Drug intelligence / Profile preview

fludarabine

Development stage
Approved
Lead developer
Bayer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Fludarabine is a purine analogue antimetabolite chemotherapy drug primarily used in the treatment of B-cell chronic lymphocytic leukemia (CLL), especially in patients who have not responded to or whose disease has progressed during treatment with at least one alkylating-agent-containing regimen[1][4][5]. It is also used off-label for other hematologic malignancies such as non-Hodgkin's lymphoma and acute leukemias[6]. Fludarabine works by interfering with DNA synthesis through inhibition of DNA polymerase alpha, ribonucleotide reductase, and DNA primase after intracellular conversion to its active triphosphate form. This results in the inhibition of cancer cell growth and eventual cell death[2][8]. The drug is administered intravenously or orally (though oral formulations are no longer available in some markets)[1][3]. Common side effects include myelosuppression, immunosuppression leading to increased infection risk, nausea, vomiting, fever, fatigue, and neurologic symptoms. Severe adverse effects can include profound immunosuppression and neurotoxicity[5][8].

Brand names
FludaraOforta
Other names
fludarabine phosphate2-fluoro-ara-adenineF-ara-A氟达拉滨
02

Targets

POLA1 (DNA polymerase alpha)RNR (Ribonucleotide reductase)DNA-directed primase/polymerase protein (PrimPol)

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