renal impairment not manageable with dose adjustmentÂ
CautionsÂ
Streptozocin carries a significant risk of severe nephrotoxicity, which is both dose-related and cumulative—doses exceeding 1500 mg/m² may lead to azotemia. Patients may also experience intense nausea and vomiting, which can be challenging to manage. Rapid intravenous infusion of the drug may cause a burning sensation at the injection site. Additionally, streptozocin can alter glucose metabolism in some individuals, potentially leading to hypo- or hyperglycemia. Due to its potential teratogenic effects, pregnancy should be avoided during treatment.Â
Pregnancy warnings:   Â
Breastfeeding warnings:   Â
Pregnancy Categories:     Â
Streptozocin is a naturally derived nitrosourea-based antineoplastic agent primarily used in the treatment of pancreatic islet cell carcinoma, especially in cases with metastasis. Its antitumor activity stems from its role as an alkylating agent, where it causes DNA damage by forming crosslinks and interfering with DNA synthesis and replication. This disruption leads to cell cycle arrest and apoptosis, effectively inhibiting the growth of cancer cells.Â
PharmacokineticsÂ
AbsorptionÂ
Streptozocin has a low bioavailability of approximately 17–25%, indicating limited absorption when administered by non-intravenous routes.Â
DistributionÂ
It has a volume of distribution (Vd) of 43.8 liters, suggesting moderate tissue penetration.Â
MetabolismÂ
It is primarily metabolized in the liver.Â
Elimination/ExcretionÂ
The drug is mainly eliminated via the urine, with 60–70% excreted unchanged.Â
Half-life: The elimination half-life of streptozocin is about 35–40 minutes.SÂ
Clearance: Its systemic clearance ranges from 173 to 718 mcg/min, with an average of 478 mcg/min.Â
Onset and Peak Response: With a dose schedule of 1500 mg/m², the onset of action occurs around 17 days, and the peak therapeutic response is typically seen by 35 days.Â
PharmacodynamicsÂ
Streptozocin is an antitumor antibiotic composed of a nitrosourea group linked to a methyl group and a glucosamine moiety. It is primarily used for the treatment of metastatic pancreatic islet cell carcinoma. Streptozocin works by inhibiting DNA synthesis in both bacterial and mammalian cells. In bacteria, it specifically interacts with cytosine residues, leading to DNA degradation. Although the exact mechanism of action in mammalian cells is not fully understood, streptozocin is known to inhibit cell proliferation and delay mitotic progression, without targeting any particular phase of the cell cycle.Â
Streptozocin should be reconstituted with 9.5 mL of D5W or NS to prepare a 100 mg/mL pale gold solution. Although stable for up to 96 hours when refrigerated, it is best used within 12 hours due to the absence of preservatives. As a vesicant, it must be diluted in over 100 mL of D5W or NS and infused over 15 minutes to 6 hours. Prolonged infusions (e.g., 5 days) may increase the risk of CNS toxicity and require caution.Â
It is compatible with D5W and NS, and Y-site compatible with several drugs (e.g., filgrastim, ondansetron, vinorelbine), but incompatible with allopurinol, aztreonam, cefepime, and piperacillin/tazobactam. Vials should be refrigerated and protected from light for optimal stability.Â
Pronunciation:Â strep-to-zo-cin
Use:Â It is an anti-cancer agent used to treat metastatic cancer in Islet Cells of the pancreas.
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