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Tetrahydrouridine | CAS No: 18771-50-1 | GMP-certified suppliers

A medication that acts as an investigational antimetabolite studied for potential applications in oncology and hematology, particularly targeting various cancers and sickle cell disease.

Therapeutic categories

AntimetabolitesNoxaeNucleic Acids, Nucleotides, and NucleosidesNucleosidesPyrimidine NucleosidesPyrimidines
Generic name
Tetrahydrouridine
Molecule type
small molecule
CAS number
18771-50-1
DrugBank ID
DB12484
Approval status
Investigational drug

Product Snapshot

  • Tetrahydrouridine is a small molecule primarily developed for oral formulation
  • It is investigated for use as a cytidine deaminase inhibitor in oncology applications
  • The compound is currently in the investigational stage and has not received FDA or EMA approval

Clinical Overview

Tetrahydrouridine (CAS number 18771-50-1) is a pyrimidine nucleoside derivative characterized by a tetrahydro modification of the uridine base. As an organic compound, it consists of a pyrimidine ring linked to a ribosyl sugar moiety, placing it within the broader class of pyrimidine nucleosides.

This compound has been primarily explored in investigational settings and preclinical or clinical trials involving various neoplastic conditions including lung, breast, and head and neck cancers, as well as sickle cell disease. However, it currently lacks a specified clinical indication and has not received regulatory approval for therapeutic use.

Pharmacodynamic and pharmacokinetic data for tetrahydrouridine remain limited in the public domain. Its biological activity is generally related to its properties as an antimetabolite, potentially influencing nucleic acid metabolism. The mechanism of action is not fully elucidated but may involve interference with enzymes involved in pyrimidine metabolism or nucleoside processing pathways.

Absorption, distribution, metabolism, and excretion parameters have not been comprehensively described in clinical literature. Safety and toxicity profiles are not explicitly characterized but, given its classification and investigational status, careful evaluation of off-target cytotoxicity and the potential for nucleic acid metabolic disruption is warranted.

Tetrahydrouridine belongs to investigational drug categories including antimetabolites and compounds associated with toxic actions related to nucleic acid metabolism. Notable usage contexts revolve around its experimental use as a biochemical tool or adjunct in oncology and hematology research.

For active pharmaceutical ingredient (API) sourcing, quality considerations include stringent control of purity, stereochemistry, and stability due to its nucleoside structure. Given the investigational nature of tetrahydrouridine, procurement should prioritize suppliers compliant with Good Manufacturing Practice (GMP) standards and with validated analytical characterization to ensure consistency and suitability for research or development applications.

Identification & chemistry

Generic name Tetrahydrouridine
Molecule type Small molecule
CAS 18771-50-1
UNII 0NIZ8H6OL8
DrugBank ID DB12484

Formulation & handling

  • Tetrahydrouridine is a small molecule with high aqueous solubility, suitable primarily for oral formulations. Its low logP indicates hydrophilic nature, affecting permeability and formulation strategies. Stability considerations should focus on protecting the pyrimidine nucleoside structure from hydrolytic degradation.

Regulatory status

Tetrahydrouridine is a type of Antimetabolites


Antimetabolites are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) utilized in the treatment of various diseases, particularly cancer. These compounds are structurally similar to naturally occurring metabolites essential for cellular processes such as DNA and RNA synthesis. By mimicking these metabolites, antimetabolites interfere with the normal functioning of cellular pathways, leading to inhibition of cancer cell growth and proliferation.

One of the widely used antimetabolites is methotrexate, a folic acid antagonist that inhibits the enzyme dihydrofolate reductase, disrupting the production of DNA and RNA. This disruption impedes the growth of rapidly dividing cancer cells. Another common antimetabolite is 5-fluorouracil (5-FU), which inhibits the enzyme thymidylate synthase, thereby interfering with DNA synthesis and inhibiting cancer cell proliferation.

Antimetabolites can be classified into several subcategories based on their mechanism of action and chemical structure. These include purine and pyrimidine analogs, folic acid antagonists, and pyrimidine synthesis inhibitors. Examples of antimetabolites in these subcategories include azathioprine, cytarabine, and gemcitabine.

Despite their effectiveness, antimetabolites can exhibit certain side effects due to their interference with normal cellular processes. These side effects may include gastrointestinal disturbances, myelosuppression (reduced production of blood cells), and hepatotoxicity.

In conclusion, antimetabolites are a vital category of pharmaceutical APIs used in the treatment of various diseases, especially cancer. By mimicking natural metabolites and disrupting crucial cellular processes, these compounds effectively inhibit cancer cell growth and proliferation. However, their usage should be carefully monitored due to potential side effects.