Leustatin Cladribine Injection

1. Indications and Usage
Hairy Cell Leukemia (HCL):
Indicated for the treatment of patients with active Hairy Cell Leukemia, defined by clinically significant anemia, neutropenia, thrombocytopenia, or disease-related symptoms.
2. Dosage and Administration
Recommended Dosage:
Standard Regimen: 0.09 mg/kg/day administered as a continuous intravenous infusion over 24 hours for 7 consecutive days.
Administration Instructions:
Diluent: Must be diluted with 0.9% Sodium Chloride Injection.
Contraindicated Diluent: Do not use 5% Dextrose Injection or any dextrose-containing solution for dilution, as it accelerates the degradation of cladribine.
3. Mechanism of Action
Antimetabolite:
Cladribine is a purine nucleoside antimetabolite.
Physiological Effect:
It enters cells via passive diffusion and is phosphorylated by deoxycytidine kinase to its active triphosphate metabolite. This metabolite incorporates into DNA, interfering with DNA repair and synthesis, leading to DNA strand breaks, depletion of NAD and ATP, and ultimately cell death. It is toxic to both dividing and resting lymphocytes and monocytes.
4. Safety and Warnings
Bone Marrow Suppression:
Severe myelosuppression (neutropenia, anemia, thrombocytopenia) is the most common toxicity, usually occurring within the first month. Monitor complete blood counts (CBC) regularly.
Neurotoxicity:
Severe, irreversible neurotoxicity (including lower extremity paraparesis and quadriplegia) has been reported, particularly with high doses (4–9 times the recommended dose).
Nephrotoxicity:
Acute nephrotoxicity may occur, especially with high doses or concurrent use of other nephrotoxic drugs.
5. Adverse Reactions
Most Common:
Fever (69%), neutropenia (70%), infection (28%), fatigue (45%), nausea (28%), rash (27%), headache (22%), and injection site reactions (19%).
6. Drug Interactions
Contraindicated Combinations:
Do not administer cladribine concomitantly with ganciclovir or valganciclovir, as this combination may increase the risk of severe myelosuppression.
Vaccinations:
Live virus vaccines should be avoided during and after treatment.
7. Pharmaceutical Information
Storage:
Store at controlled room temperature (20°C to 25°C). Protect from light.