II. Indications

  1. FDA Approved (in combination regimens)
    1. Hairy Cell Leukemia
  2. Off-Label Use
    1. Graft Versus Host Disease (acute or chronic)
    2. Chronic Lymphocytic Leukemia (CLL)
    3. Cutaneous T-Cell Lymphoma
    4. Mycosis Fungoides
    5. T-Cell Prolymphocytic Leukemia

III. Mechanism

  1. Purine Nucleotide analog
    1. Extracted from bacterium Streptomyces Antibioticus
    2. More active in lymph cells, esp. T-Cells, and esp. malignant T Cells and CD26+ Lymphocytes
  2. Inhibits adenine deaminase (ADA)
    1. Blocks Purine metabolism
    2. Increases intracellular dATP levels, inhibiting ribonucleotide reductase
    3. Inhibits DNA synthesis
    4. Inhibits RNA synthesis

IV. Medications

  1. Pentostatin powder for IV Solution in 10 mg vials

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Adverse Effects

  1. Alopecia
  2. Myelosuppression
  3. Hepatotoxicity
  4. Impaired future fertility
  5. Lung Toxicity
  6. Nephrotoxicity
  7. Neurotoxicity (CNS)
  8. Rash (severe)

VII. Safety

  1. Avoid in Pregnancy (any trimester)
    1. Use reliable Contraception
  2. Avoid in Lactation
  3. Monitoring
    1. Complete Blood Count
    2. Renal Function Tests

IX. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Ontology: Pentostatin (C0030896)

Definition (NCI_NCI-GLOSS) The active ingredient in a drug that is used to treat hairy cell leukemia and is being studied in the treatment of other types of cancer. Pentostatin blocks a protein needed for cell growth and may kill cancer cells. It is made by a bacterium. It is a type of adenosine deaminase inhibitor.
Definition (NCI) A purine nucleotide analogue antibiotic isolated from the bacterium Streptomyces antibioticus. Also known as 2'-deoxycoformycin, pentostatin binds to and inhibits adenine deaminase (ADA), an enzyme essential to purine metabolism; ADA activity is greatest in cells of the lymphoid system with T-cells having higher activity than B-cells and T-cell malignancies higher ADA activity than B-cell malignancies. Pentostatin inhibition of ADA appears to result in elevated intracellular levels of dATP which may block DNA synthesis through the inhibition of ribonucleotide reductase. This agent may also inhibit RNA synthesis and may selectively deplete CD26+ lymphocytes. (NCI04)
Definition (CSP) adenine nucleotide analog which inhibits adenine deaminase, used as an immunosuppressant to augment antineoplastics.
Definition (PDQ) A purine nucleotide analogue antibiotic isolated from the bacterium Streptomyces antibioticus. Also known as 2'-deoxycoformycin, pentostatin binds to and inhibits adenine deaminase (ADA), an enzyme essential to purine metabolism; ADA activity is greatest in cells of the lymphoid system with T-cells having higher activity than B-cells and T-cell malignancies higher ADA activity than B-cell malignancies. Pentostatin inhibition of ADA appears to result in elevated intracellular levels of dATP which may block DNA synthesis through the inhibition of ribonucleotide reductase. This agent may also inhibit RNA synthesis and may selectively deplete CD26+ lymphocytes. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39210&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39210&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C732" NCI Thesaurus)
Definition (MSH) A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.
Concepts Nucleic Acid, Nucleoside, or Nucleotide (T114) , Antibiotic (T195)
MSH D015649
SnomedCT 28149003, 387154004
English 2' Deoxycoformycin, 2'-Deoxycoformycin, Deoxycoformycin, Imidazo(4,5-d)(1,3)diazepin-8-ol, 3-(2-deoxy-beta-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (R)-, pentostatin, (R)-3-(2-Deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol, Pentostatine, DEOXYCOFORMYCIN 02, pentostatin (medication), PENTOSTATIN, Pentostatin [Chemical/Ingredient], Co-Vidarabine, Pentostatin, (R)-3-(2-Deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7, 8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol, Pentostatin (product), Pentostatin (substance), deoxycoformycin, 2'-deoxycoformycin, DCF
Swedish Pentostatin
Czech pentostatin
Finnish Pentostatiini
Russian PENTOSTATIN, 2'-DEZOKSIKOFORMITSIN, 2'-ДЕЗОКСИКОФОРМИЦИН, ПЕНТОСТАТИН
German DESOXYCOFORMYCIN 02, 2'-Desoxycoformycin, Pentostatin
Polish Pentostatyna
Japanese 2'-デオキシコホルマイシン, ペントスタチン, デオキシコフォルマイシン
Spanish desoxicoformicina, pentostatina (producto), pentostatina (sustancia), pentostatina, 2'-Desoxicoformicina, Pentostatina
French Pentostatine
Italian Pentostatina
Portuguese 2'-Desoxicoformicina, Pentostatina