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 |
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 Drug Interaction
Moderate: hydroxyurea, hepatitis b pediatric vaccine, chlorambucil, interferon alfa-2aUnknown: crizanlizumab, phytonadione, vandetanib, sulfamethoxazole / trimethoprim, prochlorperazine, sulfamethoxazole / trimethoprim, risdiplam, ceftazidime, obinutuzumab, givosiran, ibrutinib, propranolol, valbenazine, saquinavir, antihemophilic factor, fluvoxamine
Pentostatina Disease Interaction
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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