Drug reference

Pentostatin

Antimetabolite · Antineoplastic

Also known as Nipent, 2′-deoxycoformycin

AntimetaboliteAntineoplastic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid (teratogenic in animal studies).

FDA category + note

Top interactionssee all 12 →

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Mechanism

Pentostatin (2'-deoxycoformycin) is a potent irreversible inhibitor of adenosine deaminase (ADA), the enzyme that catalyzes the deamination of adenosine and deoxyadenosine. ADA inhibition causes intracellular accumulation of deoxyadenosine triphosphate (dATP), which inhibits ribonucleotide reductase and S-adenosylhomocysteine hydrolase, leading to impaired DNA synthesis and apoptosis. Lymphocytes are particularly sensitive because of their high ADA activity and dependence on the purine salvage pathway, making pentostatin highly effective in hairy cell leukemia.

Indications

Hairy cell leukaemia (initiated in specialist centres)Chronic lymphocytic leukemiaSmall cell non-Hodgkin's lymphomaHairy cell leukemia

Dosing

Adult: To be given by intravenous injection or intravenous infusion on alternate weeks (consult product literature)
Renal adjustment: Avoid if creatinine clearance less than 60 mL/minute

Pharmacokinetics

Half-life

5.7 h (mean terminal t1/2)

Excretion

Almost entirely by renal excretion.

Contraindications

Creatinine clearance less than 60 mL/minute
Men should not father children during and for 6 months after treatment

Side effects

Common

Agranulocytosisalopeciaamenorrhoeaanaemiaangina pectorisanxietyappetite decreasedarrhythmiasarthritisastheniaasthmaatrioventricular blockblood disorderbone disorderbone marrow disordersbreast masscardiac arrestchest painchillsconfusionconstipationcoughdeafnessdeathdepersonalisationdepressiondiarrhoeadizzinessdrowsinessdry eyedry mouthdysarthriadysphagiadyspnoeaear painelectrolyte imbalanceembolism and thrombosisemotional labilityeosinophiliaeye disorderseye inflammationeye painfebrile neutropeniafeverfluid imbalanceflushinggastrointestinal discomfortgastrointestinal disordersgoutgraft versus host diseasehaemorrhagehallucinationhangoverheadachesheart failurehostilityhyperbilirubinaemiahyperglycaemiahyperhidrosishypersensitivityhypertensionhypotensionincreased risk of infectioninfluenza like illMyelosuppressionGastrointestinal symptomsSkin rashesAbnormal liver function studiesNeutropenic fever

Serious