List of antineoplastic agents
This is a list of antineoplastic agents used to treat cancer.
| Antineoplastic agents | ||||
|---|---|---|---|---|
| INN | Route[1] | Mechanism of action[1][2][3][4] | Indications[1][2][4] | Major toxicities[1][2][4][5] |
| 1. Cytotoxic antineoplastics | ||||
| 1.01 Nucleoside analogues | ||||
| Azacitidine | SC, IV | DNA methyltransferase inhibitor and incorporates itself into RNA, hence inhibiting gene expression.[6] | Myelodysplastic syndromes, acute myeloid leukaemia and chronic myeloid leukaemia | Myelosuppression, kidney failure (uncommon/rare), renal tubular acidosis and hypokalaemia. |
| Capecitabine | PO | Fluorouracilprodrug | Breast, colorectal, gastric and oesophageal cancer | Myelosuppression, cardiotoxicity, hypertriglyceridaemia, GI haemorrhage (uncommon), cerebellar syndrome (uncommon), encephalopathy (uncommon) and diarrhoea. |
| Carmofur | PO | Fluorouracil prodrug | Colorectal, breast and ovarian cancer | Myelosuppression, neurotoxicity and diarrhoea. |
| Cladribine | SC, IV | DNA methyltransferase inhibitor, metabolites incorporate themselves into DNA.[7][8][9][10] | Hairy cell leukaemia, chronic lymphocytic leukaemia | Myelosuppression, haemolytic anaemia (uncommon), neurotoxicity (rare), renal impairment (rare), pulmonary interstitial infiltrates (rare), Stevens–Johnson syndrome (rare) and toxic epidermal necrolysis (rare). |
| Clofarabine | IV | Ribonucleotide reductase and DNA polymerase inhibitor.[11] | Acute lymphoblastic leukaemia and acute myeloid leukaemia | Myelosuppression, hypokalaemia, cytokine release syndrome, Stevens–Johnson syndrome (uncommon), toxic epidermal necrolysis (uncommon) and pancreatitis (uncommon) |
| Cytarabine | SC, IM, IV, IT | DNA 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 leukaemia | Myelosuppression, 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). |
| Decitabine | IV | DNA methyltransferase inhibitor. | Myelodysplastic syndrome, sickle cell anaemia (orphan), acute myeloid leukaemia and chronic myeloid leukaemia. | Myelosuppression, hyperglycaemia, hypoalbuminaemia, hypomagnesaemia, hypokalaemia, hyperkalaemia and thrombocythaemia. |
| Floxuridine | IA | Fluorouracil analogue. | Metastatic GI adenocarcinoma and stomach cancer | Myelosuppression. |
| Fludarabine | PO, IV | DNA 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). |
| Fluorouracil | IV, Topical | Thymidylate 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). |
| Gemcitabine | IV | DNA 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). |
| Mercaptopurine | PO | Purine synthesis inhibitor. | Acute lymphoblastic leukaemia, acute promyelocytic leukaemia, lymphoblastic lymphoma and inflammatory bowel disease.[12] | Myelosuppression, hepatotoxicity, GI ulceration (rare), pancreatitis (rare) and secondary leukaemia (rare) or myelodysplasia (rare). |
| Nelarabine[13] | IV | Purine synthesis inhibitor. | Acute lymphoblastic leukaemia and chronic lymphocytic leukaemia. | Myelosuppression, pleural effusion, seizures, tumour lysis syndrome and a condition similar to Guillain-Barré syndrome. |
| Pentostatin | IV | Adenosine 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. |
| Tegafur | PO | Thymidylate synthase inhibitor. | Breast, colorectal cancer, gallbladder, gastrointestinal tract, head and neck, liver and pancreas cancer. | Myelosuppression, diarrhoea, neurotoxicity and hepatitis (rare). |
| Tioguanine | PO | Purine synthesis inhibitor. | Acute lymphoblastic leukaemia and acute myeloid leukaemia | Myelosuppression, hepatotoxicity, peripheral neuropathy (uncommon), intestinal necrosis (rare) and perforation (rare). |
| 1.02 Antifolates | ||||
| Methotrexate | SC, IM, IV, IT, PO | Dihydrofolate 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). |
| Pemetrexed | IV | Dihydrofolate 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). |
| Raltitrexed | IV | Dihydrofolate reductase and thymidylate synthase inhibitor. | Colorectal cancer | Myelosuppression |
| 1.03 Other antimetabolites | ||||
| Hydroxycarbamide | PO | Inhibits DNA synthesis by inhibiting the enzyme ribonucleotide reductase. | Chronic myeloid leukaemia, essential thrombocytosis, polycythaemia vera, myelofibrosis, acute myeloid leukaemia and sickle cell anaemia | Myelosuppression, skin cancer (rare), oedema (rare), hallucinations (rare), seizures (rare) and pulmonary toxicity (rare). |
| 1.04 Topoisomerase I inhibitor | ||||
| Irinotecan | IV | Inhibits topoisomerase I. | Colorectal cancer | Diarrhoea, myelosuppression, pulmonary infiltrates (uncommon), bradycardia (uncommon), ileus (rare) and colitis (rare). |
| Topotecan | IV | Inhibits topoisomerase I. | Small cell lung cancer, ovarian cancer and cervical cancer | Diarrhoea, myelosuppression, interstitial lung disease and allergy. |
| 1.05 Anthracyclines | ||||
| Daunorubicin | IV | Inhibits DNA and RNA synthesis by intercalating DNA base pairs. Inhibits DNA repair by inhibiting topoisomerase II. | Acute leukaemias | Myelosuppression, cardiotoxicity, anaphylaxis (rare), secondary malignancies (particularly acute myeloid leukaemia and myelodysplastic syndrome) and radiation recall. |
| Doxorubicin | IV | As above. | Breast cancer, lymphomas, sarcomas, bladder cancer, acute lymphoblastic leukaemia, Wilms' tumour, AIDS-related Kaposi's sarcoma, neuroblastoma and multiple myeloma | As above. |
| Epirubicin | IV | As above. | Breast cancer, gastric cancer and bladder cancer | As above. |
| Idarubicin | IV, PO | As above. | Acute leukaemias. | As above. |
| Mitoxantrone | IV | As above. | Non-Hodgkin lymphoma, acute myeloid leukaemia, prostate cancer and multiple sclerosis | As above. |
| Valrubicin | IV | As above. | Bladder cancer. | As above. |
| 1.06 Podophyllotoxins | ||||
| Etoposide | IV, PO | Topoisomerase II inhibitor. | Testicular cancer, ovarian cancer, lung cancer, acute myeloid leukaemia, lymphomas and sarcomas | Myelosuppression, hypersensitivity reactions, Stevens–Johnson syndrome (rare), peripheral neuropathy (uncommon) and secondary malignancies (especially acute myeloid leukaemia). |
| Teniposide | IV | Topoisomerase II inhibitor. | Lymphomas, acute lymphoblastic leukaemia and neuroblastoma | As above. |
| 1.07 Taxanes | ||||
| Cabazitaxel | IV | Microtubule disassembly inhibitor. Arrests cells in late G2 phase and M phase. | Prostate cancer | Myelosuppression, diarrhoea, kidney failure, hypersensitivity, severe GI reactions (including perforation, ileus, colitis, etc.; all rare) and peripheral neuropathy |
| Docetaxel | IV | As 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) |
| Paclitaxel | IV | As above. | Ovarian cancer, breast cancer, non-small cell lung cancer, AIDS-related Kaposi's sarcoma, cervical cancer, germ cell cancer and endometrial cancer | Hypersensitivity, 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 | ||||
| Vinblastine | IV | Microtubule assembly inhibitor. Arrests cells in M phase. | Hodgkin lymphoma, germ cell tumours, non-small cell lung cancer, bladder cancer and primary immune thrombocytopenia | Neurotoxicity, myelosuppression, myocardial ischaemia (rare) and myocardial infarction (rare). |
| Vincristine | IV | As above. | Lymphomas, acute lymphoblastic leukaemia, multiple myeloma, sarcoma, brain tumours, Wilms' tumour, neuroblastoma and primary immune thrombocytopenia | Neurotoxicity, anaphylaxis (rare), myocardial ischaemia (rare) and myocardial infarction (rare). |
| Vindesine | IV | As 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. |
| Vinflunine | IV | As above. | Bladder cancer | As per vinblastine. |
| Vinorelbine | IV | As above. | Breast cancer and non-small cell lung cancer. | As above. |
| 1.09 Alkylating agents | ||||
| Bendamustine | IV | Alkylates DNA. | Chronic lymphocytic leukaemia, mantle cell lymphoma and non-Hodgkin's lymphoma. | Myelosuppression, hypokalaemia and tachycardia. |
| Busulfan | IV, PO | Alkylates DNA. | Conditioning treatment before haematopoietic stem cell transplantation (high dose, IV), chronic myeloid leukaemia, myelofibrosis, polycythaemia vera and essential thrombocytosis | Myelosuppression, 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.[1][14] |
| Carmustine | IV | Alkylates 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.[1][14] |
| Chlorambucil | IV | Alkylates DNA. | Lymphoma, chronic lymphocytic leukaemia and Waldenström's macroglobulinaemia | Myelosuppression, 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.[1][14] |
| Chlormethine | IV, topical | Alkylates DNA. | Cutaneous T-Cell Lymphoma, metastatic carcinoma, leukaemias, lymphomas, polycythemia vera and bronchogenic carcinoma | Thrombosis, myelosuppression (common), hyperuricaemia, erythema multiforme, haemolytic anaemia, nausea and vomiting (severe) and secondary malignancies.[14] |
| Cyclophosphamide | IV | Alkylates 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 polyangiitis | Myelosuppression, 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.[14] |
| Dacarbazine | IV | Alkylates DNA. | Hodgkin lymphoma, metastatic malignant melanoma and soft tissue sarcoma | Myelosuppression, agranulocytosis (uncommon), hepatic vein thrombosis (rare) and hepatocellular necrosis (rare). Secondary malignancies.[14] |
| Fotemustine | IV | Alkylates DNA. | Metastatic malignant melanoma. | Myelosuppression. |
| Ifosfamide | IV | Alkylates DNA. | Sarcomas, testicular cancer and lymphomas. | Myelosuppression, haemorrhagic cystitis, nephrotoxicity, neurotoxicity and cardiac toxicity (rare). Secondary malignancies.[14] |
| Lomustine | PO | Alkylates DNA. | Glioma and medulloblastoma. | Myelosuppression, pulmonary infiltration and fibrosis. Secondary malignancies.[14] |
| Melphalan | IV, PO | Alkylates 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.[14] |
| Streptozotocin | IV, PO | Alkylates DNA. | Pancreatic cancer and carcinoid syndrome. | Nephrotoxicity, hypoglycaemia, myelosuppression, nausea and vomiting (>90%), jaundice and nephrogenic diabetes insipidus (rare). |
| Temozolomide | PO | Alkylates DNA. | Anaplastic astrocytoma, glioblastoma multiforme, metastatic malignant melanoma | Myelosuppression, Stevens–Johnson syndrome (rare), pneumonitis (rare) and hepatitis (rare). |
| 1.10 Platinum compounds | ||||
| Carboplatin | IV | Reacts with DNA, inducing apoptosis, non-cell cycle specific. | Ovarian cancer, lung cancer and squamous cell head and neck cancer | Myelosuppression, nausea and vomiting (30-90%), peripheral neuropathy, ototoxicity, anaphylaxis, acute kidney failure (rare), haemolytic uraemic syndrome (rare) and loss of vision (rare). |
| Cisplatin | IV | As 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 osteosarcoma | Nephrotoxicity, 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). |
| Nedaplatin | IV | As above. | Non-small cell lung cancer, oesophageal cancer, uterine cervical cancer, head and neck cancer and urothelial cancer | Nephrotoxicity, myelosuppression and nausea and vomiting (30-90%). |
| Oxaliplatin | IV | As above. | Colorectal cancer, oesophageal cancer and gastric cancer | Myelosuppression, 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 | ||||
| Altretamine | PO | Unclear, reactive intermediates covalently bind to microsomal proteins and DNA, possibly causing DNA damage | Recurrent ovarian cancer | Myelosuppression, peripheral neuropathy, seizures and hepatotoxicity (rare). |
| Bleomycin | IM, SC, IA, IV or IP | Inhibits 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. |
| Bortezomib | IV, SC | Proteasome 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. |
| Dactinomycin | IV | Complexes with DNA interfering with DNA-dependent RNA synthesis | Gestational trophoblastic disease, Wilms' tumour and rhabdomyosarcoma | Myelosuppression, anaphylaxis, radiation recall, hepatotoxicity and hepatic sinusoidal obstruction syndrome (common in Wilms' tumour). |
| Estramustine | PO | Antimicrotubule and oestrogenic actions | Prostate cancer. | Cardiovascular complications, such as ischaemic heart disease, venous thromboembolism, congestive heart failure, pulmonary embolism, myocardial infarction and cerebrovascular failure. |
| Ixabepilone | IV | Promotes tubulin polymerisation and stabilises microtubular function, causing cell cycle arrest at G2/M phase and subsequently induces apoptosis | Locally advanced or metastatic breast cancer. | Myelosuppression, peripheral neuropathy, myocardial ischaemia (uncommon/rare), supraventricular arrhythmia (uncommon/rare) and hypersensitivity reaction (uncommon/rare). |
| Mitomycin | IV | Cross-links DNA | Anal, bladder, and upper tract urothelial cancers | Myelosuppression, pulmonary toxicity and haemolytic uraemic syndrome (rare). |
| Procarbazine | IM, IV | Inhibits 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 | ||||
| Alemtuzumab | IV | CD52 antibody induces apoptosis in the tagged cells. | Chronic lymphocytic leukaemia | Pancytopenia, pneumonitis, arrhythmias and hypersensitivity reactions (rare), autoimmune haemolytic anaemia (rare), autoimmune thrombocytopenia (rare) and progressive multifocal leucoencephalopathy (rare). |
| Bevacizumab | IV | VEGF inhibitor. | Colorectal, breast, ovarian, renal cell and non-squamous non-small cell lung cancer and glioblastoma | Hypertension, 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. |
| Cetuximab | IV | EGFR 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. |
| Denosumab | SC | RANKL inhibitor. | Osteoporosis, including drug- and cancer-related osteoporosis, giant cell tumour of bone and hypercalcaemia of malignancies | Hypercholesterolaemia, cataract, urinary retention, hypocalcaemia, osteonecrosis of the jaw and anaphylaxis. |
| Gemtuzumab ozogamicin | IV | CD33 antibody that induces apoptosis of the tagged cell. | Acute myeloid leukaemia | Hepatic veno-occlusive disease, myelosuppression, cytokine release syndrome, hypersensitivity and electrolyte anomalies. |
| Ibritumomab tiuxetan | IV | CD20 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. |
| Ipilimumab | IV | CTLA4 antibody that causes immune system-mediated lysis of the tagged cell | Unresectable or metastatic malignant melanoma. | Life-threatening immune mediated reactions and fever. |
| Nivolumab | add | add | add | |
| Ofatumumab | IV | Anti-CD20 antibody. | Chronic lymphocytic leukaemia | Neutropenia, pneumonia, infusion reactions, cytopenias |
| Panitumumab | IV | EGFR inhibitor. | RAS (KRAS or NRAS) wild-type metastatic colorectal cancer | Skin reactions, electrolyte anomalies, anaphylaxis and angiooedema (rare). |
| Pembrolizumab | IV | Anti-PD-1 monoclonal antibody. | Melanoma, lung cancer, head and neck cancer, Hodgkin lymphoma, and stomach cancer. | Fatigue, rash, itchiness (pruritus), diarrhea, nausea, joint pain (arthralgia). |
| Pertuzumab | IV | HER2 inhibitor. | HER2-positive breast cancer. | Anaphylaxis, cardiac dysfunction and anaemia. |
| Rituximab | IV | Anti-CD20 antibody. | CD20-positive B cell non-Hodgkin lymphoma, chronic lymphocytic leukaemia, rheumatoid arthritis, granulomatosis with polyangiitis and microscopic polyangiitis | Infusion-related reactions, neutropenia, arrhythmias, infection, thrombocytopenia (uncommon), anaemia (uncommon), angina (uncommon), myocardial infarction (uncommon), heart failure (uncommon), haemolytic anaemia (rare), aplastic anaemia (rare), serum sickness (rare), severe skin conditions (rare), pulmonary infiltrates (rare), pneumonitis (rare), cranial neuropathy (vision or hearing loss; rare) and progressive multifocal leucoencephalopathy (rare). |
| Tositumomab | IV | Anti-CD20 antibody which is tagged with I131. | Non-Hodgkin's lymphoma | Grade 3-4 cytopenias, methaemoglobinaemia, acute myeloid leukaemia or myelodysplastic syndrome, anaphylaxis and hyperthyroidism. |
| Trastuzumab | IV | Anti-HER2 antibody. | HER2-positive breast cancer, gastric cancer, pancreatic cancer (orphan) and gastro-oesophageal junction cancer. | Cardiac dysfunction, infusion-related reactions, peripheral neuropathy and pulmonary toxicity (rare). |
| 2.2 Tyrosine kinase inhibitor | ||||
| Afatinib | PO | EGFR, HER2 and HER4 inhibitor. | Non-small cell lung cancer. | Diarrhoea, hypokalaemia, interstitial lung disease and hepatotoxicity. |
| Aflibercept | IV | VEGF and PGF inhibitor. | Colorectal cancer. | Myelosuppression, hypertension, dehydration, blood clots, GI perforation and reversible posterior leucoencephalopathy syndrome (uncommon). |
| Axitinib | PO | Multikinase inhibitor. | Renal cell carcinoma | Hypertension, thyroid dysfunction, blood clots, electrolyte disturbances, GI perforation (rare), fistula formation (rare), reversible posterior leucoencephalopathy syndrome (rare) and polycythaemia (uncommon). |
| Bosutinib | PO | Bcr-Abl and SRc kinase inhibitor. | Chronic myeloid leukaemia | Diarrhoea, thrombocytopenia, neutropenia, hepatotoxicity, QT interval prolongation, kidney failure, pleural effusion, pericarditis (uncommon/rare), acute pancreatitis (uncommon/rare), GI haemorrhage (uncommon/rare), anaphylactic shock (uncommon/rare), acute pulmonary oedema (uncommon/rare), respiratory failure (uncommon/rare), pulmonary hypertension (uncommon/rare) and erythema multiforme (uncommon/rare). |
| Crizotinib | PO | ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d'Origine Nantais (RON) inhibitor. | Non-small cell lung cancer | Lymphopenia, neutropenia, hypophosphataemia, hypokalaemia, peripheral neuropathy, blood clots, QT interval prolongation, bradycardia, pneumonia, pneumonitis, kidney cyst, ARDS and liver failure. |
| Dasatinib | PO | BCR-ABL, SRC family, c-Kit, EPHA2 and PDGFR-β kinase inhibitor. | Philadelphia positive chronic myeloid leukaemia and acute lymphoblastic leukaemia. | Fluid retention, myelosuppression, haemorrhage, hypertension, electrolyte anomalies, cardiac dysfunction (rare), heart failure (rare), myocardial infarction, arrhythmia (rare), prolonged QT interval (rare), kidney failure (rare), hypersensitivity (rare) and hepatic failure (rare). |
| Erlotinib | PO | EGFR inhibitor. | Non-small cell lung cancer and pancreatic cancer. | Skin reactions, diarrhoea, GI bleeds, anaemia, dehydration, interstitial lung disease (uncommon), hepatic failure (rare), hepatorenal syndrome (rare), GI perforation (rare) and ulcerative keratitis (rare). |
| Gefitinib | PO | EGFR inhibitor. | EGFR-mutation positive non-small cell lung cancer. | Skin reactions, diarrhoea, dehydration, haemorrhage, interstitial lung disease (uncommon), pancreatitis (uncommon), hepatitis (uncommon), allergy (uncommon), hepatic failure (rare), toxic epidermal necrolysis (rare) and Stevens–Johnson syndrome (rare). |
| Imatinib | PO | Bcr-Abl kinase inhibitor. | Philadelphia chromosome-positive acute lymphoblastic leukaemia, chronic myeloid leukaemia, GI stromal tumour and myelodysplastic/myeloproliferative diseases. | Myelosuppression, fluid retention, GI bleeding, electrolyte anomalies, left ventricular dysfunction (uncommon), heart failure (uncommon), pulmonary oedema (uncommon), kidney failure (uncommon), angiooedema (rare), anaphylaxis (rare), GI perforation (rare), hepatotoxicity (rare), avascular necrosis (rare), myopathy (rare) and rhabdomyolysis (rare). |
| Lapatinib | PO | HER2 inhibitor. | HER2-positive breast cancer, stomach cancer (orphan) and oesophageal cancer (orphan). | Diarrhoea, interstitial lung disease (uncommon), hepatotoxicity (uncommon) and anaphylaxis (rare). |
| Nilotinib | PO | Bcr-Abl kinase inhibitor. | Chronic myeloid leukaemia. | Myelosuppression, electrolyte disturbances, hyperglycaemia, prolonged QT interval (uncommon), peripheral arterial occlusive disease (uncommon), pancreatitis (uncommon), pleural effusion (uncommon) and pericardial effusion (uncommon). |
| Pazopanib | PO | Multikinase inhibitor, including c-KIT, FGFR, PDGFR and VEGFR. | Renal cell carcinoma and soft tissue sarcoma. | Hypertension, QT interval prolongation, haemorrhage, blood clots, neutropenia, thrombocytopenia, neutropenia, thrombocytopenia, elevated thyroid-stimulating hormone, hypothyroidism, electrolyte disturbances, hypo- or hyperglycaemia, torsades de pointes (uncommon), heart failure (uncommon), hepatic failure (uncommon), GI perforation (uncommon), fistula formation (uncommon) and reversible posterior leucoencephalopathy syndrome (rare). |
| Ponatinib | PO | Multikinase inhibitor (BEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2 and FLT3), that also inhibits T135I Bcr-Abl kinase. | T135I positive Chronic myeloid leukaemia and Philadelphia chromosome positive acute lymphoblastic leukaemia. | Hypertension, neutropenia, leucopenia, anaemia, thrombocytopenia, lymphopenia, pleural effusion, heart failure, peripheral neuropathy, haemorrhage, blood clots, pancreatitis and infection. |
| Regorafenib | PO | Multikinase inhibitor for RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, Trk2A, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Bcr-Abl. | Colorectal cancer and GI stromal tumours. | Anaemia, lymphopenia, thrombocytopenia, electrolyte anomalies, hepatotoxicity, hypertension, hypothyroidism, neutropenia, myocardial ischaemia or infarction. |
| Ruxolitinib | PO | JAK1 and JAK2 inhibitor. | Myelofibrosis and pancreatic cancer (orphan). | Anaemia and thrombocytopenia. |
| Sorafenib | PO | Multikinase inhibitor (including VEGF and PDGF receptor kinases). | Renal cell carcinoma and hepatocellular carcinoma. | Hypertension, skin reactions, bleeding, neutropenia, thrombocytopenia, lymphopenia, peripheral neuropathy, thyroid dysfunction, electrolyte anomalies, myocardial ischaemia or infarctions, heart failure (uncommon), GI perforation (uncommon), pancreatitis (uncommon), reversible posterior leucoencephalopathy syndrome (rare), hepatitis (rare), nephrotic syndrome (rare) and prolonged QT interval (rare). |
| Sunitinib | PO | Multikinase inhibitor (including VEGF & PDGF receptor tyrosine kinases) | renal cell carcinoma, GI stromal tumour and pancreatic neuroendocrine tumour | Neutropenia, thrombocytopenia, lymphopenia, hypertension, left ventricular dysfunction, heart failure, blood clots, thyroid dysfunction, electrolyte anomalies, pancreatitis (uncommon), hepatic failure (uncommon), prolonged QT interval (rare), torsades de pointes (rare), GI perforation (rare), fistula formation (rare), seizures (rare), reversible posterior leucoencephalopathy syndrome (rare), haemolytic uraemic syndrome (rare), thrombotic thrombocytopenic purpura (rare), nephrotic syndrome (rare), hypersensitivity (rare), angiooedema (rare), toxic epidermal necrolysis (rare) and Stevens–Johnson syndrome (rare). |
| Vandetanib[15] | PO | Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR | Medullary thyroid cancer. | Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). |
| 2.3 mTOR inhibitors | ||||
| Everolimus | PO | mTOR inhibitor. | Renal cell cancer, pancreatic neuroendocrine tumour and breast cancer | Pleural effusion, hyperglycaemia, hypercholesterolaemia, hypertriglyceridaemia, neutropenia, lymphopenia, thrombocytopenia, anaemia, bleeding, kidney failure, hypokalaemia, hypophosphataemia, pneumonitis, impaired wound healing (uncommon), anaphylaxis (rare) and angiooedema (rare). |
| Temsirolimus | IV | mTOR inhibitor. | Renal cell cancer and mantle cell lymphoma. | Infusion reactions, impaired wound healing, hyperglycaemia, hypercholesterolaemia, hypertriglyceridaemia, neutropenia, lymphopenia, thrombocytopenia, anaemia, bleeding, kidney failure, hypokalaemia, hypophosphataemia, pneumonitis, bowel perforation (uncommon) and intracerebral bleeding and Stevens–Johnson syndrome (rare). |
| 2.4 Retinoids | ||||
| Alitretinoin | Topical | Retinoic acid receptor (RAR) and retinoid X receptor (RXR) agonist. | Kaposi's sarcoma. | Oedema, rashes |
| Bexarotene[16] | PO, topical | RXR agonist. | Cutaneous T cell lymphoma | Leucopenia, anaemia, lactic dehydrogenase increased, hypochromic anaemia, hyperlipidaemia, hypercholesteraemia, hypothyroidism, haemorrhage, hypertension and kidney dysfunction. |
| Isotretinoin | PO, topical | RXR & RAR agonist. | Neuroblastoma[17] and acne. | Topical: Skin reactions, blood lipid anomalies, increased platelet count and osteoporosis.[18] Oral: Anaemia, Red blood cell sedimentation rate increased, thrombocytopenia, thrombocytosis, neutropenia, anaphylaxis, hypersensitivity, diabetes mellitus, hyperuricaemia, psychiatric disturbances (rare), convulsions (very rare), conjunctivitis, vasculitis (very rare), GI haemorrhage (very rare), hepatitis (very rare), erythema multiforme, Stevens–Johnson syndrome, toxic epidermal necrolysis, arthritis (very rare), rhabdomyolysis and glomerulonephritis (very rare).[19] |
| Tamibarotene | PO | RAR agonist. | Refractory acute promyelocytic leukaemia and Alzheimer's disease. | Hypercholesterolaemia, hypertriglyceridaemia, gastrointestinal disturbances, liver damage, leucocytosis and differentiation syndrome. |
| Tretinoin | PO, topical | RXR & RAR agonist. | Acne and acute promyelocytic leukaemia. | Oral: Differentiation syndrome, hyperleucocytosis, elevated cholesterol and triglycerides, arrhythmias, pancreatitis, elevated liver enzymes, thrombosis, intracranial hypertension and pseudotumour cerebri (mainly in children), anxiety, depression and genital ulceration (rare). Topical: Erythema. |
| 2.4 Immunomodulatory Agents (IMiDs) | ||||
| Lenalidomide | PO | Numerous actions; anti-angiogenesis (via inhibition of VEGF release), anti-TNF, IL-6 and pro-IL-2, IFN-γ effects. Also stimulates T cells and apoptosis in cancer cells. | Multiple myeloma | Blood clots, neutropenia (dose-limiting), thrombocytopenia (dose-limiting), anaemia, infection, hypotension, hypokalaemia, hypothyroidism, Stevens–Johnson syndrome, toxic epidermal necrolysis, angioedema, pneumonitis, hepatotoxicity and secondary malignancies (mostly myelodysplastic syndrome and acute myeloid leukaemia). |
| Pomalidomide | PO | As above. | Multiple myeloma and systemic sclerosis (orphan). | Neutropenia, anaemia, pneumonia, thrombocytopenia, hypercalcaemia, hyperglycaemia, kidney failure, lymphopenia, hyponatraemia, hypocalcaemia, hypokalaemia, peripheral neuropathy and thromboembolism. |
| Thalidomide | PO | As above. | Multiple myeloma, erythema nodosum leprosum and the following orphan indications: graft versus host disease, mycobacterial infection, recurrent aphthous ulcers, severe recurrent aphthous stomatitis, primary brain malignancies, HIV-associated wasting syndrome, Crohn's disease, Kaposi's sarcoma, myelodysplastic syndrome and haematopoietic stem cell transplantation. | Peripheral neuropathy, depression, thromboembolism, bradycardia, orthostatic hypotension, leucopenia, hypothyroidism, thrombocytopenia (uncommon), Stevens–Johnson syndrome (rare), toxic epidermal necrolysis (rare), pneumonitis (rare), hepatotoxicity (rare) and hearing loss (rare). |
| 2.5 Histone deacetylase inhibitors | ||||
| Panobinostat | add | add | add | add |
| Romidepsin | IV | Histone deacetylase inhibitor, hence inducing alterations in gene expression in the affected cells. | Peripheral and cutaneous T cell lymphoma. | Electrolyte anomalies, anaemia, thrombocytopenia, neutropenia, lymphopenia and ECG anomalies. |
| Valproate[Note 1] | PO, IV | As above. | Migraine prophylaxis, mania, epilepsy, fragile X syndrome (orphan), familial adenomatous polyposis (orphan) and the following off-label uses: cervical cancer, melanoma, mesothelioma, acute myeloid leukaemia and myelodysplastic syndrome. | Hyperammonaemia, thrombocytopenia, polycystic ovaries, SIADH (uncommon), hepatic failure (rare), pancreatitis (rare), leucopenia (rare), neutropenia (rare), pure red cell aplasia (rare), agranulocytosis (rare), extrapyramidal syndrome (rare), reduced BMD with long-term use, pleural effusion (rare) and multiorgan hypersensitivity reaction (rare). |
| Vorinostat | PO | As above. | As per romidepsin. | Thrombocytopenia, anaemia, QT interval prolongation and pulmonary embolism. |
| 2.6 Other Agents | ||||
| Anagrelide | PO | Phosphodiesterase 3 inhibitor. | Essential thrombocythaemia | Fluid retention, palpitations, tachycardia, hepatotoxicity (uncommon), heart failure (uncommon), hypertension (uncommon), arrhythmia (uncommon), syncope (uncommon), cardiomyopathy (rare), cardiomegaly (rare), MI (rare), pulmonary hypertension (rare), interstitial lung disease (rare) and pancreatitis (rare). |
| Arsenic trioxide[Note 2] | IV | Not fully understood. Induces partial differentiation and promotes apoptosis of leukaemic cells and may also inhibit angiogenesis. | Refractory or relapsed acute promyelocytic leukaemia. Orphan indications include: acute myeloid leukaemia, chronic lymphocytic leukaemia, malignant glioma, myelodysplastic syndrome, multiple myeloma, liver cancer and chronic myeloid leukaemia. | Differentiation syndrome, hyperleucocytosis, neutropenia, thrombocytopenia, ventricular tachycardia, prolonged QT interval, torsades de pointes, complete atrioventricular block, peripheral neuropathy, hyperglycaemia, hypokalaemia, hypomagnesaemia, elevation of bilirubin or aminotransferases, hepatotoxicity and secondary malignancies. |
| Asparaginase [Note 3] | IM, IV | Catalyses the conversion of the amino acid L-asparagine to aspartic acid and thereby reduces the availability of L-asparagine to leukaemic cells. Unlike normal cells, certain types of leukaemic cells do not synthesise L-asparagine, which is essential for cell growth and survival. | Acute lymphoblastic leukaemia and lymphoblastic lymphoma. | Allergic reactions, haemorrhagic and thrombotic events, uraemia, pancreatitis, hyperglycaemia, hyperammonaemia, acute kidney failure and diabetic ketoacidosis. |
| BCG vaccine [Note 4] | IB | Live, attenuated Mycobacterium bovis, which produces a local inflammatory reaction, resulting in elimination or reduction of superficial tumour lesions of the bladder. | Bladder cancer | Cystitis, BCG infection and contracted bladder. |
| Denileukin diftitox | IV | Interleukin 2 combined with diphtheria toxin which binds to the interleukin receptor on immune cells and introduces the diphtheria toxin into the cell. | Cutaneous T cell lymphoma and peripheral T cell lymphoma (orphan). | Infusion reactions, hypocalcaemia, hypotension, thrombocytopenia, Acute kidney injury (uncommon/rare), Hyper/hypothyroidism (uncommon/rare), pancreatitis (uncommon/rare) and toxic epidermal necrolysis (uncommon/rare). |
| Vemurafenib | PO | BRAF kinase inhibitor. | BRAF kinase mutation V600E-positive Metastatic melanoma. | Skin reactions, secondary malignancies (mostly squamous cell carcinoma), anaphylaxis (rare) and hypotension (rare). |
| Abbreviations/Acronyms: IM – Intramuscular. IV – Intravenous. IA – Intra-arterial. SC – Subcutaneous. PO – Per os, oral. IP – Intrapleural. IB – Intrabladder. Preg. cat. - Pregnancy category. The preferred pregnancy category is Australian, but if it is unavailable the pregnancy category given is American. | ||||
| Notes | ||||
References
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- 1 2 3 Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. ISBN 978-0-85711-084-8.
- ↑ Brunton LL, Chabner B, Knollmann BC, eds. (2011). Goodman & Gilman's The Pharmacological Basis of Therapeutics (12th ed.). New York: McGraw-Hill. ISBN 978-0-07-162442-8.
- 1 2 3 Alldredge BK, Corelli RL, Ernst ME, Guglielmo BJ, Jacobson PA, Kradjan WA, Williams BR (February 2012). Applied therapeutics: the clinical use of drugs. Koda Kimble and Youngs Applied Therapeutics (10th ed.). Baltimore, MD: Lippincott Williams & Wilkins. ISBN 978-1-60913-713-7.
- ↑ Sweetman, S (ed.). Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 8 February 2014.
- ↑ Martens, UM, ed. (2010). "11 5-Azacytidine/Azacitidine". Small molecules in oncology. Recent Results in Cancer Research. Vol. 184. Heidelberg: Springer. pp. 159–170. doi:10.1007/978-3-642-01222-8. ISBN 978-3-642-01222-8.
- ↑ Spurgeon, Stephen; Yu, Margaret; Phillips, John D.; Epner, Elliot M. (2009-08-01). "Cladribine: not just another purine analogue?". Expert Opinion on Investigational Drugs. 18 (8): 1169–1181. doi:10.1517/13543780903071038. ISSN 1354-3784. PMID 19604118. S2CID 22355364.
- ↑ Bryson, Harriet M.; Sorkin, Eugene M. (1993-11-01). "Cladribine". Drugs. 46 (5): 872–894. doi:10.2165/00003495-199346050-00007. ISSN 0012-6667. PMID 7507037.
- ↑ Robak, Tadeusz; Korycka, Anna; Robak, Ewa (2005-12-31). "Older and New Formulations of Cladribine. Pharmacology and Clinical Efficacy in Hematological Malignancies". Recent Patents on Anti-Cancer Drug Discovery. 1 (1): 23–38. doi:10.2174/157489206775246467. PMID 18221024.
- ↑ Hentosh, Patricia; Peffley, Dennis M. (2010-01-01). "The cladribine conundrum: deciphering the drug's mechanism of action". Expert Opinion on Drug Metabolism & Toxicology. 6 (1): 75–81. doi:10.1517/17425250903393745. ISSN 1742-5255. PMID 19968576. S2CID 41433204.
- ↑ Ghanem H, Kantarjian H, Ohanian M, Jabbour E (Apr 2013). "The role of clofarabine in acute myeloid leukemia". Leukemia & Lymphoma. 54 (4): 688–698. doi:10.3109/10428194.2012.726722. PMC 5681218. PMID 22957815.
- ↑ Timmer, Antje; Patton, Petrease H.; Chande, Nilesh; McDonald, John W. D.; MacDonald, John K. (2016-05-18). "Azathioprine and 6-mercaptopurine for maintenance of remission in ulcerative colitis". The Cochrane Database of Systematic Reviews (5): CD000478. doi:10.1002/14651858.CD000478.pub4. ISSN 1469-493X. PMC 7034525. PMID 27192092.
- ↑ "Arranon (nelarabine) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 11 February 2014.
- 1 2 3 4 5 6 7 8 9 Bhatia, S (2008). "Secondary Malignancies: Therapy-Related t-MDS/AML". Medscape Reference. WebMD. Retrieved 7 February 2014.
- ↑ "Vandetanib dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 February 2014.
- ↑ "Targretin (bexarotene) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 February 2014.
- ↑ Matthay KK (Jan 2013). "Targeted isotretinoin in neuroblastoma: kinetics, genetics, or absorption". Clinical Cancer Research. 19 (2): 311–313. doi:10.1158/1078-0432.CCR-12-3313. PMC 5892183. PMID 23209029.
- ↑ "Amnesteem, Claravis (isotretinoin) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 February 2014.
- ↑ "Isotretinoin 20mg capsules – Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Alliance Pharmaceuticals. 12 April 2013. Retrieved 9 February 2014.
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