Pentostatina

Pentostatina Uses, Dosage, Side Effects, Food Interaction and all others data.

A potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.

Pentostatina is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia and hairy cell leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. 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).

Trade Name Pentostatina
Availability Prescription only
Generic Pentostatin
Pentostatin Other Names Co-vidarabine, Pentostatin, Pentostatina, Pentostatine, Pentostatinum
Related Drugs interferon alfa-2b, cladribine, Intron A, Nipent, Leustatin
Type
Formula C11H16N4O4
Weight Average: 268.2691
Monoisotopic: 268.11715502
Protein binding

4%

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Pentostatina
Pentostatina

Uses

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

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

Pentostatina is also used to associated treatment for these conditions: B-Lymphocytic, prolymphocytic leukemia (Kiel Classification) refractory, Chronic Lymphocytic Leukaemia (CLL), Graft Versus Host Disease, Acute, Hairy Cell Leukemia (HCL), Mycosis Fungoides (MF), Sezary Syndrome, Chronic, steroid refractory Graft versus host disease

How Pentostatina works

Pentostatina 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).

Toxicity

LD50=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression.

Food Interaction

No interactions found.

Pentostatina Disease Interaction

Major: infections, myelosuppression, renal dysfunction

Elimination Route

Not absorbed orally, crosses blood brain barrier.

Half Life

5.7 hours (with a range between 2.6 and 16 hrs)

Clearance

  • 68 mL/min/m2

Elimination Route

In man, following a single dose of 4 mg/m2 of pentostatin infused over 5 minutes, approximately 90% of the dose was excreted in the urine as unchanged pentostatin and/or metabolites as measured by adenosine deaminase inhibitory activity.

Innovators Monograph

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