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5-fluorodeoxyuridine + arabinosyl cytosine
- Development stage
- Unknown
- Lead developer
- National Cancer Institute
- 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, Intra-arterial
01
Overview
This drug is a combination of two antimetabolite chemotherapeutic agents: - **5-fluorodeoxyuridine (also known as floxuridine or 5-FdUrd)** is a pyrimidine analog that inhibits thymidylate synthase, thereby blocking DNA synthesis and repair. It is primarily used in the treatment of colorectal cancer and other solid tumors[6]. - **Arabinosyl cytosine (also known as cytarabine or ara-C)** is a nucleoside analog that inhibits DNA polymerase, leading to impaired DNA synthesis. It is widely used in the treatment of leukemias. The combination has been studied for synergistic effects against leukemia cells and some solid tumors. Preclinical studies show more than additive (synergistic) effects in certain leukemia cell lines; clinical trials have explored its use in advanced breast cancer and other malignancies[2][7][9]. The main toxicities are hematologic (myelosuppression), with gastrointestinal side effects also reported.
- Other names
- 5-FdUrd + ara-Cfloxuridine + cytarabine5-fluorodeoxyuridine plus arabinosyl cytosine
02
Targets
TS (Thymidylate synthase)POLA1 (DNA polymerase alpha)
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