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leucovorin + 5-fluorouracil + capecitabine
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination regimen consisting of leucovorin (folinic acid), 5-fluorouracil (5-FU), and capecitabine. Leucovorin is not a chemotherapy agent but enhances the effectiveness of 5-fluorouracil by stabilizing the binding of its active metabolite to thymidylate synthase, thereby increasing cytotoxicity. 5-Fluorouracil is an antimetabolite that inhibits DNA synthesis by blocking thymidylate synthase, leading to cell death in rapidly dividing cancer cells. Capecitabine is an oral prodrug that is converted enzymatically into 5-FU within tumor tissues, providing similar mechanisms and efficacy as intravenous 5-FU regimens. This combination targets DNA synthesis in cancer cells and is primarily used for the treatment of colorectal cancer, especially as adjuvant or first-line therapy for high-risk stage II or III colon cancer[1][2][4]. The regimen leverages both intravenous (leucovorin/5-FU) and oral (capecitabine) fluoropyrimidine approaches.
- Brand names
- Xeloda
- Other names
- folinic acid + 5-fluorouracil + capecitabine5-FU + LV + capecitabineleucovorin + 5-fluorouracil + capecitabine
02
Targets
TS (Thymidylate synthase)
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