Cladribine

CLINICAL USE

Antineoplastic agent:Hairy cell leukaemia (HCL) Chronic lymphocytic leukaemia (CLL) in patients who have failed to respond to standard regimens

DOSE IN NORMAL RENAL FUNCTION

Leustat:HCL: 0.09 mg/kg (3.6 mg/m 2) daily for 7 daysCLL: 0.12 mg/kg (4.8 mg/m 2) daily for 2 hours on days 1 to 5 of a 28 day cycleLitak:HCL: 0.14 mg/kg/day for 5 days by subcutaneous injectionor according to local protocol

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :285.7

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :20

%Excreted unchanged in urine &nbsp &nbsp : 18

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :9

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :3–22/No data

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Use with caution.

10 to 20 &nbsp &nbsp : Use with caution

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Use with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsCaution when administering with any other immunosuppressive or myelosuppressive therapy

ADMINISTRATION

Reconstition

–

Route

SC,

IV infusion

Rate of Administration

24 hours or 2 hours depending on condition being treated

Comments

Add to 100–500 mL of sodium chloride 0.9%

OTHER INFORMATION

Prodrug – activated by intracellular phosphorylation. The nucleotide that is formed accumulates in the cell and is incorporated into the DNA. Regular monitoring is recommended in renal failure Acute renal insufficiency has developed in some patients receiving high-dose . Inadequate data on dosing of patients with renal insufficiency therefore use according to clinical needStudy showed that

<10

% of dose is excreted in urine as metabolites and <20% as parent drug.