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Arranon

nelarabine
Purine Nucleoside Analog (Deoxyguanosine) FDA Approved 2005 Novartis
1. Indications and Usage

T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL) in patients whose disease has not responded to or has relapsed following treatment with at least two chemotherapy regimens.

2. Dosage and Administration

Adults: 1,500 mg/mΒ² IV over 2 hours on Days 1, 3, and 5, repeated every 21 days
Pediatric: 650 mg/mΒ² IV over 1 hour daily for 5 consecutive days, repeated every 21 days
Hydration: IV hydration recommended to reduce risk of tumor lysis syndrome and hyperuricemia

3. Dosage Forms and Strengths

Injection: 5 mg/mL (250 mg/50 mL) in single-dose vials

4. Contraindications

None listed.

5. Warnings and Precautions
⚠ Boxed Warning
NEUROLOGIC ADVERSE REACTIONS: Severe neurologic adverse reactions have been reported, including altered mental states including severe somnolence, central nervous system effects including convulsions, and peripheral neuropathy ranging from numbness and paresthesias to motor weakness and paralysis. There have also been reports of events associated with demyelination, and ascending peripheral neuropathies similar in appearance to Guillain-BarrΓ© syndrome.
  • Neurotoxicity: Dose-limiting toxicity. Includes somnolence (23%), peripheral neuropathy (21%), hypoesthesia (17%), paresthesia (15%), seizures (6%), ataxia (9%), tremor (5%), and demyelination. Monitor closely and discontinue for Grade 2 or greater neurologic events.
  • Hematologic Toxicity: Leukopenia, thrombocytopenia, anemia, neutropenia, and febrile neutropenia. Monitor CBC regularly.
  • Tumor Lysis Syndrome: Provide IV hydration and consider allopurinol prophylaxis.
  • Hepatotoxicity: Grade 3-4 elevations in transaminases and bilirubin reported.
6. Adverse Reactions
Most Common Adverse Reactions

Fatigue (50%), nausea (41%), somnolence (23%), diarrhea (22%), peripheral neuropathy (21%), vomiting (22%), anemia (99% any grade), thrombocytopenia (86%), neutropenia (81%), hypoesthesia (17%), cough (25%), dyspnea (20%)

Thrombocytopenia
86%
Neutropenia
81%
Fatigue
50%
Nausea
41%
Cough
25%
Somnolence
23%
Diarrhea
22%
Vomiting
22%
Peripheral Neuropathy
21%
Dyspnea
20%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

7. Drug Interactions

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

8. Use in Specific Populations
Pregnancy

Consult the full prescribing information for pregnancy-related considerations.

Lactation

Refer to prescribing information for lactation guidance.

Pediatric Use

Pediatric safety and efficacy information is detailed in the full label.

Hepatic/Renal Impairment

Dose modifications for organ impairment are specified in the complete prescribing information.

12. Clinical Pharmacology
Mechanism of Action

Nelarabine is a prodrug of ara-G (9-Ξ²-D-arabinofuranosylguanine), a deoxyguanosine analog. It is demethylated by adenosine deaminase (ADA) to ara-G, which is then phosphorylated intracellularly to the active triphosphate ara-GTP. Ara-GTP accumulates preferentially in T-cells due to higher dGTP levels and is incorporated into DNA during synthesis, leading to inhibition of DNA synthesis and cell death. T-cell selectivity is due to relatively high intracellular levels of deoxyguanosine kinase activity in T-lymphoblasts.

Pharmacokinetics

Nelarabine and ara-G are rapidly eliminated; nelarabine tΒ½: ~30 min, ara-G tΒ½: ~3 hours. Nelarabine is partially protein bound (< 25%). Metabolized by ADA and phosphorylated intracellularly. Excreted renally: 5-10% as nelarabine, 20-30% as ara-G.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
πŸ“‹ All Trials on ClinicalTrials.gov β†— πŸ“š PubMed Clinical Trials β†—
FDA-Approved Tumor Types

Arranon has FDA-approved indications across the following cancer types covered on PipelineEvidence:

Acute Lymphoblastic Leukemia
External Resources
πŸ“‹ DailyMed Label β†— πŸ›οΈ FDA Drugs@FDA β†— πŸ”¬ ClinicalTrials.gov β†— πŸ“š PubMed Pivotal Trials β†—
Important Notice: This page is intended as a navigational reference to the FDA-approved prescribing information for Arranon. It does not replace the full prescribing information. Healthcare professionals should consult the complete package insert available at DailyMed before making prescribing decisions. Patient-specific factors should always guide clinical decision-making.
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