CAS · 103766-25-2
Product Overview
Gimeracil丨CAS 103766-25-2 is a pharmacologically active compound primarily known as a potent inhibitor of dihydropyrimidine dehydrogenase (DPD) - the enzyme responsible for the catabolism of 5-fluorouracil (5-FU) and related fluoropyrimidine drugs. By inhibiting DPD, gimeracil increases the bioavailability and therapeutic efficacy of 5-FU, making it an important agent in cancer chemotherapy.
Gimeracil is a key component of the oral anticancer drug S-1, a combination formulation containing tegafur, gimeracil, and oteracil potassium, designed to enhance 5-FU effectiveness while reducing toxicity.
Product Specifications
| Appearance | White to pale yellow crystalline powder |
|---|---|
| Purity | 99.7% min |
| Identification | Maximum wavelength absorption at 289 nm |
| Individual impurity | 0.1% max |
| Total impurities | 0.3% max |
| Loss on drying | 1.0% max |
| Residue on ignition | 0.2% max |
Applications
1. Cancer Chemotherapy
● Enhancer of fluoropyrimidine drugs: Gimeracil丨CAS 103766-25-2 is used to inhibit DPD, slowing the breakdown of 5-FU in the body.
● This prolongs the plasma concentration of 5-FU, enhancing its anticancer activity against solid tumors, such as colorectal, gastric, pancreatic, and head & neck cancers.
● Improves efficacy of oral 5-FU prodrugs (like tegafur) by maintaining therapeutic drug levels.
2. Combination Drug Formulations
● Integral part of the S-1 formulation (Tegafur + Gimeracil + Oteracil potassium), used widely in Asia and increasingly globally.
● S-1 provides oral administration convenience, better patient compliance, and reduced side effects compared to intravenous 5-FU therapy.
3. Pharmacokinetic Modulator
● Modulates the pharmacokinetics of fluoropyrimidines, leading to improved dose control and reduced variability in drug exposure.
● Helps tailor cancer therapy regimens to maximize efficacy and minimize toxicity.
Benefits
1. Increased Efficacy of Chemotherapy
● By inhibiting DPD, gimeracil enhances the concentration and duration of 5-FU in the plasma.
● This leads to stronger antitumor effects and potentially improved patient outcomes.
2. Oral Drug Convenience
● Enables effective oral fluoropyrimidine chemotherapy, offering better quality of life compared to intravenous treatments.
● Facilitates outpatient treatment and reduces hospital visits.
3. Reduced Side Effects
● By controlling 5-FU levels more precisely, it helps to mitigate common toxicities like hand-foot syndrome, gastrointestinal irritation, and myelosuppression.
● Contributes to a more manageable safety profile in cancer patients.
4. Pharmacological Specificity
● Gimeracil selectively inhibits DPD without affecting other enzymes, leading to targeted pharmacokinetic modulation.
● Minimizes off-target effects.
Conclusion
Gimeracil丨CAS 103766-25-2 is a critical DPD inhibitor used to enhance the therapeutic efficacy of 5-fluorouracil and related anticancer drugs. Its role in oral chemotherapy formulations such as S-1 represents a significant advancement in cancer treatment by improving drug bioavailability, efficacy, and patient convenience while reducing toxicity. Gimeracil continues to be a key agent in modern oncology, contributing to better cancer management outcomes.
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