Cladribine


Generic Medicine Info
Contraindications
HIV infection, active chronic infections (e.g. hepatitis, TB), active malignancy, immunocompromised patients, men or women of reproductive potential who do not plan to use effective contraception during dosing and for 6 months after the last dose in each treatment course (oral). Moderate to severe hepatic (Child-Pugh score >6) impairment (SC); moderate to severe renal impairment (oral/SC). Pregnancy and lactation. Co-administration with live or live-attenuated vaccines during treatment. Concomitant immunosuppressive or myelosuppressive therapy (oral/SC).
Special Precautions
Oral: Patient with prior malignancy or increased risk of malignancy. Patient without a history of exposure to varicella-zoster virus (VZV); vaccination is recommended before treatment initiation if VZV antibody-negative, and delay therapy for 4-6 weeks after vaccination. Consider delaying treatment in patients with lymphocyte count <500 cells/mm3 and signs and symptoms of infection (particularly herpes zoster) until full infection resolution. Anti-herpes prophylaxis based on local standard practice may be given if lymphocyte count is <200 cells/mm3. Not indicated for use in patients with clinically isolated syndrome. Administration of any other oral drugs must be separated from oral cladribine by at least 3 hours. Not recommended for moderate to severe hepatic (Child-Pugh score >6) impairment. IV/SC: Patient with high tumour burden, primary haematologic malignancy, severe bone marrow impairment (any aetiology); increased infection risk, manifestation of bone marrow failure or infiltration, myelosuppressive pre-treatment. Administer hyperuricaemia prophylaxis with adequate or increased hydration before starting therapy in patients with high tumour burden. Patient with active/acute infection must be treated before therapy initiation. Not recommended for use in chronic lymphocytic leukaemia (CLL) patients whose disease has progressed during fludarabine treatment. Discontinue treatment if patient is suspected of PML. Cellular blood components or products should be irradiated prior to blood transfusion. Renal and hepatic impairment. Patient Counselling IV/SC: This drug may cause dizziness or drowsiness, if affected, do not drive or operate machinery. Monitoring Parameters Before therapy initiation, evaluate pregnancy status in women of reproductive potential. Closely monitor for haematologic (e.g. myelosuppression) and non-haematologic toxicity (e.g. cardiac changes, renal failure) periodically during and after treatment; signs and symptoms of infection, PML or neurotoxicity. Oral: Determine HIV, active or latent TB, active or latent hepatitis B and C, and varicella-zoster antibody status prior to each course of treatment. Perform standard cancer screening guidelines. Monitor CBC including lymphocyte count (before each treatment course, 2 and 6 months after the initiation of each annual course [if 2-month lymphocyte count is <200 cells/mm3, monitor monthly till month 6], then periodically during and after treatment); LFTs (e.g. serum aminotransferase, alkaline phosphatase, total bilirubin levels) before starting each therapy course and as clinically necessary; MRI (at baseline [within 3 months] before the 1st course); signs and symptoms of PML. Closely assess patients with lymphocyte count <500 cells/mm3 for signs and symptoms of infection (particularly herpes zoster). IV/SC: Screen for hepatitis B virus with hepatitis B surface antigen or core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen before or during initiation of therapy. Obtain CBC with differential (specifically during the 1st 4-8 weeks of post-treatment), bone marrow biopsy (after CBC has normalised); renal and hepatic function (periodically and as clinically indicated). Monitor for haemolysis (particularly in patients who are or become Coombs' positive).
Adverse Reactions
Significant: Increased risk of malignancy, herpes zoster, and lymphopenia (oral); severe bone marrow suppression (e.g. neutropenia, anaemia, thrombocytopenia), prolonged immunosuppression; fever (with or without neutropenia); hepatotoxicity (e.g. serious liver injury); acute nephrotoxicity with high doses (e.g. acidosis, anuria, increased serum creatinine); hypersensitivity reactions. Rarely, severe neurotoxicity including irreversible paraparesis and quadriparesis (high IV doses). Blood and lymphatic system disorders: Haemolytic anaemia, febrile neutropenia, pancytopenia. Cardiac disorders: Myocardial ischaemia, tachycardia, heart murmur. Eye disorders: Conjunctivitis. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, flatulence, constipation. General disorders and administration site conditions: Inj site reaction, fatigue, chills, asthenia, malaise, pain, peripheral oedema, crepitations. Infections and infestations: Dermatomal herpes zoster, oral herpes (oral); pneumonia, septic shock, bacteraemia, localised infection. Injury, poisoning and procedural complications: Contusion. Investigations: Decreased neutrophil count (oral); increased transaminases and bilirubin. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Myalgia, arthralgia, muscle weakness, bone pain, arthritis; back pain (oral). Neoplasms benign, malignant and unspecified: Primary haematological malignancies, secondary malignancies. Nervous system disorders: Headache, dizziness. Psychiatric disorders: Insomnia, confusion, anxiety; depression (oral). Renal and urinary disorders: Renal failure. Respiratory, thoracic and mediastinal disorders: Abnormal breath or chest sounds, cough, epistaxis, dyspnoea, rales, pulmonary interstitial infiltrates; upper respiratory tract infection, bronchitis (oral). Skin and subcutaneous tissue disorders: Rash, alopecia, urticaria, pruritus, ecchymosis, hyperhidrosis, petechiae, cellulitis, erythema, localised exanthema. Vascular disorders: Phlebitis, purpura, hypotension; hypertension (oral).
Potentially Fatal: Severe bacterial, viral, and fungal infections; cardiotoxicity including acute cardiac failure with myocarditis; progressive multifocal leucoencepalopathy (PML); graft-versus-host disease (may occur after transfusion of non-irradiated blood). Rarely, tumour lysis syndrome and subsequent hyperuricaemia (in patients with high tumour burden).
Drug Interactions
Due to similar intracellular metabolism, cross-resistance may occur with other nucleoside analogues (e.g. fludarabine). Increased risk of lymphopenia with interferon-β. May cause additive haematologic adverse effect when given with or prior to other substances that affect the haematological profile (e.g. carbamazepine). May increase the oral bioavailability and systemic exposure with breast cancer resistance protein (BCRP) inhibitors (e.g. eltrombopag). May alter the bioavailability, intracellular distribution and renal elimination with potent equilibrative nucleoside (ENT1) and concentrative nucleoside (CNT3) transporter inhibitors (e.g. nifedipine, nimodipine, dilazep, cilostazol, reserpine, sulindac). May decrease exposure with potent BCRP inducer (e.g. corticosteroids) or P-glycoprotein transporter inducers (e.g. rifampicin). Cladribine tab contains hydroxypropylbetadex that may form complex with other oral agents (specifically those with low solubility), leading to increased bioavailability of these agents; doses of other oral agents must be separated by at least 3 hours.
CIMS Class
Cytotoxic Chemotherapy / Immunosuppressants
ATC Classification
L04AA40 - cladribine
L01BB04 - cladribine ; Belongs to the class of antimetabolites, purine analogues. Used in the treatment of cancer.
Disclaimer: This information is independently developed by CIMS based on cladribine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
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