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- Tezacitabine
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Tezacitabine | CAS No: 171176-43-5 | GMP-certified suppliers
A medication that is investigated for treating colorectal, lung, gastric cancers, and leukemia by targeting tumor cell proliferation through antineoplastic and enzyme inhibition properties.
Therapeutic categories
Primary indications
- Investigated for use/treatment in colorectal cancer, lung cancer, leukemia (unspecified), and gastric cancer
Product Snapshot
- Tezacitabine is an oral small molecule nucleoside analog
- It is under investigation for therapeutic use in colorectal cancer, lung cancer, leukemia, and gastric cancer
- Tezacitabine currently holds an investigational status without regulatory approval from FDA or EMA
Clinical Overview
Pharmacologically, tezacitabine exerts its effects through metabolic activation by cellular kinases, leading to the formation of active diphosphate and triphosphate metabolites. The diphosphate form of tezacitabine irreversibly inhibits ribonucleotide reductase (RNR), a critical enzyme responsible for the reduction of ribonucleoside 5'-diphosphates into deoxyribonucleoside 5'-diphosphates, essential precursors for DNA synthesis. Overexpression of RNR is commonly observed in tumor cells, making it a relevant target for antineoplastic therapy. Inhibition of RNR by tezacitabine diphosphate impairs DNA synthesis, resulting in tumor cell apoptosis. Additionally, tezacitabine triphosphate serves as a substrate for DNA polymerase, disrupting DNA replication mechanisms. Notably, tezacitabine shows resistance to deamination by cytidine deaminase, a metabolic pathway that often reduces the efficacy of nucleoside analogues.
While detailed pharmacokinetic parameters have not been fully elucidated in the public domain, tezacitabine's resistance to cytidine deaminase-mediated deactivation suggests potentially favorable metabolic stability. Safety and toxicity profiles remain under investigation, with no established data from large-scale clinical trials due to its investigational status.
Tezacitabine has not been approved for commercial use and is primarily employed in research settings and clinical trials focused on solid tumors and hematologic malignancies. No marketed brand names are currently associated with this compound.
For API procurement, sourcing tezacitabine requires stringent quality controls, including verification of chemical purity, stereochemistry, and compliance with current Good Manufacturing Practices (cGMP). Given its investigational status, suppliers should provide comprehensive documentation on synthesis routes, impurity profiles, and stability data to ensure suitability for pharmaceutical development and regulatory submission purposes.
Identification & chemistry
| Generic name | Tezacitabine |
|---|---|
| Molecule type | Small molecule |
| CAS | 171176-43-5 |
| UNII | 7607Y95N9S |
| DrugBank ID | DB06433 |
Pharmacology
| Summary | Tezacitabine is a nucleoside analog prodrug activated intracellularly to diphosphate and triphosphate metabolites. The diphosphate metabolite irreversibly inhibits ribonucleotide reductase, impairing deoxyribonucleotide synthesis essential for DNA replication, while the triphosphate metabolite integrates into DNA via DNA polymerase, disrupting DNA synthesis. This dual mechanism targets rapidly proliferating tumor cells and demonstrates resistance to cytidine deaminase-mediated degradation. |
|---|---|
| Mechanism of action | Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication. This agent is relatively resistant to metabolic deactivation by cytidine deaminase. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates necessary for DNA synthesis and is overexpressed in many tumor types. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Ribonucleoside-diphosphate reductase large subunit | Humans |
Formulation & handling
- Tezacitabine is a small molecule suitable for oral formulation due to its solid state and moderate water solubility. Its low LogP value (-1.9) indicates favorable aqueous solubility but potential challenges in permeability. Stability considerations should include protection from moisture given its investigational status and pyrimidone structure.
Regulatory status
Tezacitabine is a type of Antineoplastics
Antineoplastics are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) primarily used in the treatment of cancer. These powerful substances inhibit or destroy the growth of cancer cells, thus impeding the progression of malignancies.
Antineoplastics exert their therapeutic effects through various mechanisms. Some APIs interfere with DNA replication, inhibiting the division and proliferation of cancer cells. Others target specific proteins or enzymes involved in tumor growth, effectively blocking their function. Additionally, certain antineoplastic agents induce programmed cell death, known as apoptosis, in cancer cells.
These APIs find application in a wide range of cancer treatments, including chemotherapy, targeted therapy, immunotherapy, and hormone therapy. They are often administered in combination with other drugs to optimize therapeutic outcomes and minimize drug resistance.
Antineoplastics are typically synthesized through complex chemical processes, ensuring high purity and potency. Stringent quality control measures are implemented throughout manufacturing to meet regulatory standards and ensure patient safety.
Although antineoplastics offer significant benefits in treating cancer, they can also cause adverse effects due to their cytotoxic nature. Common side effects include bone marrow suppression, gastrointestinal disturbances, hair loss, and immune system suppression. Close monitoring and supportive care are essential to manage these side effects effectively.
In conclusion, antineoplastics are a vital category of pharmaceutical APIs used in the treatment of cancer. Through their diverse mechanisms of action, these compounds play a critical role in combating malignancies and improving patient outcomes.
