List of antineoplastic agents

This is a list of antineoplastic agents used to treat cancer.

Antineoplastic agents
INNRoute[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
AzacitidineSC, IVDNA methyltransferase inhibitor and incorporates itself into RNA, hence inhibiting gene expression.[6]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.[7][8][9][10]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.[11]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.[12]Myelosuppression, hepatotoxicity, GI ulceration (rare), pancreatitis (rare) and secondary leukaemia (rare) or myelodysplasia (rare).
Nelarabine[13]IVPurine 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.[1][14]
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.[1][14]
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.[1][14]
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.[14]
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.[14]
DacarbazineIVAlkylates DNA.Hodgkin lymphoma, metastatic malignant melanoma and soft tissue sarcomaMyelosuppression, agranulocytosis (uncommon), hepatic vein thrombosis (rare) and hepatocellular necrosis (rare). Secondary malignancies.[14]
FotemustineIVAlkylates DNA.Metastatic malignant melanoma.Myelosuppression.
IfosfamideIVAlkylates DNA.Sarcomas, testicular cancer and lymphomas.Myelosuppression, haemorrhagic cystitis, nephrotoxicity, neurotoxicity and cardiac toxicity (rare). Secondary malignancies.[14]
LomustinePOAlkylates DNA.Glioma and medulloblastoma.Myelosuppression, pulmonary infiltration and fibrosis. Secondary malignancies.[14]
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.[14]
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.
Nivolumabaddaddadd
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 (rare).
PembrolizumabIVAnti-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).
PertuzumabIVHER2 inhibitor.HER2-positive breast cancer.Anaphylaxis, cardiac dysfunction and anaemia.
RituximabIVAnti-CD20 antibody.CD20-positive B cell non-Hodgkin lymphoma, chronic lymphocytic leukaemia, rheumatoid arthritis, granulomatosis with polyangiitis and microscopic polyangiitisInfusion-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).
TositumomabIVAnti-CD20 antibody which is tagged with I131.Non-Hodgkin's lymphomaGrade 3-4 cytopenias, methaemoglobinaemia, acute myeloid leukaemia or myelodysplastic syndrome, anaphylaxis and hyperthyroidism.
TrastuzumabIVAnti-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
AfatinibPOEGFR, HER2 and HER4 inhibitor.Non-small cell lung cancer.Diarrhoea, hypokalaemia, interstitial lung disease and hepatotoxicity.
AfliberceptIVVEGF and PGF inhibitor.Colorectal cancer.Myelosuppression, hypertension, dehydration, blood clots, GI perforation and reversible posterior leucoencephalopathy syndrome (uncommon).
AxitinibPOMultikinase inhibitor.Renal cell carcinomaHypertension, thyroid dysfunction, blood clots, electrolyte disturbances, GI perforation (rare), fistula formation (rare), reversible posterior leucoencephalopathy syndrome (rare) and polycythaemia (uncommon).
BosutinibPOBcr-Abl and SRc kinase inhibitor.Chronic myeloid leukaemiaDiarrhoea, 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).
CrizotinibPOALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d'Origine Nantais (RON) inhibitor.Non-small cell lung cancerLymphopenia, neutropenia, hypophosphataemia, hypokalaemia, peripheral neuropathy, blood clots, QT interval prolongation, bradycardia, pneumonia, pneumonitis, kidney cyst, ARDS and liver failure.
DasatinibPOBCR-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).
ErlotinibPOEGFR 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).
GefitinibPOEGFR 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).
ImatinibPOBcr-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).
LapatinibPOHER2 inhibitor.HER2-positive breast cancer, stomach cancer (orphan) and oesophageal cancer (orphan).Diarrhoea, interstitial lung disease (uncommon), hepatotoxicity (uncommon) and anaphylaxis (rare).
NilotinibPOBcr-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).
PazopanibPOMultikinase 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).
PonatinibPOMultikinase 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.
RegorafenibPOMultikinase 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.
RuxolitinibPOJAK1 and JAK2 inhibitor.Myelofibrosis and pancreatic cancer (orphan).Anaemia and thrombocytopenia.
SorafenibPOMultikinase 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).
SunitinibPOMultikinase inhibitor (including VEGF & PDGF receptor tyrosine kinases)renal cell carcinoma, GI stromal tumour and pancreatic neuroendocrine tumourNeutropenia, 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]POTyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFRMedullary thyroid cancer.Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon).
2.3 mTOR inhibitors
EverolimusPOmTOR inhibitor.Renal cell cancer, pancreatic neuroendocrine tumour and breast cancerPleural effusion, hyperglycaemia, hypercholesterolaemia, hypertriglyceridaemia, neutropenia, lymphopenia, thrombocytopenia, anaemia, bleeding, kidney failure, hypokalaemia, hypophosphataemia, pneumonitis, impaired wound healing (uncommon), anaphylaxis (rare) and angiooedema (rare).
TemsirolimusIVmTOR 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
AlitretinoinTopicalRetinoic acid receptor (RAR) and retinoid X receptor (RXR) agonist.Kaposi's sarcoma.Oedema, rashes
Bexarotene[16]PO, topicalRXR agonist.Cutaneous T cell lymphomaLeucopenia, anaemia, lactic dehydrogenase increased, hypochromic anaemia, hyperlipidaemia, hypercholesteraemia, hypothyroidism, haemorrhage, hypertension and kidney dysfunction.
IsotretinoinPO, topicalRXR & 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]
TamibarotenePORAR agonist.Refractory acute promyelocytic leukaemia and Alzheimer's disease.Hypercholesterolaemia, hypertriglyceridaemia, gastrointestinal disturbances, liver damage, leucocytosis and differentiation syndrome.
TretinoinPO, topicalRXR & 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)
LenalidomidePONumerous 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 myelomaBlood 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).
PomalidomidePOAs above.Multiple myeloma and systemic sclerosis (orphan).Neutropenia, anaemia, pneumonia, thrombocytopenia, hypercalcaemia, hyperglycaemia, kidney failure, lymphopenia, hyponatraemia, hypocalcaemia, hypokalaemia, peripheral neuropathy and thromboembolism.
ThalidomidePOAs 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
Panobinostataddaddaddadd
RomidepsinIVHistone 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, IVAs 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).
VorinostatPOAs above.As per romidepsin.Thrombocytopenia, anaemia, QT interval prolongation and pulmonary embolism.
2.6 Other Agents
AnagrelidePOPhosphodiesterase 3 inhibitor.Essential thrombocythaemiaFluid 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]IVNot 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, IVCatalyses 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]
IBLive, attenuated Mycobacterium bovis, which produces a local inflammatory reaction, resulting in elimination or reduction of superficial tumour lesions of the bladder.Bladder cancerCystitis, BCG infection and contracted bladder.
Denileukin diftitoxIVInterleukin 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).
VemurafenibPOBRAF 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
  1. Its use in cancer treatment is purely investigational at present
  2. There is no INN for arsenic trioxide, just the USAN
  3. There is no INN for asparaginase, only a USAN
  4. There is no INN for BCG

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