Ethynyluracil (Not yet branded)

Description

Ethynyluracil (also known as eniluracil) is a dihydropyrimidine dehydrogenase (DPD) inhibitor designed to enhance the efficacy of fluorouracil-based chemotherapy in colorectal cancer. This compound works by blocking the enzyme responsible for fluorouracil degradation, allowing for oral administration of fluorouracil and potentially improved therapeutic outcomes. Ethynyluracil was developed specifically to overcome the rapid metabolism of fluorouracil that limits its oral bioavailability and therapeutic window.

Mechanism of Action

Ethynyluracil irreversibly inhibits dihydropyrimidine dehydrogenase, the rate-limiting enzyme in fluorouracil catabolism that normally degrades over 80% of administered fluorouracil within the first pass through the liver. By blocking this enzymatic pathway, ethynyluracil significantly increases fluorouracil plasma levels and prolongs its half-life, theoretically allowing for more consistent drug exposure and enhanced antitumor activity.

Molecular Targets

Side Effects

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials