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dexamethasone + floxuridine + leucovorin + mitomycin C

Development stage
Unknown
Lead developer
Merck
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
Intra-arterial
01

Overview

This is a multi-agent chemotherapy regimen combining four drugs: - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties. - **Floxuridine** is an antimetabolite chemotherapeutic agent that inhibits DNA synthesis by acting as a pyrimidine analog. - **Leucovorin** (folinic acid) enhances the cytotoxic effects of fluoropyrimidine drugs like floxuridine by stabilizing the binding of their active metabolites to thymidylate synthase. - **Mitomycin C** is an alkylating agent that crosslinks DNA, leading to inhibition of DNA synthesis and function. This combination has been studied primarily for intrahepatic arterial infusion in patients with unresectable hepatic metastases from colorectal cancer. The addition of dexamethasone to floxuridine and leucovorin reduces hepatic toxicity while maintaining or improving response rates. Mitomycin C adds further cytotoxic activity. The regimen has shown notable activity even in patients pretreated or resistant to systemic chemotherapy, though gastrointestinal toxicity (notably diarrhea) can be significant[1][2][4].

Other names
dexamethasonefloxuridineleucovorinmitomycin C
02

Targets

GR (Glucocorticoid receptor)TS (Thymidylate synthase)DNA

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