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Tegafur | CAS No: 17902-23-7 | GMP-certified suppliers
A medication that supports combination treatment of advanced gastric and metastatic colorectal cancers by providing a prodrug of 5-fluorouracil with targeted antineoplastic activity.
Therapeutic categories
Primary indications
- Indicated for the treatment of cancer usually in combination with other biochemically modulating drugs
- Indicated in adults for the treatment of advanced gastric cancer when given in combination with [DB00515]
- Indicated for the first-line treatment of metastatic colorectal cancer with [DB03419] and calcium folinate
Product Snapshot
- Tegafur is an oral small molecule formulated as capsules and tablets
- It is primarily used in oncology for the treatment of advanced gastric cancer and metastatic colorectal cancer in combination with other chemotherapy agents
- Tegafur is approved and marketed within the European Union and holds both approved and investigational status
Clinical Overview
Pharmacologically, tegafur is converted enzymatically to 5-FU in vivo. The active metabolite 5-FU exerts cytotoxic effects by inhibiting thymidylate synthase, a key enzyme in the pyrimidine biosynthesis pathway responsible for converting deoxyuridylate (dUMP) to deoxythymidylate (dTMP). This inhibition disrupts DNA synthesis and repair, particularly impairing rapidly dividing cancer cells. Additionally, 5-FU metabolites incorporate into RNA, disturbing RNA processing and function. These mechanisms collectively result in antitumor activity.
Key ADME characteristics include oral bioavailability of tegafur, its hepatic metabolism primarily to 5-FU, and clearance involving multiple cytochrome P450 enzymes such as CYP1A2 and CYP2A6. The narrow therapeutic index of this agent requires careful dosing and monitoring, especially in combination regimens. Renal excretion of metabolites also underscores the need for caution in patients with impaired kidney function.
Safety concerns center on myelosuppression, a common dose-limiting toxicity, as well as gastrointestinal adverse effects. Other toxicities may arise from 5-FU exposure, including mucositis, hand-foot syndrome, and cardiotoxicity. Concomitant administration of enzyme inhibitors or modulators can affect 5-FU plasma levels, altering therapeutic outcomes and toxicity profiles.
Tegafur is included in several globally recognized combination therapies and is part of the WHO List of Essential Medicines as an important fluoropyrimidine derivative.
From a sourcing perspective, API quality should meet stringent regulatory standards, emphasizing consistent purity, stereochemical composition, and absence of impurities that might affect conversion to 5-FU. Given its complex metabolism and narrow therapeutic window, reliable supply chains and validated quality control processes are essential for ensuring clinical safety and efficacy.
Identification & chemistry
| Generic name | Tegafur |
|---|---|
| Molecule type | Small molecule |
| CAS | 17902-23-7 |
| UNII | 1548R74NSZ |
| DrugBank ID | DB09256 |
Pharmacology
| Summary | Tegafur is a pyrimidine analogue prodrug metabolized into fluorouracil, which inhibits thymidylate synthase, disrupting the synthesis of deoxythymidine monophosphate (dTMP) and subsequently DNA replication. Its active metabolites also interfere with RNA function by incorporation of fluorouridine triphosphate. Tegafur's mechanism results in antineoplastic effects primarily through inhibition of DNA synthesis and RNA processing, targeting rapidly proliferating cancer cells. |
|---|---|
| Mechanism of action | The transformation of 2'-deoxyurindylate (dUMP) to 2'-deoxythymidylate (dTMP) is essential in driving the synthesis of DNA and purines in cells . Thymidylate synthase catalyzes the conversion of dUMP to dTMP, which is a precursor of thymidine triphosphate (TTP), one of the four deoxyribonucleotides required for DNA synthesis . After administration into the body, tegafur is converted into the active antineoplastic metabolite, fluorouracil (5-FU). In tumour cells, 5-FU undergoes phosphorylation to form the active anabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP) . FdUMP and reduced folate are bound to thymidylate synthase leading to formation of a ternary complex which inhibits DNA synthesis . In addition, 5-fluorouridine-triphosphate (FUTP) is incorporated into RNA causing disruption of RNA functions . |
| Pharmacodynamics | Tegafur is an antineoplastic agent that belongs in the class of pyrimidine analogues. It interferes with the 2'-deoxythymidylate (DTMP) synthesis in the pyrimidine pathway, resulting in inhibition of DNA synthesis . In a phase III trial investigating the clinical efficacy of S-1 (tegafur/gimeracil/oteracil) in patients with advanced or recurrent gastric cancer, treatment resulted in a high response rate and was associated with a longer overall survival and longer progression-free survival rate when used in combination with cisplatin . In a meta analysis, triple combination therapy consisting of tegafur, gimeracil and oteracil showed longer survival times and well tolerance in patients with advanced gastric cancer . Tegafur and its active metabolites are potent myleosuppressive agents . |
Targets
| Target | Organism | Actions |
|---|---|---|
| Thymidylate synthase | Humans | inhibitor |
ADME / PK
| Absorption | Tegafur displays a dose-proportional pharmacokinetic properties. Tegafur is rapidly and well absorbed into the systemic circulation, reaching the peak plasma concentration within 1 to 2 hours of administration . |
|---|---|
| Half-life | The elimination half life of tegafur is approximately 11 hours . |
| Protein binding | Tegafur is 52.3% bound to serum proteins and 5-FU is 18.4% protein bound [L933, L934]. |
| Metabolism | Hepatic CYP2A6 is the predominant enzyme that mediates 5-hydroxylation of tegafur to generate 5'-hydroxytegafur. This metabolite is unstable and undergoes spontaneous degradation to form 5-FU, which is an active antineoplastic agent that exerts a pharmacological action on tumours. 5-FU is rapidly metabolised by the liver enzyme dihydropyrimidine dehydrogenase (DPD) . |
| Route of elimination | Following oral administration, about less 20% of total tegafur is excreted unchanged in the urine . |
| Volume of distribution | The volume of distribution based on apparent volume of distribution and urinary excretion data of tegafur is 16 L/m^2 . |
| Clearance | No pharmacokinetic data available. |
Formulation & handling
- Tegafur is formulated for oral administration primarily in capsule and tablet forms.
- It is a small molecule with moderate water solubility, facilitating oral bioavailability.
- Intake should be managed on an empty stomach with adequate hydration to support renal clearance.
Regulatory status
| Lifecycle | The API has reached patent expiry in the EU, enabling generic competition and indicating a mature market with established product availability. Market dynamics are driven by pricing and accessibility rather than patent protection. |
|---|
| Markets | EU |
|---|
Supply Chain
| Supply chain summary | Tegafur is primarily supplied by a limited number of originator companies, with branded formulations such as Teysuno marketed predominantly in the EU. The presence of a single brand across multiple samples suggests a concentrated originator role. Patent expirations in key markets may facilitate existing or forthcoming generic competition, influencing the supply dynamics. |
|---|
Safety
| Toxicity | Oral LD50 value in rat, mouse and dog are 930mg/kg, 775mg/kg, and 34mg/kg, respectively [MSDS]. Continuous exposure to tegafur may cause physical defects in the developing embryo (teratogenesis). Acute toxicity from the combination use of tegafur was associated with nausea, vomiting, diarrhoea, mucositis, gastrointestinal irritation, bleeding, bone marrow depression, and respiratory failure . Overdose may lead to fatal complications . In case of overdose, appropriate therapeutic and supportive medical interventions should be implemented. |
|---|
- Tegafur exhibits variable acute oral toxicity across species, with LD50 values of 930 mg/kg (rat), 775 mg/kg (mouse), and 34 mg/kg (dog)
- Chronic exposure presents teratogenic risks, with potential to cause embryonic developmental defects
- Overdose may induce severe systemic toxicity, including gastrointestinal, hematologic, and respiratory complications, potentially resulting in fatality
Tegafur 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.
Tegafur API manufacturers & distributors
Compare qualified Tegafur API suppliers worldwide. We currently have 3 companies offering Tegafur API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Cipla | Producer | India | India | CoA, GMP, WC | 164 products |
| Qilu Tianhe | Producer | China | China | CoA, JDMF, WC | 16 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, MSDS | 55 products |
When sending a request, specify which Tegafur 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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