1. Table 12.1 Drugs used in the treatment of leukaemia and lymphoma.
Mechanism of action Particular side-effects*
Alkylating agents
Bendamustine Alylating agent and purine
analogue
Myelosuppression
Cyclophosphamide Cross-link DNA, impede RNA
formation
Haemorrhagic cystitis,
cardiomyopathy, loss of hair
Chlorambucil Marrow aplasia, hepatic toxicity,
dermatitis
Busulfan Marrow aplasia, pulmonary
fibrosis, hyperpigmentation
Melphalan Marrow aplasia
Nitrosoureas (BCNU, CCNU) Renal and pulmonary toxicity
Cisplatin Intrastrand DNA linkage Renal dysfunction, neurotoxicity,
ototoxicity
Antimetabolites
Hydroxycarbamide (hydroxyurea) Inhibits ribonucleotide
reductase
Pigmentation, nail dystrophy,
skin ulceration
Methotrexate Inhibit pyrimidine or purine
synthesis or incorporation
into DNA
Mouth ulcers, gut toxicity
Cytosine arabinoside Inhibits DNA synthesis CNS especially cerebellar
toxicity and conjunctivitis at
high doses
6-Mercaptopurine†, 6-thioguanine† Purine analogue Jaundice, gut toxicity
Clofarabine Purine analogue Myelosuppression
Fludarabine
Inhibit adenosine deaminase
2-Chlorodeoxyadenosine
or other purine pathways
Deoxycoformycin
Immunosuppression (low CD4
counts); renal and
neurotoxicity (at high doses)
Cytotoxic antibiotics
Anthracyclines (e.g.
daunorubicin)
Hydroxodaunorubicin
(Adriamycin)
Mitoxantrone
Idarubicin
Bind to DNA and interfere
with mitosis
Cardiac toxicity, hair loss
Bleomycin DNA breaks Pulmonary fibrosis, skin
pigmentation
Plant derivatives
Vincristine (Oncovin®) Spindle damage Neuropathy (peripheral or
bladder or gut)
Vinblastine myelosuppression
Vindesine
Etoposide Mitotic inhibitor Hair loss, oral ulceration
Demethylating agents
Azacytidine, decytabine Inhibit DNA methlytransferase Myelosuppression
Signal transduction inhibitors
Imatinib, dasatinib, nilotinib Inhibit tyrosine kinase Myelosuppression, fluid
retention
Miscellaneous
Corticosteroids Lymphoblast lysis Peptic ulcer, obesity, diabetes,
osteoporosis, psychosis,
hypertension
Trans-retinoic acid Induces differentiation Liver dysfunction, skin
hyperkeratosis, leucocytosis
and hyperviscosity, pleural or
pericardial effusion
Arsenic Induces differentiation or
apoptosis
Hyperleucocytosis, cardiac
α-Interferon Activation of RNAase and
natural killer activity
Flu-like symptoms,
thrombocytopenia, leucopenia,
weight loss
2. Mechanism of action Particular side-effects*
Bortezomid Proteasome inhibition Neuropathy
L-Asparaginase Deprive cells of asparagine Hypersensitivity, low albumin
and coagulation factors,
pancreatitis
Thalidomide Lenalidomide Immuno-modulation Neuropathy, constipation,
thrombosis
Monoclonal antibodies
Rituximab (anti-CD20) Induction of apoptosis Infusion reactions,
immunosuppression
Alemtuzumab (anti-CD52) Lysis of target cell by
complement fixation
Infusion reactions,
immunosuppression
Lumiliximab (anti-CD23) Induction of apoptosis Infusion reactions,
immunosuppression
Ibritumomab (Zevalin®)
(anti-CD20+90Y)
Toxicity to bound cell Myelosuppression, nausea
Mylotarg® (anti-CD33) Kills myeloid cells Myelosuppression
* Many of the drugs cause nausea, vomiting, mucositis and bone marrow toxicity, and in large doses infertility. Tissue
necrosis is a problem if the drugs are extravasated during infusion.
† Allopurinol potentiates the action and side-effects of 6-mercaptopurine.