喷司他丁 (Nipent)

概览

Pentostatin is an adenosine deaminase inhibitor used to treat hairy cell leukemia.

作用机制

Pentostatin is a potent transition state inhibitor of adenosine deaminase (ADA), the greatest activity of which is found in cells of the lymphoid system. T-cells have higher ADA activity than B-cells, and T-cell malignancies have higher activity than B-cell malignancies. The cytotoxicity that results from prevention of catabolism of adenosine or deoxyadenosine is thought to be due to elevated intracellular levels of dATP, which can block DNA synthesis through inhibition of ribonucleotide reductase. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Cytotoxicity is cell cycle phase-specific (S-phase).

适应症

For the treatment of hairy cell leukaemia refractory to alpha interferon.

• Acute Graft-Versus-Host Disease (GVHD)
• B-Lymphocytic, prolymphocytic leukemia (Kiel Classification) refractory
• Chronic Lymphocytic Leukemia
• Hairy Cell Leukemia (HCL)
• Mycosis Fungoides (MF)
• Sezary Syndrome
• Steroid refractory Chronic graft versus host disease