list of antineoplastic agents list of antineoplastic agents this is a list of antineoplastic agents used to treat cancer. antineoplastic agents innroutemechanism of actionindicationsmajor toxicities 1. cytotoxic antineoplastics 1.01 nucleoside analogues azacitidinesc, ivdna methyltransferase inhibitor and incorporates itself into rna, hence inhibiting gene expression.myelodysplastic syndromes, acute myeloid leukaemia and chronic myeloid leukaemiamyelosuppression, kidney failure (uncommon/rare), renal tubular acidosis and hypokalaemia. capecitabinepofluorouracilprodrugbreast, colorectal, gastric and oesophageal cancermyelosuppression, cardiotoxicity, hypertriglyceridaemia, gi haemorrhage (uncommon), cerebellar syndrome (uncommon), encephalopathy (uncommon) and diarrhoea. carmofurpofluorouracil prodrugcolorectal, breast and ovarian cancermyelosuppression, neurotoxicity and diarrhoea. cladribinesc, ivdna methyltransferase inhibitor, metabolites incorporate themselves into dna.hairy cell leukaemia, chronic lymphocytic leukaemiamyelosuppression, haemolytic anaemia (uncommon), neurotoxicity (rare), renal impairment (rare), pulmonary interstitial infiltrates (rare), stevens–johnson syndrome (rare) and toxic epidermal necrolysis (rare). clofarabineivribonucleotide reductase and dna polymerase inhibitor.acute lymphoblastic leukaemia and acute myeloid leukaemiamyelosuppression, hypokalaemia, cytokine release syndrome, stevens–johnson syndrome (uncommon), toxic epidermal necrolysis (uncommon) and pancreatitis (uncommon) cytarabinesc, im, iv, itdna polymerase inhibitor, s-phase specific. incorporates its metabolites into dna.acute myeloid leukaemia, acute lymphoblastic leukaemia, chronic myeloid leukaemia, lymphomas, progressive multifocal leucoencephalopathy and meningeal leukaemiamyelosuppression, gi bleeds, pancreatitis (uncommon/rare), anaphylaxis (uncommon/rare), pericarditis (uncommon/rare) and conjunctivitis (uncommon/rare). high dose: cerebral and cerebellar dysfunction, ocular toxicity, pulmonary toxicity, severe gi ulceration and peripheral neuropathy (rare). decitabineivdna methyltransferase inhibitor.myelodysplastic syndrome, sickle cell anaemia (orphan), acute myeloid leukaemia and chronic myeloid leukaemia.myelosuppression, hyperglycaemia, hypoalbuminaemia, hypomagnesaemia, hypokalaemia, hyperkalaemia and thrombocythaemia. floxuridineiafluorouracil analogue.metastatic gi adenocarcinoma and stomach cancermyelosuppression. fludarabinepo, ivdna polymerase and ribonucleotide reductase inhibitor.acute myeloid leukaemia, chronic lymphocytic leukaemia, non-hodgkin lymphoma and waldenstrom macroglobulinaemia.myelosuppression, hyperglycaemia, gi bleeds (uncommon), pneumonitis (uncommon), haemolytic anaemia (uncommon), severe neurotoxicity (rare), haemorrhagic cystitis (rare), stevens–johnson syndrome (rare) and toxic epidermal necrolysis (rare). fluorouraciliv, topicalthymidylate synthase inhibitor.anal, breast, colorectal, gastric, head and neck, oesophageal and pancreatic cancer. bowen's disease and actinic keratoses.myelosuppression, diarrhoea, cardiotoxicity, gi ulceration and bleeding (uncommon), cerebellar syndrome (uncommon), encephalopathy (uncommon) and anaphylaxis (rare). gemcitabineivdna synthesis inhibitor, induces apoptosis specifically in s-phase.bladder, breast, nasopharyngeal, non-small cell lung, ovarian and pancreatic cancer, lymphomas and inflammatory bowel disease.myelosuppression, pulmonary toxicity, kidney failure (rare), haemolytic uraemic syndrome (rare), thrombotic thrombocytopenic purpura (rare), anaphylactoid reaction (rare), reversible posterior leucoencephalopathy syndrome (rare), myocardial infarction (rare) and heart failure (rare). mercaptopurinepopurine synthesis inhibitor.acute lymphoblastic leukaemia, acute promyelocytic leukaemia, lymphoblastic lymphoma and inflammatory bowel disease.myelosuppression, hepatotoxicity, gi ulceration (rare), pancreatitis (rare) and secondary leukaemia (rare) or myelodysplasia (rare). nelarabineivpurine synthesis inhibitor.acute lymphoblastic leukaemia and chronic lymphocytic leukaemia.myelosuppression, pleural effusion, seizures, tumour lysis syndrome and a condition similar to guillain-barré syndrome. pentostatinivadenosine deaminase inhibitor.hairy cell leukaemia, peripheral t-cell lymphoma (orphan), cutaneous t cell lymphoma (orphan) and chronic lymphocytic leukaemia (orphan).myelosuppression, neurotoxicity, immune hypersensitivity, hyponatraemia, thrombotic thrombocytopenic purpura and microangiopathic hemolytic anaemia. tegafurpothymidylate synthase inhibitor.breast, colorectal cancer, gallbladder, gastrointestinal tract, head and neck, liver and pancreas cancer.myelosuppression, diarrhoea, neurotoxicity and hepatitis (rare). tioguaninepopurine synthesis inhibitor.acute lymphoblastic leukaemia and acute myeloid leukaemiamyelosuppression, hepatotoxicity, peripheral neuropathy (uncommon), intestinal necrosis (rare) and perforation (rare). 1.02 antifolates methotrexatesc, im, iv, it, podihydrofolate reductase inhibitor.bladder and breast cancer. squamous cell carcinoma of head and neck, gestational trophoblastic disease, acute leukaemias, non-hodgkin lymphoma, osteosarcoma, brain tumours, graft-versus-host disease and systemic sclerosis.myelosuppression, pulmonary toxicity, hepatotoxicity, neurotoxicity (high dose or intrathecal administration), anaphylactic reactions (rare), stevens–johnson syndrome (rare), toxic epidermal necrolysis (rare), kidney failure (rare), osteoporosis (rare), skin and bone necrosis (rare) and macrocytic anaemia (rare). pemetrexedivdihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase inhibitors.malignant mesothelioma and non-squamous non-small cell lung cancer.myelosuppression, renal impairment, peripheral neuropathy, supraventricular tachycardia (uncommon), hepatitis (rare), colitis (rare), pneumonitis (rare), radiation recall (rare), stevens–johnson syndrome (rare) and toxic epidermal necrolysis (rare). raltitrexedivdihydrofolate reductase and thymidylate synthase inhibitor.colorectal cancermyelosuppression 1.03 other antimetabolites hydroxycarbamidepoinhibits dna synthesis by inhibiting the enzyme ribonucleotide reductase.chronic myeloid leukaemia, essential thrombocytosis, polycythaemia vera, myelofibrosis, acute myeloid leukaemia and sickle cell anaemiamyelosuppression, skin cancer (rare), oedema (rare), hallucinations (rare), seizures (rare) and pulmonary toxicity (rare). 1.04 topoisomerase i inhibitor irinotecanivinhibits topoisomerase i.colorectal cancerdiarrhoea, myelosuppression, pulmonary infiltrates (uncommon), bradycardia (uncommon), ileus (rare) and colitis (rare). topotecanivinhibits topoisomerase i.small cell lung cancer, ovarian cancer and cervical cancerdiarrhoea, myelosuppression, interstitial lung disease and allergy. 1.05 anthracyclines daunorubicinivinhibits dna and rna synthesis by intercalating dna base pairs. inhibits dna repair by inhibiting topoisomerase ii.acute leukaemiasmyelosuppression, cardiotoxicity, anaphylaxis (rare), secondary malignancies (particularly acute myeloid leukaemia and myelodysplastic syndrome) and radiation recall. doxorubicinivas above.breast cancer, lymphomas, sarcomas, bladder cancer, acute lymphoblastic leukaemia, wilms' tumour, aids-related kaposi's sarcoma, neuroblastoma and multiple myelomaas above. epirubicinivas above.breast cancer, gastric cancer and bladder canceras above. idarubiciniv, poas above.acute leukaemias.as above. mitoxantroneivas above.non-hodgkin lymphoma, acute myeloid leukaemia, prostate cancer and multiple sclerosisas above. valrubicinivas above.bladder cancer.as above. 1.06 podophyllotoxins etoposideiv, potopoisomerase ii inhibitor.testicular cancer, ovarian cancer, lung cancer, acute myeloid leukaemia, lymphomas and sarcomasmyelosuppression, hypersensitivity reactions, stevens–johnson syndrome (rare), peripheral neuropathy (uncommon) and secondary malignancies (especially acute myeloid leukaemia). teniposideivtopoisomerase ii inhibitor.lymphomas, acute lymphoblastic leukaemia and neuroblastomaas above. 1.07 taxanes cabazitaxelivmicrotubule disassembly inhibitor. arrests cells in late g2 phase and m phase.prostate cancermyelosuppression, diarrhoea, kidney failure, hypersensitivity, severe gi reactions (including perforation, ileus, colitis, etc.; all rare) and peripheral neuropathy docetaxelivas above.breast cancer, non-small cell lung cancer, ovarian cancer, prostate cancer, squamous cell head and neck cancer and gastric cancer.myelosuppression, peripheral neuropathy, hypersensitivity, fluid retention, heart failure (uncommon), pulmonary toxicity (rare), radiation recall (rare), scleroderma-like skin changes (rare), stevens–johnson syndrome (rare), toxic epidermal necrolysis (rare), seizures (rare) and encephalopathy (rare) paclitaxelivas above.ovarian cancer, breast cancer, non-small cell lung cancer, aids-related kaposi's sarcoma, cervical cancer, germ cell cancer and endometrial cancerhypersensitivity, myelosuppression, peripheral neuropathy, myocardial infarction (uncommon), arrhythmias (uncommon), pulmonary toxicity (rare), radiation recall (rare), scleroderma-like skin changes (rare), stevens–johnson syndrome (rare), toxic epidermal necrolysis (rare), seizures (rare) and encephalopathy (rare). 1.08 vinca alkaloids vinblastineivmicrotubule assembly inhibitor. arrests cells in m phase.hodgkin lymphoma, germ cell tumours, non-small cell lung cancer, bladder cancer and primary immune thrombocytopenianeurotoxicity, myelosuppression, myocardial ischaemia (rare) and myocardial infarction (rare). vincristineivas above.lymphomas, acute lymphoblastic leukaemia, multiple myeloma, sarcoma, brain tumours, wilms' tumour, neuroblastoma and primary immune thrombocytopenianeurotoxicity, anaphylaxis (rare), myocardial ischaemia (rare) and myocardial infarction (rare). vindesineivas above.refractory metastatic melanoma, childhood acute lymphoblastic leukaemia, chronic myeloid leukaemia in blast crises, neuroblastoma, non-small cell lung cancer and breast cancer.myelosuppression, neurotoxicity and paralytic ileus. vinflunineivas above.bladder canceras per vinblastine. vinorelbineivas above.breast cancer and non-small cell lung cancer.as above. 1.09 alkylating agents bendamustineivalkylates dna.chronic lymphocytic leukaemia, mantle cell lymphoma and non-hodgkin's lymphoma.myelosuppression, hypokalaemia and tachycardia. busulfaniv, poalkylates dna.conditioning treatment before haematopoietic stem cell transplantation (high dose, iv), chronic myeloid leukaemia, myelofibrosis, polycythaemia vera and essential thrombocytosismyelosuppression, seizures (high dose), tachycardia (high dose), hepatic sinusoidal obstruction syndrome (high dose), addison-like syndrome (rare), pulmonary fibrosis (rare), cataracts (rare) and hepatitis (rare). secondary malignancies. carmustineivalkylates dna.anaplastic astrocytoma, glioblastoma multiforme and mycosis fungoides (topical)myelosuppression, pulmonary fibrosis, pulmonary infiltrates, seizure, brain oedema, cerebrospinal leaks, subdural fluid collection, intracranial infection, hypotension (uncommon), tachycardia (uncommon), decrease in kidney size (reversible), uraemia (uncommon), kidney failure (uncommon), severe hepatic toxicity (rare), thrombosis (rare) and neuroretinitis (rare). secondary malignancies. chlorambucilivalkylates dna.lymphoma, chronic lymphocytic leukaemia and waldenström's macroglobulinaemiamyelosuppression, hallucinations (rare), seizures (rare), sterile cystitis (rare), hepatotoxicity (rare), severe pneumonitis (rare), stevens–johnson syndrome (rare), toxic epidermal necrolysis (rare) and drug fever (rare). secondary malignancies. chlormethineiv, topicalalkylates dna.cutaneous t-cell lymphoma, metastatic carcinoma, leukaemias, lymphomas, polycythemia vera and bronchogenic carcinomathrombosis, myelosuppression (common), hyperuricaemia, erythema multiforme, haemolytic anaemia, nausea and vomiting (severe) and secondary malignancies. cyclophosphamideivalkylates dna.breast cancer, lymphoma, acute lymphoblastic leukaemia, chronic lymphocytic leukaemia, sarcoma, multiple myeloma, waldenström's macroglobulinaemia, systemic lupus erythematosus, glomerulonephritis, systemic vasculitis and granulomatosis with polyangiitismyelosuppression, nausea and vomiting (>30%), haemorrhagic cystitis, heart failure (rare), pulmonary fibrosis (rare), hepatic sinusoidal obstruction syndrome (rare), water retention resembling siadh (rare) and seizures (rare). secondary malignancies. dacarbazineivalkylates dna.hodgkin lymphoma, metastatic malignant melanoma and soft tissue sarcomamyelosuppression, agranulocytosis (uncommon), hepatic vein thrombosis (rare) and hepatocellular necrosis (rare). secondary malignancies. fotemustineivalkylates dna.metastatic malignant melanoma.myelosuppression. ifosfamideivalkylates dna.sarcomas, testicular cancer and lymphomas.myelosuppression, haemorrhagic cystitis, nephrotoxicity, neurotoxicity and cardiac toxicity (rare). secondary malignancies. lomustinepoalkylates dna.glioma and medulloblastoma.myelosuppression, pulmonary infiltration and fibrosis. secondary malignancies. melphalaniv, poalkylates dna.malignant melanoma of the extremities, multiple myeloma, conditioning treatment before haemopoietic stem cell transplant.myelosuppression, pulmonary fibrosis and pneumonitis (uncommon), skin necrosis (uncommon), anaphylaxis, hepatic sinusoidal obstruction syndrome and siadh. secondary malignancies. streptozotociniv, poalkylates dna.pancreatic cancer and carcinoid syndrome.nephrotoxicity, hypoglycaemia, myelosuppression, nausea and vomiting (>90%), jaundice and nephrogenic diabetes insipidus (rare). temozolomidepoalkylates dna.anaplastic astrocytoma, glioblastoma multiforme, metastatic malignant melanomamyelosuppression, stevens–johnson syndrome (rare), pneumonitis (rare) and hepatitis (rare). 1.10 platinum compounds carboplatinivreacts with dna, inducing apoptosis, non-cell cycle specific.ovarian cancer, lung cancer and squamous cell head and neck cancermyelosuppression, nausea and vomiting (30-90%), peripheral neuropathy, ototoxicity, anaphylaxis, acute kidney failure (rare), haemolytic uraemic syndrome (rare) and loss of vision (rare). cisplatinivas above.germ cell tumours (including testicular cancer), ovarian cancer, cervical cancer, small cell and non-small cell lung cancer, mesothelioma, squamous cell head and neck cancer, oesophageal cancer, gastric cancer, bladder cancer and osteosarcomanephrotoxicity, nausea and vomiting (30-100%), myelosuppression, electrolyte anomalies, peripheral neuropathy, ototoxicity and anaphylaxis, haemolytic anaemia (rare), optic neuritis (rare), reversible posterior leucoencephalopathy syndrome (rare), seizures (rare), ecg changes (rare) and heart failure (rare). nedaplatinivas above.non-small cell lung cancer, oesophageal cancer, uterine cervical cancer, head and neck cancer and urothelial cancernephrotoxicity, myelosuppression and nausea and vomiting (30-90%). oxaliplatinivas above.colorectal cancer, oesophageal cancer and gastric cancermyelosuppression, peripheral neuropathy, anaphylaxis, nausea and vomiting (30-90%), hypokalaemia, metabolic acidosis, interstitial lung disease (uncommon), ototoxicity (rare), reversible posterior leucoencephalopathy syndrome (rare), immune-mediated cytopenias (rare) and hepatic sinusoidal obstruction syndrome (rare). 1.11 miscellaneous others altretaminepounclear, reactive intermediates covalently bind to microsomal proteins and dna, possibly causing dna damagerecurrent ovarian cancermyelosuppression, peripheral neuropathy, seizures and hepatotoxicity (rare). bleomycinim, sc, ia, iv or ipinhibits dna and to a lesser extent rna synthesis, produces single and double strand breaks in dna possibly by free radical formation.germ cell tumours, squamous cell carcinoma, pancreatic cancer, non-hodgkin's, pleural sclerosing and hodgkin's lymphoma.pulmonary toxicity, hypersensitivity, scleroderma and raynaud's phenomenon. bortezomibiv, scproteasome inhibitor.multiple myeloma, mantle cell lymphoma and follicular lymphoma (orphan).peripheral neuropathy, neutropenia, thrombocytopenia, anaemia, orthostatic hypotension, hepatitis (uncommon/rare), haemorrhage (uncommon/rare), heart failure (uncommon/rare), seizures (uncommon/rare), progressive multifocal leucoencephalopathy (pml) and hearing loss. dactinomycinivcomplexes with dna interfering with dna-dependent rna synthesisgestational trophoblastic disease, wilms' tumour and rhabdomyosarcomamyelosuppression, anaphylaxis, radiation recall, hepatotoxicity and hepatic sinusoidal obstruction syndrome (common in wilms' tumour). estramustinepoantimicrotubule and oestrogenic actionsprostate cancer.cardiovascular complications, such as ischaemic heart disease, venous thromboembolism, congestive heart failure, pulmonary embolism, myocardial infarction and cerebrovascular failure. ixabepiloneivpromotes tubulin polymerisation and stabilises microtubular function, causing cell cycle arrest at g2/m phase and subsequently induces apoptosislocally advanced or metastatic breast cancer.myelosuppression, peripheral neuropathy, myocardial ischaemia (uncommon/rare), supraventricular arrhythmia (uncommon/rare) and hypersensitivity reaction (uncommon/rare). mitomycinivcross-links dnaanal, bladder, and upper tract urothelial cancersmyelosuppression, pulmonary toxicity and haemolytic uraemic syndrome (rare). procarbazineim, ivinhibits dna, rna and protein synthesis.glioma and hodgkin's lymphoma.myelosuppression, neurotoxicity, pulmonary fibrosis (uncommon/rare), pneumonitis (uncommon/rare), haemolysis (uncommon/rare) and hepatic dysfunction (uncommon/rare). 2. targeted antineoplastics 2.1 monoclonal antibodies alemtuzumabivcd52 antibody induces apoptosis in the tagged cells.chronic lymphocytic leukaemiapancytopenia, pneumonitis, arrhythmias and hypersensitivity reactions (rare), autoimmune haemolytic anaemia (rare), autoimmune thrombocytopenia (rare) and progressive multifocal leucoencephalopathy (rare). bevacizumabivvegf inhibitor.colorectal, breast, ovarian, renal cell and non-squamous non-small cell lung cancer and glioblastomahypertension, thromboembolisms, heart failure, bleeding, neutropenia, thrombocytopenia, gi perforation, fistula formation, hypertensive encephalopathy, pulmonary hypertension, reversible posterior leucoencephalopathy syndrome, nasal septum perforation and osteonecrosis of the jaw. cetuximabivegfr inhibitor.squamous cell head and neck cancer or egfr-positive and kras wild-type metastatic colorectal cancer.infusion-related reactions, skin reactions, hypomagnesaemia, hypocalcaemia, hypokalaemia, blood clots, interstitial lung disease and aseptic meningitis. denosumabscrankl inhibitor.osteoporosis, including drug- and cancer-related osteoporosis, giant cell tumour of bone and hypercalcaemia of malignancieshypercholesterolaemia, cataract, urinary retention, hypocalcaemia, osteonecrosis of the jaw and anaphylaxis. gemtuzumab ozogamicinivcd33 antibody that induces apoptosis of the tagged cell.acute myeloid leukaemiahepatic veno-occlusive disease, myelosuppression, cytokine release syndrome, hypersensitivity and electrolyte anomalies. ibritumomab tiuxetanivcd20 antibody bound with the radioactive isotope, 90y, induces radiation-dependent cell lysis.non-hodgkin's lymphoma and follicular lymphoma.thrombocytopenia, neutropenia, anaemia, hypotension and secondary malignancies. ipilimumabivctla4 antibody that causes immune system-mediated lysis of the tagged cellunresectable or metastatic malignant melanoma.life-threatening immune mediated reactions and fever. nivolumabivigg4 antibody that functions as a checkpoint inhibitor, specifically inhibiting pd-1melanoma, lung cancer, malignant pleural mesothelioma, renal cell carcinoma, hodgkin lymphoma, head and neck cancer, urothelial carcinoma, colon cancer, esophageal squamous cell carcinoma, liver cancer, gastric cancer, and esophageal or gastroesophageal junction (gej) cancer.fatigue, rash, musculoskeletal pain, itching, diarrhea, nausea, asthenia, cough, shortness of breath, constipation, decreased appetite, back pain, joint pain, upper respiratory tract infection, abnormal temperature increases, headache, abdominal pain, and vomiting. ofatumumabivanti-cd20 antibody.chronic lymphocytic leukaemianeutropenia, pneumonia, infusion reactions, cytopenias panitumumabivegfr inhibitor.ras (kras or nras) wild-type metastatic colorectal cancerskin reactions, electrolyte anomalies, anaphylaxis and angiooedema