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methotrexate + 5-fluorouracil + leucovorin
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Intravenous, Oral, Intramuscular, Intrathecal, Topical
01
Overview
This is a combination chemotherapy regimen consisting of methotrexate, 5-fluorouracil (5-FU), and leucovorin (also known as folinic acid). Methotrexate is an antimetabolite that inhibits dihydrofolate reductase, blocking DNA synthesis. 5-Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and disrupts DNA and RNA synthesis. Leucovorin is a reduced form of folic acid used to "rescue" normal cells from the toxic effects of methotrexate and to enhance the cytotoxicity of 5-fluorouracil by stabilizing its binding to thymidylate synthase. This combination has been used in various solid tumors including colorectal cancer[4][7].
- Other names
- methotrexate5-FUleucovorinfolinic acid
02
Targets
DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)
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