eniluracil + fluorouracil + leucovorin

This is an oral combination regimen of three agents: - **Eniluracil** is a potent irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for the rapid breakdown of fluorouracil (5-FU). By inactivating DPD, eniluracil increases the oral bioavailability and systemic exposure to 5-FU. - **Fluorouracil (5-FU)** is a pyrimidine analog antimetabolite that inhibits thymidylate synthase, thereby blocking DNA synthesis and exerting cytotoxic effects on rapidly dividing cancer cells. - **Leucovorin (folinic acid)** enhances the binding of 5-FU’s active metabolite to thymidylate synthase, further potentiating its antitumor activity. The combination was developed to allow effective oral administration of 5-FU with improved pharmacokinetics and efficacy. It has been studied primarily in metastatic colorectal carcinoma and metastatic breast cancer patients who have failed capecitabine therapy. While it demonstrated some clinical activity—such as partial responses or stable disease in heavily pretreated patients—its use has been limited by significant toxicity at certain dosing regimens[1][2][3]. The regimen may offer an alternative for patients unable to tolerate intravenous chemotherapy or those progressing on capecitabine.

Other names

eniluracil plus 5-fluorouracil and leucovorineniluracil/5-FU/leucovorin