Nelarabine

What it is and how it works

Mechanism of Action Nelarabine is a prodrug of the deoxyguanosine analogue 9-β- D -arabinofuranosylguanine (ara-G), a nucleoside metabolic inhibitor. Nelarabine is demethylated by ADA to ara-G, mono-phosphorylated by deoxyguanosine kinase and deoxycytidine kinase, and subsequently converted to the active 5'-triphosphate, ara-GTP. Accumulation of ara-GTP in leukemic blasts allows for incorporation into deoxyribonucleic acid (DNA), leading to inhibition of DNA synthesis and cell death. Other mechanisms may contribute to the cytotoxic and systemic toxicity of nelarabine.

Mechanism class: Nucleic Acid Synthesis Inhibitors

Indications

Nelarabine Injection is indicated for the treatment of T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL) in adult and pediatric patients age 1 year and older whose disease has not responded to or has relapsed following treatment with at least 2 chemotherapy regimens. Nelarabine Injection is a nucleoside metabolic inhibitor indicated for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL) in adult and pediatric patients age 1 year and older whose disease has not responded to or has relapsed following treatment with at least two chemotherapy regimens.

Dosage and administration (summary)

Adult Dose : 1,500 mg/m² administered by intravenous infusion over 2 hours on Days 1, 3, and 5 repeated every 21 days. Pediatric Dose : 650 mg/m² administered by intravenous infusion over 1 hour daily for 5 consecutive days repeated every 21 days. Discontinue treatment for neurologic reactions greater than or equal to Grade 2. Dosage may be delayed for hematologic reactions. Take measures to prevent hyperuricemia. Recommended Dosage This product is for intravenous use only. Adult Dosage The recommended adult dose of nelarabine injection is 1,500 mg/m² administered by intravenous infusion over 2 hours on Days 1, 3, and 5 repeated every 21 days. Administer nelarabine injection undiluted.

Contraindications

None. None

Warnings and precautions

Neurologic Adverse Reactions : Severe neurologic reactions have been reported. Monitor for signs and symptoms of neurologic toxicity. Hematologic Reactions : Complete blood counts including platelets should be monitored regularly. Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to the fetus and to use effective contraception; and advise males to use condoms. ( 5.3 , 8.1 , 8.3 ) Effects on Ability to Drive and Use Machines : Somnolence may occur. Advise patients to refrain from these activities until somnolence has resolved.

Pregnancy

Pregnancy Risk Summary Based on its mechanism of action and findings in animal studies, nelarabine can cause fetal harm when administered to a pregnant woman . Limited available data with nelarabine use in pregnant women are insufficient to determine a drug-associated risk for major birth defects, miscarriage or adverse maternal, or fetal outcomes.…

Storage and supply

Nelarabine Injection is a clear, colorless, sterile solution in Type I, clear glass single-dose vials with a gray bromobutyl rubber stopper (not made with natural rubber latex) and an aluminum seal with a snap-off cap.

Source: Nelarabine (Nelarabine) — US FDA prescribing information, 2025-10-01, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.