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Eniluracil is an orally active small molecule that acts as a potent, irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the rate-limiting enzyme in the catabolism of fluoropyrimidines such as 5-fluorouracil (5-FU). By inhibiting DPD, eniluracil prevents rapid degradation of 5-FU, thereby increasing its oral bioavailability and prolonging tumor exposure to the drug. This mechanism allows for more predictable pharmacokinetics and toxicity profiles when using oral fluoropyrimidine chemotherapy. Eniluracil itself has no significant antitumor activity but is used to modulate and enhance the efficacy of chemotherapeutic agents like 5-FU. It has been investigated primarily in combination with fluoropyrimidines for various cancers including colorectal cancer, breast cancer, pancreatic cancer, hepatocellular carcinoma, and other solid tumors[1][2][3][4][6].
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