Pentostatin

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Pentostatin
Pentostatin structure.svg
Pentostatin ball-and-stick.png
Names
Trade namesNipent
Other names2'-deoxycoformycin (DCF)
  • (R)-3-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol
Clinical data
Drug classPurine antagonist[1]
Main usesHairy cell leukemia, chronic lymphocytic leukemia (CLL), cutaneous T-cell lymphoma[1]
Side effectsNausea, fever, rash, cough, shortness of breath, itchiness, headache, low blood cells[1]
Pregnancy
category
  • US: D (Evidence of risk)
Routes of
use
Intravenous
Typical dose4 mg/m2[1]
External links
AHFS/Drugs.comMonograph
US NLMPentostatin
MedlinePlusa692004
Legal
Legal status
Pharmacokinetics
Bioavailabilityn/a
Protein binding4%
MetabolismHepatic, minor
Elimination half-life2.6 to 16 hours, mean 5.7 hours
Chemical and physical data
FormulaC11H16N4O4
Molar mass268.273 g·mol−1
3D model (JSmol)
  • n1c3c(n(c1)[C@@H]2O[C@@H]([C@@H](O)C2)CO)N\C=N/C[C@H]3O
  • InChI=1S/C11H16N4O4/c16-3-8-6(17)1-9(19-8)15-5-14-10-7(18)2-12-4-13-11(10)15/h4-9,16-18H,1-3H2,(H,12,13)/t6-,7+,8+,9+/m0/s1 checkY
  • Key:FPVKHBSQESCIEP-JQCXWYLXSA-N checkY
  (verify)

Pentostatin, sold under the brand name Nipent, is a medication used to treat hairy cell leukemia, chronic lymphocytic leukemia (CLL), and cutaneous T-cell lymphoma.[1][2] It is given by injection into a vein.[1]

Common side effects include nausea, fever, rash, cough, shortness of breath, itchiness, headache, and low blood cells.[1] Other side effects may include seizures, coma, kidney problems, lung toxicity, and infection.[1] Use in pregnancy may harm the baby.[1] It is a purine antagonist.[1]

Pentostatin was approved for medical use in the United States in 1991.[1] In the United Kingdom 10 mg of medication costs the NHS about £730 as of 2021.[3] This amount in the United States is about 2,300 USD.[4]

Medical uses

Pentostatin is used to treat hairy cell leukemia.[5] 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.[6]

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

Dosage

It may be used at a dose of 4 mg/m2 every two weeks.[1]

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.[7]

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.

References

  1. 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 "Pentostatin Monograph for Professionals". Drugs.com. Retrieved 27 October 2021.
  2. "DailyMed - NIPENT- pentostatin injection, powder, lyophilized, for solution". dailymed.nlm.nih.gov. Retrieved 27 October 2021.
  3. BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 964. ISBN 978-0857114105.
  4. "Nipent Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 27 October 2021.
  5. 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.
  6. 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.
  7. 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.

External links

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