Drug intelligence / Profile preview

eniluracil + fluorouracil

Development stage
Unknown
Lead developer
Fennec Pharmaceuticals
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Eniluracil + fluorouracil is a combination drug used in cancer treatment, primarily investigated for metastatic adenocarcinoma of the pancreas and metastatic colorectal cancer. Eniluracil is an orally active irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the major enzyme responsible for catabolizing 5-fluorouracil (5-FU). By inhibiting DPD, eniluracil significantly increases the plasma half-life, concentration, and oral bioavailability of 5-FU, thereby prolonging tumor exposure to 5-FU. This combination allows oral administration of 5-FU with enhanced pharmacokinetics compared to intravenous regimens. Clinical trials have shown limited activity in advanced pancreatic cancer with notable toxicities such as neutropenia and diarrhea. In metastatic colorectal cancer, efficacy was observed but did not meet equivalence criteria compared to standard 5-FU/leucovorin therapy; however, it showed a more favorable hematologic toxicity profile[1][2][3].

Other names
5-FU and eniluracilEU/5-FU
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)

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