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capecitabine + trimetrexate
- Development stage
- Unknown
- 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
- Oral, Intravenous
01
Overview
Capecitabine + trimetrexate is a combination chemotherapy regimen investigated primarily for the treatment of metastatic colorectal cancer. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), a fluoropyrimidine antimetabolite that interferes with DNA synthesis by inhibiting thymidylate synthase and incorporating into RNA and DNA, leading to cell death. Trimetrexate is a non-classical folic acid antagonist that inhibits dihydrofolate reductase (DHFR), thereby depleting tetrahydrofolic acid required for thymidylate and purine synthesis, disrupting DNA, RNA, and protein synthesis. The combination aims to enhance antitumor activity through dual inhibition of nucleotide biosynthesis pathways. Clinical studies have shown this regimen to be tolerable but with limited efficacy compared to other available therapies in previously treated metastatic colorectal cancer patients[1][2][3].
- Other names
- capecitabine + trimetrexateCAP + TMTX
02
Targets
DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)
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