Drug intelligence / Profile preview

Dipyridamole, Fluorouracil, and Folinic Acid Chemotherapy Regimen

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination therapy consisting of three components: 1. **Dipyridamole**: A nucleoside transport inhibitor that can potentially enhance the cytotoxicity of fluorouracil in a dose-dependent manner. 2. **Fluorouracil (5-FU)**: A chemotherapy drug that destroys quickly dividing cells, such as cancer cells. It works by interfering with DNA synthesis and RNA function. 3. **Folinic acid (Leucovorin)**: Not a chemotherapy drug itself, but a biochemical modulator that enhances the efficacy of fluorouracil by stabilizing the binding of fluorouracil to its target enzyme, thymidylate synthase. The rationale behind this combination is that dipyridamole may increase the intracellular concentration of fluorouracil by inhibiting nucleoside transport, while folinic acid enhances fluorouracil's cytotoxic effects by providing an expanded folate pool. This combination has been studied in Phase I and Phase II clinical trials for various advanced malignancies, particularly colorectal cancer.

Other names
Dipyridamole/Fluorouracil/Folinic AcidDipyridamole, 5-FU, Leucovorin
02

Targets

PDE5 (Phosphodiesterase 5A)ENT1 (Solute carrier family 29 member 1)DNATS (Thymidylate synthase)DHFR (Dihydrofolate reductase)

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