Zanosar

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Zanosar

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Treatment option: Carcinoma

Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Zanosar

What is Zanosar? (Streptozocin Identity and Classification)

Property Description
Active ingredient Streptozocin (Streptozotocin)
Form Sterile powder for injection
Pharmacological class Alkylating agent (Antineoplastic)
Common use Cancer chemotherapy
Origin Naturally derived (from Streptomyces achromogenes)

What Type of Medicine is Zanosar?

Zanosar is a potent antineoplastic agent used in chemotherapy, with Streptozocin (Streptozotocin) as its sole active compound. It is specifically categorized as an alkylating agent, belonging to the nitrosoureas chemical subclass. This classification defines its core high-level purpose: to chemically interfere with the genetic material of rapidly dividing abnormal cells.

The medication's role is strictly confined to cellular disruption, achieved through a mechanism that involves damaging the DNA within the cell. Pharmacological studies have widely supported the drug's activity, establishing its role as a key cytotoxic agent in specific neuroendocrine applications. The utility of this agent has been recognized in treating conditions like certain metastatic pancreatic islet cell cancers.

Composition, Origin, and Form

The composition of the active compound, Streptozocin, is chemically unique, featuring a glucosamine moiety linked to a potent nitrosourea group. This specific structure, which resembles a glucose molecule, is essential as it governs the compound's cellular uptake. This antineoplastic agent is not purely synthetic; it is a derivative of a substance originally isolated from the naturally occurring soil microbe Streptomyces achromogenes.

The brand product, Zanosar, is typically manufactured in the European Union and is a prescription-only (Rx) medicine due to its complex administration and therapeutic profile. It is supplied as a sterile powder for injection—a freeze-dried preparation—and its sole authorized route of administration is through intravenous administration (IV). This ensures the necessary systemic distribution required for therapeutic effect against susceptible cells.

Regulatory References

  1. Streptozocin LiverTox profile

What side effects are possible with Zanosar?

Possible Side Effects and Safety Information: Zanosar (Streptozocin)

Zanosar is a chemotherapy drug with a serious, documented safety profile, primarily characterized by dose-limiting organ toxicities and significant adverse reactions. Its use requires specialized medical supervision.


Serious and Clinically Significant Adverse Reactions

Adverse Reaction Category Severity & Characteristics
Renal Toxicity The most serious and dose-limiting toxicity. It is cumulative and dose-related, occurring in approximately 25-75% of patients. Manifestations include azotemia, anuria, glycosuria, and renal tubular acidosis, which can be severe or fatal.
Gastrointestinal Severe nausea and vomiting occur in most patients, often requiring antiemetics and occasionally necessitating discontinuation. Diarrhea is also commonly reported.
Hematologic Myelosuppression (bone marrow suppression) is possible, with rare reports of fatal leukopenia or thrombocytopenia.
Hepatic Liver toxicity may occur, evidenced by elevations in liver enzymes and decreases in serum albumin.
Metabolic Abnormalities of glucose tolerance are common, ranging from mild impairment to severe hypoglycemia and insulin shock (due to the drug's effect on pancreatic beta cells).

Safety Restrictions and Monitoring

Zanosar is a known vesicant; extravasation during injection may lead to severe local tissue damage and necrosis. The drug is classified in regulatory documents as a possible carcinogen and mutagen, and is contraindicated in pregnancy due to the risk of fetal harm.

Patient monitoring must be rigorous and include frequent checks of renal function, hepatic function, and complete blood counts before and during therapy. Adequate hydration is often recommended to help mitigate the risk of nephrotoxicity. Use with other nephrotoxic agents is generally contraindicated.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Zanosar (streptozocin) overdose centers strictly on the documented, serious toxicities and mandated emergency actions. Overexposure is explicitly documented to cause severe and potentially fatal toxicity, with effects classified within the following domains:

Documented Overdose Manifestations and Risks

Domain Regulatory Statement Summary
Primary Manifestation Dose-related and cumulative nephrotoxicity (kidney damage), which may include azotemia, anuria, and renal tubular acidosis.
Systemic Risks The potential for fatal hematological toxicity (myelosuppression) and hepatotoxicity is officially documented. Acute effects may include severe nausea and vomiting and CNS signs like confusion or lethargy.
Antidote Status No specific antidote is known for Streptozocin overdose.

When to Seek Urgent Medical Attention

The regulatory labeling requires immediate medical intervention for suspected overdose or when severe symptoms arise. Seek immediate medical attention (e.g., calling emergency services) if the individual has collapsed, had a seizure, has trouble breathing, or cannot be awakened. Management of overdose should consist solely of supportive and symptomatic measures in a facility equipped with the necessary laboratory and resources to monitor toxicity.

Therapeutic Uses of Zanosar

What Zanosar Treats: Main Uses and Benefits

Zanosar (streptozocin) is a specialized medication primarily used in the therapeutic domain of oncology to manage specific, advanced cancers. Its principal role is applied in addressing metastatic pancreatic islet cell carcinoma, a rare form of pancreatic neuroendocrine tumor (pNET).

The medication is commonly used to help with insulin-secreting islet cell tumors and related hormone-secreting tumors arising from the pancreas. Its application is relevant for easing conditions where functional stability becomes affected by the tumor's presence and associated hormone overproduction. This approach helps ease the overall symptom burden for patients with progressive disease.

The drug provides support for symptoms related to systemic imbalance that can result from hormone hypersecretion. The clinical context is often described as symptomatic management for advanced disease, and it may be part of symptomatic management when supportive relief is needed. The medication is considered relevant in contexts involving heightened systemic burden.


Quick Fact: Supports Symptom Clusters that interfere with daily comfort

Regulatory References

  1. NIH LiverTox overview

Eligibility and Restrictions for Use

Official Eligibility and Non-Eligibility for Zanosar

Official regulatory documentation defines eligibility for Zanosar (streptozocin) through a strict framework of contraindications, organ function status, and reproductive constraints.

Category Regulatory Status
Populations Allowed Patients with metastatic islet cell carcinoma of the pancreas (symptomatic or progressive metastatic disease).
Absolute Contraindications Hypersensitivity to streptozocin; Pre-existing renal disease or severe renal impairment; Concomitant use with live or live-attenuated vaccines.

Conditional Use and Age Limitations

The drug is not established for the pediatric population (patients under 18 years) as safety and effectiveness data are insufficient. Use in older adults requires caution, often starting at the lower end of the dosing range, due to the higher frequency of decreased organ function in this group.

Category Condition-Based Rule
Renal Function Use requires close monitoring of renal function; dose must be adapted, and use is contraindicated if the Estimated Glomerular Filtration Rate (eGFR) is below 30 mL/min.
Hepatic Function Requires close monitoring of hepatic function (liver function tests).
Pregnancy Not recommended; women of child-bearing potential must use effective contraception during treatment due to the risk of fetal harm.
Lactation Breastfeeding must be discontinued during therapy.

These constraints dictate that eligibility is strictly limited to patients where the potential benefit, as judged by a physician, outweighs the known risk of serious, often cumulative, toxicity.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Zanosar (streptozocin) has officially documented interaction patterns that primarily concern additive toxicity and the clearance of co-administered agents, as defined in regulatory labeling. Certain combinations are strictly contraindicated to mitigate the risk of serious adverse outcomes.

Co-administration with other potential nephrotoxic drugs is contraindicated due to the high risk of exacerbating renal insult, which may lead to serious kidney damage. This prohibition includes specific agents such as tenofovir disoproxil fumarate. Additionally, administration of live or live-attenuated vaccines is contraindicated, as the immunosuppressive effect of Zanosar may result in serious or fatal infections.

The product labeling also documents pharmacodynamic and pharmacokinetic interactions that require caution. When Zanosar is used concurrently with antineoplastic drugs having similar effects, additive toxicity (such as myelosuppression) is likely to occur. A specific pharmacokinetic outcome involves Doxorubicin, where streptozocin is reported to prolong the elimination half-life, thereby increasing the exposure and risk of severe bone marrow suppression from doxorubicin. Furthermore, concurrent use of steroids may result in severe hyperglycemia.

A procedural constraint is also present: the reconstituted product must not be mixed with other medicinal products, especially other cytotoxic drugs, in the intravenous line, apart from specified diluents.

Mechanism of Action

The mechanism of Streptozocin (Zanosar) is a multi-step cytotoxic action defined by three sequential effects on the target cell: selective entry, genetic damage, and metabolic depletion.

Selective Targeting and Cellular Entry

This domain covers the critical first step where the drug achieves selective cellular exposure. Its glucosamine structure allows it to act as a toxic substrate mimic for the Solute Carrier Family 2, Facilitated Glucose Transporter Member 2 ( GLUT2). This transport enables high-concentration uptake primarily into cells that express this system, concentrating the subsequent cytotoxic mechanism to GLUT2-expressing cells.

DNA Alkylation and Metabolic Sabotage

The primary action is initiated by the drug's nitrosourea moiety, which breaks down to form an alkylating agent that directly and covalently modifies the cell's DNA, causing strand breaks and cross-linking. This damage triggers a rapid but futile repair attempt involving the hyperactivation of the PARP enzyme. This cascade rapidly depletes the cell's stores of the essential cofactor NAD^+ and, consequently, cellular ATP.

Final Physiological Consequences

The combination of DNA damage and this self-induced metabolic collapse creates a terminal energy crisis within the cell. This systemic failure results in the initiation of cytotoxicity (cell death). This destructive physiological consequence defines the terminal effect of the drug's action against the susceptible cell population.

Dosage and Administration Information

Zanosar is administered exclusively as an intravenous (IV) infusion, as the medication is not active when taken orally. The medicine is supplied as a sterile powder in 1 gram vials, and the total dose is calculated based on the patient's Body Surface Area (m^2).

Two standardized cyclic dosing regimens are officially utilized. The Daily Schedule involves administering 500 mg/m^2 over five consecutive days, with the entire cycle repeated every six weeks. Alternatively, the Weekly Schedule starts at 1000 mg/m^2 once weekly, with a maximum single dose not exceeding 1500 mg/m^2.

The preparation of Zanosar requires the powder to be reconstituted with a specific volume of 5% Dextrose or 0.9% Sodium Chloride Injection, and the resulting solution must be used within 12 hours. Administration must be through a free-flowing IV line and typically requires hyperhydration to support proper usage. The infusion itself is delivered over a specific period, generally ranging from 30 minutes to 4 hours.

Dose adjustments are required based on the patient's functional health status. For instance, the label mandates a 50% dose reduction if signs of renal impairment are present, such as an eGFR between 45 and 60 mL/min. Treatment is continued until maximum benefit is achieved or until predefined clinical standards for discontinuation are observed. Safety and usage standards are not established for pediatric patients under 18 years.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Zanosar

Evidence for Use in Metastatic Pancreatic Islet Cell Carcinoma

Zanosar (streptozocin) was studied for use in people diagnosed with metastatic pancreatic islet cell carcinoma, a rare type of neuroendocrine tumor. The research base includes historical Randomized Controlled Trials (RCTs), which are highly controlled studies that compare one group of patients receiving streptozocin-based treatment to a group receiving a different treatment. These RCTs were followed by many larger retrospective cohort analyses and smaller Phase I/II clinical trials. This body of evidence was used in research exploring streptozocin, often used in combination with other agents, in patients with this condition.

The studies primarily enrolled adult patients whose cancer was advanced, meaning it was unresectable, or had metastasized (spread) to other parts of the body. The research explored outcomes in patients with both functional tumors and non-functional tumors. The findings describe patterns observed in the studies regarding tumor response and patient survival.


What Outcomes Studies Measured

Researchers in these trials focused on several key outcomes related to how the disease evolved during the study period. One major measurement was the Objective Response Rate (ORR), which is a measure of tumor size change (reduction or stability) recorded using standard imaging criteria. The studies also monitored time-based measures, such as Overall Survival (OS) and Progression-Free Survival (PFS), which track how long patients lived, or lived without the cancer progressing, respectively.

For patients with functional tumors, a critical measurement was the Biochemical Response. This was studied for how the elevated levels of hormones or tumor markers in the blood changed while patients were on treatment. The ability to monitor these outcomes related to systemic or functional imbalance is relevant in evidence describing how symptoms are measured in people with this condition.


The Study Landscape and Research Quality

The research base for Zanosar was associated with initial evidence from historical RCTs that often compared streptozocin combined with other drugs, like 5-fluorouracil, against other regimens. This evidence described the patterns of change observed in treated populations. However, the evidence quality varies across studies. The evidence is generally regarded as Moderate, which reflects the support from those earlier controlled trials, but it also acknowledges the limited information available from historical studies compared to contemporary trial designs.

Frequently Asked Questions (FAQ)

Common questions about Zanosar (FAQ)


Q: Are the side effects of Zanosar permanent?

Official documents indicate that the most serious side effect, renal toxicity (kidney damage), is dose-related and cumulative, meaning the risk of harm increases over time. The drug is also classified as a possible carcinogen and mutagen, which suggests the potential for long-lasting effects on the body. Other effects, such as severe nausea and vomiting, are often acute and are not typically cited as permanent.


Q: Can Zanosar cause long-term health problems?

Yes, the official product information indicates Zanosar is a known carcinogen and mutagen, meaning it may interfere with genetic material. Additionally, its most significant toxicity, kidney damage, is described as cumulative and can be severe. Because of these potential long-term risks, rigorous monitoring of kidney function is mandated by the label before and during therapy.


Q: How long does the effect of Zanosar last in the body?

According to regulatory pharmacokinetic data, the active ingredient in Zanosar, streptozocin, has a short elimination half-life of approximately 35 to 40 minutes in the bloodstream. Up to 20% of the drug or its metabolites (breakdown products) is reported to be excreted by the kidney.


Q: Can Zanosar be used by people with liver disease?

Official product information requires close monitoring of hepatic function (liver function tests) during Zanosar treatment. The drug label emphasizes the need for caution in patients with liver disease, as the effects of the medicine may potentially be increased due to potentially slower processing and removal by the liver.


Q: Why do some patients need to stop Zanosar treatment?

Treatment is officially administered until the maximum clinical benefit is achieved or until predefined clinical standards for discontinuation are met. Severe, dose-limiting side effects, such as critical renal toxicity or severe nausea and vomiting, are among the clinical standards that may lead to discontinuation.


Q: What is the typical length of time a person takes Zanosar?

The total length of time a person receives Zanosar treatment is determined by the prescribing physician based on the individual's condition and tolerance of the medicine. The drug is administered in cycles, with one common regimen repeated every six weeks, but the overall duration varies.


Q: Does Zanosar interact with common over-the-counter pain relievers?

Official regulatory documents contain a strict prohibition against using Zanosar alongside other potentially nephrotoxic drugs (medicines that can harm the kidneys). Official guidance indicates that patients should inform their physician of all co-administered medicines, including over-the-counter (OTC) products, to avoid potential harmful interactions.


Q: What lifestyle changes are often suggested while on Zanosar?

Regulatory documents note the importance of maintaining adequate hydration to help reduce the risk of kidney toxicity. Furthermore, the product label states that women of childbearing potential must use effective contraception during treatment, and breastfeeding must be discontinued due to the risk of harm to the infant.


Q: Is Zanosar a targeted therapy?

Zanosar is chemically classified as an alkylating agent, which is a type of general chemotherapy that damages genetic material. However, its mechanism of action includes a feature of selective cellular entry because its structure resembles glucose, allowing it to be taken up more efficiently by cells that use the GLUT2 transporter.


Q: What happens when treatment with Zanosar is stopped?

Treatment is stopped either when the maximum therapeutic benefit is achieved or when toxicity (such as severe kidney damage or bone marrow suppression) is deemed too great. The label notes that monitoring of organ function and blood counts may continue after stopping therapy due to the drug's potential for cumulative toxicity.


Q: Are there specific vitamins or supplements to avoid while on Zanosar?

Official patient guidance indicates the need to inform a healthcare provider of all concomitant therapy, which includes dietary and herbal supplements. While not contraindications, some non-prescription substances, such as Vitamin A and Vitamin E, have been noted in research to have the potential for mild interactions.


Q: Does Zanosar have a generic version available?

Yes, the active ingredient, Streptozocin (or Streptozotocin), is available under the brand name Zanosar and as an officially recognized generic formulation for injection.


Q: How quickly does Zanosar start working after the first use?

Clinical studies indicate the median time to the onset of a therapeutic response (a measurable change in the tumor) is reported to be around 17 days after starting the medicine.


Q: What are the restrictions on food or drink when taking Zanosar?

Because the drug is administered via an intravenous (IV) infusion, there are no specific food or drink contraindications listed in the principal regulatory labeling. However, official guidance advises discussing the use of the medicine alongside food, alcohol, or tobacco with a healthcare professional, as interactions may occur.


Q: Does Zanosar affect a person's ability to drive or operate machinery?

Official regulatory warnings note the need to avoid hazardous activities, such as driving or operating complex machinery, after administration. This is because certain side effects, including confusion, lethargy, and depression, have been reported in some patients.


Q: Is it normal to feel tired or fatigued after taking Zanosar?

The official product information lists lethargy (a lack of energy) and unusual tiredness or weakness among the potential less common side effects reported during treatment. Additionally, conditions like anemia, which can cause fatigue, are possible due to the drug's effect on bone marrow.


Q: Where can I find the official prescribing information for Zanosar?

The official prescribing information for the US market is published on the FDA's DailyMed website, which provides the full drug label. For information relevant to European Union markets, documents are available from the European Medicines Agency (EMA) SmPC (Summary of Product Characteristics).


Q: Is there any research looking at Zanosar and fertility?

Regulatory documents classify Zanosar as a possible mutagen, meaning it can cause genetic changes, and the drug has been linked to potential female and male reproductive toxicity. The product label states that women of childbearing potential must use effective contraception during treatment due to the risk of fetal harm.


Q: Does Zanosar interact with herbal supplements?

Yes, the official labeling specifically advises patients to inform their healthcare professional about all existing or planned concurrent therapies, including the use of herbal supplements.


Q: Why is Zanosar sometimes administered in a hospital setting?

Zanosar should be administered under the supervision of a qualified physician in a facility that is equipped to closely monitor the patient's drug tolerance and manage serious complications. The risk of severe nephrotoxicity (kidney damage) and the requirement for hyperhydration during the IV infusion contribute to the need for specialized medical oversight.


Q: Does Zanosar affect the heart?

Official FDA labeling lists serious heart symptoms as potential adverse effects that have been reported in some patients. These include symptoms such as fast or pounding heartbeats and a fluttering sensation in the chest. Official guidance states that symptoms related to the heart should be reported immediately.


Q: Are there different brand names for the same drug as Zanosar?

The trade name for the drug is Zanosar, but the active ingredient is Streptozocin (or Streptozotocin). The generic form of Streptozocin is widely available under multiple different manufacturer labels.


Q: Is Zanosar a controlled substance?

According to official regulatory documents, the active ingredient in Zanosar, Streptozocin, is not listed as a controlled substance under the U.S. Controlled Substances Act (CSA) or similar international frameworks.


Q: How is Zanosar typically eliminated from the body?

The drug is primarily cleared from the body via hepatic metabolism (processed by the liver). However, official pharmacokinetic data indicates that up to 20% of the drug or its metabolites is excreted by the kidney.


Q: Can Zanosar affect mental clarity or mood?

Yes, regulatory documents note that some patients have experienced effects on the central nervous system, including confusion, lethargy, and depression, particularly during continuous IV infusions. Less common effects such as anxiety, nervousness, and shakiness have also been reported.


Q: Is Zanosar only used for serious conditions?

Zanosar is indicated for the treatment of metastatic islet cell carcinoma of the pancreas, a serious type of cancer. Due to its intrinsic and potentially severe toxicity to the kidneys and bone marrow, its use is reserved in official guidance for patients with symptomatic or progressive metastatic disease.

How should Zanosar be stored and disposed of?

Storage and Disposal Requirements for Zanosar

Zanosar (streptozocin) sterile powder requires specific conditions to maintain its potency, as mandated by regulatory documents.

Item Requirement
Storage Temperature Store unopened vials in a refrigerator (2 C to 8 C).
Light Protection Keep the vial in the outer carton to protect the contents from light.
Child Safety Store the medicine out of the reach and sight of children.

The reconstituted solution is for single-use only and its total storage time should not exceed 12 hours. As a cytotoxic agent, disposal must follow established local procedures for cytotoxic agents and must not be performed via household waste or wastewater. Personnel handling the powder or solution must use appropriate protective equipment, and accidental contact requires immediate washing with soap and water.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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