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Streptozocin | CAS No: 66395-18-4 | GMP-certified suppliers
A medication that treats malignant pancreatic neoplasms, particularly metastatic islet cell carcinoma, with antineoplastic and myelosuppressive properties requiring strict quality control.
Therapeutic categories
Primary indications
- For the treatment of malignant neoplasms of pancreas (metastatic islet cell carcinoma)
Product Snapshot
- Streptozocin is an injectable small molecule provided as a powder for solution for intravenous administration
- It is indicated primarily for the treatment of malignant pancreatic neoplasms, specifically metastatic islet cell carcinoma
- Streptozocin holds approved status in the US and Canada, with additional investigational uses under evaluation
Clinical Overview
Pharmacodynamically, streptozocin combines a nitrosourea moiety with a glucosamine sugar, enabling it to inhibit DNA synthesis in both bacterial and mammalian cells. While in bacteria it targets cytosine residues causing DNA degradation, its precise mechanism in mammalian cells remains incompletely understood. It inhibits cell proliferation at concentrations lower than those needed to block DNA precursor incorporation or enzyme activity related to DNA synthesis. The compound affects cell cycle progression without specificity to any particular mitotic phase.
The mechanistic basis of streptozocin involves the formation of methylcarbonium ions, which alkylate intracellular molecules including nucleic acids, leading to DNA cross-linking that inhibits replication. Additionally, streptozocin disrupts biochemical pathways involving NAD and NADH and inhibits certain gluconeogenic enzymes. These actions collectively contribute to its cytotoxic effects on pancreatic islet tumor cells.
Pharmacokinetic data on streptozocin are limited in public scientific sources; however, it is known to be a substrate for cytochrome P450 enzymes, particularly CYP1A2 and CYP2E1, indicating potential induction of these enzymes. It is also a P-glycoprotein inducer, which may affect drug disposition. Streptozocin exhibits myelosuppressive effects and possesses a narrow therapeutic index, necessitating careful dosing and monitoring.
Safety considerations include potential nephrotoxicity, hepatotoxicity, and gastrointestinal toxicity, which have been reported in clinical use. As an alkylating agent, it requires appropriate handling precautions to avoid exposure.
There are limited commercial brands of streptozocin globally, mostly utilized in specialized oncology settings. Regulatory approval status defines it as an approved investigational agent in specific territories.
For API procurement, stringent controls on purity, identity, and residual solvents are critical due to the compound’s cytotoxicity and narrow therapeutic range. Documentation confirming compliance with pharmacopeial standards and traceability to the producing strain of Streptomyces achromogenes is recommended to ensure quality and consistency.
Identification & chemistry
| Generic name | Streptozocin |
|---|---|
| Molecule type | Small molecule |
| CAS | 66395-18-4 |
| UNII | 8H27GUR065 |
| DrugBank ID | DB00428 |
Pharmacology
| Summary | Streptozocin is a nitrosourea alkylating agent that exerts cytotoxic effects primarily through DNA cross-linking, leading to inhibition of DNA synthesis and cell proliferation. It targets DNA, O-GlcNAcase, and glucose transporters, disrupting cellular metabolism and biochemical reactions involving NAD and NADH. Its therapeutic application is focused on the treatment of metastatic islet cell carcinoma of the pancreas. |
|---|---|
| Mechanism of action | Although its mechanism of action is not completely clear, streptozocin is known to inhibit DNA synthesis, interfere with biochemical reactions of NAD and NADH, and inhibit some enzymes involved in gluconeogenesis. Its activity appears to occur as a result of formation of methylcarbonium ions, which alkylate or bind with many intracellular molecular structures including nucleic acids. Its cytotoxic action is probably due to cross-linking of strands of DNA, resulting in inhibition of DNA synthesis. |
| Pharmacodynamics | Streptozocin is an antitumour antibiotic consisting of a nitrosourea moiety interposed between a methyl group and a glucosamine. Streptozocin is indicated in the treatment of metastatic islet cell carcinoma of the pancreas. Streptozocin inhibits DNA synthesis in bacterial and mammalian cells. In bacterial cells, a specific interaction with cytosine moieties leads to degradation of DNA. The biochemical mechanism leading to mammalian cell death has not been definitely established; streptozocin inhibits cell proliferation at a considerably lower level than that needed to inhibit precursor incorporation into DNA or to inhibit several of the enzymes involved in DNA synthesis. Although streptozocin inhibits the progression of cells into mitosis, no specific phase of the cell cycle is particularly sensitive to its lethal effects. |
Targets
| Target | Organism | Actions |
|---|---|---|
| O-GlcNAcase BT_4395 | Bacteroides thetaiotaomicron (strain ATCC 29148 / DSM 2079 / NCTC 10582 / E50 / VPI-5482) | antagonist |
| DNA | Humans | cross-linking/alkylation |
| Solute carrier family 2, facilitated glucose transporter member 2 | Humans | ligand |
ADME / PK
| Absorption | Poor oral absorption (17-25%) |
|---|---|
| Half-life | 5-15 minutes |
| Metabolism | Primarily hepatic |
| Route of elimination | As much as 20% of the drug (or metabolites containing an N-nitrosourea group) is metabolized and/or excreted by the kidney. |
Formulation & handling
- Streptozocin is administered exclusively via intravenous injection as a powder for solution, indicating sterile handling during reconstitution is required.
- Its low LogP and high water solubility support formulation in aqueous injectable solutions but may require attention to stability in solution.
- As a small molecule hexose derivative, it does not exhibit peptide or biologic characteristics, reducing concerns related to enzymatic degradation.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has reached patent expiry in both the US and Canada, allowing for the availability of generic formulations. The API is currently in the mature phase of its market lifecycle in these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Streptozocin is primarily manufactured and packaged by a limited number of companies, including Teva and Pharmacia, indicating a concentrated manufacturing landscape. Its branded products, such as Zanosar, are available mainly in the US and Canadian markets, with no significant presence noted in the EU or other regions. The patent status suggests existing generic competition is likely, reflected by the involvement of generic manufacturers like Teva. |
|---|
Safety
| Toxicity | Symptoms of overdose include nausea and vomiting, anorexia, myelosuppression; and nephrotoxicity. |
|---|
- Overdose may result in nausea, vomiting, and anorexia
- Myelosuppression is a reported adverse effect requiring monitoring
- Nephrotoxicity has been observed
Streptozocin is a type of Cytostatic antibiotics
Cytostatic antibiotics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the treatment of various types of cancer. These antibiotics possess powerful cytostatic or cell-inhibiting properties, which impede the growth and division of cancer cells.
Cytostatic antibiotics work by selectively targeting and inhibiting specific enzymes and proteins necessary for the replication and proliferation of cancer cells. By interrupting these vital cellular processes, these APIs effectively hinder the progression of cancer and prevent the spread of malignant cells.
One prominent example of a cytostatic antibiotic is Doxorubicin, which belongs to the anthracycline class of antibiotics. Doxorubicin functions by intercalating with DNA molecules, preventing DNA replication and inhibiting the activity of topoisomerase enzymes. These mechanisms effectively impede the growth and division of cancer cells.
Another commonly used cytostatic antibiotic is Mitomycin C. It exerts its anticancer effects by inducing DNA cross-linking, leading to the inhibition of DNA synthesis and cell division. This antibiotic is particularly effective against a variety of solid tumors.
Cytostatic antibiotics are administered in different ways, such as intravenous injection or oral consumption, depending on the specific drug. These APIs are often used in combination with other chemotherapy agents or treatment modalities to achieve optimal therapeutic outcomes.
In conclusion, cytostatic antibiotics are a vital subcategory of pharmaceutical APIs used in cancer treatment. Their ability to inhibit cell growth and division makes them essential in combating various types of cancer, ultimately improving patient outcomes.
Streptozocin (Cytostatic antibiotics), classified under Anticancer drugs
Anticancer drugs belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category designed specifically to combat cancer cells. These powerful medications play a crucial role in cancer treatment and are developed to target and destroy cancerous cells, preventing their growth and spread.
Anticancer drugs are classified based on their mode of action and can include various types such as chemotherapy drugs, targeted therapy drugs, immunotherapy drugs, and hormonal therapy drugs. Chemotherapy drugs work by interfering with the cell division process, thereby inhibiting the growth of cancer cells. Targeted therapy drugs, on the other hand, are designed to attack specific molecules or genes involved in cancer growth, minimizing damage to healthy cells. Immunotherapy drugs stimulate the body's immune system to recognize and destroy cancer cells. Hormonal therapy drugs are used in cancers that are hormone-dependent, such as breast or prostate cancer, to block the hormones that fuel cancer cell growth.
These APIs are typically synthesized through complex chemical processes in state-of-the-art manufacturing facilities. Stringent quality control measures ensure the purity, potency, and safety of these drugs. Anticancer APIs undergo rigorous testing and adhere to stringent regulatory guidelines before being approved for clinical use.
Due to their critical role in cancer treatment, anticancer drugs are in high demand worldwide. Researchers and pharmaceutical companies continually strive to develop new and more effective APIs in this category to enhance treatment outcomes and minimize side effects. The ongoing advancements in the field of anticancer drug development offer hope for improved cancer therapies and better patient outcomes.
Streptozocin API manufacturers & distributors
Compare qualified Streptozocin API suppliers worldwide. We currently have 1 companies offering Streptozocin API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Ferro Pfanstiehl Labs. | Producer | United States | United States | CoA, USDMF | 6 products |
When sending a request, specify which Streptozocin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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