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Nelarabine

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Nelarabine
Names
Trade namesArranon, Atriance
Other names506U78
Clinical data
Drug classAntimetabolite[1]
Main usesAcute T-cell lymphoblastic leukemia and lymphoma[2]
Side effectsBone marrow suppression, sleepiness, headache, numbness, fever, swelling, vomiting[2]
Pregnancy
category
  • US: N (Not classified yet)
Routes of
use		Intravenous
External links
AHFS/Drugs.comMonograph
MedlinePlusa607077
Legal
License data
Legal status
Pharmacokinetics
Protein binding<25%
MetabolismBy adenosine deaminase, to 9-β-D-arabinofuranosylguanine
Elimination half-life30 minutes (nelarabine)
3 hours (ara-G)
ExcretionKidney
Chemical and physical data
FormulaC11H15N5O5
Molar mass297.271 g·mol−1
3D model (JSmol)
  • n2c1c(nc(nc1OC)N)n(c2)[C@@H]3O[C@@H]([C@@H](O)[C@@H]3O)CO
  • InChI=1S/C11H15N5O5/c1-20-9-5-8(14-11(12)15-9)16(3-13-5)10-7(19)6(18)4(2-17)21-10/h3-4,6-7,10,17-19H,2H2,1H3,(H2,12,14,15)/t4-,6-,7+,10-/m1/s1 checkY
  • Key:IXOXBSCIXZEQEQ-UHTZMRCNSA-N checkY

Nelarabine, sold under the brand names Arranon and Atriance , is a medication used to treat T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL).[2] It is used when other treatments are not effective.[2] It is given by gradual injection into a vein.[2]

Common side effects include bone marrow suppression, sleepiness, headache, numbness, fever, swelling, and vomiting.[2] Other side effects may include confusion, seizures, tumor lysis syndrome, and peripheral neuropathy.[2] Use in pregnancy may harm the baby.[2] It is an antimetabolite which replaces guanine and interferes with the making of new DNA.[1]

Nelarabine was approved for medical use in the United States and Europe in 2005.[5][1] In the United Kingdom six vials of 250 mg cost the NHS about £1,300 as of 2021.[6] In the United States this amount costs about 4,600 USD.[7] A generic version was approved in 2021 in the USA.[8]

Medical uses

Dosage

In adults it is used at a dose of 1500 mg/m2 on day 1, 3, and 5 out of 21 days.[5]

Mechanism of action

Mechanism of nelarabine[9]

In terms of the mode of action we find that nelarabine acts as prodrug, rapidly converted into ara-G, which is phosphorylated into ara-GTP(the active metabolite).[9]

Ara-GTP incorporates into DNA during replication, causing chain termination and apoptosis, particularly in T-lymphoblasts due to their high enzymatic activity for this conversion[9]

References

  1. ↑ 1.0 1.1 1.2 "Atriance". Archived from the original on 12 November 2020. Retrieved 12 November 2021. Archived 12 November 2020 at the Wayback Machine
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 2.7 "Nelarabine Monograph for Professionals". Drugs.com. Archived from the original on 6 May 2021. Retrieved 12 November 2021. Archived 6 May 2021 at the Wayback Machine
  3. ↑ "Atriance EPAR". European Medicines Agency (EMA). Archived from the original on 12 November 2020. Retrieved 4 December 2020. Archived 12 November 2020 at the Wayback Machine
  4. ↑ "Arranon- nelarabine injection". DailyMed. 11 June 2020. Archived from the original on 17 October 2020. Retrieved 4 December 2020. Archived 17 October 2020 at the Wayback Machine
  5. ↑ 5.0 5.1 "DailyMed - ARRANON- nelarabine injection". dailymed.nlm.nih.gov. Archived from the original on 17 October 2020. Retrieved 12 November 2021. Archived 17 October 2020 at the Wayback Machine
  6. ↑ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 960. ISBN 978-0857114105.
  7. ↑ "Arranon Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 20 October 2021. Retrieved 12 November 2021.
  8. ↑ Research, Center for Drug Evaluation and (10 February 2022). "2021 First Generic Drug Approvals". FDA. Archived from the original on 21 June 2022. Retrieved 22 October 2022. Archived 21 June 2022 at the Wayback Machine
  9. ↑ 9.0 9.1 9.2 Hormann, Femke M.; Rudd, Sean G. (March 2025). "Nelarabine in T-cell acute lymphoblastic leukemia: intracellular metabolism and molecular mode-of-action". Leukemia. 39 (3): 531–542. doi:10.1038/s41375-025-02529-2. ISSN 1476-5551. Archived from the original on 17 March 2025. Retrieved 27 September 2025.

External links

External sites:
Identifiers:

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