Drug intelligence / Profile preview

pentostatin

Development stage
Approved
Lead developer
Supergene
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Covalent 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

Pentostatin is a purine analog antimetabolite and antineoplastic agent used primarily in the treatment of hairy cell leukemia. It is also used for T-cell prolymphocytic leukemia and has been employed in chronic lymphocytic leukemia (CLL) patients who have relapsed, as well as in steroid-refractory acute and chronic graft-versus-host disease[1][5][10]. Pentostatin acts as a potent transition state inhibitor of adenosine deaminase (ADA), an enzyme with high activity in lymphoid cells. Inhibition of ADA leads to accumulation of intracellular deoxyadenosine triphosphate (dATP), which blocks DNA synthesis by inhibiting ribonucleotide reductase and can also interfere with RNA synthesis. This results in cytotoxicity that is most pronounced during the S-phase of the cell cycle[2][9]. Pentostatin is administered intravenously, typically every two weeks over several months[3][5].

Brand names
Nipent
Other names
2′-deoxycoformycinDCF
02

Targets

ADA (Adenosine deaminase)

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