Pentostatin

Pentostatin (or deoxycoformycin, trade name Nipent, manufactured by SuperGen) is an anticancer chemotherapeutic drug.[1]

Pentostatin
Clinical data
Trade namesNipent
AHFS/Drugs.comMonograph
MedlinePlusa692004
Pregnancy
category
  • US: D (Evidence of risk)
    Routes of
    administration
    Intravenous
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailabilityn/a
    Protein binding4%
    MetabolismHepatic, minor
    Elimination half-life2.6 to 16 hours, mean 5.7 hours
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.164.991
    Chemical and physical data
    FormulaC11H16N4O4
    Molar mass268.273 g·mol−1
    3D model (JSmol)
      (verify)

    Mechanism

    It is classified as a purine analog, which is a type of antimetabolite.

    It mimics the nucleoside adenosine and thus inhibits the enzyme adenosine deaminase, interfering with the cell's ability to process DNA.[2]

    Cancer cells generally divide more often than healthy cells; DNA is highly involved in cell division (mitosis) and drugs which target DNA-related processes are therefore more toxic to cancer cells than healthy cells.

    Uses

    Pentostatin is used to treat hairy cell leukemia.[3] It is given by intravenous infusion once every two weeks for three to six months.

    Additionally, pentostatin has been used to treat steroid-refractory acute and chronic graft-versus-host disease.[4]

    Pentostatin is also used in chronic lymphocytic leukemia (CLL) patients who have relapsed.

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    References

    1. Kay NE, Geyer SM, Call TG, et al. (January 2007). "Combination chemoimmunotherapy with pentostatin, cyclophosphamide, and rituximab shows significant clinical activity with low accompanying toxicity in previously untreated B chronic lymphocytic leukemia". Blood. 109 (2): 405–11. doi:10.1182/blood-2006-07-033274. PMC 1785105. PMID 17008537.
    2. Sauter C, Lamanna N, Weiss MA (September 2008). "Pentostatin in chronic lymphocytic leukemia". Expert Opin Drug Metab Toxicol. 4 (9): 1217–22. doi:10.1517/17425255.4.9.1217. PMID 18721115.
    3. Cannon T, Mobarek D, Wegge J, Tabbara IA (October 2008). "Hairy cell leukemia: current concepts". Cancer Invest. 26 (8): 860–5. doi:10.1080/07357900801965034. PMID 18798068.
    4. Bolaños-Meade J, Jacobsohn DA, Margolis J, Ogden A, Wientjes MG, Byrd JC, Lucas DM, Anders V, Phelps M, Grever MR, Vogelsang GB (April 2005). "Pentostatin in steroid-refractory acute graft-versus-host disease". J Clin Oncol. 23 (12): 2661–8. doi:10.1200/JCO.2005.06.130. PMID 15837980.
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